Abstract

This work deals with development of a simple, precise, accurate and economical high performance liquid chromatographic (HPLC) method with ultraviolet (UV) detection for the analysis of antihyperlipidemic drug Simvastatin from human plasma. Nicardipine hydrochloride was employed as the internal standard. Liquid-liquid extraction technique with ethyl acetate solvent was used for preparation of biological samples. Analysis was performed on a HiQSil C₁₈HS (250X4.6 mm, 5μm) HPLC column using Acetonitrile: 10 mM Ammonium acetate buffer (pH 5.9) (80:20 v/v) as mobile phase at a flow rate of 1 mL/min. Sample injection was done by means of an auto sampler and detection was carried out using UV detector at a wavelength of 238 nm. A good linearity was found in the concentration range of 100-1000 ng/mL. The developed method was validated according to US-FDA and European Medicines Agency (EMEA) guidelines for linearity, accuracy, precision and stability. The values obtained were found to be within the prescribed limits. The described method can be applied for pharmacokinetic analysis in real clinical samples.

Abstract

Neurotoxicity of individual metals such as arsenic (As) and lead (Pb) are well investigated, as humans in reality are exposed to combination of metals in the environment. We studied the alterations in motor behavior, cholinergic system, gene expression levels of acetylcholinesterase (AChE) and neuronal nitric oxide synthase (nNOS) in different brain regions (cerebral cortex, hippocampus and cerebellum) of rats exposed to As and/or Pb.  Pregnant rats were exposed to sodium meta-arsenite (50 ppm) and lead acetate (0.2%) individually, and in a combination (As=25 ppm+Pb=0.1%) via drinking water throughout perinatal period (GD6 to PND 21). After the behavioral activities were examined, the pups were sacrificed and brain synaptosomal preparations were used for biochemical studies. The metal mixture exposure significantly decreased the activity of AChE with consequent increase in ACh than individual metals. The gene expression levels of AChE and nNOS were also down regulated following exposure to As, Pb and As+Pb. The hippocampus region showed greater decrease in AChE specific activity and expression levels whereas cerebellum exhibited diminished nNOS expression. The exploratory behavior, locomotor activity and grip strength also showed a significant decrease in metal mixture (As+Pb) exposed rats than exposure to individual metals. These results suggest that behavioral dysfunctions observed in either Pb and/or As exposed rats can be correlated with the alterations observed in cholinergic system and nNOS levels in different brain regions of rats. In conclusion, these data suggest that the toxicity of As or Pb is exacerbated when exposed to metal mixture than individual metals.

Abstract

A simple, rapid, specific, linear, accurate and precise RP-HPLC method for simultaneous estimation of febuxostat and ketorolac in bulk and pharmaceutical dosage form using rat plasma was developed and validated. The chromatographic separation was achieved on symmetry C18 (150 X 4.6 mm) 5µm in column. The mobile phase consists of tri ethyl amine buffer and acetonitrile (60:40 %v/v) and pH is adjusted to 6.0 using orthophosporic acid operated an isocratic mode. The flow rate of mobile was 1.0ml per minutes and effluents were monitored at 255nm. The injection volume was 20 µL. The retention time of febuxostat and ketorolac was found to be 2.465 and 3.740 minutes respectively and run time of analysis was 5 minutes. The correlation coefficient was found that near to 1 for both drugs. The accuracy of the method was evaluated by recovery studies and good recovery results were obtained between 98 % and 102% and relative standard deviation was found to be below 2%. This method is simple, specific and accurate and precise for the estimation of Febuxostat and ketorolac in rat plasma.

Abstract

Chronic kidney disease (CKD) is a global health threat associated with an alarming increase in morbidity and mortality. There are many mechanisms explaining the link between thyroid and kidney disease. Thyroid hormones have pre-renal and intrinsic renal effects by which they increase the renal blood flow and glomerular filtration rate (GFR). Hypothyroidism is associated with reduced GFR and hyperthyroidism results in increased GFR as well as increased renin-angiotensin-aldosterone activation. CKD patients also have increased incidence of primary and sub-clinical hypothyroidism. The physiological benefits of a hypothyroid state in CKD, and the risk of CKD progression with hyperthyroidism emphasize on a conservative approach in the treatment of thyroid hormone abnormalities in CKD. Thyroid dysfunction is also associated with glomerulonephritis often by a common autoimmune etiology. Several drugs could affect both thyroid and kidney functions. All of these aspects are covered in the present review. The variable association of low T₃ to inflammation, endothelial dysfunction, and poor survival in CKD and transplant patients is of importance. A detailed knowledge of these interactions is important for both the nephrologists and endocrinologists for optimal diagnosis and management of the patient.

Abstract

The current review describes the morphological, phytochemical and ethnopharmacological aspects of Asclepias curassavica L. (Asclepiadaceae). Asclepias curassavica has been known since ancient times for its curative properties and has been utilized for the treatment of various ailments such as tumor, asthma, fever, homeostasis, inflammation, diarrhoea, catharitic, emetic, expectorant, warts, and acesodyne. In recent decades, a great number of chemical and pharmacological studies have been done on Asclepias curassavica. This contribution provides a comprehensive review of the pharmacologically relevant compounds of Asclepias curassavica characterized so far and of the studies supporting its use as a medicinal plant. Particular attention has been given to cardiovascular, cytotoxicity, urinary stimulatory, antifertility, antiviral, antifungal, anticrustacean, insecticidal, antiamoebic, anti-inflammatory, anticoagulatory, antioxidant and antibacterial effects. Several chemical constituents including cardenolides, flavanols, phenols, aliphatic, alicyclic compounds and alkaloids were present in this plant. The present outcome of review summarizes the most interesting findings related to the traditional and folkloric uses, phytoconstituents and pharmacological aspects of Asclepias curassavica.

Abstract

Senna occidentalis L. is a common traditional herbal medicine and is one among the most controversial species related with its multiple morphoforms.  The present study was aimed to differentiate the medicinal accessions collected from ten localities of Thiruvananthapuram in terms of anatomy, IR and biochemical characters. Foliar trichomes, palisade ratio (6:8 to 8:10) and stomatal indices (19.55-25.53) among the accessions showed variations. The analytical parameters like chlorophyll a and b, total chlorophyll (0.348 – 3.27 mg/g) total phenols (4.73 to 9.85 mg/g), flavonoids (2.9 to 23.31 mg/g) and total protein (1.05- 13.05 mg/g) also displayed sound variations. The infrared spectra of Senna occidentalis accessions in terms of fingerprint were highly typical for different accessions. The principal component analysis of Fourier Transform Infrared (FTIR) data confirmed most of the visual morphological variations between the accessions. The proteins absorption bands located between 1800 – 1500 and the bands between 1500 - 1000 cm^-1 (finger print region) showed variation between the accessions. SDS polypeptide banding pattern could resolve many bands most of them shared and others were unique among the accessions. Similarly the intensity of bands also showed marked variations among the accessions. Protein diversity strongly supported the anatomical variabilities observed among the Senna occidentalis in the present study. Further studies are planned to screen the therapeutic potentialities of valid accession.

Abstract

Abnormalities of red blood cell enzymes result in diverse phenotypes, including hemolytic anemia, methemoglobinemia, polycythemia, and non-erythroid effects such as neurological and developmental abnormalities. Glucose 6-phosphate dehydrogenase (G6PD) deficiency is the most common enzymopathy of red blood cells. 58 years ago, Alving and his colleagues discovered G6PD deficiency while investigating the unusual primaquine sensitivity of erythrocytes in Blacks. Clinically, deficiency of G6PD affects as many as 400 million individuals worldwide. The risk of drug induced G6PD deficiency related hemolysis depends on a number of factors including the G6PD variants which itself differ in various geographical locations. With the advancements in the field of G6PD research in the past few years, it has become certain that G6PD is an indispensable component of antioxidant defense. Its diagnosis should be considered in children with a family history of jaundice, anemia, splenomegaly, or cholelithiasis, especially in those of Mediterranean or African ancestry. Whether G6PD deficiency plays pathogenic roles in diseases other than hemolytic disorders, such as cancer and diabetes mellitus, remains to be clearly defined.

Abstract

A novel series of trisubstituted pyrimidines (5a-5j) were synthesized by reaction of various substituted chalcones with guanidine hydrochloride in presence of potassium hydroxide in alcoholic medium and subjected to molecular properties prediction by molinspiration, molsoft and osiris softwares. The structures of new compounds were established by ¹HNMR, IR, mass spectral data and elemental analysis. The newly synthesized compounds were evaluated for anti-inflammatory, antimicrobial, and anticancer activities and were found to be in conformity with lipinski’s “rule of five” and other parameters, for their onward screening for biological activity as active leads/ drugs. The % inhibition values of trisubstituted pyrimidines 5c,5d were found to be excellent anti-inflammatory agents.The compounds 5g,5i,5j showed good antibacterial activity whereas compounds 5c,5d showed promising antifungal activity. The IC50 values of compounds 5c,5d proved to be the potent anticancer agents.

Abstract

Inflammation is a reaction of a living vascularised tissue to an injury. Conventional or synthetic drugs used in the treatment of inflammatory diseases are inadequate, it sometimes have serious side effects. So, number of herbal medicines is recommended for the treatment of inflammation that has no side effects. The present study is aimed to evaluate the anti inflammatory activity of Delonix elata on collagen induced paw edema in mice as for controlling inflammatory disorders. The objectives of the present study are to carry out phytochemical screening of selected plant, to prepare a methanolic extract from Delonix elata and to screen the in vivo anti inflammatory effect of Delonix elata. For phytochemical screening, the secondary metabolites like alkaloid, flavonoid, saponin, carotenoids were tested using qualitative spot tests. For anti inflammatory activity, swiss albino mice were used and divided into 4 groups and treated accordingly: Normal control, collagen induced group (50ug/kg bw), collagen + Delonix elata (60mg/kg bw), and standard (Diclofenac) treated (15mg/kg bw). After the experimental period of 56 days, the blood samples were collected and biochemical parameter studies were carried out. The phytochemical screening suggests the presence of phytochemicals like alkaloids saponin, flavonoids, carotenoids and cardiac glycosides. Administration of collagen to the experimental animals produced reduction in the levels of serum protein and total RBC and Hb. The animals pretreated with Delonix elata extract at dose level of 60mg/kg bw were significantly increased the levels of the above parameters. A significant increase in the level of serum enzymes (SGOT, SGPT, ALP) and Lipid peroxide (LPO), in the level of hydroxy proline, hexosamine and leucocytes was noted in the mice induced with collagen, while these levels were normalized by pretreatment with Delonix elata extract. The western blot assay was carried out to study the expression of pro and anti-inflammatory cytokines. Western blot analysis revealed that the methanolic crude extract of Delonix elata inhibited TNF- α, IL-6 and IL-1 β production in collagen induced mice (expression of TNF - α, IL-6 and IL-1 β lesser than that of inflammation induced group). The anti-inflammatory cytokines counteracted the cytotoxic effects of pro inflammatory cytokines during inflammation. Thus, IL-10 and IL-4 levels are increased in the collagen induced mice, whereas the levels are reduced in the methanolic crude extract of Delonix elata pre treated mice. From the present observation, it is evidenced that Delonix elata would be an effective drug for the treatment of inflammatory reactions.

Abstract

A simple efficient, precise and accurate spectroscopic method has been developed and validated for quantitative estimation of EZETIMIBE in bulk drug and pharmaceutical dosage form. EZETIMIBE is dissolved in 0.1M Hydrochloric and the resulting solution was then scanned in the UV range (200-400nm) in a 10 mm quartz cell in a double beam UV spectrophotometer. The λmax of EZETIMIBE was found to be 314nm.The method obey’s Beers law in the concentration range from 3-18 µg/ml. The correlation coefficient was found to be 0.9997 (r²═ 0.9997). The LOD and LOQ were found to be 0.9882 and 1.9482mg/ ml respectively. The result of estimation of marketed tablet formulation (Allegro) was found to be 99.47% with their % RSD 0.4362.The accuracy of the method was determined by recovery studies. The percentage recovery was found to be 99.83%. The method was validated statistically as per ICH guidelines. The method showed good reproducibility and recovery with % RSD less than 2. So, the proposed method was found to be simple, specific, precise, accuracy, linear, and rugged. Hence it can be applied for routine analysis of EZETIMIBE in bulk drug and the Pharmaceutical formulations.

Abstract

Transdermal drug delivery system was introduced to overcome the difficulties of drug delivery through oral route. A Transdermal patch is medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the blood stream. Transdermal drug delivery systems (TDDS) are defined as self contained, discrete dosage forms which, when applied to intact skin, deliver the drug(s), through the skin, at a controlled rate to systemic circulation.  The Transdermal route of administration is recognized as one of the potential route for the local and systemic delivery of drugs. Transdermal delivery provides a leading edge over injectables and oral route by increasing patient compliance and avoiding first pass metabolism. Transdermal delivery not only provides controlled, constant administration of the drug, but also allows continuous input of drugs with short biological half-lives and eliminates pulsed entry into systemic circulation, which often causes undesirable side effects. In this era transdermal drug delivery is a successful method to deliver the drug into the bloodstream without pain.The present review article explores the overall study on transdermal drug delivery systems which lead to novel drug delivery systems.

Abstract

The aim of present study was an attempt to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing bilayered sustained release matrix tablets of Valsartan. Matrix tablets are formulated by HPC, HPMCK₁₅ M, Xanthan gum, Guar gum individually and in combination containing different drug, polymer ratio such as 1:2, 1:2.5, 1:3.5 and 1:4 by direct compression method. The influence of different proportions of polymers and nature of polymer was studied. In vitro drug release studies were performed in USP type II apparatus for 24 hours in phosphate buffer. The prepared bilayered matrix tablets are within house specifications for all the physicochemical properties. In vitro release data shows drug release was decreased with increasing polymer proportion. The in vitro drug release study reveals HPC individually with different ratios of polymer content able to sustain the drug release upto 24 hours. Xanthan gum with different ratios of polymer able to sustained drug release upto 20 hours. Based on in vitro drug release data and f2 factor, F1, F10, F12 (1: 2 of HPC, 1: 3of xanthan gum, 1:3.5 of guar gum) formulations are optimized. Mathematical analysis of the release kinetics indicated that drug release mechanism was fickian diffusion. No compatibility was observed between the drug and excipients used in the formulation of matrix tablets.

Abstract

A simple reverse phase HPLC method was developed for the determination of Aripiprazole present in pharmaceutical dosage forms. A Discovery HSF5 C18, 4.6mm x 250 mm, 5 μm column from Supelco (India), with mobile phase methanol: Acetonirile:sodium sulphate buffer (pH-4) (25:25:50) was used. The flow rate was 1.2 ml/min and effluent was monitored at 254 nm. Caffeine is used as internal standard. Calibration standards were prepared by spiking working standard solutions into methanol containing 25 mL volumetric flasks to yield concentrations of 20, 40, 60,100,140,160 and 200 μg /mL. The retention times were 2.85 min and 6.74 min for APZ and RIT respectively. The linearity range was found to be 20-200 µg/ml for APZ. The proposed method was also validated.

Abstract

A good Transdermal patch containing can be formulated by solvent casting technique using as film former and propylene glycol as plasticizer such Transdermal patches are advantages in providing effective treatment for Hypertension with enhanced patient compliance. From the in-vitro release results observed that the films prepared by using  different ratios of HPMCK 15M,PVPK30 and EC Transdermal Ramipril  patches were formulated using DBP as a plasticizer and DMSO as a penetration enhancer proved to exhibit better release characteristics. It can be reasonably concluded that Ramipril can be formulated into Transdermal patches to prolong its release characteristics. Thus the formulation HPMCK15M and Ethyl Cellulose was found to be the best for controlled release. The Cumulative drug release from Formulation RM4 was found to be 99.64% after 24 hrs. So the formulation RM4 is emerged as ideal formulation for Ramipril because it showed better release with sustained effect as compared to other formulations.

Abstract

Dengue is a mosquito-borne disease that present as a health burden in many countries especially the South East Asia countries: Thailand, Philippines, Indonesia, Singapore, Malaysia, Myanmar, Lao People's Democratic Republic, Brunei Darussalam, Cambodia and Vietnam. This is a disease that requires behavioural change that emphasise on the social mobilisation and communication activities to prevent and control dengue transmission.¹ Communication is vital to achieve a common understanding that in turn allows social mobilisation to be implemented.¹ Social mobilisation involves all relevant segments of society that engage the people’s participation to achieve a goal with a direction.

Abstract

The key objective of this study was to develop combinational herbal oral antidiabetic suspension containing indigenous ethnomedicinal plants extract. The amount of individual plant’s extract required for formulation was based on the effective dose of plant’s extract. The maximum therapeutic effective dose for diabetic wistar rats was found to be 50 mg/kg b.w. of Phyllanthus emblica, 50 mg/kg b.w. of Annona squamosa, 100 mg/kg b.w. of Curcuma longa and 100 mg/kg b.w. Berberis aristata. Suspension was prepared by using effective doses with suitable suspending and stabilizing agents. The formulated suspension was evaluated viz., organoleptic and accelerated stability studies at variable (different) temperature. Suspension exhibited pleasant appearance and texture; there were no changes in sedimentation, flow rate, pH, viscosity and other physiochemical parameters. All the stability parameters in formulated suspension are stable and acceptable. It is concluded that suspension of ethanolic extract of Phyllanthus emblica, Annona squamosa, Berberis aristata and methanolic extract of Curcuma longa formulated in combinational therapy could be effective and safe for antidiabetic use.

Abstract

A basic definition of nanotechnology is the building of functional systems at the molecular scale. This covers both current work and concepts that are more advanced. Carbon nanotube are allotropes of carbon with a cylindrical nanostructure. Nanotubes have been constructed with length-to-diameter ratio of up to 132,000,000:1,which is significantly larger than any other material. Because of their nanostructure they are now used as drug delivery system in many disease mainly in cancer treatments. There are various techniques used for synthesis of nanotubes such as arc discharge, laser ablation, high pressure carbon monoxide, and chemical vapor deposition (CVD). These are the grapheme cylinders about 12 nm in diameter and capped with end containing pentagonal rings. The review opens the use of these nanotubes in various disease alongwith its pharmacology. The properties and characteristics of CNTs are still being researched heavily and scientists have barely begun to tap the potential of these structures. Carbon nanotubes can be used in various therapeutic applications like cancer therapy, vaccine, tissue regeneration, platelet activation, cardiac autonomic regulation, bioengineering, dignostic tool, catalyst.

Abstract

The paper presents the ring opening reaction of itaconic anhydride with 4-aminoantipyrine resulted in the formation of title compound, 4-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino]-2-methylidene-4-oxobutanoic acid (1). The structure of the newly synthesized compound was characterized by IR, ¹H NMR, ¹³C NMR, mass, elemental and thermal analysis data. The present study examines the possible antioxidant, antimicrobial and thermal properties of the titled compound 1. In order to evaluate the antioxidant activity, different in vitro methodologies such as DPPH radical scavenging, nitric oxide radical scavenging and reducing power assays were used. In addition, in vitro antimicrobial activity of the compound 1 was tested against four microorganisms. Antioxidant and antimicrobial activities of the compounds 1 were found to be significant in comparison with standard in all the in vitro methodologies adopted. Thermal stability of the compound 1 was determined by using TGA, DTA, DSC analysis  and the results showed that endothermic peak is correlate with the value (189–190 ^oC) measured by a capillary method.

Abstract

Plants serves as a major source of food and derived proteins provides the basic maintenance of cellular functions, various plants derived non-steroidal weakly estrogenic compounds are defined as phytoestrogens. Isoflavones, rich in soybean, are currently receiving much attention because of their potential role in preventing and treating cancer and other human chronic diseases. All the available proteins in an organism are not used for the target purpose. Many antibiotics are available for the diseases but they have many side effects. Also the antibiotic resistance towards the organisms is increasing nowadays. So the idea to use natural food products as medicine came into existence. Soy is widely used in human nutrition and in livestock production is a rich source of isoflavones like genistein and daidzein. The impact of isoflavones on the growth and metabolism has received very little attention. In addition to the estrogenic or antiestrogenic effects via estrogen receptors, isoflavones are suggested to affect cell growth in intrinsic apoptosis via mitochondrial pathways. Daidzein is a natural estrogenic isoflavone. We report here that Daidzein weakly bind to apoptosis regulator Bcl-2 compared to other available drugs. To increase the agonist effect of Daidzein, a series of daidzein analogues have been designed by structural modifications. The pharmacophoric mapping and SAR study of basic scaffold of Daidzein resembled a significant active points, which helped in designing a combinatorial library of daidzein, implementing the molecular modelling and docking strategies helped in identifying approximate analogs with a favourable binding energy, screening of such compounds helps to validate the result against the toxic effects; considering the dock score and Lipinski rule of five the outliers are filtered out, further implementing parallel studies in wet lab and dry lab may help to find more approximate solutions against various infection, disease and disorders, where the drugs won’t be our food but the food will be our drugs.

Abstract

The present research work discusses the development of UV spectrophotometry method for estimation of Tetramisole Hydrochloride Simple and sensitive Spectrophotometric methods have been developed for the estimation of Tetramisole Hydrochloride [TH] in standard pure drug and pharmaceutical dosage forms. There is no official monograph for Tetramisole Hydrochloride Veterinary Powder. So approach of study is to develop a method which gives excellent result. The developed methods are validated in terms of Specificity and Selectivity, Linearity, Accuracy, Precision, Robustness, Solution Stability, as per International Conference on Harmonization Guidelines.  UV spectroscopic determination showed absorbance maxima at 213nm using Distilled water as solvent. Beer’s law is obeyed by showing linearity in the concentration ranges between 2-10 μg/ml respectively with a correlation coefficient of 1.000. The methods are applied for the determination of drugs in commercial soluble powder and results of analysis were validated statistically through recovery studies showing results from 98.42±0.41 to 100.01±0.19.The result of analysis were validated according to ICH guidelines and were found to be satisfactory. Hence present studies gives excellent method for determination of Tetramisole HCL.Method can be used for routine Quality Control and Stability Study analysis.

Abstract

Herbal plants are used as medicines in folk and traditional medicinal practice based on the plants and plant extracts. The present study was carried out to evaluate the hypoglycemic activity and antihyper glycemic activity of aqueous extracts of whole plant of Tinospora cordifolia in normal and in alloxan induced diabetic rats. The aqueous extract of Tinospora cordifolia (30mg/Kg, 100mg/Kg, 200mg/kg, 300mg/Kg bd.wt) and the dose(200mg/Kg) that produced an optimal reduction (30-40%)of blood glucose was selected for the study. Blood samples were collected at desired intervals of time and analyzed for blood glucose by GOD-POD method. Gliclazide a second generation sulfonyl urea was selected for the interaction study with that of the Tinospora cordifolia. The doses of gliclazide (1mg/Kg, 2mg/Kg and 4mg/Kg bd.wt) were given to normal and diabetic rats and the dose (2mg/Kg bd.wt) that produced an optimal reduction of blood glucose was selected for the study. The aqueous extract of Tinospora cordifolia has shown reduction in blood glucose level in both normal and diabetic rats which were compared with the standard drug gliclazide. To find the interaction of aqueous extract of Tinospora cordifolia with the standard drug gliclazide, the extract was given prior to the gliclazide administration. The results have shown that the prior administration of Tinospora cordifolia significantly increased the hypoglycemic and antihyperglycemic activity of gliclazide.

Abstract

Though oral delivery is the most convenient route of drug administration, it is limited to few drugs because they may either degrade in the gut or be poorly transported across gastro intestinal epithelium. An alternative way to such drugs is transdermal drug delivery. Among the different approaches available for drug release through this route, microneedles are the best choice as they pierce the barrier layer of stratum corneum more effectively without causing pain to the patient. Microneedles are an array of micro structured projections. They can be classified as solid or hollow microneedles.  In this article we will describe the need of microneedles, their types and applications.  This review also covers the different methods of drug delivery like poke and patch, poke and release, coat and poke, poke and flow. A lot of research is being done on microneedles which allow integration with other devices in order to release the drug in a more controlled manner and overcomes the possible limitations.

Abstract

Nonmotor manifestations are integral components of Parkinson disease (PD), and they have a greater impact on the health as well as on total quality of life. Nonmotor features of PD, such as dementia, may be an intrinsic feature of the disorder and persist regardless of the medication        on or off state ; some of the nonmotor features, such as psychotic symptoms, may be difficult complications of pharmacologic intervention for the treatment of the motor manifestations of PD. Difficult complications, such as psychosis and impulse control disorders, may respond to modify  of the PD treatment regimen at the risk of worsening motor symptoms. Thus, a balance must be required between controlling nonmotor manifestations and motor features of the disease . although the definition of Parkinson disease (PD) is based on the presence of motor features .Nonmotor manifestations are nearly related in PD, with behavior problems often being the most malignant. Almost all patients with PD have nonmotor and neuropsychiatric features, including sleep disturbances, compulsive and impulsive behaviors, autonomic dysfunction, and psychosis. The neuropsychiatric and behavioral features of PD can be classified as intrinsic features, which occur as part of PD, and iatrogenic features, which are complications that arise from treatments used to manage the motor symptoms of PD.

Abstract

The objective of the present work is set to assess the antioxidant and antibacterial properties of Albizia amara (F: Mimosaceae) leaves and seed. Estimations likely, total phenolic, total flavonoid, carbohydrate and protein estimations, in vitro antioxidant assays like, DPPH, superoxide, hydrogen peroxide radical scavenging studies, reducing power and inhibition of lipid peroxidation (TBARS) study were performed, tagged with disc diffusion antibacterial assay, for various solvent extracts with respect to each part. Results revealed the excellence of seeds compared to leaves with a significant SC₅₀/IC₅₀/EC₅₀ values, aligned with the estimations and antibacterial activity against the standards used. In particular, methanol extract has played a vital role, recording highest values in all the assays, in both leaves and seed, at times significant than the standard. Also numerous compounds have been identified through GC-MS, thereby to document the efficiency of Albizia amara. Albizia amara seeds seem to posses excellent scavenging activities than leaves and can be evaluated for the utility of the society after proper in vivo studies.

Abstract

A simple, sensitive and specific stability-indicating high-performance liquid chromatographic method was developed and validated for the determination of clomipramine hydrochloride in bulk. In the current study, extensive testing of clomipramine hydrochloride under various stress conditions were carried out as per the ICH guidelines Q1A (R2). The system consisted of a pump (Shimadzu, prominence, LC20AD), with 20µl sample injector, along with a UV/VIS (Shimadzu, prominence, SPD20A) detector at a wavelength of 252nm. Data was compiled using Shimadzu LC Solution software. The degraded products formed under various stress conditions were separated successfully from the drug by using a RESTEX Allure C18 Column (150 x 4.6mm, 5µm) with binary gradient conditions. Acetonitrile: phosphate buffer of pH 2.5 was used as mobile phase at flow rate of 1ml/min. Clomipramine hydrochloride was exposed to different stress conditions like hydrolysis, oxidation, photolysis and neutral decomposition.  Clomipramine hydrochloride, which was found to degrade considerably in acidic, alkaline and oxidative conditions, was found to be stable in photo and neutral conditions. Apart from the formation of minor degraded products under accelerated conditions, the drug was reasonably stable in solid state. A good linear relationship over the concentration range of 150-500µg/ml was shown. Validation of the method was carried out as per the ICH guidelines. The method developed was found to be precise, accurate, specific and selective.  Clomipramine hydrochloride showed degraded in 5M Hydrochloric acid at 80^oC, in 3% hydrogen peroxide for 5min the drug showed around 45% of degradation, when exposed to sunlight for 15 min, formed around 25-30% of degradation products. Statistical analysis shows that the method is reproducible and selective for the estimation of clomipramine hydrochloride in dosage form.

Abstract

A basic fact is that antioxidants are part of our daily diet, in fruits, vegetables, beverages, spices and herbs. Though antioxidant intake is the focus of increasing attention, the initial excitement regarding the potential health benefits of dietary antioxidants has diminished. Currently, it is even claimed that increased consumption of antioxidants as nutraceuticals might increase mortality. For several decades, it has been noticed that the antioxidant pendulum appears to swing vigorously from “only healthy” to “extremely toxic”, and from “natural antioxidants are the best” to “antioxidant cannot act”. Inappropriate antioxidant vitamin intake may lead to increased antioxidative stress by acting as prooxidant and increasing oxidative stress. Our diets typically contain safe levels of vitamins; therefore, high-level antioxidant supplements may upset the physiological balance between the RONS formation and neutralization.

Abstract

Ficus bengalensis Linn. belongs to family Moraceae. Stem bark of Ficus bengalensis Linn. reported to have antidiabetic activity. It is considered as safe, effective and economical for various ailments in Indian traditional system of medicine. In present study stem bark F. bengalensis was used. The bark of the plant was collected from Hapur region of Uttar Pradesh, India. Geographical and climatic conditions may affect the chemical composition of the plant drug and it may affect the overall quality of a crude drug. In this regard we planned our work as to standardize the crude drug and extract and its evaluation for antidiabetic activity and effect on various biochemical parameters in alloxan induced diabetic rats. The results of quality control parameter are given in result section and results of antidiabetic activity showed that diabetic rats treated with hydro alcoholic extract of stem bark of Ficus bengalensis (FBE) at a dose of 120 mg/kg significantly (P<0.01) reduced fasting blood glucose. This reduced 29.26% blood glucose after 21 days treatment and normalizes the lipid profile, renal profile and hepatic profile. Improvement in the histopathology of liver & pancreas of FBE treated rats confirmed its protective role in alloxan induced diabetes. Our research project is to make a polyherbal formulation by mixing four different crude drug extracts in an optimized ratio. The study was undertaken because F. bengalensis is one of the ingredients of this proposed formulation. It can be concluded that standardized extract of FBE possess antidiabetic activity and may be beneficial improving complications associated with diabetes mellitus. Thus it may be a better ingredient for antidiabetic herbal formulations.

Abstract

The present research work describe a rapid, simple, validated and stability indicating RP-HPLC method for analysis of blonanserin in bulk and tablet dosage form performed isocratically on symmetry Shield RP18 HPLC system (Milford, MA, USA) composed of 2998 PDA detector, quaternary pump with empower-3 software using as mobile phase 10 mM potassium dihydrogen orthophosphate and acetonitrile (70:30) P^H 5 at a flow rate of 1ml.min^-1, with PDA detection at 236 nm. Blonanserin elutes at a typical retention time of 2.75 min. The detector response was linear in the concentration range of 5-35 µg/ml. The intra -day and inter day variations found to be less than 2%, LOD and LOQ were found to be 2 µg/ ml and 6.09 µg/ ml respectively. It was degrade significantly under acidic, alkaline and oxidative conditions and remain stable in thermal and photolytic stressed condition, however the selectivity of the present method for blonanserin assay against their degradation product was confirmed and it was found to sufficiently stable in solution and mobile phase up to 48 hours. The present method optimized for analysis of blonanserin as per ICH Q2B guidelines was found to be simple, precise and reproducible. The empirical evidence based on the data obtained during this work conclude that the developed method undoubtedly reliable, stable  validated method useful for routine quality control of blonanserin  in bulk and tablet dosage form.

Abstract

The present study was conducted to investigate the histoarchitectural alterations in the liver of freshwater murrel, Channa striatus after exposure to sub-lethal concentrations (20 and 30mg/l) of lead nitrate for a period of 30 and 60 days under laboratory conditions. Histopathological analysis revealed the most common changes in the liver of fishes at both doses of Lead nitrate like nuclear degeneration, deshaped hepatocytes, necrosis of hepatocytes, cytoplasmic degeneration, loosening of hepatic tissue, vacuolation in cell cytoplasm, nuclear vacuolation, eccentric nuclei and necrosis of cytoplasm. Exposure to sub-lethal concentrations of Lead nitrate caused dose and duration dependent histoarchitectural alterations in the liver of Channa striatus. The present investigation illustrates that the presence of high concentration of Lead nitrate in water are stressful to fishes.

Abstract

Interaction of copper soaps (derived from common fatty acids) with nitrogen and sulphur donor ligands is worth noticeable for their biocidal and pharmaceutical characterization. It creates zeal to study the micelle features and colloidal behavior of such novel heterocyclic complexes as it indirectly plays a significant role in their selection in various fields for multiple applications. So, aforesaid class of complexes were synthesized and their identity was confirmed by (IR, NMR, and ESR) spectral data and purity was checked by TLC. Density, Molar Volume, Apparent Molar Volume of these complexes was investigated in non-aqueous solvent at various concentrations by Springel Pyknometer to understand the nature, critical micelle concentration and micelle characteristics of the complexes. Overall, the CMC values were found to be decreased with increasing average molecular weight of soap complex. The solute – solute interactions were found to be greater before CMC whereas solute – solvent interactions was found greater after CMC.

Abstract

The oral route is the most frequently used route for the administration of drugs. Many of the pharmaceutical dosage form are formulated as sustained release dosage form to retard the release of a therapeutic agent in such a way that it prolonged its appearance in the systemic circulation and also sustained its plasma profile duration. Tablets offer the lowest cost approach to sustained and controlled release dosage forms. In an oral extended- release dosage forms Matrix tablets serves as an important tool. So the problems like patient compliance, frequent administration, drug targeting, local side effects, and fluctuations in blood concentration levels, associated with their counterparts, the conventional dosage forms were solved. In this research work Salbutamol Sulphate were selected as a model drug and HPMC and Ethyl cellulose were selected as a rate controlling polymer. The matrix tablets were formulated by wet granulation technique.

Abstract

A stability indicating reverse phase high performance liquid chromatographic (RP-HPLC) method is presented for the quantification of Sitagliptin (STG) and Simvastatin (SMV) in bulk drug and in combination tabled dosage form. Separation was achieved under optimized chromatographic condition on a BDS hypersil C₁₈, (250mm × 4.6mm × 5µm) column. The mobile phase consisting of 0.05M phosphate buffer (pH 4±0.02 adjusted with o-phosphoric acid): acetonitrile (70:30 v/v). An isocratic elution was achieved at a flow rate of 1 ml/ min at ambient temperature. The detection was carried out at 252 nm using shimadzu uv-visible detector SPD-20AT. The total run time for the developed method was 10 minutes. The calibration curve was linear in the concentration range of 7.5-52.5 μg/ ml (r²- 0.997) and 3.5-10.5 μg/ ml (r²-0.998) for STG and SMV respectively. The amount of drugs present in the formulation (Juvisync) was found to be 99.81 ± 0.73 and 99.97 ± 0.61 for STG and SMV respectively and no interference from the excipients was observed. The method was validated statistically and the values were found to be within the acceptable limits. In conclusion, the presented method was found to be simple, specific, and rugged based on the validation results which were within the acceptable limits. Hence it can be applied for routine analysis of STG and SMV in tablet dosage form. 

Abstract

Human papillomavirus is a DNA virus that is most common on sexually transmitted viruses in the world. This is responsible for benign as well as malignant. These are also involved in the development of cervical cancer. Histone decetylase (HDAC) inhibition focused a new window to the approach of designing HDAC inhibitors (HDACi) due to their low cytotoxic profiles and oncogene function of human papillomavirus. Recently class II is considered as the main target for this purpose. Therefore in the present work we just modeled HDAC II to generate a better crystallographic structure using MODELLER 9.12 and validated using PROCHECK. More than 95% of the residues were in the favored region & additional allowed region of Ramachandran plot. Active site was determined using DoGSiteScorer. Then some novel inhibitors having common pharmacophore with that of suberoyl anilide hydroxamic acid (SAHA) was designed virtually and docked using MAESTRO 9.2 (Schrodinger). The binding affinity, drug-likeliness, toxicity of the newly designed inhibitors were compared with the standard that is SAHA. The RMSD values of the inhibitors are found to be within 2.0 Å. The binding energy of the newly designed molecules are found to be quite similar to that of suberoyl anilide hydroxamic acid, which is -8.03 kcal/mol. These molecules are also found to be less toxic than others, so these can be used as good scaffold for future progress in designing of potent anti cancer agents.

Abstract

It has always been an aim for a pharmaceutical company to create a drug that would be ideal with high specificity, high affinity, solubility and safety. These attributes backed up by low cost in manufacture, easy to formulate, simplicity to deliver and proper pharmacokinetic profile seems to be unattainable characteristic in most of the drugs because of the variety of their biophysical property. Peptides and proteins have become the drugs of choice for the treatment of numerous diseases as a result of their incredible selectivity and their ability to provide effective and potent action. The past decade saw an increased interest in formulating and delivering biological drugs for a range of diseases with significant unmet medical need. Unlike conventional small molecular drugs, clinical development of these types of drug will not be possible without some sort of sophisticated pharmaceutical technology. Various strategies have been followed to overcome such blocks and to develop safe and effective oral delivery systems for proteins. This review indicates few outlines about problem statement, background information, research competition, sustained released, infusion devices designs and new frontier future work for the oral route for peptide and protein administration. However, we believe that only further research into delivery systems can make it possible for the oral route to represent a viable route of administration for peptide and protein drugs, improving convenience for, and compliance from patients who would benefit from these drugs.

Abstract

The aim of the present study is to improve the aqueous solubility and dissolution rate of ritonavir a poorly soluble drug which makes it low bioavailable. To achieve the stated objective a solid dispersion formulation of ritonavir was prepared by solvent evaporation technique using polyvinyl pyrollidone K - 30 and Polyethylene glycol 6000 as carriers. Six different formulations were prepared with varying ratios of drug and carriers (1:1, 1:2, 1:3). The optimum drug – to – carrier ratio of PEG 6000 (1:3) enhanced solubility nearly 6.3 times more as compared to pure drug.  In vitro drug release studies exhibited cumulative release of 98% in 30 min as compared to 45% release for the pure drug.  In the next step hard gelatin capsules filled with ritonavir solid dispersions together with other additives were prepared and they were evaluated for micrometric properties and in vitro drug release studies and all the resulting data is within the limits with increased dissolution rate. These results suggest that solid dispersion of ritonavir using PVP K30 and PEG 6000 as carriers is a promising approach for oral delivery of ritonavir. The amorphous form of drug and increase in surface area helped in increasing the solubility and finally dissolution rate of drug.

Abstract

The need for generating particles for various applications such as for enhanced solubility, for pulmonary drug delivery, controlled release application, taste masking or generation of nanoscale particles for targeting specific drug sites of action, protection of drugs against degradation, organ or tissue and delivery of biological molecules such as protein, peptides and oligonucleotides, has scientists reporting on numerous approaches to modify therapeutic potential of a drug candidate by particle engineering.Particle engineering techniques are developed to modifyphysicochemical, micromeritic and biopharmaceutical properties of the poorly soluble drugs and hence solubility. Various particle engineering processes like supercritical fluid technology, cryogenic technology, nanomilling, sonocrystallization, spray drying, direct controlled crystallization and electrospraying methods were developed based on the drug properties and requirement of nanoparticles characters.This article highlights several commercially available particle engineering processes recently reported in the literature. The evolution and innovation in particle engineering have progressed exponentially because of new techniques of measuring and characterizing these particles. The new frontiers in particle engineering are just opening up and it is likely that the particle engineering techniques will enhance the therapeutic applications of new and well established drug candidates.

Abstract

Essential oils produced by plants have been employed from time immemorial against infectious diseases, and are also used nowadays as ethical medicines by inhalation therapy to treat acute and chronic bronchitis, acute sinusitis, inflammation on the trachea and asthma. Artemisia, belongs to Aster family have many species with proven medicinal potentialities. Most Artemisia species produce essential oil used in traditional and modern medicine in the cosmetics and pharmaceutical companies. In the present study, the essential oil from Artemisia japonica Thunb. and A. nilagirica (Clarke) Pamp. was isolated by hot continuous hydrodistillation and subsequently analyzed by GC-MS. 19 and 30 compounds were noticed in the essential oil respectively. The predominant phytochemicals in the essential oil of A. nilagirica were camphor (41%), 8-Cineole (17.0%), Borneol (8.6%) Artemisia ketone (6.4%) and β-Thujone (6.0%). Meanwhile A. japonica contain Linalool (70.4%), Caryophyllene oxide (6.7%), trans-Linalool oxide (4.5%), p-cymene (3.4%) and 1, 8-Cineole (2.3%). Subsequently, the bactericidal potentiality of essential oil was analyzed using disc diffusion and micro broth dilution assay against 2 Gram-positive, 6 Gram-negative bacteria and a fungi. The microorganisms were used Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, Klebsiella pneunomoniae, Proteus vulgaris, Bacillus subtilis, Corynebacterium diphteriae and Candida albicans. Remarkable microbicidal activities were seen in terms of MIC and MFC against Klebsiella pneumonia, Staphylococcus aureus and Candida albicans. The results were further substantiated by time kill analysis and spore inhibition assay. The mode of action was evaluated by membrane leakage assay of sugar, ions and protein. Biological activity of cells was also evaluated in terms of dehydrogenase assay. Significant reduction was observed in the affected bacterial cells than control suggests the microbicidal action of the essential oil may be either depolarizing the membrane or inhibiting respiratory enzymes. Further studies are warranted to isolate, purify the lead phytochemical and its molecular mechanism of action.

Abstract

The increasing proportion of older people in the total population is being observed in many countries with known psychosocial and health economic consequences. More than 15 % of elderly people are suffering from dementia and the alteration in serum vitamin B₁₂ levels have been associated with ageing, diminished neuronal development and cognitive impairment. The aim of the study was to investigate the relationship between plasma vitamin B₁₂ and cognitive function in elderly. The study was conducted in Department of Biochemistry with collaboration with Department of Medicine and Department of Psychiatry, MMIMSR, Mullana. We assessed the cognitive function in 100 elderly individuals over 60 years divided into two groups: a) 50 individuals with dementia; and b) 50 healthy controls. They were assessed with Hindi Mental Status Examination (HMSE). Blood samples were analyzed for serum vitamin B₁₂ by ELISA, and the results were statistically evaluated. Group a had significantly lower levels of serum vitamin B₁₂ than group b, and the lower levels of serum vitamin B₁₂ were predictive of cognitive decline (p<0.05). Thus, lower levels of serum vitamin B₁₂ are associated with cognitive impairment in elderly individuals. Possible reasons for this relation include brain atrophy and white matter damage, both associated with vitamin B₁₂ levels. It is thus suggested that the elderly in particular should be encouraged to maintain a good, rather than just adequate, vitamin B₁₂ status by dietary means. Randomized trials are required to determine the relevance of vitamin B₁₂ supplementation for prevention of dementia.

Abstract

Plants have been an important source of medicine for thousands of years. Even today, the World Health Organization estimates that up to 80 percent of people still rely mainly on traditional remedies such as herbs for their medicines. Its civilization is very ancient and the country as a whole has long been known for its rich resources of medical plants. Studying the plants used in folklore medicine promises to yield commendable results as investigating their antibacterial activity has led to a better understanding of the use of traditional medicines as potential drugs in addition to contemporary drugs. Many efforts have been done to discover new antimicrobial compounds from various kinds of sources such as soil, micro organisms, animals and plants. One of such resources is folk medicine and systematic screening of them may result in the discovery of novel effective compounds. Tridax procumbens Linn. (Family-Asteraceae; Common name-Dhaman grass) is a common herb in India. It is employed as an indigenous medicine for a variety of ailments including jaundice. The plant also has hepatoprotective activity and it is used in Ayurveda in various liver disorders. Phytochemical screening of the plant revealed the presence of tannins, flavonoids, saponins and alkaloids. Antimicrobial activity of Tridax procumbens young leaf extracts were investigated by agar disc well-diffusion method against selected human pathogens. The leaf extracts showed inhibitory activity against the tested organisms. The results lend credence to the folkloric use of this plant in treating microbial infection and shows that Tridax procumbens young leaves could be exploited for new potent antimicrobial agents.

Abstract

This work studies the effectiveness of immobilized Lipase enzyme for pollution degradation and BOD & COD reduction of the polluted water. Biodegradation process performed in four batches with polluted water sample and immobilized beads. Beads were prepared with the use of 3% of sodium alginate and 2% of calcium chloride with Lipase enzyme. After the process both water sample (before & after process) were compared. It is found that after four batch process Lipase degrade effectively 72.07% pollution of sample water and 69.10% & 69%. of COD & BOD respectively. This study showed the effectiveness of immobilized Lipase enzyme for reduction of BOD & COD and pollution level from polluted water.

Abstract

Diabetes is a group of metabolic diseases in which a person has high blood sugar, either due to lack of production of insulin or due to the non-responsiveness of the cells to the insulin produced. Madhusanjeevini powder is an herbal formulation containing many medicinal plants which are widely used to treat diabetes. The present research is carried out to determine the preliminary phytochemical screening and quantify the amount of phytoconstituents present in the selected herbal formulation. Preliminary phytochemical screening was performed and it indicated the presence of phenols, glycosides, alkaloids, tannins, flavonoids, terpenoids etc. Hence it is necessary to quantify the amount of phenol, flavonoid, alkaloid and tannin present in selected herbal formulation .The amount of  phenol ,flavanoid ,alkaloid ,tannin were found to be 11.72±0.0062,16.35 ±0.0057 ,28.05± 0.0082 and  9.58 ±0.0010 respectively.

Abstract

A liquid chromatographic method has been developed and validated for the determination of the of Torsemide and Amiloride hydrochloride. Effective chromatographic separation was achieved on an eclipse Enable -C18 (4.6 mm X 250 mm, 5µm) column using gradient reverse phase technique. The mobile phase employed was ACN: 50Mm Potassium phosphate buffer (40:60), the pH was adjusted to 3.0 by ortho phosphoric acid. The flow rate was maintained at 1.0 mL/min and elute was monitored at 288nm. A linear response was observed over the concentration range 2-12µg/mL (R2=0.999) of AmilorideHCl and the concentration range 2-12 µg/mL (R2=0.998) of Torsemide. The limit of quantitation (LOQ) and limit of detection (LOD) for Torsemidewere 0.007 and 0.02 µg/mL, respectively and for AmilorideHClwere 0.02 and 0.07 µg/mL, respectively. The method was successfully validated in accordance to ICH guideline Q2. The RSD for intra-day and for inter-day precision were found to be lesser than 1.5% forAmilorideHCl. The RSD for intra-day and for inter-day precision were found to be lesser than 1.7% for Torsemide. The percentage recovery was found to be greater than 98.0 %.The method was found to be accurate, precise, linear, specific, sensitive, rugged, robust and stability indicating.

Abstract

Niosomes are novel/particulate drug delivery that promotes formations of vesicles by hydrating the mixture of cholesterol and non-ionic surfactants. Niosomes are vesicles composed of non-ionic surfactants, which are biodegradable, relatively nontoxic, more stable and inexpensive, an alternative and superior to liposome will be acts as a target drug delivery system/CDDS. Niosomes have become popular in the field of topical drug delivery due to their outstanding characteristics like enhancing the penetration of drugs, providing a sustained pattern of drug release, increasing drug stability and ability to carry both hydrophilic and lipophilic drugs. This article reviews the current deepening and widening of interest in research activities in such a way that to improve entrapment efficiency can be expected to prolong the duration of the drug in systemic circulation. They possess an infrastructure consisting of hydrophilic, amphiphilic and lipophilic moieties together and as a result can accommodate drug molecules with a wide range of solubilities. The present article highlights the various factors which governs the formation of niosomes.

Abstract

A simple, precise and accurate high performance thin layer chromatographic (HPTLC) method was developed and validated for the simultaneous determination of Capsaicin, Gamma Linolenic Acid (GLA) and Ferulic acid in the developed herbal formulation. The separation was carried out on Merck TLC aluminum sheets of silica gel G60 F254 of 200 µm thickness using Toluene: Ethyl acetate: Diethyl ether (7:3:1 v/v/v) as mobile phase and densitometric analysis of compound was carried out in absorbance mode at254 nm. The aforesaid mobile phase gave well defined peaks at R_fvalue of 0.31 ± 0.03 for Capsaicin, 0.81 ± 0.03 for Gamma Linolenic acid and 0.54 ± 0.03 for Ferulic acid. The linear regression analysis data for the calibration plots for Capsaicin, GLA and Ferulic acid showed good linear relationship with regression coefficient (r²) of 0.999,0.999 and 0.995 respectively; in the concentration range of 100-500 ng/spot,200-5000 ng/spot and 200-1000 ng/spot respectively. The limit of detection and quantitation were 116.7 and 353.7 ng/spot, respectively for Capsaicin and 40.5 and 126.4 ng/spot, respectively for GLA and 45.8 and 38.27 ng/spot, respectively for Ferulic acid. The method was validated for linearity, accuracy, precision, specificity, robustness, limit of detection (LOD)and limit of quantification (LOQ) as per ICH guidelines. In conclusion, the statistical analysis of the data showed that the method is reproducible and selective for estimation of the three compounds. The proposed developed HPTLC method can be applied for identification and quantitative determination of Capsaicin, GLA and Ferulic acid in their extracts and herbal formulation.

Abstract

The present research work is to formulate fast disintegrating tablets of an Anti mucolytic drug, Ambroxol hydrochloride with sufficient mechanical integrity and achieving faster disintegrating with patient convenience using natural super disintegrants such as guar gum and karaya gum by Direct compression technique. Preformulation studies such as Angle of repose, bulk density, tapped density and carr’s compressibility index for all six formulations were done. All F6 formulations were compressed after preformulation studies. The compressed tablets were evaluated for physical characteristics such as weight variation, Friability, Hardness, Disintegration test and In Vitro dissolution studies. All the formulations shows compliance with Pharmacoepial standards. In vitro dissolution studies were done for all formulation for 30 mins in USP type II (paddle type) apparatus by using phosphate buffer of pH6.8 shows 98.91%.The release kinetics were analyzed by using zero order, First order, Higuchi’s plot and Korsemeyer’s equation for the optimized formulation.The regression coefficient is obtained i.e., R² = 0.998 with n value of 0.45 following Fickian transport. No significant difference were seen in formulation F3 by doing stability studies.The results suggest that developed Fast disintegrating tablets of Ambroxol Hydrochloride shows immediate release leading to improve Patient convenience according Disintegration test and In Vitro dissolution studies.By comparing the two natural polymers in all six formulations it is concluded that guar gum of 18 mg is showing highest drug release than the karaya gum of 18 mg according to In Vitro dissolution studies.

Abstract

Kani tribal communities of Kerala meet their healthcare needs by using herbal products and preparations based on traditional knowledge for first aid remedies to treat cough, cold, fever, head ache, poisonous bites and some simple ailments. Bryophytes are transitional nonvascular plants amphibians which prefer to grow in dampy conditions. Related with the taxonomy or medicinal use, this group was poorly documented. In this juncture, a survey was carried regarding medicinal utility of lower plant group – bryophytes among the Kani tribes. In the present study a total of 35 medicinal bryophytes belonging to 3 groups have been documented. These plants were used to treat various diseases like liver, cardiac ailments, skin allergies, inflammation, diarrhoea and sterility. Marchantia polymorpha, Rhodobryum giganteum, Ceratodon purpureus and Bryum argenteum ranks the priority in terms of usage. Oral interview with local inhabitants and vendors suggests that the ethnic practice is still strong. The efficacy and safety of all the reported ethnomedicinal bryophytes needs to be evaluated for phytochemical and pharmacological studies including toxicity studies.

Abstract

The mounted expansion of industrial enzymes in global market emphasizes the screening of natural resources. Thermotolerant actinomycetes have a remarkable enzymatic potential but till now natural resources due to the difficulties in isolation and maintenance of pure culture explored only up to a extend. For this purpose, samples were collected from various raw deposits. The isolation and screening by various methods i.e., Direct plate method, Dilution plate method and Warcup’s soil plate method are used to screen out enzymatically active thermotolerant actinomyctetes strains. Enzymatic potential of the isolates were examined by using multilevel screening.  Ninety two thermotolerant actinomycetes strains were isolated from ten diverse habitats. Sediment samples were also characterized for physiochemical properties. On the basis of cultural and microscopic characteristics, the isolated genera were identified as strains of Thermopolyspora, Thermomonospora, Streptomyces, Thermoactinomyces and Pseudonocardia. The most dominant genus (55%) was Streptomyces while Pseudonocardia (6%) was lowest in occurrence. Out of the total isolates, 40 strains showed amylolytic potential while 14 strains were positive for production of amylase and xylanase simultaneously. The most suitable amylase and xylanase producing strain after tertiary screening was Streptomyces sp. MSC702. The maximum activity of amylase and xylanase were 234.54 IU/ml and 28.40 IU/ml, respectively using wheat straw as a substrate in submerged fermentation.

Abstract

A simple, rapid, precise, accurate RP-HPLC method has been developed and validated for the simultaneous estimation of Lamivudine, Zidovudine And Nevirapine in tablet dosage form. Chromatographic separation was achieved with mobile phase consisting of  Acetonitrile, Methanol and Phosphate Buffer pH 5.0±0.3 in the ratio of 20:30:50 v/v with Waters symmetry C18 (250 × 4.6 mm × 5 µm), column at a flow rate of 1 mL/min and detection wavelength was  246 nm.  The retention times of Lamivudine, Zidovudine And Nevirapine were found to be 3.085 min, 3.680 and 4.830 min respectively. The linearity range for  Lamivudine, Zidovudine And Nevirapine  were found to be 30-70 µg/mL, 60-140 µg/mL and 39.9-93.2 µg/mL, respectively. The coefficient of correlation, (R²) for Lamivudine, Zidovudine And Nevirapine were found to 0.999, 0.999 and 0.999, respectively. The method was validated as per the ICH guidelines and can be employed for routine quality control analysis.

Abstract

A simple, precise, accurate and rapid stability indicating High performance liquid chromatography method was developed and validated for the determination of Dabigatran etexilate in bulk and capsule dosage forms. Chromatographic separation was achieved by using Mobile phase "A"(phosphate Buffer pH4.5& Acetonitrile in the ratio 50:50) with Hypersil BDS C18 (150 × 4.6 mm, 5μm) as stationary phase. Diluent with composition of Acetonitrile and water in the ratio 80:20 is used for dilutions. Flow rate was optimised to 1.2 ml/min and effluents were monitored at 230 nm. The retention time was around 3.19. Linearity was observed over a concentration range of 9-113 μg/ml with correlation coefficient of 0.999.Stress conditions of degradation in acidic, alkaline, peroxide, thermal and UV radiation was studied and found that  Dabigatran etexilate  is sensitive to acidic and thermal comparative to other stress conditions. The method is validated as per ICH Guidelines and the results were well within the limits.

Abstract

Cytisus scoparius, a widely used traditional Chinese herb, belongs to the family of Leguminosae, and is taken to nourish Yin and invigorate the heart & liver in traditional Chinese medicine (TCM) and has a very high medicinal value. In recent decades, a great number of chemical and pharmacological studies have been done on Cytisus scoparius. More than 70 compounds including quinolizidine alkaloids, alkenol, benzenoid, phenyl propanoid, flavonol, carotenoid, alicyclic compounds, alkanone, steroid, lipid and monoterpene, as well as other trace elements have been found in the herb. Studies show that Cytisus scoparius and its active principles possess wide pharmacological actions on the blood system, immune system, endocrine system, cardiovascular system and the nervous system. Currently, the effective compounds or active constituents have been screened for the pharmacological activity of Cytisus scoparius and the highest quality scientific data is delivered to support the further application and exploitation for new drug development.

Abstract

Coconut palm (Cocos nucifera L.), is a versatile crop with multifold uses, important for the livelihood and security of people in Kerala. Kerala Root (wilt) disease (KWD) is a major production constraint causing an estimated yield loss of 968 million nuts in southern India. Affected palms show bending of leaflets (flaccidity), foliar yellowing, and marginal necrosis. Phytoplasma have been observed to be associated with this disease by electron (EM) and transmission microscopy. Pathogenesis induces biochemical and physiological changes in host plants that may leads to the production of ractive oxygen species (ROS) such as superoxide anion, hydrogen peroxide. As an initial part, extracts from healthy and diseased palm were screened for NADPH oxidase activity to know the level of superoxide anion production and to analyze the hypersensitive response developed in palm due to phytoplasma infection. NOX activity ranged from 132 U/mg protein in healthy to 373.5 U/mg in diseased. Subsequently,  NADPH oxidase (NOX) of Kerala wilt diseased coconut palms was extracted and purified through ammonium sulfate, gel filtration and HPLC chromatography. The purification factor for NOX was 856 fold with 5.2% yield. The enzyme was characterized for thermal stability, pH and kinetic parameters. The molecular mass of purified NOX was approximately 49 kDa estimated by gel filtration chromatography.  The purity was checked by ingel showing a single prominent band. The pH optimum was found to be 7.0. The enzyme had a temperature optimum at 30°C and was relatively stable at 70ºC with 48% loss of activity. Inhibitors such as Diphenyleneiodonium (DPI), sodium diethyldithiocarbamate (NaDCC) and sodium azide (NaN₃) significantly inhibit NOX activity. NADPH was found to be the efficient substrate for NOX considering the V_max/k_m ratio. The data obtained in this study may help to understand the properties of NOX related to superoxide anion production due to hypersensitive response of the palm. Further works are designed to trace the ROS cycle in the KWD palm and to design a biocontrol as remedy for the disease.

Abstract

The aim of our study is to analyze the relationship between dental caries, Alkaline Phosphatase and Calcium in young adults between the age group of 20 to 30 years from South Canara district, Karnataka with varying caries experience as determined by their caries progression. Eighty subjects from the outpatient department ranging between 20 to 30 years of age were screened and evaluated for their caries experience. Based on their level of caries a total of 80 subjects were selected and divided into four groups of 20 subjects each as follows; Group 1: Enamel Caries , Group 2: Dentinal Caries,  Group 3: Pulpal Caries,  Group 4: Control Group. The saliva was collected and analyzed for the presence of Alkaline Phosphatase and Calcium levels in saliva and correlated to the same levels in serum. According to the present study there was an increase in the levels of caries with increase in the levels of Alkaline Phosphatase levels in both serum and saliva. Calcium levels in serum and saliva were decreased in caries prone individuals, hence showing a significant correlation between serum and salivary Alkaline Phosphatase and Calcium levels. Hence it can be used as a biochemical indicator in evaluating the susceptibility of caries. However further investigations need to be done.

Abstract

The aim of the present research is to study the influence of Seaweed Liquid Fertilizer of Gracilaria dura (Ag.) J.Ag. on seed germination, shoot length, root length, biochemicals and pigment content of Pennisetum glaucum (L.) R.Br. The Seaweed Liquid Fertilizer prepared from Gracilaria dura (Ag.) J.Ag. was observed to have the positive effects on the shoot and root length of Pennisetum glaucum (L.) R.Br. The biochemicals such as total carbohydrates, proteins, lipids, phenols, chlorophylls and carotenoids also increased when the Pennisetum glaucum (L.) R.Br. treated with high concentration of Seaweed Liquid Fertilizer. The seed germination, shoot length, root length, biochemical and pigment content was found maximum at 10% SLF. Hence Gracilaria dura (Ag.) J.Ag. can provide dietary alternatives due to their nutritional values and can be used as biofertilizer for the growth of Pennisetum glaucum (L.) R.Br.

Background: Combined formulated  oral administration of Atorvastatin (ATVS) and Olmesartan (OLM) drugs to cardiovascular patients, reveals  negative results rather than its individual therapy. Which was sensitized on quantification of  bioanalytes of  plasma through LCMS/MS. Objective: Target was to trace  the marked bioanalytical variation in the blood plasma after administration of combined formulation, to investigate the post marketed rumor on its efficacy. Method:  For the study of this post marketing research, specific human patient volunteers were selected according to the required criteria along with ethics committee permission.  A sensitive, rapid and precise method was developed and validated to quantify  Aldosterone (ALD) , Angiotensin(ANG-II) and the Mevalonate (MVA) through LCMS/MS over twelve cardiovascular patients. Concentration of each bioanalytes were determined in three stages- Without drugs, with single drug (Olmesartan/Atorvastatin) and with their combination. The bioanalytical  levels were checked on correlating with patient’s physiological parameters. Result & Discussion: Comparative and correlative studies within these bioanalytes was established. The selectivity, specificity, linearity, precision, accuracy, extraction recovery, limit of detection (LOD) & limit of quantification (LOQ), stability were the necessary tools of validation of the developed methodology. And significance of each bioanalyte datas were estimated on p-values ≥ 0.001. Thus, lower value of Aldosterone and Angiotensin-II in single drug than its administered combination and equal concentration of Mevalonate in those stages, was estimated. Conclusion:  This concludes that the combined formulated cardiovascular drugs neither shows synergistic nor effective compared to a single drug. Thus, the combination of Atorvastatin & Olmesartan is non-effective. It might be reasons of competitive carrier receptor bindings in hepatic region.

Abstract

Background: Hypertension (HTN) with coronary heart disease (CHD) is one of the leading causes of death in worldwide. There are many studies conducted in hypertension with CHD. The aim and objectives of the present study is to analysis the different patterns and identifying the various parameters of DRPs as well as categorization of DRPs in the hypertensive with CHD who visits at a tertiary care teaching hospital.Method: The observational prospective study. The present study was conducted in hypertensive subjects with Coronary heart diseases Outpatient and Inpatient of department of medicine at a tertiary care teaching hospital located at Chidambaram, Tamil Nadu and South India. Study was conducted for two months (August and September 2013). The identification and categorization of DRPs was according to the Pharmaceutical Network Care Europe (PCNE) tool version 5.01. Results: 50 prescriptions were identified for this study. Among 35 prescriptions were analyzed clinical DRPs and 15 prescriptions were analyzed of technical DRPs. Among 35 prescriptions 75 clinical DRPs was detected with frequently identified clinical DRPs (P1 – P6) were (P1) adverse drug reactions 9(18%), (P2) drug choice problem 11(22%), (P3) dosing Problem 5(10%), (P4) drug use problem 11(22%), (P5) Potential drug–drug interactions 8(16%) were detected. Also (P6) ‘others’ were insufficient awareness of health and diseases 31(62%) and technical DRPs were identified such as “missing dose” 4(8%) and “unreadable prescription” 4(8%) and “missing diagnose” in the prescription 7(14%). The identification and categorization of causes of DRPs were observed that, 75 DRPs were detected with 92 causes of DRPs on hypertension with CHD. In that, (C2) ‘Drug use process’ 28(56%), (C3) Subject unawareness information for drug treatment’ 21(42%) cases, and then followed by (C4) ‘Subject/Psychological’ 43(86%) cases of high frequency of causes of DRPs presents in this study.Conclusion: The Pharmacist was identified 75 number of clinical DRP and 15 number of technical DRP presents in this study using PCNE tools and also elderly subjects were specially observed and found that there is no significant difference and categorized into six domains, and causes of DRP in hypertensive subjects associated with CHD at tertiary care teaching hospital.

Abstract

COMM Domain containing or COMMD proteins are a recently discovered group of factors defined by the presence of a unique motif in their extreme carboxy termini (Copper Metabolism MURR1 or COMM domain). This protein family is comprised of ten members which are widely conserved throughout evolution and share certain functional properties. A number of seemingly discrete functions have been ascribed to these factors. These include the regulation of the activity of the transcription factor NF-κB, copper homeostasis, the function of the epithelial sodium channel, cell cycle, inhibition of HIF (hypoxia inducible factor), innate and adaptive immunity, apoptosis, and oncogenesis, besides the ability to regulate various viral genomes including human immunodeficiency virus-1 (HIV-1) and Epstein Barr virus (EBV). A unifying mechanism that would explain all these events is lacking at the moment, but recent studies suggest the possibility that regulation of the ubiquitin pathway may be at the basis of many of the functions of the COMMD protein family. It is concluded that modulation of COMMD proteins or their molecular targets may find therapeutic applications in HIV, EBV, Wilson’s disease etc.

Abstract

The algae spirulina has been considered for use as a supplementary protein. It is a blue green algae having strong antioxidant activity and provokes a free radical scavenging enzyme system. The cyanobacterium Arthrospira platensis can be used to produce single cell proteins (SPN), fatty acids (which can be used for bioenergy), food and feed supplements, and biofixation of CO₂. SPN regulate gene expression and counteract oxidative stress. Its impact on communities and individuals is more dramatic in Sub-Saharan Africa, where it is compounded by widespread poverty and generalized high prevalence of human immunodeficiency virus (HIV). SPN improve the nutritional status of malnourished HIV-infected patients and nutritional rehabilitation improves on immune status with a consequent drop in viral load. Spirulina can prevent the LPS induced decrease in NPC proliferation; probably spirulina protects by non-stem cell autonomous mechanisms. A diet enriched with spirulina and other nutraceuticals may help protect the stem/progenitor cells from insults. Spirulina maxima prevents fatty liver development induced by carbon tetrachloride (CCl₄). It is concluded that the use of spirulina should be encouraged in patients suffering from malnutrition, immuno-suppression, hepatic and neural compromise, etc. although further investigations on the antiviral effects of this alga and its clinical implications are strongly needed.

Abstract

In the present work an attempt has been made to prepare Ranolazine extended release tablets where  polymers were blended with the drug and excipients. The compatibility determined by FTIR  and about nine different formulations were developed by wet granulation method. Formulation F9 containing 500mg of drug contains Micro Crystalline Cellulose, Carbopol  940, Hydroxyl Propyl Methyl Cellulose and opadry orange as the film coater  released  99% of drug  at 24hrs of time intervals under different media like 0.1HCl and phosphate buffer(7.4) and release followed zero order kinetics. All tablets were good fit for Higuchi plot (R²=0.99) therefore diffusion mechanism was found and superimposable with the market product RANEXA. Accelerated stability studies conducted at 40⁰c/75%RH for three months as per ICH guidelines.

Abstract

In the existing scenario of drug discovery and development there is an overabundance of diseases with more-complex pathological mechanisms, for which the classic ‘one target, one drug’ pattern has partially or completely unsuccessful. In these circumstances, drugs acting on multiple targets could offer superior efficacy profiles compared with single-target drugs. Hence in the current investigation as a part of our search for new computational methods, we could have established a novel In Silico method i.e. LPIIFD (Ligand Protein Inverse Induced Fit Docking) to study the inherent mechanism of action of a series of 1,3,5-triazine-Schiff base conjugates possessing potential antitubercular activity against Mycobacterium tuberculosis H37Rv. In the initial part of this LPIIFD study we provide an introduction to the role of computers in drug discovery and development. In the next part we reflect on the general introduction to tuberculosis and ten potential antitubercular drug targets followed by the description of study protocol. It is our aim to provide a brief manuscript on the results obtained in this present investigation.

Abstract

Solubility and permeability plays an important role in development of dosage form. Benchmark for solubility and permeability is the Biopharmaceutics Classification System (BCS) which demonstrates four classes based on solubility and permeability. It enables the scientist to modify chemical structure of active pharmaceutical ingredient so as to optimize chemical properties. Oral dosage form have the rate limiting steps as dissolution and permeability for which BCS plays an important role. Biowaver can be given for some dosage forms based upon its BCS classification system. Dissolution number, dose number and absorption number are the fundamental basis for BCS classification. It is also a guideline for determining the conditions under which in vitro-in vivo correlations are expected. Solubility, permeability and dissolution are the class boundaries of the BCS. As per regulatory aspects during the process of generic drug development in vitro dissolution can replace bioequivalence studies.

Abstract

Background: Globally, India is leading in the world as far as numbers of HIV positive cases, and there is paucity of studies related to socio-demographic profile of HIV/AIDS patients in Guntur. Methodology: This socio-demographic study was conducted on HIV patients attending welfare programs in AMG INDIA INTERNATIONAL ORGANIZATION, Chilakaluripet, Guntur district on 8^th and 9th of every month. At the time of study, 1020 patients were registered however study was done on 1000 cases of which 500 were males and 500 were females. Data collection was done by personal Interview and from case record. Results: Most of the study individuals (98.3%) belonged to the age group 15-45 years, Majority of the study individuals were married (75.50%). Unprotected sexual route was the most common (91.5%) mode of transmission .Lack of education, staying alone  were also identified as root causes in women being infected with HIV. Conclusion: Most of HIV positive cases belonged to the sexually active & economically productive age group, low socioeconomic status, rural area and the sexual route were the predominant factors for transmission of disease. Education and self employment or uplifting of women’s economic status can decrease the prevalence of HIV in rural areas in both the sexes.

Abstract

The effects of sub-lethal dose concentrations of aldrin were studied on blood profile of Channa gachua. For this purpose C. gachua having same weight and length were used. The RBC and Packed Cell Volume (PCV) were found to decrease considerably as compared to normal values.

Abstract

The effect of unilateral eyestalk ablation in freshwater prawn Macrobrachium lamarrei lamarrei was studied. The removal of the eyestalk has promotted the gonad development. In the present study an increase in the testicular and ovarian index in both sexes were observed in eyestalk ablated prawns as compared to normal animals. Thus our study indicates a positively co-related effect, of unilateral eyestalk ablation and is sufficient to induce gonadal development in Macrobrachium lamarrei lamarrei.

Abstract

Two chemometric procedures, based on uv-spectrophotometry, are described for the simultaneous determination of paracetamol (acetaminophen) and caffeine in a binary mixture without prior separation. In the first procedure the principle of classical least-squares has been adopted using the function SOLVER of Excel spreadsheet program. After measuring absorbance of the sample mixture,A_m, at several selected wavelengths, and calculating the value, A_cal, and realizing the minimization condition, the mean % recoveries were 96.36 ± 0.91, and 94.74 ± 3.50 for paracetamol and caffeine respectively. In the second procedure, absorbance measurements were made at the wavelengths 242, 251, and 273 nm for known mixtures of pure paracetamol and caffeine. Two linear calibration equations giving concentration as a function of absorbance were worked out by employing multiple regression via Minitab 14 software program. The mean % recoveries obtained for the sample mixture using the calibrated equations were 96.59 ± 2.16, and 95.48 ± 1.85 for paracetamol and caffeine, respectively. When the official HPLC method was applied analysis of the commercial tablets, the mean % recoveries 97.0 ± 3.2 and 99.2 ± 1.3 for paracetamol and caffeine respectively. Based on the student's t-test, satisfactory agreement was observed when the results of the chemometric procedures were compared with those of the official HPLC method. Furthermore, any of the two chemometric procedures may be employed for the routine analysis of paracetamol-caffeine mixture in tablets. It is clear that there is an advantage of the chemometric procedure over HPLC in terms of simplicity, expense, and rapidity.

Abstract

Diabetic mellitus (DM) is considered as a serious global health problem that is characterized by hyperglycemia. Type 2 diabetes mellitus is most common among the diabetic population. In Type 2 diabetes mellitus, inhibition of α-amylase offers an effective strategy to lower the blood sugar level via control of starch breakdown. The current study was carried out to evaluate α-amylase inhibitory activity of Siddha poly herbal formulation Madhumegachooranam which is being used by the Siddha physicians to treat Type 2 diabetes mellitus. The assay revealed the presence of the α-amylase activity in a significant manner. Further the anti oxidant activity assessed by two different methods exhibited the good inhibition results compared with that of control. The results revealed that when the concentration increased from 12.5 to 100ug/ml, percentage of inhibition increased from 37.22 % to 61.65 % and at a concentration of 100 ug/ml there was a decrease in cell viability. The IC50 value was obtained at 20.2ug/ml. Phytochemical screening of the tested sample revealed the presence of plant constituents alkaloid, flavanoid, glycosides and terpinoids. This study lends hope for treating Type 2 diabetes mellitus in a combined way in that of mixture of α-amylase inhibition, anti-oxidant activity and presence of useful active principles.

Abstract 

Oral route of drug administration remains the most favored preference for majority of therapeutic application, with obvious advantages including ease of administration, patient compliance and flexibility in formulation. Numerous oral controlled release the drug at a predetermined, predictable rate and also optimize the therapeutic effect by controlling the drug release. However this approach is be ditched with several physiological difficulties such as inability to restrain and localize the drug delivery system within the desired region of the gastrointestinal tract due to variable gastric emptying and motility. Gastric emptying time in humans results in an incomplete drug release from controlled DDS. The ability of a dosage form to prolong and control the gastric emptying time is a valuable asset for drug acting locally in GIT. These considerations led to the development of gastro retentive dosage forms increase they one of the most feasible approaches for achieving a prolonged and predictable drug delivery profiles in the GIT is to control the gastric residence time, using gastro retentive dosage form that will provide us with new and therapeutic option Oflaxacin polymers and gums like guargum, xanthangum other than HPMC in different concentration. Tablets were compressed and In-vitro and in-vivo release profile. Prevent study involves an overview formulation and evaluation of FDDS for a prolonged and predictable and HPMC with swellable polymers.