Abstract

Curcuma neilgherrensis is known as “Adavi Pasupu” an important herbal medicinal plant of Tirumala and Talakona area. It is rhizomatous herb found during June-November with vegetative growth of scape and leaves; during November-March with inflorescence and flowers. It is distributed with limited number of individuals at about 3000 meters of altitude on rocky substratum. It is also used by the local people as spice instead of normal Curcuma powder (Haldi) in the preparation of curries. Hence the phytochemical screening, antimicrobial activities (Human pathogenic bacteria and fungi) were carried out to prove scientifically its herbal usages. Further it is also important to characterize different bioactive constituents like phenols, flavonoids and anthocyanidins in leaf, scape, rhizome and roots. The Qualitative analysis through paper chromatography resulted 27 phenolic compounds, 7 flavonoids and 9 anthocyanidin compounds. It supports the bioactivity of each component to that of the herbal uses of Curcuma neilgherrensis against inflammations, skin diseases, wounds, ulcers, arthritis, and menstrual disorders as used by the local herbalists. 

Abstract

C-peptide, a cleavage product of proinsulin, is an active biomolecule. Measurement of serum C-peptide is useful in the classification and clinical management of patients with diabetes mellitus. In addition, serum C-peptide determination plays a key role in the evaluation of hypoglycemia and insulinoma. But lack of standardization of C-peptide assays and reference range of C-peptide for specific populations makes the interpretation of serum C-peptide values quite difficult for clinicians. The present study made an attempt to establish the reference interval of fasting serum C-peptide amongst healthy subjects of Haryana. The study was undertaken in the Department of Biochemistry, Maharishi Markandeshwar Institute of Medical Sciences and Research, Mullana, Ambala (Haryana). Overnight fasting samples of 200 apparently healthy subjects in the age range of 30-70 years were tested for serum C-peptide. The range of serum C-peptide levels varied from 0.08-6.60 ng/ml which was quite different from that supplied in the manufacturer’s kit insert. Therefore, the present study suggests that every clinical biochemistry laboratory should establish its own reference range of C-peptide instead of simply using the manufacturer’s insert.

Abstract

The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating mucoadhesive microspheres of valsartan. Frequent administration and variable low bioavailability (20-25%) after oral administration are problems of conventional dosage forms of valsartan. This can be attenuated by designing it in form of mucoadhesive microspheres which would prolong the residence time at the absorption site to facilitate intimate contact with absorption surface and there by improve and enhance bioavailability. Valsartan microspheres were formulated by orifice–ionic gelation technique using combination of three polymers i.e. sodium alginate, carbopol, and HPMC. Optimised formulation F9 which was formulated by taking a combination of 3 polymers sodium alginate, carbopol and HPMC in 1:1 ratio showed good mucoadhesion property and entrapment efficiency of (87.21%).The scanning electron microscopy indicated that microspheres were spherical in shape and drug remained dispersed in polymer matrix. The invitro drug release mechanism was non-fickian type controlled by swelling and relaxation of polymer. Thus it can be concluded that mucoadhesive microspheres prepared by using sodium alginate, carbopol and HPMC in 1:1 ratio, were found to be promising to reduce the dosing frequency with enhanced patient compliance.

Abstract

Pongamia well known as ganuga is one the richest trees of India with invaluable medicinal uses. Almost all plant parts are of medicinal importance and used traditionally in the treatment of various ailments. Like  cold and cough relieving agent, diarrhoea curing, dyspepsia curing, flatulence  treatment gonorrohea treatment, leprosy treatment ,digestive and laxative agent, anti-inflammatory agent, piles and wounds treatment, anti-oxidant and anti-ulcerogenic agent, anti-hyperammonemic agent, hepatoprotective agent, anti-convulsant agent, anti-diabetic agent, antihelmentic agent. The review discuses pharmacognostic studies, phyto chemicals and pharmacological uses of ganuga.

Abstract

In the present study HPTLC method was developed for the estimation of Telmisartan and Chlorthalidone in commercial brand of ERITEL-CH40mg containing 40mg Telmisartan and 12.5mg Chlorthalidone. The evaluation of obtained values suggests that the proposed HPTLC method provide simple, precise, rapid and robust quantitative analytical method for determination of Telmisartan and Chlorthalidone in tablet dosage form. The mobile phase is simple to prepare and economical. After validating proposed method as per ICH guidelines and correlating the obtained values with the standard values, satisfactory results were obtained. The sample recoveries in all formulations were in good agreement with their respective label claims and they suggested noninterference of formulation excipients in the estimation. Hence, the method can be easily and conveniently adopted for routine estimation of Telmisartan  and Chlorthalidone in tablet dosage form.

Abstract

Siddha herbo-mineral formulations are gaining popularity worldwide due to its nano medicine form, increased bioavailability, minimal side effect, longer shelf life period and need less dosage. Till date, lesser studies have been conducted on standardization of such preparations. Sangu Chunnam, a traditional Siddha herbo-mineral drug was prepared as per the procedure mentioned in Siddha literature. The chemical finger print was engaged by using modern techniques like Fourier Transform Infra-Red Spectroscopy (FTIR) and Inductively Coupled Plasma Optical Emission Spectroscopy (ICP-OES). The particle size and chemical elements of both quantitative and qualitative analysis of Sangu Chunnam were also assessed by Scanning Electron Microscope with Energy Dispersive X-Ray Analysis (SEM EDAX) and X-Ray Fluorescence Spectroscopy (XRF) respectively. The FTIR results showed the presence of O-H stretching and bend, C-H stretching and bend, C=O stretching as functional groups. The SEM image of Sangu Chunnam has numerous nano particles which ranges between 56-172nm denoting a better bio-availability. The XRF results attributed the presence of 76% of CaO. The ICPOES analysis revealed that the heavy metals such as Ar, Pb, Cd and Ni were below detectable limits thereby proving Sangu Chunnam to be safe. Thus, Sangu Chunnam proves to be a safe medicine and underlines the words of Siddhars, the great saints to be true. 

Abstract

The present study deals with noxious effects of sodium cyanide on some biochemical aspects in the liver of freshwater fish Cyprinus carpio. Fish which were exposed to a sublethal concen¬tration (0.l mg/L) of sodium cyanide, for a period of 10 and 20 days and further allowed to undergo a recovery of 14 days, resulted in variation of levels of protein, free amino acid and protease enzyme activity with respect to control. The changes were in a manner that suggested the possible existence an oscillatory phase in biochemical turnover towards a more synthetic phase leading to the establishment of convalescence and adaptation phenomena. Yet, sodium cyanide being toxic component needs attention towards its neutralization prior to its disposal. Hence, it is inferred that necessary care should be taken during its disposal, as it possesses a serious threat to fish.

Abstract

Aptamers are single stranded nucleic acids that specifically recognize and bind tightly to their cognate targets due to their stable three dimensional structures. Nucleic acid aptamers have been developed for various applications, including diagnostics, molecular imaging and biomarker discovery along with target validation, therapeutics, and drug delivery. Since its discovery in the early 1990s, aptamer technology has progressed tremendously. Automated selection procedures now allow rapid identification of DNA and RNA sequences that can target a broad range of extra and intracellular proteins with nanomolar affinities and high specificities. The unique binding properties of nucleic acids, which are amenable to various modifications, make aptamers perfectly suitable for different areas of biotechnology. RNA aptamers represent an emerging class of pharmaceuticals with great potential for targeted cancer diagnostics and therapy. Several RNA aptamers that bind cancer cell-surface antigens with high affinity and specificity have been described. However, their clinical potential has yet to be realized the demand for diagnostic assays to assist in the management of existing and emerging diseases is increasing, and aptamers could potentially fulfill molecular recognition needs in those assays. Compared with the bellwether antibody technology, aptamer research is still in its infancy, but it is progressing at a fast pace. The potential of aptamers may be realized in the near future in the form of aptamer-based diagnostic products in the market. In such products, aptamers may play a key role either in conjunction with, or in place of antibodies. It is also likely that existing diagnostic formats may change according to the need to better harness the unique features. This review summarizes aptamers as valuable tools for diagnostics, target validation, drug discovery, and even therapeutic approaches.

Abstract

Ivermectin is broad spectrum antiparasitic drug. Fish acute toxicity tests were carried out in zebra fish (Danio rerio) and catla fish (Catla catla) to assess the comparative tolerance to ivermectin induced toxicity and pathological alterations. The fishes were exposed to various concentrations of ivermectin (1, 3, 5, 7 and 9µg/l) and observed for behavioral changes in swimming pattern, maintaining equilibrium, pigmentation and mortality at various time intervals (24, 48, 72 and 96h). The brain and the liver samples were collected from the experimental fishes every 24h for histopathalogical analysis. The behavioural changes and mortality in fishes increased with the increase in ivermectin concentration and exposure time. Neurotoxic (gliosis and neuron degeneration) and hepatotoxic changes (necrosis and acute hepatitis) were observed in the brain and liver of zebrafish respectively when exposed to 7µg/l of ivermectin for 96h. In catlafish, the same concentration (7µg/l) of ivermectin induced neuronal degeneration and necrosis in brain and hepatotoxic signs (hepatic cell degradation, vacuolations) in liver at 24 h exposure. The results of this study conclude that zebrafish is more tolerant to higher concentrations and prolonged exposure to ivermectin compared to catla fish

Abstract

Alzheimer’s is the most common cause of dementia in adult life and is associated with the selective damage of brain regions and neural circuits critical for memory and cognition. The neurons in the neocortex, hippocampus, amygdala, and the basal forebrain cholinergic system are the most affected brain regions. The major factors leading to Alzheimer`s are 1) amyloid plaque diposition in brain. 2) Disruption in the cholinergic activity. 3) Oxidative stress in  brain 4) inflammation accompanying the disease. The continuing expansion of life expectancy, leading to a fast growing number of patients with Alzheimer’s disease, has led to an enormous increase in research focused on the discovery of drugs for primary, secondary or tertiary prevention of the disease. Despite all scientific efforts, at the moment, there are no effective pharmacotherapeutic options for prevention and treatment of Alzheimer’s disease. The subject of our study in this review is Chitin that is a naturally abundant polysaccharide. In fact, chitin is a constituent of the outer structure of insects, fungi and crustaceans. Chitin is also significant because of its relationship to some components of foods of animal, and fungal origin, and its potential medical and pharmaceutical uses. Current understanding of the role of chitin like polysaccharides in the pathogenesis of amyloid deposition of Alzheimer disease is developing fast. Polysaccharides may play a broader role in light of 1) the role of amyloid in Alzheimer disease pathogenesis. 2) anticholinesterase activity. 3) oxidative stress in Alzheimer`s disease and 4) inflammation accompanying the disease. Considering the side effects of synthetic neuroprotective agents, the search for natural neuroprotective agents has received great attention. Hence, the objective of this review is to discuss neuroprotective properties of chitin and its derivatives.

Abstract

The classical Siddha poly-mineral drug Panchalavana Thiraavagam has unique properties being a specialized liquid form of medicine indicated for PCOS as per traditional Siddha literature Kannusamiyam Ennum Vaidhiya Saegaram. The aim of this present study was to standardize the purity, quality and safety of Panchalavana Thiraavagam. The physico-chemical characterization of the drug was revealed by qualitative biochemical analysis and modern instrumental techniques such as Fourier Transformation Infrared Spectroscopy (FT-IR), Scanning Electron Microscopy (SEM), Energy Dispersive X-ray analysis (EDAX). Physico-chemical parameters revealed that the drug is clear, colourless fluid with no characteristic odour and weak acidic (pH 6.2) in nature. The qualitative biochemical analysis revealed that the presence of Sulphate, Chloride, Phosphate, Calcium, Sodium and Potassium. The FT-IR study revealed the presence of functional groups like aliphatic bromo compounds, nitro group, ketones, carbonyl group, phenols and alcohols in Panchalavana Thiraavagam.  The SEM analysis showed that the size of the particles to be 80.0 nm, 94.1nm, 102nm, 113nm, 330 nm in the sample. So it was concluded that the Panchalavana Thiraavagam contains essential elements required to the body. Also the drug possesses no toxic effects because of absence of toxic metals. Thus the present study paves the way for toxicological and pharmacological activities.

Abstract

An isocratic HPLC method and two classical UV spectrophotometric methods i.e first derivative zero crossing point method (FDZCP) and ratio derivative spectrophotometry (RDS) were developed for the simultaneous estimation of Ambrisentan (AMB) and Tadalafil (TAD) in its laboratory sample. The HPLC method was developed using Phenomenex Luna C18 column (250× 4.6 mm i.d., 5 particle size), with mobile phase composition of methanol: acetonitrile: ammonium acetate buffer pH 6.0 (ratio of 35: 30: 35). The flow rate was 1 ml min-1 and effluent was detected at 264 nm. The retention time of AMB was 4.49 minand forTAD 5.97 min. All the three methods were successfully applied for the analysis of laboratory mixture. The recovery for AMB was found to be 100.2-101.18% by HPLC method, 98.19-101.35% by FDZCP method and 99.64-102.09 by RDS method. The recovery for TAD was found to be 98.04-101.63% by HPLC method, 99.73-102.98% by FDZCP method and 100.36-102.11 by RDS method. One way ANOVA was performed and it was found that there is no significance difference between the results of the three methods i.e. the UV spectrophotometric methods were found to be as good as HPLC method and hence any of these methods can be used for the simultaneous estimation of AMB and TAD.

Abstract

The present Study is to evaluate the Antioxidant and Hepatoprotective Activity of Extracts of Flowers of Tridax Procumbens Linn, against Dgalectosamine induced Hepatotoxicity in Male Wister Albino Rats.The flowers of Tridex procumben Linn. Was extracted out by petroleum ether, methanol and chloroform water. The phytochemical investigation and its Phenolic content were determined. The antioxidant activity was evaluated by two methods reducing power ability method and lipid peroxidation method. The dose of the extract was fixed by acute oral toxicity as Per OECD guideline 423. Then it was subjected for Hepatoprotective activity on rats by Dgalectosamine induced model and Histopathological changes were also observed. The yield of the drug was 2.22% and 2.5% in Methanolic and Aqueous extract. The extracts contain Alkaloids, Flavanoids, Carbohydrates, and Tannins etc. The total Phenolic content found to be 59.87 and 53.12 μg/ml as compared to the gallic acid. In the Hepatoprotective Activity the extracts shows significant effect. But as compared to aqueous extract, the Methanolic Extract shows potent effect.

Abstract

Adverse Drug Reactions are acknowledged as one of the hazardous consequences of the drug therapy. A wide range of surveillance programs on adverse drug reactions should be emphasized, in our Indian scenario to strengthen the database. Hence, in our study, we focused on the incidence of adverse drug reactions, their causality & severity assessment and the reporting strategies of ADRs among health care professionals in the department of internal medicine especially, where the exposure of drugs to the patient would be more. This was a prospective observational study conducted for a period six months. Patients with suspected ADRs from the internal medicine department with both the genders and all age groups were included in the study. Patients with drug abuse and patients with intentional or accidental poisoning with drugs were excluded from the study. For the assessment of causality and severity Naranjo’s scale and modified Hartwig & Siegal scale were used respectively and the reactions were classified based on Wills and Brown classification. In our study, the overall incidence of ADRs was found to be 2.66% and the main predisposing factor was observed to be poly pharmacy (43.9%). Majority of the ADRs were possible (54.9%) with moderate severity (86.6%) and a maximum number of type A (78.1%) reactions were observed. Specific or symptomatic treatment was provided for 44% of the ADRs. Anti ulceratives caused maximum number of ADRs (42.6%). In conclusion, females are more prone to ADRs than males in our study. All health care professionals and patient volunteers must come forward to report adverse drug reactions in order to minimize the ADRs incidence and to improve the quality of life of the patients.

Abstract

Diabetic nephropathy is the leading cause of chronic kidney disease and is associated with increased cardiovascular mortality. Diabetic nephropathy has been classically defined by the presence of proteinuria >0.5 g/24 h. This stage has been referred to as overt nephropathy, clinical nephropathy, proteinuria, or macro albuminuria. It seems to occur as a result of an interaction between metabolic and hemodynamic factors. Hyperglycemia induces oxidative stress and leads to activation of multiple biochemical pathways which are the source of renal damage. Limited therapies are available as a symptomatic treatment which empathize the need for more therapies to treat diabetic nephropathy. Monoamine oxidase (MAO) and its substrates are found in both the exocrine and endocrine parts of pancreatic beta cells. Many studies have showed that MAO-catalyzed reaction may cause structural damage to pancreatic beta cells resulting in disturbances in catecholamine’s metabolism and MAO also generate reactive oxygen species, which plays important role in pathogenesis of diabetic complications. Therefore inhibition of MAO can lead to the secretion of insulin. Thus the purpose of this review is to cover the role of MAO inhibitors as the new therapeutic approach in diabetic nephropathy.

Abstract

Anxiety is an emotional state caused by the perception of real or perceived danger that threatens the security of an individual. Benzodiazepines are first line approach in the management of anxiety related disorders. However, their inherent side effects are an inducement to the search for newer safe anxiolytic drug. In the present study, Vanda tessellata has been investigated for its anxiolytic activity in mice. The anxiolytic activity was screened by using two well validated methods namely elevated plus maze and open field test. Vanda tessellata extract has shown a dose-dependent anxiolytic effect similar to the diazepam in animal model of anxiety as revealed by a significant increase in the time spent in open arms of the elevated plus maze and significant increase of ambulatory behavior in open field test, the results of the present study has identified a novel anxiolytic compound.

Abstract

A series of 2-substituted 7-chloro-1, 3-benzoxazin-4-ones are synthesized from 2, 4-dichlorobenzamide and readily available N-acylbenzotriazole in one step. The final compound has been characterized by 1H NMR and 13C-NMR.This work have demonstrated that N-acylbenzotriazoles are valuable precursors in the synthesis of 2-furyl and 2-thienyl 1, 3-benzoxazin-4-one in high yields.

Abstract

In the last few years there has been an exponential growth in the field of herbal medicine and these drugs are gaining popularity both in developing and developed countries because of their natural origin and less side effects. Today, 60% of world‟s population uses medicines obtained from plants. This review focuses on the ongoing research on spices found to be beneficial for neuropsychiatric disorders like, stress, depression, dementia and Alzheimer‟s disease.

Abstract

Esomeprazole Magnesium Trihydrate is a proton pump inhibitor, belongs to the group of benzimidazole, used for the treatment of gastric and duodenum ulcers. Esomeprazole undergoes degradation in acidic medium of the stomach, can be coated with enteric coating polymer that will safely deliver the drug in the small intestine. In this study an attempt was made to formulate and evaluate Esomeprazole enteric coated tablets. Different core tablets of Esomeprazole were prepared by direct compression using Starch as a disintegrant and microcrystalline cellulose as a filler. Core tablet of Formulation F3 was selected and coated with a seal coating dispersion of hydroxyl propyl methyl cellulose and subsequently with a dispersion of enteric polymer such as hydroxyl propyl methyl cellulose phthalate using a syringe, where coating dispersion was applied on to the tablets manually. Seal coating was applied to achieve 1% weight gain using hydroxy propyl methyl cellulose dispersion. Enteric coating was carried out using hydroxy propyl methyl cellulose phthalate dispersion to achieve a 10%, 20% and 30% weight gain. Enteric coated tablets with and without a seal coat, which gained a 30% weight gain after enteric coating with hydroxy propyl methyl cellulose phthalate were found to show a delayed release when tested for the dissolution. They were studied for their stability under long term and accerelerated conditions for about 3 weeks. The results indicated the necessity of a seal coat between core and enteric coat in the formulation. By using this method, tablets can be coated until an optimum weight gain is obtained to get a delayed drug release, hence reducing the over usage of materials. So, by utilizing this syringe method, a variety of enteric polymers can be coated onto seal coated esomeprazole magnesium trihydrate core tablets, which are stable and exhibit a delayed drug release.

Abstract

The aim of the present work was to design and synthesize 4-(4-bromophenyl)-5-((5-((quinolin-8-yloxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-4H-1,2,4-triazole-3-thiol derivatives and evaluate them for in-vitro Antioxidant, Antibacterial, Antihypertensive activities against standards. Antioxidant properties by DPPH, 2-Deoxyribose assay and Lipid peroxidation assay against ascorbic acid, Mannitol and R-tocopherol standards were evaluated respectively. Antibacterial activity against Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae were evaluated. Angiotensin-I-converting enzyme (ACE-I) inhibition was studied by using standard lisinopril. 3 out of 10 synthesized compounds showed good in-vitro antioxidant and antibacterial activities. In antioxidant activity the compound 4d, which is 2-methyl 5,7-dichloro substitution on core 8-hydroxyquinoline showed least IC50(highest active) value i.e. 98.8 mg/ml in DPPH against 106.12 mg/ml of standard ascorbic acid, 127.2 mg/ml in 2-deoxyribose assay against 130.4 mg/ml of the standard mannitol and 131.6 mg/ml in lipid peroxidation assay against 138.81 mg/ml of standard R-tocopherol. Compounds 4b, 4c, 4a and 3d showed moderate antioxidant activity. The compounds 3d and 4d were found to have higher antimicrobial activity on E. coli and S. aureus. The compounds 4e, 4a and 4d showed % inhibition of 85.81, 68.53 and 55.66 at higher concentrations (1000 µg/µl) respectively when compared to standard lisinopril (73.33 % inhibition) in ACE-I inhibitory activity. Halo substituted 8-hydroxyquinoline moiety may be responsible for the effective antibacterial and antioxidant activities. Similarly methyl substituted 8-hydroxyquinoline moiety may be responsible for the effective ACE-I activity. Hence, further studies are also required to confirm the influence of electron withdrawing and donating group on the substitution moiety.

Abstract

Acute poisoning with organophosphorus compound (OPC) agents is a major clinical problem globally, with thousands of deaths occurring every year. The desire of this study is to determine the pattern of OPC poisoning deaths. It was a descriptive study. All consecutive deceased in the department of Forensic Medicine with history and clinical evidence of organophosphorus poisoning deaths during the study period of 18 months were considered eligible for participation in the study. The present study shows that OPC compound poisoning deaths constitute about 11% of the total number of cases autopsied. The maximum numbers of patients were between 21- 30 years with male predominance, rural background and belonging to lower socioeconomic status. Highest number of poisoning cases are encountered in the daytime (6AM – 6PM). Stomach pain and family problem were the common causative factor in OPC poisoning. Most of the cases were survived more than 48 hours. To avoid such high incidence, exposure and death due to OPC poisoning, marketing of insecticides to the public should be strictly controlled by law. Farmers and other people involved in spraying of insecticides must be educated regarding prophylactic measures.

Abstract

Phylogenetic investigation of communities by reconstruction of unobserved states (PICRUSt) is a recently developed computational approach for prediction of metagenomics , comparing marker gene data with a reference genome database. In the current study, we used PICRUSt for predicting metagenomics in broilers subjected to heat stress, and supplemented with prebiotic and probiotic. Cecal digesta were taken for DNA extraction. DNA was sequenced using 16S rRNA pyrosequencing. Sequences were analyzed using Qiime and PICRUSt to predict metagenomics. Functional genes content inference was consigned according to Kyoto Encyclopedia of Genes and Genomics Orthology Hierarchy and compared using Linear Discriminant Analysis and the Kruskal-Wallis test. The core gene contents of broilers gut microbiome were predominantly associated with metabolism (52.3%) and environmental information processing (27.4%). Among metabolic processes, carbohydrates metabolism (20.0%) was highest, followed by xenobiotics (11.0%), amino acids (7.9%), and lipids metabolism (3.3%). The information processing gene included; membrane transportation (21.0%), signal transduction (3.1%), and signaling molecules interaction (3.2%). Other significant pathways identified in the broilers gut microbiome are genetic information (7.6%), cellular (0.86%), and organismal (0.21%) processes. About 12.3% genome in this study was unclassified. Among different treatment groups, genetic information processing was higher (P<0.05) in the probiotic supplemented group compared to all the other groups. However, no significant differences (P>0.05) were observed for other metabolic and cellular processes. In conclusion, the present study reveals that gut microbiome of broilers significantly contributes to the host metabolism and nutrients absorption, and the stress and supplements have no significant effects to change these functions.

Abstract

Most convention route for drug delivery is oral route but the bioavailability is very poor by this route. To overcome hazards or limitations of oral route a new & novel approach of Gastro-retentive drug delivery have been developed. By using this system drugs having local effect or high absorption in stomach with narrow therapeutic window have higher GRT so prolonged and mostly sustained effect in stomach. The variability in drug concentration can also overcome by this technique. Several approaches have been developed to formulate expandable, floating, non-floating, expanding type of dosage forms and various others which have been discussed in this review. It also includes advantages, disadvantages, and suitable, unsuitable candidates for GRDDS. In-vitro &In-vivo Evaluation techniques are also discussed here. It also include future trends of GRDDS.

Abstract

Various esters of (5,6-dimethoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid and (5-ethoxy-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid were synthesized. Anti-inflammatory and analgesic activities of these compounds were evaluated. Possibly higher lipophilicity of the ester derivatives of (5-ethoxy-6-methoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid was responsible for greater activity of these compounds compared to the esters of (5,6-dimethoxy-3-oxo-2,3-dihydro-1H-inden-1-yl)acetic acid. Compound 11d was found to be the biologically most active one. It showed 47.69% inhibition in carrageenan–induced rat paw edema in anti-inflammatory screening. It also exhibited 51.19% inhibition in acetic acid-induced writhing in analgesic screening. A few selected compounds were also screened for their antipyretic and gastrointestinal ulcerogenic potential. Promising antipyretic activity was exhibited by these compounds at the dose level of 100mg/kg p.o. These compounds also did not cause any ulceration at the highest tested dose level of 300mg/kg p.o. Experimental data indicate that better anti-inflammatory-analgesic-antipyretics can be designed using compound 11d as a lead.

Abstract

Cyperus rotundus is a traditional herbal medicine used as analgesic, sedative antispasmodic, antimalarial, stomach disorders and to relieve diarrhea. Diabetes is a group of metabolic disorder of carbohydrate, fat, and protein metabolism resulted from destruction of insulin secreting pancreatic beta-cells, defects in insulin production, insulin action, or both, characterized by hyperglycemia. In the present investigation the ethanolic extracts of Cyperus rotundus has been screened for the presence of phytoconstituents, acute toxicity, hypoglycemic, antidiabetic activity and wound healing activities.The plant extract is obtained by using soxhlet apparatus extraction procedure and phytochemical studies of ethanolic extract showed the presence of alkaloids, steroids, tannins, phytosterols and flavonoids.Acute toxicity studies have revealed that the ethanolic extract of Cyperus rotundus were safe upto 2000 mg/kg..The ethanolic extract of Cyperus rotundus showed the significant decrease in serum glucose level (p< 0.001) in both oral glucose tolerance test and alloxan induced diabetic rats. There is also a significant reduction in serum triglycerides, total cholesterol, LDL, and liver enzymes. The reduction in wound contraction was statistically significant as compared control group. So we can conclude that ethanolic extract of Cyperus rotundus has shown significant antidiabetic, antihyperlipidimic and wound healing activity in alloxan induced diabetic rats.

Abstract

Obesity is presently a global epidemic, which is associated with many major co-morbid disorders. Orlistat is used for the treatment of obesity. Fast disintegrating mini-tablets are compressed tablets of size up to 3mm that disintegrate rapidly and can be swallowed without water for better patient compliance. The objective of the present work is to develop the fast disintegrating Orlistat mini-tablets that can be administered whole as a unit dose sachet. Orlistat has a very less aqueous solubility, and to enhance the solubility and stability different methods were tried. In that, Orlistat β-cyclodextrin (1:2M) complex was found to be more feasible to prepare, 3mm mini-tablets each containing 6mg Orlistat, [20 mini-tablets for 120mg dose sachet]. Nine formulation trials using novel co-processed excipients were done. No drug excipients interaction was found by the XRD and IR Spectrum. The optimized formulation (ORDT-9) mini-tablets were evaluated for weight variation, hardness, friability, drug content and wetting time, all the results were within the standard limits. The in vitro disintegration and dissolution tests results of the optimized formulation containing the 40% of ludiflash have shown to be disintegrating in 55 seconds and releasing the 86% of drug within 10 minutes. And in the comparative in-vitro dissolution study with the existing marketed product the optimized formulation (ORDT-9) was releasing three fold faster and complete drug was released in the 15 minutes. Hence, the developed fast disintegrating mini-tablets of Orlistat with enhanced dissolution rate could be a viable ready-to-use single dose sachet dosage form, for better patient compliance.

Abstract

For the first time two simple and selective spectrophotometric methods have been developed for the determination of Retigabine in pure and pharmaceutical formulations. Of two methods, method M1 was based on the oxidative coupling of Retigabine with 3-Methyl-2-Benzothiazolinone hydrazone hydrochloride reagent in the presence of 0.1 % FeCl3 formed red coloured complex showed maximum absorbance at 501.6 nm at reagent blank. Under the reaction conditions, MBTH on oxidation with Fe (III) loses two electrons and one proton forming an electrophilic intermediate which has been postulated to be the active coupling species and to form colored species and in method M2 based on reaction of Retigabine on treatment with 1, 10-phenanthroline to give blood red coloured chromogen which shows the absorbance maximum at 508 nm under the optimized experimental conditions. The developed method obeyed Beer’s law over the concentration ranges of 2-10 µg/mL and 1-5 µg/mL for method M1 and method M2 respectively. In both cases the R2 is more than 0.9997. These methods were validated in pursuance of ICH Q2 (R1) guidelines. The % recovery was found to be in the range of 99.05 to 99.98 % for M1 and 99.06 to 99.86 % for method M2. With regard to precision, the intraday and interday precision for methods M1 and M2 were found to be 0.144 µg/mL, 0.219 µg/mL and 0.206 µg/mL, 0.203 µg/mL, respectively. The results relating to LOD and LOQ for methods M1 and M2 were found to be 0.207µg/mL, 0.049 µg/mL and 0.629 µg/mL, 0.150 µg/mL respectively. The molar absorptivity, Sandell’s sensitivity, for both methods were also reported. No interference due to the commonly used excipients as well as the method is specific for detecting Retigabine. So the developed methods can be applied successfully for the determination of Retigabine in bulk and pharmaceutical formulations.

Abstract

The aim of the present study was to develop RP-HPLC-PDA method for the estimation of Macitentan in bulk and pharmaceutical dosage forms. The method uses an Inertsil (250 mm x 4.6, 5 m) with mobile phase consisting ofAcetonitrile: 10 mM Ammonium acetate (60:40 v/v) in an isocratic mode with an injection volume of 10μL and the eluents were monitored at 255 nm. The retention time of Macitentan 5.578 min, it showed linearity in the concentration range of 2-10 μg/mL with a good correlation coefficient of 0.999. The validation parameters like specificity, system suitability, linearity, LOD (0.4042 μg/mL), LOQ (1.225 μg/mL), precision (%RSD >1), robustness were all within the limits stated in ICH guidelines. The developed RP-HPLC-PDA method is specific, accurate, robust and economic, hence it can be successfully applied in routine quality control for the determination of Macitentan in bulk and tablet dosage forms.

Abstract

A series of new Coumarin linked pyrazoline derivatives were synthesized by condensation of 3-Acetylcoumarin with substituted aryl benzaldehydes in chloroform in the presence of piperidine which resulted in intermediate compounds (D1-D10; 3-aryl substituted-1-(3-coumarinyl) propen-1-one`s). These chalcones upon cyclisation with 2, 4-Dinitrophenylhydrazine(2,4-DNP) yielded desired target compounds (E1-E10; 1, 5-disubstituted-3-(4,5-dihydro-1h-pyrazol-3yl)-2h-chromen-2-one) with the yield in the range of 28-55%. All the synthesized compounds were characterized by 1HNMR. The synthesized compounds were screened for anti bacterial activity against bacterial strains viz. Bacillus subtilis, Bacillus Cereus, Escherichia coli Klebsiella pneumonia. All the compounds were found to posses moderate to good activity, out of all the synthesized compounds (E3) i.e 3-(5-(4-(dimethylamino) phenyl)-1-(2, 4-dinitrophenyl)-4,5-dihydro-1H –pyrazol-3-yl)-2H-chromen-2-one was screened with highest activity.

Abstract

Dendrimers are macromolecules having highly branched, 3D structure, nanoscale architecture with monodispersity and high functionality. Dendrimer as a drug delivery system is based on the approach of sending a nanoparticle (10-9) to the body, loaded with drug. The drug might be loaded on its terminal surface or encapsulated within the branches of a dendrimer. Dendrimers help in achieving increased bioavailability, controlled as well as targeted release of drug. There is reduction in the amount of drug and systemic toxicity while the therapeutic efficacy increases. This approach as a drug delivery system certainly promises a reliable, safe, selective and precise method of drug delivery. This review covers the points of structure, properties, types, factors affecting dendrimer properties, encapsulation, applications, characterisation etc.

Abstract

Through medication increasing number of novel drug delivery systems are being employed to manage illness and are offered for therapeutic use. Gastro retentive drug delivery systems have potential to permit improved penetration of the mucus layer and as a result better concentration of drug at the specific site ,ensure optimal bioavailability to poorly absorbed drugs and a desired release profile. This drug delivery system potentially overcomes a drawback of non-site specificity and short gastric resident time that are associated with oral route of administration. At present numerous approaches are utilized to prolong the gastric residence time, Including floating systems, Magnetic system swellable/expanding systems, gastric mucohedhesive systems, sedimentation /high density system by incorporating suitable polymers in dosage form. This study describes the different structural components like polymers and other excipients (formulation variables) that can be utilized to formulate the suitable and effective gastro-retentive drug delivery system. In the aspect of recent development, different formulation variables that have direct effect on gastric residence time, floating, high density, bioadhesion, expending and magnetic properties of GRDDS are covered in detail in this review.

Abstract

The aim of current study was to optimize the effect of process and formulation parameters and to develop nanoparticulate drug delivery system to achieve sustained release of Prednisolone (PS) from a biodegradable polymer; PLGA. PS loaded PLGA nanoparticles were fabricated using nanoprecipitation technique with poloxamer 188 as a stabilizer. Quality by design approach was implemented to optimize effect of parameters and generate the design space using selected I-Optimal RSM design for design of experimentation (DoE) based on the risk assessment, an element of QbD approach. The effect of critical material; PLGA: Poloxamer 188 ratio and process parameter; stirring speed were linked to CQAs; particle size and % entrapment efficiency. The prepared PS loaded PLGA nanoparticles were characterized for particle size, polydispersity index (PDI) (Malvern Zetasizer ZS 90), entrapment efficiency, in-vitro diffusion study, DSC, XRD, SEM. Acceptance criteria for CQAs were considered as particle size in the range of 150-350 nm and entrapment efficiency in the range of 55-78.14 % w/w, which gave the design space with combination of selected critical parameters assuring robust formulation with desired Quality Target Product Profile (QTPP). PS loaded PLGA nanoparticles were spherical in shape, has narrow PDI. In-vitro diffusion study showed initial burst effect due to surface embedded drug and further gives sustained drug release which might be due to PLGA nanoparticles matrix system. Validation of model performed by comparing experimental values with predicted value of representative formulation within design space, confirming validity of generated mathematical model. Optimized formulations of PS loaded PLGA nanoparticles showed 78.14±0.20 % entrapment efficiency, particle size 173.7 nm with 0.103 PDI within design space which demonstrated effective drug delivery providing sustained drug release for a period of more than 4 weeks. Hence it can be concluded that QbD approach can be successfully implemented to optimize the effect of process and formulation parameters resulting the effective targeting of drug for long term therapy with PLGA as biodegradable polymer.

Abstract

Crystal form can be vital to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as poor aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first pass metabolism. The nature of the physical form and formulation tends to display the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co crystals. Co-crystal is crystalline structure consisting of two or more components that form a unique structure having specific properties. The physical and chemical property improvements through pharmaceutical co-crystals draw closer the fields of crystal engineering and pharmaceutical sciences. A pharmaceutical co-crystal is single crystalline solid that incorporates two neutral molecules one being an active pharmaceutical ingredient (API) and the other a co-crystal former. This technology is used to identify and develop new proprietary forms of widely prescribed drugs and offer a chance to increase the number forms of an API. This review focuses on the properties of co-crystals, their method of synthesis and applications in the field of pharmacy

Abstract

Clitoria ternatea is a medicinal herb with great therapeutic applications. It is commonly known as butterfly pea which belongs to the Fabaceae family, it is native to tropical regions of India. In the present study, the leaves and flower extracts of Clitoria ternatea were used for carrying out phytochemical screening by FTIR spectroscopic ananlysis qualitatively, as well as quantitative analysis of total phenolic content (TPC), total flavonoid content (TFC) and also in vitro antioxidant activity were estimated. For estimation of antioxidant activity, DPPH, hydroxyl radical and hydrogen peroxide methods were used. From the FTIR spectral analysis, it was revealed that the leaf and flower methanolic extracts of Clitoria ternatea possess wide range of bioactive compounds such as alcohols, phenols, primary, secondary amines, carboxylic acids, nitro compounds, etc. Clitoria ternatea leaves and flower extracts exhibited the significant quantity of phenols and flavonoids, which were compared with standard gallic acid and quercetin. From the results, it was shown that the leaf and flower extracts have antioxidant activity against in vitro generated radicals like DPPH, hydroxyl radical and hydrogen peroxide. Hence it is concluded from the results that the significant amount of phytochemicals, phenolic and flavonoid contents present both in leaves and flowers are responsible for the in vitro antioxidant activity of Clitoria ternatea, and it is potential to be an alternative source of natural antioxidants.

Abstract

Microspheres can be tailored to provide targeted and/or sustained release in different parts of the body, including those of eye, nasal cavity, urinary, colon and gastrointestinal tract, thus offering the possibilities of localized as well as systemic controlled release of drugs. Prolonged release of drugs and a reduction in frequency of drug administration can highly improve the patient compliance. Recent advances in targeted drug delivery and sustained release of drug uses this mechanism even for the delivery of protein and peptide drugs, antigens for vaccination and plasmid DNA for gene therapy. In the present work we have developed the formulation of microspheres for an antiretroviral drugs  combination of  Lamivudine and Stavudine  which has  less plasma half life   hence it is necessary to develop the formulation which will provide the sustained release of the drug thereby reducing the dose of the drug. We developed and characterized the microsphere formulation which improved the efficacy of the drug and hence reduce the side effects. Characterization also showed that there is no drug excipient interaction.  The Physical characteristics like Particles size, Drug entrapment, FTIR, SEM, XRD,DSC and In-vitro drug release profiles will be studied.

Abstract

A series of novel 4-aryl-8-arylidene-5,6-dihydro-2-imino-6-methoxy-4H,7H-[3,1] benzothiazines were synthesized and structures were elucidated by UV, IR, 1H NMR and Mass spectral data. These compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The compounds were also screened for their antifungal activity against Aspergillus niger and Candida albicans. The antibacterial and antifungal results are compared against standard reference Ampicillin and Amphotericin B respectively.