Abstract

Nutraceuticals are food product that provides health as well as medical benefits; including the prevention and treatment of disease. Few nutraceuticals are being used as pharmaceutical and a number of other being used and purchased by the general public as self-medication. Such products may range from dietary supplements to genetically engineered foods, herbal products and processed foods. Clinical research on nutraceutical product is going on for integrating and assessing information. Size of the Market at Rs 65 billion in India is just 2 % of the global nutraceutical market. So India will be a strong market to grow for Nutraceutical products as the players in the industry will be a combination of large multi-nationals global for nutraceuticals is growing day by day & it is expected to reach $176.7 billion in 2013, a compound annual growth rate (CAGR) of 7.4%. The demand for herbal and non-herbal extracts is likely to rise by 6.5 % annually to USD2.5 billion and that of nutrients and minerals by 6.3 %, to USD1.27 billion and for vitamins the growth will be slower at 4.6 % annually to USD5.2 billion in 2015.

Abstract

Ulcerative colitis (UC) is a chronic relapsing and remitting inflammatory disorder of the gastrointestinal tract, and, besides Crohn’s disease (CD), it is one of the two major forms of inflammatory bowel disease (IBD). The clinical course is characterized by exacerbations and spontaneous or drug-induced remissions. UC primarily affects the mucosa of the large bowel, while in chronic condition it can affect the whole gastrointestinal tract. The etiology of UC remains unclear. Medical therapies to completely cure the disease are not available. Currently, the most widely accepted hypothesis implicates a combination of the following factors: immune deregulation, abnormal gastrointestinal (GI) tract luminal factors, oxidative stress, tumour necrosis factor (TNF) -alpha) and interleukin (IL)-6 defects in the GI mucosal barrier that allow luminal factors to penetrate into the mucosa. Several drugs interacting with various points along the immune and inflammatory cascades are currently available for the treatment of UC. Corticosteroids, Aminosalicylates, Immunomodulators are the mainstay of medical treatment. In the present study, our efforts have been devoted to investigate the prophylactic effects of Zileuton in acetic acid induced experimental colitis by using rat model. We have investigated the histopathological changes by Zileuton (50 mg/kg, p.o) on acetic acid induced colitis in rat model finally; histopathological changes were nearly restored by Zileuton pretreatment. The findings of the present study provide evidence that Zileuton a novel 5-LOX inhibitor potentially protect the colonic mucosa against acetic acid-induced colitis may be due to inhibition of Leukotrienes synthesis there by it may be beneficial in Ulcerative Colitis.

Abstract

In present research an attempt has been made to formulate sustained release matrix tablet of Simvastatin and studied the effect of matrix former Xanthum Gum and Guar Gum separately. Simvastatin is a anti-hyperlipidemic drug and short half life (t1/2) and usually oral dose regimen (5 to 40 mg) taken to 4 times a day. To reduce the frequency of administration and to improve the patient compliance, sustained release formulation of simvastatin is desirable. Formulations (F1 to F6) were prepared by direct compression method in the ratio (1:1, 1:2, 1:3) [Table-1]. The granules were evaluated for angle of repose, bulk density, and compressibility index [Table-3]. The tablets were evaluated to thickness, weight variation, friability, hardness, Drug uniformity [Table-4] and Invitro-dissolution studies [Table-5] [Fig-2]. All the tablet formulation showed compliance with pharmacopeial standards. The in-vitro dissolution results show that an increased amount of polymer resulted in retarded drug release. The maximum drug release was found to be 90% over a period of 12 hours in guar gum based tablets (F₄). Similarly maximum drug release was found to be 90% over a period of 12 hours in Xanthan gum based tablets (F₁). This indicates that the minimum quantity of guar gum and Xanthan gum that is drug to gum ratio of 1:1 is  required  to prepare the sustain release matrix tablets of Simvastatin.

Abstract

Lubricants are the essential components of all solid dosage forms. Sodium stearyl fumarate is sparingly soluble in water. An attempt has been made to improve solubility of sodium stearyl fumarate to become it highly soluble. Sodium stearyl fumarate was compared with other conventional lubricants to check the impact of lubricants on flow properties, hardness, and disintegration and dissolution characteristics. Different concentrations of lubricants were used to prepare uncoated tablets and evaluated for its activity. All the tablets prepared with sodium stearyl fumarate were found to be better in terms of variations in hardness, disintegration and dissolution property. Hence, sodium stearyl fumarate was a super lubricant in tablet dosage form.

Abstract

The successful delivery of drugs across the oral mucosa represents a continuing challenge, as well as a great opportunity. Buccal delivery has progressed far beyond the use of traditional dosage forms with novel approaches emerging continuously. Buccal drug delivery system in which drug enters directly in systemic circulation thereby by passing the first pass effect. Contact with digestive food of gastrointestinal tract is avoided which might be unsuitable for stability of many drugs.. Moreover it shows better stability, patient compliance; uniform and sustained drug release and above all easy and cheap methods of preparation which can be done with various commonly available biocompatible polymers. The buccal route has been researched for a wide variety of drugs like miconazole nitrate, Aceclofenac, Cyproheptadine Hydrochloride and various different categories and has gained significant attention and momentum since it offers remarkable advantages. Over past few decades, buccal route for systemic drug delivery using mucoadhesive polymers to significantly improve the performance of many drugs has been of profound interest. Many ways of research work may be carried out to develop more this formulation for delivery of drug.

Abstract

The objective of the present work was to develop and validate a simple, selective, linear, precise, accurate RP-HPLC method for the simultaneous determination of Levocetrizine Dihydrochloride (LD) and Phenylephrine Hydrochloride (PH) in tablet. The method involves the use of easily available inexpensive laboratory reagents. The proposed method is based on the separation of two drugs in the reversed phase mode using Thermo Hypersil BDS–C₁₈ (250 mm × 4.6 mm, 5.0 µ) from Germany with isocratic conditions. The optimum mobile phase containing methanol: Aq. Phosphate Buffer (10mM of KH₂PO₄, P_H - 4.55) (90: 10 v/v) at flow rate of 1 ml/min and the effluents were monitored at 218 nm. R_f of LD and PH were 3.108 and 4.367 respectively. Linearity was obtained in the concentration range of 3-8 µg/ml and 3-8 µg/ml respectively for both LD and PH. The mean values of correlation coefficient, slope and intercept were 0.9991 ± 0.96, 23400 ± 1.08 and 14602 ± 1.24 for LD and 0.9994 ± 1.04, 21888 ± 1.01 and 8680 ± 1.09 for PH. The method was validated for precision, robustness and recovery. The LOD and LOQ were 1 μg/ml and 2 μg/ml for LD and 1 μg/ml and 2 μg/ml for PH respectively. As per ICH guidelines HPLC method for LD and PH was developed and validated.

ABSTRACT

Chalcones – one of the major classes of natural products with widespread distribution in fruits, vegetables, spices, tea and soy based foodstuff, have been recently subjects of great interest for their interesting pharmacological activities. Synthesis of chalcones and their related compounds has attracted considerable attention from organic and medicinal chemists for many years as a large number of natural products contain this heterocyclic nucleus as precursor for their synthesis. In this investigation 2’-hydroxychalcones were selected because of its wide range of pharmacological activity such as analgesic, anticancer, antioxidant and the reactive hydroxy moiety helps in cyclodehydration with formation of benzopyrone ring system which is primary structural part of all flavonoids and some other important glycosides. A series of 2’-hydroxychalcones have been synthesized in microwave oven and through conventional method also. All chalcones by conventional method takes 12-15hrs and same chalcones are developed in microwave which requires 1.5-4min. Condensation of o-hydroxyacetophenone with substituted aromatic aldehydes in well closed vessel using microwave irradiation provides fast and simple method for synthesis of 2’-hydroxychalcones without formation of any by products. Considerable increase in reaction rate has been observed with better yield and with high purity. By comparing with Conventional method and Microwave irradiation method later procedure provides faster route for synthesis of chalcones which found to be more economic, ecofriedly and convenient.

Abstract

A simple, specific, accurate and precise reversed phase high performance liquid chromatographic method was developed for the simultaneous estimation of Eperisone Hydrochloride and Diclofenac Sodium in capsule dosage form. The determination was carried out by Waters C18 (250 mm x 4.6 mm x 5μm) column using a mobile phase of   Methanol: Water (90:10 v/v) at a flow rate of 1 mL/minute. Detection was carried out at 269 nm with UV-visible detector. Calibration curves were linear with correlation coefficient (r ²) 0.999 over a concentration range of 15-90 μg/mL for Eperisone Hydrochloride and 0.999 over a concentration range of 10-60 μg/mL for Diclofenac Sodium.  The retention time for Eperisone Hydrochloride and Diclofenac Sodium was found to be 4.34 and 2.99 minutes, respectively. The mean recoveries were found 100.95±0.94 and 100.73±0.38 for Eperisone Hydrochloride and Diclofenac Sodium respectively. The suitability of this method for the quantitative determination of Eperisone hydrochloride and Diclofenac Sodium was proved by evaluating different validation parameters. Relative standard deviation values were found to be ≤2%. The results of analysis of capsule dosage form were in good agreement with the labeled claim i.e. 100.22% ± 0.50 for Eperisone Hydrochloride and 100.90% ± 0.16 for Diclofenac Sodium. The proposed method was found simple and sensitive for the routine estimation of Eperisone Hydrochloride and Diclofenac Sodium in combined solid dosage form.

Abstract

Tinospora cordifolia is a well-known medicinal shrub in Asia, belongs to family Menispermaceae, commonly known as Guduchi is a large, deciduous climbing shrub of the family Menispermaceae. It is found throughout the great parts of India but now it is listed amongst threatened species in many areas in the country. Many medicinal plants are also in trouble from over harvesting and destruction of habitat. Population growth, urbanization and the unrestricted collection of medicinal plants from the wild is resulting in an overexploitation of natural resources. Hence there is an urgent need for its conservation.

Abstract

A study was conducted to investigate the anthelmintic and cytotoxic activities of methanolic extracts of Typha elephantina Roxb. Although many investigations have previously been reported with this plant, the species growing in swampy areas of Bangladesh has not been studied much. Typha elephantina was extracted with organic solvent (methanol). In anthelmintic activity test (using Pheretima posthuma model), the parameters like: time of paralysis (vermifuge) and time of death (vermicidal activity) were determined by using the methanolic extract at various concentrations. The methanolic extract exhibited anthelmintic activity comparable with standard reference. On the other hand, brine shrimp cytotoxicity test was carried out by using Artemia salina. A reputed cytotoxic agent vincristine sulphate was used as a positive control. The extracts have exhibited considerable and significant cytotoxic activity as compared to the standard compound. From these observations, it was concluded that extracts have potential anthelmintic and cytotoxic properties. The plant may further be explored for its various pharmacological activities.

Abstract

Several techniques are used to increase the aqueous solubility of poorly water soluble drugs. Hydrotropic solubilization technique is one of them. A simple, efficient and new spectrophotometric method has been developed for spectroscopic estimation of Terconazole in bulk form. In the present study, a very slightly soluble drug, Terconazole has been solubilize in water using hydrotropic agent of urea and scanned between 200-400nm taking respective reagent blanks in a double beam spectrophotometer. The λ max was found to be 286nm and Terconazole was found to be linear in the range of 50-250 μg/ml. In this proposed method, organic solvents are not used which makes it eco-friendly. Thus, hydrotropic solubilization technique, a novel approach can be used not only for estimation but also used to increase solubility and release of poorly water soluble drugs. The hydrotropic agent used is cost efficient, safe and non-harmful to environment, hence it can be employed for routine analysis of Terconazole in bulk form. Hydrotropic agent urea did not interfere in spectrophotometric determination. From the results it was justified that hydrotropic solubilization technique is one of the best method used to increase the solubility of the Terconazole as it shows a gradual linearity values with increase in amount of urea and so finally this method is used for routine quantitative analysis of terconazole samples.

Abstract

Drug dissolution testing plays an important role as a routine quality control test, for characterizing the quality of the product, for accepting product sameness under SUPAC (Scale-Up and Post-Approval Changes) related changes, in waiving bioequivalence requirements for lower strengths of a dosage form and in supporting waivers for other bioequivalence requirements. Absorption of a drug is possible only after dissolution i.e. when drug molecule is present in solution form. Thus, dissolution is a prerequisite step for the drug absorption. It can help to identify potential problems of in vivo release and bioavailability/absorption following administration and thereby guiding the selection of prototype formulations. This review article is focus on the history of dissolution, importance and application of dissolution, mathematical concept and validation method of dissolution study. This review article is also focus on the construction and specification of dissolution test apparatus and its acceptance criteria as per different pharmacopoeias like Indian pharmacopeia, US pharmacopoeia, British pharmacopoeia and international pharmacopoeia.

Abstract

Carbon nanotubes (CNTs) up to now are the most researched materials of the 21st century with an international intention of growing industrial quantities due to their superior properties for use in many applications either in medical or other potential applications. These compounds have become increasingly popular in various fields simply because of their small size and amazing optical, electric and magnetic properties when used alone or with additions of metals. These are often described as a graphene sheet rolled up into the shape of a cylinder. To be precise, they are graphene cylinders about 12 nm in diameter and capped with end containing pentagonal rings. Carbon nanotubes have potential therapeutic applications in the field of drug delivery, diagnostics, and biosensing. Functionalized carbon nanotubes can also act as vaccine delivery systems. The basic concept is to link the antigen to carbon nanotubes while retaining its conformation, thereby, inducing antibody response with the right specificity. In present paper the different types of CNTs, their methods of preparation & purification are discussed .The paper opens the recent trends towards CNTs in drug delivery. With the increasing interest shown by the nanotechnology research community in this field, it is expected that plenty of applications of CNTs will be explored in future. Current work is focused on the recent developments, particularly of Nanoparicles and Nanotubes. The materials developed from such as the hollow nanospheres, core shell structures, nanocomposites, nonporous materials, and nanomembranes will play a growing role in materials development for the Medical and Nonmedical industry.

Abstract

For the treatment of pain and inflammation Non-steroidal anti-inflammatory drugs are the most frequently used medications, but because of number of side effects limit their uses. Transdermal drug delivery system (TDDS) provides sustain drug release for systemic as well as local treatment and reduces the side effects associated with its oral therapy. Transdermal delivery of NSAIDs has advantages of avoiding hepatic first pass effect, drug degradation in GIT, specific problems associated with the drug like gastric irritation and lower absorption. By TDDS of NSAIDs can be deliver the drug for extended period of time at a sustained level. The present article gives the brief view on the formulation, development and evaluation been done on various NSAIDs transdermal patches to reduce the side effects associated with the oral delivery. The various NSAIDs included in this article are Diclofenac Acid, Aceclofenac, Lornoxicam, Celecoxib, Ketoprofen, Ibuprofen Naproxen, Indomethacin, Ketorolac, Meloxicam, Tenoxicam. Transdermal delivery of NSAIDs has advantages over oral delivery by avoiding hepatic first pass effect, drug degradation in GIT, dose dumping, specific problems associated with the drug like gastric irritation and lower absorption and hence increases the patient compliance. The market of transdermal product has been in significant upward trend and likely to continue in future.

Abstract

A simple reverse phase HPLC method was developed and validated for the Simultaneous determination of Diacerein and Aceclofenac in pharmaceutical dosage form. The separation of the analytes was performed on a Hypersil ODS column (250 x 4.6 mm, 5 micron) is used as a stationary phase with a mobile phase consisting of acetonitrile:buffer (pH-5.6)  (40:60 v/v), set at a flow rate of 1ml/min and separation was monitored by UV detector, at a detection wavelength of 228 nm. Retention time of Diacerein and Aceclofenac was, 3.43 and 5.03 min. respectively.  Validation of the method for linearity, precision, ruggedness, accuracy, specificity, robustness was performed. The linearity range was found to be 12.5-75 mg/ml for Diacerein and 25-150 mg/ml for Aceclofenac. Recovery of Diacerein and aceclofenac was found to be in the range of 98.0-102.0%. Proposed method was simple, fast, precise, accurate & was found to be suitable for the routine analysis and quality control of pharmaceutical preparations containing these drugs either individually or in combination.

Abstract

The present study deals with the design and optimization of Prednisolone sodium phosphate (PSP) microspheres to target and activate the drug release at specific sites in colon. Combinations of pH dependent and microbially triggered polymers were employed to target the drug at the colonic region. PSP loaded guar gum microspheres were prepared using emulsion solvent evaporation technique and were further microencapsulated by an enteric polymer, HPMC acetate succinate. For the development of PSP microspheres, Quality by Design approach was implemented. Based on risk assessment of critical quality attributes (CQAs), the effect of independent parameters, surfactant concentration (Span 80) and Coat: Core ratio (HPMC AS MF: PSP-GG microspheres) on microsphere size, encapsulation efficiency, drug release after 2 and 5 hrs was optimized using 3² Factorial design. For the optimized formulation, microspheres size was ranging from 214-250 µm and encapsulation efficiency was 84-86 %. The in vitro drug release from the microspheres after 2 and 5 hrs was found to be less than 6.25% and 26.39% respectively. To confirm the role of native microbial flora as triggering mechanism for burst release of drug from Guar gum core microspheres, the in vitro dissolution studies were carried out using ceacal content of rats fed on Guar gum. The microspheres clearly indicated burst release due to enzymatic degradation of Guar gum. The scanning electron micrographs of microspheres revealed perfect spherical shape of microspheres as well as double encapsulation of drug. X-ray diffraction patterns of microspheres did not show any change in the amorphous state of the drug during process.  The values of micromeritics properties indicated good flow properties of these microspheres. Conclusively, GG-HPMC AS MF microspheres were found to target PSP efficiently at distal part of small intestine and colon by using the combined approach of pH-dependent and microflora activated system. It was demonstrated that the use of Quality by Design (QbD) principles, provide an effective means to achieve a greater understanding of process and formulation parameters for microsphere preparation.

Abstract

Plants have been utilized as medicines from thousands of years. Today’s most common medicines are developed from compounds found within the medicinal herbs. With this increase in the demand of medicinal plants, they are being overexploited and are under threat. Also many medicinal plants are disappearing at an alarming rate due to rapid agricultural and urban development, uncontrolled deforestation and indiscriminate collection. Plant tissue culture is the only technique for conserving the rare, endangered and threatened medicinal plants within a short period of time. Tinospora cordifolia is one such plant which is facing alarming threat. The purpose of this work was to establish an effective in vitro micropropagation protocol for Tinospora cordifolia using nodal segments as explants. The nodal segments inoculated in MS basal medium supplemented with 0.5 mg/l BA + 0.2mg/l NAA produced multiple shoots with an average height of 9.98±0.88 after 2 weeks of incubation. Regenerated shoots were rooted on half strength MS basal medium containing 1.0mg/L BA = 0.2mg/L IAA. Rooted plantlets were transferred to pots containing soil for acclimatization, for a period of three weeks and were successfully established in soil. After acclimatization and transplantation 100% acclimatized plantlets were found healthy in ex-vivo conditions.

Abstract

Recent advances in Novel Drug Delivery System (NDDS) aims to enhance safety and efficacy of drug molecule by formulating a convenient dosage form for administration and to achieve better patient compliance. One such approach is Fast Dissolving Tablet. The development of new drug delivery systems for existing drug with an improved efficacy and bioavailability together with reduced dosing frequency to minimize side effects. Who may experience problems in swallowing solid dosage forms, are the mentally ill, they are mentally disabled, uncooperative patient and reduced liquid intake plans or nausea. In some cases such as motion sickness, sudden episode of allergic attack or coughing and an unavailability of water, swallowing tablet may become difficult. Fourier transform Infrared spectroscopy confirmed the absence of any drug/polymers/excipients interactions. SEM and stability studies were carried out only for best release formulations.  Formulations were formulated by various materials like. Ac – Di- Sol, Crosspovidone, SSG. Avicel pH 102. The prepared tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, in-vitro dissolution studies .Prepared tablets exhibited first order kinetics and the drug release profile was matrix diffusion formulation was optimized by fitting the data into various kinetic Models.

Abstract

Literature review revealed that no method has been reported for simultaneous estimation of Vardenafil and Dapoxetine by spectrophotometry or RP-HPLC. In present research work attempt was made to develop the methods for simultaneous estimation of Vardenafil hydrochloride (VRDC) and Dapoxetine hydrochloride (VRDC) in combined pharmaceutical dosage form by spectrophotometry and RP-HPLC. Two simple, rapid, accurate, precise, reliable and economical methods have been proposed. They are absorbance ratio (Q-ratio) method and RP- HPLC. For absorbance ratio method wavelength selected were 280nm, isoabsorptive point and 292nm (λ_max of DPH).  The linearity range for VRDC and DPH were found to be 6-18 µg/ml and 18-54 μg/ml for absorbance ratio method. A RP-HPLC method was developed on Lichrospher® 100, RP-18 C (5 µm), Merck Ltd., India, 250 mm L × 4.6 mm Æ in size using mobile phase Methanol: Acetonitrile (95: 5 v/v) with 0.5 % triethyl amine. The flow rate was 1.2 ml/min and column effluents were monitored at 280nm. Retention times were 2.25 min and 3.45 min for VRDC and DPH respectively. For RP- HPLC method linearity range were found to be 10-30 µg/ml and 30-90 µg/ml for VRDC and DPH, respectively. Both the developed methods were validated in terms of linearity, limit of detection, limit of quantification, accuracy, precision, and robustness according to ICH guideline. The value of %RSD for intraday and interday precision was found to be less than2 for both the methods. This value confirms that methods are precise. The value of % recovery between 98-102shows that the methods are accurate and free from the interference of excipients used in formulation. The developed methods were successfully applied to perform assay of marketed tablet dosage form and the results were found in good agreement with % labelled claim.

Abstract

Diabetes mellitus, a complex metabolic disorder is an increasing concern, worldwide in terms of health. It is characterized  by chronic  hyperglycemia with disturbances  of  carbohydrate,  fat  and  protein  metabolism resulting  from  defects  in  insulin  secretion,  insulin  action  or both.  The disorder affects more than 100 million people worldwide and by 2030 it is predicted to affect 366 million. Therefore, the human population worldwide appears to be in the midst of an epidemic of diabetes. The introduction of insulin and oral hypoglycaemic agents revolutionized the management of diabetes mellitus. In spite of advances in drug management of diabetes, there are still complications and adverse drug reactions. So the searching for new anti-diabetic drugs continued. Hence the present study was aimed to assess the hypoglycemic activity of Evolvulus alsinoides in streptozotocin induced diabetic rats. In this study the estimation of glucose, urea, uric acid, creatinine, hemoglobin and glycosylated hemoglobin were done in plasma and serum of experimental rats. Oral administration of plant extract at 150 mg/kg for 45 days showed the reduction of glucose level and helps to restore the serum metabolites in streptozotocin induced rats as to that of control. The present study clearly indicated that the whole plant ethanolic extract of Evolvulus alsinoides has significant effect on glucose and protein metabolism. It also helps to improve the hemoglobin level streptozotocin induced rats. Hence, it could be concluded that ethanolic extract of Evolvulus alsinoides may be used clinically in the management of diabetes mellitus.

Abstract

Solubility is an essential characteristic as well as influences the efficiency of the drug. The solubility problem can be solved by changing the crystal habit of drug, which improves the solubility and dissolution. Crystallization is also a purification process to remove the impurities from pharmaceutical products. In the present investigation an attempt has been made to improve the solubility characteristics of Tinidazole using crystallization method by solvent evaporation technique. Different ratios of drug and lactose were selected for the preparation of co-crystals. The formulated crystals of tinidazole were subjected to various physico-chemical parameters like microscopic observation, melting point, angle of repose, carr’s index, solubility study, dissolution study, Infra-red study, X-ray diffraction study, Differential scanning calorimetry study. Solubility of Co-crystal was found to be 10.95 ± 0.30 mg/ml which is more than physical mixture and pure drug. Co-crystals having best release profile than physical mixture as well as pure drug. IR spectra of Physical mixture and co-crystal indicated no change in functional group. DSC study indicated no chemical but only physical interaction was observed between lactose and tinidazole in co-crystal preparation. The present study can conclude that co-crystallization with lactose through solvent evaporation can be the best tool for enhancement of flow property, solubility and dissolution profile of poorly water soluble drug like tinidazole via covalent or non-covalent interaction such as hydrogen bonding, ionic interaction van der Waals interactions.

Abstract

Human brain is the most evolved complex structure in the body. Neurodegenerative disorders such as Parkinson's disease (PD), Alzheimer's disease (AD), Huntington's disease (HD) and amyotrophic lateral sclerosis (ALS) are relatively common and represent a substantial medical and societal problem. Presently available pharmacological treatment for neurodegenerative disorders are symptomatic and do not alter the course or progression of the neurodegenerative disorders. Hence, this study was carried out with an interest and contribution for herbal medicines as essential potent drug. Dalbergia sissoo (family: Fabaceae) is an Asian deciduous rosewood tree. It is the state tree of Punjab state (India) called as Shisham used for aphrodisiac, abortifacient, expectorant, anthelmintic and antipyretic, memory enhancer etc. The leaf extract of Dalbergia having more concentration of flavonoids and its neuroprotective effect in animals is unclear. To validate the ethno therapeutic claims of the plant, ethanolic extract of Dalbergia sissoo leaves was evaluated by checking brain weight, antioxidant levels, histopathological and TTC staining studies in cerebral ischemia induced rats. The extracts (ethanolic 300,600 mg/kg) were compared to negative control (global cerebral ischemic rats). It is observed that prior treatment of Dalbergia sissoo extract (DSE) (300mg/kg and 600mg/kg, p.o. for 10days) markedly reversed the brain weight, antioxidant levels and restored to normal levels as compared to I/R groups. Moreover, brain coronal sections staining and histopathological studies revealed protection against ischemic brain damage in the DSE treated groups. From the results obtained, it is evident that the traditional herbal leaf extract had a significant neuroprotective activity.

Abstract

Endophytes which reside in the plant tissues have potential in producing novel metabolites for exploitation in medicine. Crocus sativus was investigated for potential of endophytes. A total 47 endophytes were isolated from 220 segments of 40 saffron plants, Fungal endophytes were identified as Fusarium sp. Rhizoctonia sp. Trichoderma sp. Phytophthora sp. Penicillium sp. and Alternaria sp. Frequency of Rhizoctonia sp. was dominant followed by Fusarium sp. Phytophthora sp. Alternaria sp. and Trichoderma sp. Penicillium sp. Overall colonization frequency of endophytes in both corm and stem was found to be 21%. The stem showed low percentage frequency of colonization of endophytic fungi when compared to corm segments. The extract of all 47 endophytes were prepared from the fermented broth  tested for antimicrobial activity against Staphylococcus aureus ATCC-6538, Bacillus subtilis ATCC-2063, Pseudomonas aeruginosa MTCC 741, Escherichia coli ATCC 2065 Candida albicans and Aspergillus niger ATCC 1197. Antimicrobial screening was carried out by using the agar diffusion method. The extract of two Penicillium sp. demonstrated strong antimicrobial activity against E. coli, S. aureus, B. subtilis and P. aeruginosa. The extract of Alternaria sp.  Significantly inhibitory to Candida albicans and A. niger also to E. coli, S. aureus B. subtilis and P. aeruginosa. Least antimicrobial activity was showed by Fusarium sp. extract. The result of this study suggested biodiversity of endophytes in Crocus sativus and their metabolites could be a source of bioactive natural product against some microbial pathogens mentioned above.

Abstract

We report the organic synthesis of some novel 3-Hydroxy-2phenyl-chromene-4-ones (flavonols) by oxidative cyclisation of corresponding chalcones in cold alkaline hydrogen peroxide. These newly synthesized compounds were evaluated  for their antioxidant potential using DPPH screening method.The promising feature of this reaction is  excellent yield with high purity of compounds synthesized. All the synthesized compounds were confirmed by IR, ¹HNMR and MS data. Synthesized compounds exhibited potent antioxidant activity, which is close to standard flavonoid Quercetin.

Abstract

Baclofen is structural analog of gamma aminobutyric acid is a centrally acting skeletal muscle relaxant, which is widely used in the treatment of spasticity resulting from multiple sclerosis, muscle spasms, muscular rigidity and spinal cord injuries, where pain persist predominantly, in such cases the quick onset of action is of prime importance. In present research work an attempt has been made to prepare fast dissolving tablets of Baclofen were prepared by using vacuum drying technique. Camphor and Menthol are used as a sublimating agent. The blend was examined for the pre-compression parameters. The prepared tablets formulations were evaluated for post-compression parameters. The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. All the post-compression parameter are evaluated were prescribed limits and results were within IP acceptable limits. The weight variation in the range 98 to 101 mg which is below ± 7.5%, hardness of 2.5 to 3.5 kg/cm², disintegration time of 13 to 58 sec. The tablets prepared by direct compression technique posses a weight variation in the range 98 to102 mg which is below ± 7.5%, hardness of 3 to 3.5 kg/cm², disintegration time 12 to 50 in vitro drug release showed 39.44% - 99.15% within 4 min. The prepared tablets were characterized by FTIR Studies. No chemical interaction between drug and excipients was confirmed by FTIR studies. The disintegration time of promising formulations BS₃ and BS₆  were found 13 and 27 sec respectively. By the addition of superdisintegrants and sublimating agents the disintegration time increased significantly (P<0.05) tablets prepared. In case of sublimation method Before subjecting to vacuum drying the tablets images were taken with scanning electro microscopy and found that there was no formation of pores in the tablets. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. The results concluded that fast dissolving tablets of Baclofen showing enhanced dissolution will lead to improved bioavailability and effective therapy by using sublimation method.

ABSTRACT

Asmarihara Kasaya Curna (ASM), a classical ayurvedic preparation which is widely used in urolithiasis. The present study was designed for observing its effect on the liver function parameters on rat’s (albino rats -70 - 90 g) plasma after chronic administrations for 45 consecutive days. Various parameters that demonstrates liver functions (Bilirubin, Albumin, Total protein, ALP, sGOT, sGPT) were observed in both male and female rats.

ABSTRACT

A simple, rapid, specific, precise and accurate reverse phase high performance liquid chromatographic (RP-HPLC) method has been developed and validated for the simultaneous estimation of Paracetamol and Etodolac in tablet dosage form. The chromatographic separation was achieved on Sunfire C18 (150mm x 4.6mm, 5µm) column at a detector wavelength of 233nm using an isocratic mobile phase comprising a mixture of methanol and 0.01M KH₂PO₄ buffer (pH adjusted to 7.5 using 5N NaOH) in the ratio of 55:45(v/v) pumped at a flow rate of 1.0ml/min. Paracetamol and Etodolac eluted at the retention times of 2.588 and 5.786min respectively. The method was validated with respect to parameters such as specificity, linearity, precision, accuracy, robustness, limit of detection, limit of quantification, system suitability. The proposed RP-HPLC method can be used for the estimation of these drugs in bulk and in its pharmaceutical dosage form.

ABSTRACT

Solubility is one of the most important parameter to achieve desired concentration of drug in the systematic concentration for pharmacological response to be shown. Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system.  Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration.   A more than 40% drug suffers from poor water solubility. Currently number of techniques addressed the enhancement of solubility and dissolution rate of poorly soluble drugs. Hydrotropic solubilization is one of them. Hydrotropy is a solubilization phenomenon whereby addition of large amounts of a second solute results in an increase in the aqueous solubility of another solute.   Hydrotropy is one of the solubility enhancement techniques which enhance solubility to many folds with use of hydrotropes like sodium benzoate, sodium citrate, urea, niacinamide etc. and have many advantages like; it does not require chemical modification of hydrophobic drugs, use of organic solvents, or preparation of emulsion system etc.

Abstract

A sensitive, selective and precise UV method for analysis of Donepezil Hydrochloride (DH) as bulk drug and in formulations was developed and validated. Donepezil Hydrochloride is a reversible inhibitor of acetylcholinesterase, indicated for the treatment of mild to moderate dementia of the Alzheimer’s type. In the present work an attempt has been made to estimate the drug by three methods. Method A is absorption maxima method in which λ_max was found to be 270nm. Method B is first order derivative spectroscopy where drug showed λmaxima=280nm and λminima=258nm.In this method amplitude difference (dA/dλ) was calculated and was plotted against concentration and regression equation was calculated. Method C is area under the curve (AUC) in which area in the wavelength range of 265nm - 275nm was selected for analysis of Donepezil Hydrochloride. Linearity was observedin the concentration range 5-25 µg/ml (r² =0.999) for all the three methods. The % assay for the marketed formulation for absorption maxima, first order derivative and area under the curve method was found to be 99.73%, 101.31% and 100.81% respectively. The methods were validated with respect to linearity, precision and accuracy studies. Recovery studies for absorption maxima, first order derivative and area under the curve was found to be100.73%, 100.71% and 99.85% respectively. The methods were found to be simple, rapid, economical, precise and accurate and can be employed for routine quality control analysis of Donepezil Hydrochloride in bulk as well as from its dosage form.

Abstract

The objective of present work was to develop and validate a  simple, linear, precise, accurate and stability indicating RP‐HPLC method  for quantitative determination of Enalapril Maleate and Losartan Potassium in tablet formulation. This developed HPLC method, is cost effective as it does not involve use of expensive solvents and clean up. This method is very Simple and Robust as both peaks are well separated from its excipient peaks and with total runtime of 10 min, makes the developed method  suitable for routine quality control analysis work. Moreover proposed method is more accurate, more precise, more stable and robust developed method.  In RP-HPLC, analysis is carried out using Buffer-Acetonitrile(60:40 v/v) pH4.5 adjusted With o-Phosphoric Acid  as a mobile phase and Hyperchrom phase C-18 BDS Hypersil column (250mm ×  4.6 mm id 5µm) as stationary phase at 235nm and 1 ml/min flow rate. The retention time of Enalapril Maleate  and Losartan Potassium  was found to be 3.150 and 5.420 minutes respectively.  Linearity was obtained in the concentration range of 5-15 μg/ml and 25-75 μg/ml with % recoveries were found to be 98.47% – 100.68% and 98.49% –100.61% for Enalapril Maleate and Losartan Potassium respectively. LOD were   found   to   be   0.120μg/ml   and   0.606μg/ml  at  235 nm  for  Enalapril Maleate and Losartan Potassium respectively. Limit of Quantification and Limit of Detection for Enalapril Maleate  was found to be 0.365 µg/ml and 0.120 and for Losartan Potassium 1.839 µg/ml and 0.606  respectively. Stability method shows that in stress conditions i.e. acidic, basic, oxidation, thermal and photolytic, comparison of  % degradation of tablet dosage form of  drug and its Active Pharmaceutical Ingredient( API)  is satisfactory and less. As per ICH guidelines HPLC method for  Enalapril Maleate  and Losartan Potassium  was developed and validated.

Abstract

From the last decade great interest generated on replacing conventional administration of drug by delivery system which would release effective quantities from a protected supply at a controlled rate over a long period of time. Developing oral sustained release matrix tablet with constant release rate has always been a challenge to the pharmaceutical technologist. So that selecting appropriate polymers have become product of choice as an important ingredient for formulating sustained release formulations. An appropriately designated controlled release drug delivery system is the major advance toward solving problems concerning targeting of a drug to a specific organ or a tissue and controlling the rate of a drug delivery to the target site. Matrix type drug delivery systems are an interesting and promising option when developing an oral controlled release system. This review focuses on the progress made in the design of controlled release dosage forms employing various types of matrices as carriers for the active ingredients.

Abstract

The purpose of the article is to investigate the correlation between the biological activity (pIC50) and topological properties along with fewer indicator parameters. A QSAR study has been carried out on 16 set of TIBO derivatives to know the structural requirement of the molecule. Our previous studied data set for the same compounds showed the importance of Balaben 3D index (J3D). In the present work, role of indicator parameter (presence of halogen atom) along with Balaban-type index (polarizability, Jhetp and Z weighted, JhetZ) is very important to achieve the required lower concentration of the drug. Multiple Linear Regression (MLR) analysis method is obtained to develop the best QSAR model and this best QSAR model is further validated by various statistical parameter viz. Fisher statics (F), Standard error (Se) and Quality factor (Q). The best QSAR model (R² = 0.8566, R²_CV = 0.8328 and Se = 0.4096), consisted of I_X, Jhetp and JhetZ. I_X and Jhetp show the positive correlation with pIC50 whereas JhetZ shows the negative correlation with pIC50. This QSAR study provides important structural insights in design and development of potent anti-HIV agents. This finding supports and shows the importance of Balaben and its types indices to lowering the concentration of the drug molecule. The future synthesis of these compounds can be done in order to keep all this parameter in mind. 

Abstract

To overcome the drawback of oral delivery of drugs with a narrow absorption window in the gastrointestinal tract and to maximize the oral absorption of these drugs, novel drug delivery systems have been developed. In-situ gel provides the best way to overcome the problems of immediate release and short gastrointestinal residence of liquids. The aim of the present work was to develop and evaluate the novel floating in-situ gelling system of Azithromycin dihydrate for controlling the drug release. Gellan based Azithromycin dihydrate floating in situ gelling systems were prepared by dissolving varying concentrations of gellan gum in deionized water containing sodium citrate, to which varying concentrations of drug and calcium carbonate, as gas-forming agent, was added and dissolved by stirring. The formulation variables like concentration of gellan gum and calcium carbonate significantly affected the in vitro drug release from the prepared in-situ gels. Compatibility studies of drug and excipients were carried out using FTIR. The developed formulations were characterized for buoyancy studies, gel strength, microbiological studies, drug content, in-vitro drug release and in-vitro drug release kinetics. The gelation strength was found to be increased with increased concentrations of CaCO₃ and gellan gum. Therefore formulations F5 and F8 had more gelation capacity as they contain more amounts of gellan gum and CaCO₃ respectively. Among all the formulations the F8 formulation showed better sustained release of the drug. From the results, it was observed that the feasibility of in-vitro gel was formed from aqueous solutions of gellan gum containing Ca++ ions in a complexed form, as they possess the gelation capacity and useful for increasing the floating time of the formulations.

Abstract

Objective: To evaluate antibacterial potential and phytochemical analysis of Flacourtia indica (F. indica) root extract.

Methods: Phytochemical screening of the root extract was done to determine the phytochemicals in the methanol extract. The study included the determination of antibacterial activity by agar well diffusion assay, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of methanolic root extract. The antibacterial activity of the root extract was tested against selected human pathogenic bacteria. Further, the methanolic extract of F. indica was screened for the range of phytochemicals by thin layer chromatography and bioactive compound was identified using GC-MS. Results: The extract was effective on tested pathogenic bacteria and MIC values ranged between 50-200mg/ml. While the phytochemical screening of the root extract revealed the presence of flavonoids, saponins, alkaloids, tannins, terpenoids, glycosides and phenolic compounds.

Conclusion: These findings indicate that the root extract of F. indica possesses pharmacological activity and potential to develop natural products based pharmaceutical drugs. The result of this study justifies the use of the plant in folk medicine.

Abstract

A simple UV spectrophotometric method has been developed for the simultaneous analysis of Amlodipine and Clopidogrel in tablet dosage form is based on the absorbance ratio method. The acidic methanol was used as solvent. The two wavelengths were selected 239.4nm as isosbestic point and 361.8 nm as absorption maxima for Amlodipine for the analysis. Amlodipine and Clopidogrel obeyed Beer‐Lambert’s law in the concentration range of 1‐3μg/ml and 30‐90μg/ml with coefficient of correlation 0.9970 and 0.9960 at 239.4 nm respectively. Amlodipine was obeyed Beer‐Lambert’s law in the concentration range1‐3μg/ml with coefficient of correlation 0.999 at 361.8 nm. Recovery of the developed method was found to be in the range of 100.60% for CL and 100.7% for AM.  This proposed method was statistically validated in accordance with ICH guidelines. This method was found to be accurate, precise and rugged as indicated by low values (<2%) of % RSD. This method was also found to be rapid and economical can successfully be applied for the routine analysis of bulk and combined tablet dosage form.

ABSTRACT

A novel, simple, accurate, sensitive and reproducible first order derivative spectroscopic method was developed and validated for the estimation of Ebastine and Montelukast Sodium in combined dosage form. The method obeys Beer’s Law in concentration ranges of 7.5-17.5 µg/ml for Ebastine and Montelukast sodium both. The method was validated for linearity, accuracy and precision as per ICH guidelines. The zero crossing point for Ebastine and Montelukast Sodium was 231.73 nm and 256.30 nm respectively in methanol. The LOD and LOQ value were found to be 0.29 µg/ml and 0.87 µg/ml for Ebastine, 2.44 µg/ml and 7.39 µg/ml for Montelukast sodium respectively. The accuracy of the method was assessed by recovery studies was found to be 99.91 ± 0.080 and 99.47 ± 0.073 for Ebastine and Montelukast sodium respectively. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage forms. The developed method further can be useful for dissolution study and bio analytical study for these drugs in combinations. (EBAST-M).

Abstracta

A simple, economical, specific, accurate & precise validated Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method has been developed for simultaneous estimation of Cetirizine HCl and Phenylephrine HCl in combined dosage form. The RP-HPLC separation was achieved on Phenomenex Luna C₁₈ column (250 mm x 4.6 mm i.d., 5 µm particle size) at ambient temperature using mobile phase Methanol : Water(pH 3.5 ± 0.02) (80 :20  v/v) at flow rate 1.0 mL/min. Quantification was achieved with photodiode array (PDA) detection at 225 nm. The retention time was found to be 4.92min and 2.24 min for cetirizine HCl & phenylephrine HCl respectively. The method was validated in terms of linearity, precision, accuracy, LOD, LOQ and ruggedness according to ICH guideline. The linearity was found to be 5-30 µg/ml with correlation coefficient 0.9999 and 0.995.The mean recovery was found to be 100.73 ± 0.69 % and 100.43 ± 0.503 % for Cetirizine HCl and Phenylephrine HCl, respectively. There was no chromatographic interference of any excipients of tablet dosage form. The developed method with good separation, successfully applied for determination of cetirizine HCl and Phenylephrine HCl in its pharmaceutical dosage form.

Abstract

A new simple, accurate, precise and reproducible RP-HPLC method was developed for the simultaneous estimation of Losartan Potassium, Ramipril and Hydrochlorothiazide in bulk as well as in pharmaceutical dosages form using Symmetry C18 column (4.6 x 150mm, 5mm, Make: Hypersil) in isocratic mode. The mobile phase was consisting of Potassium dihydrogen phosphate (KH₂PO₄) and Acetonitrile in the ratio of 68:32(%v/v). The detection was carried out at 210 nm. The % mean recoveries of Losartan Potassium, Ramipril and Hydrochlorothiazide were found to be 98.0 to 100.8%, 98.9-100.7%and 98.3 to 101.2% respectively. The method was linear over the concentration range for Losartan 50.0 ppm-110.0 ppm, Ramipril 1.255ppm-2.75ppm & Hydrochlorothiazide 12.5ppm-27.5 ppm. The Limit of Detection and Limit of Quantification of the method were calculated basing on standard deviation of the response and the slope (s) of the calibration curve at approximate level. The Limit of Detection for Hydrochlorothiazide, Ramipril and Losartan were found to be 0.01, 0.078 & 0.07μg/mL respectively and Limit of Quantification for Hydrochlorothiazide, Ramipril and Losartan were found to be 0.05, 0.27 and 0.24μg/mL respectively. The validation of method was carried out utilizing ICH-guidelines. The described HPLC method was successfully employed for the analysis of pharmaceutical formulations containing combined dosage form.

Abstract

India is sitting on a gold mine of well-recorded and traditionally well practiced knowledge of herbal medicine. General phytochemical screening of Citrus sinensis (Orange) belonging Rutaceae family revealed the presence of flavones glycoside. The aim of this study is to identify and characterize the bioactive principle compound (Hesperidin) from the peel of C. sinensis fruit. It has wide folk medicinal uses. The isolation and characterization of phytoconstituents was done from the alkaline (KOH) extract of peels.

Abstract

The objective of the present investigation was aimed to reveal the inte-specific variation among the three Plumbago species viz., Plumbago zeylanica Linn, Plumbago auriculata Lam, Plumbago rosea Linn using preliminary phytochemical screening and TLC profiles. To identify the various phytoconstituents and functional groups present in the Plumbago species, the preliminary phytochemical analysis was carried out using Harborne et al., method. TLC chromatographic technique was used to predict the secondary metabolites presence in the screened extracts of Plumbago species based on the band formation. The preliminary phytochemical assay reported the presence and absence of thirteen different compounds in varied degree among these ethanolic extract of all the three Plumbago species showed maximum number of eight compounds.  TLC profiling of the extracts of Plumbago depicted the presence phenol and steroid in different range of band formation. Among all the plant extracts chloroform and ethanolic extract reported maximum number of spots compared to all the other extracts. These techniques paved a way to predict and compare the phytoconstituents present in all the three selected Plumbago species which can be used for further medicinal properties.

Abstract

Indian Curcuma is well known to cure skin infections and its traditional uses as facial cosmetic. Curcuminoids and volatile oils of Curcuma species are known for their therapeutic activities as antiasthamatic, antitumour, stomachic, hepatoprotective, antiarthritis, antiseptic and to cure menstrual disorders. C. neilgherrensis is a wild Curcuma of Eastern Ghats also possesses essential oils, phenols, flavonoids, tannins, saponins and alkaloids. To prove its therapeutic activities against antiasthamatic, antitumour, stomachic, hepatoprotective, antiarthritis, antiseptic, antifungal activity of C. neilgherrensis leaves and rhizome extracts was carried out. Both leaf and rhizome methanol and alcohol extracts are proved most effective on Candida albicans than Aspergillus niger. But antifungal activity of all extracts showed most effective than the reference drug Nystatin and also the MIC values are proved with lowest concentrations. Hence the bioactive constituents may be isolated and further the drug may be formulated to prove its therapeutic activities in support of its herbal uses.

Abstract

In the present investigation, we studied the effect of hydroethanolic extract of an Ayurvedic drug, Bharangyadi on various experimental models of bronchial asthma. The polyherbal compound Bharangyadi contains Bharangi (Clerodendrum serratum), Sati (Hedychium spicatum) & Pushkarmula (Inula racemosa) as ingredient herbs. Significant (P < 0. 05) increase in preconvulsion time was observed on pre-treatment with Bharangyadi extract when the guinea pigs were exposed to histamine aerosol. This bronchodilating effect of Bharangyadi compound was comparable to Mepyramine malate. Alcoholic extract of Bharangyadi produced significant dose dependent protection by egg albumin induced anaphylaxis. Antimicrobial activity of the polyherbal compound was tested against various respiratory pathogens like Escherichia coli (E. coli), Staphylococus aureus (S. aureus) and Pseudomonas aeruginosa (P. aeruginosa). Our data suggest that antiasthmatic activity of  Bharangyadi compound may be due to its bronchodilator, anti-allergic and antimicrobial activity. The study evidence that drug has potent bronchodilator and anti-anaphylactic properties.

Abstract

A novel, simple and economic reverse phase high performance liquid chromatography (RP-HPLC) method has been developed for the simultaneous estimation of Levosulpiride and Rabeprazole sodium in bulk and tablet dosage form with greater precision and accuracy. Separation was achieved on C18 column (250X4.6mm i.d.,5μm) in isocratic mode with mobile phase consisting of acetonitrile, methanol and potassium dihydrogen phosphate (pH was adjusted to 7.4 by using Triethylamine) in the ratio of 50:25:25(v/v/v) at a flow rate 1 mL/min. The detection was carried out at 289nm for both drugs. The retention times of Levosulpiride and Rabeprazole sodium were found to be 2.76 and 4.20 min respectively. The method was validated as per ICH guidelines. Validation studies demonstrated that the proposed RP-HPLC method is simple, specific, rapid, reliable and reproducible. The high recovery and low relative standard deviation confirm the suitability of the proposed method for the simultaneous estimation of these drugs in bulk and tablet dosage.

Abstract

Drugs on diarrhoea, infant immunity, neck and back aches has been become very much essential now- a- days due to stress and strain of present day life style and food habits . Hence herbal drugs like Indigofera hirsuta has the ability in healing above problems as reported by African tribals and also the local herbalists. Studies on antibacterial activity and MIC values of fruit extracts of I. hirsuta on certain human pathogens were carried out as per the standard methods. Fruits consists nearly 14 Phyto constituents mainly in aqueous, methanol, alcohol, ethyl acetate and chloroform extracts. Fixed oils are totally absent. Antibacterial activity against selected four bacterial strains was very effective than the control drug Ampicillin and the MIC values ranges from 0.019mg to 0.312mg. Hence I. hirsuta proved its herbal usage against diarrohea, chest and body pains, infant immunity and skin diseases.

Abstract

Exploration of Tin oxide based `herbal drug formulation Vanga Parpam in terms of crystallographic structural aspects is crucial to assess the quality and performance of the drug.  The present report is the second part of the research study on the drug formulation on the basis of phase purity, crystallite size and surface area, and porosity using Powder X-ray diffractograms, Raman spectra, adsorption isotherms, microscopic image during its ten step calcinations process.The results of the study confirmed the formation of nanocrystalline tin (IV) oxide without impurity in the crystal lattice of the metal oxide. The strong aggregation of the crystallites with the presence of the therapeutic elements at the surface of the crystallites indicated surface active principle of the drug and hence therapeutic activity.  The above results provided an authentic assessment of the crystallite size, chemical stability of the drug sample during the preparation which could be used for the optimisation of the process parameters, standardisation of the formulation for wider acceptability and usage.

ABSTRACT

This study was designed to evaluate the antipyretic activity of triterpenoids isolated from methanolic extract of Ziziphus mauritiana Lam root by using yeast-induced pyrexia model in rats at a dose of 200 mg/kg b.w. The results indicated Maslinic acid, 2 α–hydroxyurosilic acid and Betullinic acid (P<0.01) compounds from methanolic extract of Z. mauritiana root at a dose level of 200 mg/kg p.o., showed significant (P<0.01) reduced the elevated body temperature in  experimental rat. This antipyretic activity in brewer yeast-induced pyrexia in rats throughout the observation period of 4 hours. Hence, this Plant has significant antipyretic activity when compared with the standard drug. So. It can be recommended for further studies.

Abstract

Caesalpinia pulcherrima L. (Caesalpiniaceae) is an attractive plant due to its array of flowers, which appear yellow, pink, off-white, and red with yellow margins. Caesalpinia pulcherrima is also known as peacock flower. It is a common medicinal plant in India, Taiwan and South-East Asian countries. In alternative medicine, the different parts of this plant have been used as an anti-inflammatory, abortifacient, emmenagogue, bronchitis and malarial infection while fruits are employed to cure diarrhea and dysentery. In the present investigation Evaluation of Membrane Stabilizing Potential (HRBC) and antimicrobial activity of the Pods of Caesalpinia pulcherrima (Caesalpiniaceae) against Selected Microorganisms. HRBC membrane stabilization method used for evaluation of in-vitro anti-inflammatory activity and Diffusion assay (Plate method) for Antimicrobial Activity. In-vitro anti-inflammatory activity (HRBC Stabilization) of Caesalpinia pulcherrima of extracts showed good inhibitory activity in petroleum ether extract as % Inhibition of  Haemolysis 7.5 %, 22 %, 27 % and 37 % in 10, 25, 50 and 100 μg/ ml Concentration respectively. Chloroform extract and methanolic extracts of Caesalpinia pulcherrima showed moderate to good zone of inhibition against Selected Microorganisms compared with standard as Gentamicin. The HRBC membrane stabilizing property of Caesalpinia pulcherrima was found to be promising and also exhibited good antimicrobial activity.

Abstract

The present investigations deals with the formulation of fast dissolving tablet of Meloxicam with the effect of different Novel co-processed superdisintegrants by solvent evaporation method that disintegrate in oral cavity on contact with saliva & thereby improve therapeutic efficacy. Over the past three decades, mouth dissolving or orally disintegrating tablets have gained considerable attention as a preferred alternative to conventional tablets due to better patient compliance. Meloxicam is a newer selective cox-1 inhibitor & the present research shows that the use of different co-processed superdisintegrants enhance the activity of meloxicam through rapid release. The tablet containing drug were prepared by direct compression methods using  Novel co-processed superdisintegrants as Starlac, Ludipress, Ran explo-S, Ran explo-C, Pan-excea MH-300G. The tablets were evaluated for thickness, weight variation test, drug content, hardness, friability and in-vitro drug release studies. In-vitro drug release studies of the prepared tablets were conducted for a period of 25 minutes using an USP dissolution test apparatus (type II Paddle) at 37±0.5°C and 75 rpm. The optimized formulation-F8 containing Ran explo-S  showed 99.15 % drug release in 25minutes. The tablets prepared from Co-processed superdisintegrants shows optimum result as compared to other superdisintegrants if use alone. Thus result shows that Co-processing of superdisintegrants is most suitable approach for formulation of Fast dissolving tablet.

Abstract

Solid lipid nanoparticles (SLN) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicine and research as well as in other varied sciences. The era of nanotechnology has revolutionized the drug delivery system and persuades new research strategies to flourish. SLN have attracted various research groups and companies since the early 1990s, however research in the SLNs is still in its infancy. SLN technology based therapy has made available a novel and sound platform for therapeutics. They have been developed as an important strategy to deliver drugs by modifying their release, body distribution and kinetics of associated along with tissue and cell targeting of drugs and reduction of unwanted side effects by controlled release of the medicament. They are interesting vectors for oral delivery of lipophilic and to a certain extent, hydrophilic substances. The presence of lipids in the absorption process or transfer of hydrophilic molecules to more lipophilic molecules by conjugation has been reported to increase the oral absorption. The lipid absorption enhancing effect can even be more pronounced when combining lipid technology with nanotechnology, which is creating lipidic solid nanoparticles. 

Abstract

The methanol extract of Allium hookerii leaves was investigated for its anti-diabetic effect in Wistar Albino rats. Diabetes was induced in Wistar Albino rats by administration of single dose of Streptozotocin (70mg/kg). The methanol extract of Allium hookerii at the dose of 150mg/kg and 300mg/kg, p.o. was administered as single dose per day to diabetes induced rats for a period of 21 days. The effect of Allium hookerii extract on body weight of the animals, blood glucose, serum lipid profile [cholesterol, triglycerides], serum enzymes [serum glutamate oxaloacetate transamines (SGOT), Serum glutamate pyruvate transaminases (SGPT), SALP, total protein were measured in the diabetic rats. Allium hookerii extract elicited significant (p< 0.01) reductions of blood glucose, lipid parameters and serum enzymes and significant (p<0.01) reductions of blood glucose. From the above result, it is concluded that methanolic extract of Allium hookerii leaf extract possesses significant anti-diabetic effects in Streptozotocin induced diabetic rats.

Abstract

Oral sustained release gastroretentive dosage forms offer many advantages for drugs with absorption from upper parts of gastrointestinal tract and for those acting locally in the stomach. Floating drug delivery system is one amongst the gastroretentive dosage forms used to achieve prolonged gastric residence time. Bilayer floating drug delivery system is combined principle of bilayer tablet as well as floating mechanism. Bilayer floating tablet is new era for the successful development of controlled release formulation along with various features to provide a way of successful drug delivery system. Bilayer floating tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances and also for sustained release tablet in which one layer is immediate release as initial dose and second layer is maintenance dose. The purpose of this paper is to review the current technology used in the development of bilayer floating drug delivery system as well as summarizes the applications, characterization, evaluation methods and future potential for bilayer floating tablets.

Abstract

Solanum indicum Linn. (Solanaceae) is grown in waste places, road sides and in open scrublands in different parts of India and other Asian countries. Its roots and leaves are used in traditional system of medicine for a long time. Several phytochemicals like fatty acids, alkaloids, steroids, flavonoids and saponins have been reported from the different parts of the plant but their biological efficacies were not evaluated. Hence, the berries of the plants were collected, authenticated and extracted with MeOH for screening antioxidant and also anthelmintic activity. In vitro DPPH radical scavenging activity using BHT as a standard and anthelmintic activity on Indian earth-worm (Pheretima posthuma) using Albendazole as a standard of crude MeOH extract of Solanum indicum berries were evaluated. Nine different concentrations (200, 100, 80, 60, 40, 20, 10, 1, 0.5 µg/ml) of MeOH extract were studied for DPPH scavenging activity. The maximum DPPH radical scavenging activity with inhibition was found at the concentration 200 µg/ml and it was 70.007 ± 0.841% as comparable to that of BHT having 95.023 ± 0.091% inhibition at the same concentration. Three concentrations (25, 50, 100 mg/ml) of extract were studied for anthelmintic activity which involved the determination of time of paralysis and time of death of the worms. All the concentration of extracts exhibited significant dose dependent activity.

Abstract

Considering that oxidative stress is strongly implicated in the toxicity of chemotherapy, much effort is focused on the research of diverse antioxidants as protective agents. Benzophenone and its derivatives play an important role in medicinal field with many pharmacological activities. An efficient synthesis and antimicrobial efficacy of novel benzophenones containing 3-(2-aroylaryloxy) methyl-6-phenyl-1,2,4-triazolo[3,4-b][1,3,4] thiadiazine 6a-e is described previously. Further to ensure antioxidant properties of compounds 6a-e we have subjected all the compounds to DPPH, nitric oxide and hydrogen peroxide scavenging assay. Compounds 6b, 6e and 6d were showed potent antioxidant activity near to standard ascorbic acid due to the presence of chloro, methoxy and methyl substituent’s respectively and remaining analogues in the series shown moderate to poor potency.

Abstract

Functional foods provide health benefit beyond nutrition and target body functions. They play an important role in modern nutrition which is expected to promote health and reduce the risk of chronic diseases. One of the most urgent tasks concerns the conditions for health claims are prebiotic nondigestible fructooligosaccharide (FOS) which selectively stimulate the activity of bacterial populations already resident in the consumer’s intestinal tract. A newly fructosyl transferase (FTase) producer microorganism Aspergillus flavus (NFCCI 2364) was investigated for conversion of sucrose to fructooligosaccharides. The effect of fermentation parameters on fructosyltransferase was evaluated to enhance biotransformation of sucrose to fructooligosaccharides. By altering certain parameters, best transfructosylating activity was observed from cultivation medium containing pH 6 at agitation speed of 200 rpm. Various carbon and nitrogen sources were used to enhance enzyme production and highest yield was obtained when media were optimized by applying 10% (w/v) sucrose as sole carbon source and 1% (w/v) peptone as best nitrogen source. In enzyme substrate reaction of 24 h, fructooligosaccharide yield was elevated up to 68.38% (w/w) using sucrose concentration 60% (w/v). The HPLC analysis elucidates Kestose (GF2) as main constituent oligomer than other saccharides which is beneficial for its sweetening capability

Abstract

Recent advances in Novel Drug Delivery Systems (NDDS) aim for designing dosage forms, convenient to be manufactured and administered, free of side effects, offering immediate release and enhanced bioavailability, so as to achieve better patient compliance. Though oral drug delivery systems, preferably, tablets are the most widely accepted dosage forms, for being compact, offering uniform dose and painless delivery. Yet, dysphagia is the most common disadvantage of conventional tablets. This is seen to afflict nearly 35% of the general population and associated with a number of conditions, like Parkinsonism, mental disability, motion sickness, unconsciousness, unavailability of water etc. To overcome such problems, certain innovative drug delivery systems, like ‘Orodispersible tablets’ (ODT) have been developed. These are novel dosage forms which dissolve in saliva within a few seconds, when put on tongue. Such ODTs can be administered anywhere and anytime, without the need of water and are thus quite suitable for children, elderly and mentally disabled patients. The aim of this article is to review the ideal properties, significance, characteristics, choice of drug candidates, challenges informulation, various technologies for preparation of ODTs, Patented technologies on ODTs, Suitable drug candidates for ODTs, Evaluation tests of ODTs and Marketed product of ODTs.

Abstract

The manuscript describes validated Reverse Phase High Performance Liquid Chromatographic (RP-HPLC) method for the simultaneous estimation of Amlodipine Besylate and Indapamide in combined dosage form. The RP-HPLC separation was achieved on Intersil ODS C₁₈ column (250 mm x 4.6 mm i.d., 5 µm particle size) at 40^oC using mobile phase Acetonitrile : Acid Phthalate Buffer (pH 3.0 ± 0.05) (50 :50, v/v) at flow rate 1.0 mL/min. Retention time was found to be 2.31 and 5.11 for Amlodipine and Indapamide, Respectively. Quantification was achieved with photodiode array (PDA) detection at 240 nm over the concentration range of 10 - 50 µg/mL for Amlodipine Besylate and 3 - 15 µg/mL for Indapamide with mean recovery of 100.09 ± 0.52 % and 100.13 ± 0.09 % for Amlodipine Besylate and Indapamide, respectively. LOD and LOQ were found to be 0.69 µg/mL and 2.08 µg/mL for Amlodipine and 0.19 µg/mL and 0.58 µg/mL for Indapamide. These methods were found to be simple, sensitive, accurate, precise and economical and applicable for the simultaneous determination of Amlodipine Besylate and Indapamide in combined dosage form.