In the recent years considerable research efforts have been directed towards developing safe and efficient chitosan-based particulate drug delivery systems. Chitosan nanoparticles are good drug carriers because of their good biocompatibility and biodegradability, and can be readily modified. The primary hydroxyl and amine groups located on the backbone of chitosan allow for chemical modification to control its physical properties. When the hydrophobic moiety is conjugated to a chitosan molecule, the resulting amphiphile may form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site of action. Chemical attachment of the drug to the chitosan throughout the functional linker may produce useful prodrugs, exhibiting the appropriate biological activity at the target site. Mucoadhesion and absorption enhancement properties of chitosan increase the in vivo residence time in the gastrointestinal tract and improve the bioavailability of various insoluble drugs. The present review outlines the major new findings on the pharmaceutical applications of chitosan-based nanoparticulate drug delivery systems. The first part of the review is concerned with the organ-specific delivery system using chitosan and its derivatives. The subsequent section covers methods of their preparation, drug loading, release characteristics, and applications. Chemically modified chitosan have increased attention for their wide applications and their research discussed critically to evaluate usefulness of these systems in delivering the bioactive molecules. From literature survey, it is realized that research activities on chitosan nanoparticulate systems containing various drugs for different therapeutic applications have increased at the rapid rate. Hence, the present review is timely.

Key Words: Chitosan, nanoparticles

Diabetes mellitus is a group of metabolic disorders of fat, carbohydrate, and protein it cause defects in insulin secretion, insulin action or both. These days the incidence of type -2 DM is increasing word wide; it’s due to western life style. The present review article gives a general idea of diabetic mellitus, its treatment by using insulin, oral hypoglycemic drugs and herbal drugs. Despite considerable progress in the treatment of diabetes by oral hypoglycemic agents, search for newer drugs continues because the existing synthetic drugs have several limitations .The herbal drugs with antidiabetic activity are yet to be commercially formulated as modern medicines, even though they have been acclaimed for their therapeutic properties in the traditional systems of medicine. A number of plants have been described in Ayurveda and other traditional medicine for the treatment of diabetes. But  information about them is not easily available, in present review article author trying to summarize the various  medicinal plant, there botanical name ,common name and part of plant’s used in  treatment and control hyperglycemia. Goals of therapy in diabetes are directed towards attaining normal glucose level in blood and improved life style by using of herbal medication. India, with their reach sources of medicinal plant which may be used for the treatment of DM.

Kew words – Diabetes, medicinal plant, source of plant, metabolic disorder, and insulin

Piperine (1-peperoyl piperidine), a pungent alkaloid, is found in various Pipper species. Piperine produces antioxidant, antiplatelet, anti-inflammatory, antihypertensive, hepatoprotective, antithyroid, antitumor, antiasthmatic activities and also a fertility enhancer. Piperine enhances absorption from gastrointestinal tract by various mechanisms and reduces gut metabolism of drugs. Piperine modulates membrane dynamics and lipid environment and increases permeability at site of absorption Molecular structure of piperine is suitable for enzyme inhibition and it inhibits various metabolizing enzymes like cytochrome bs, NADPH cytochrome, CYP3A4, UDP-glucose dehydrogenase (UDP-GDH), aryl hydrocarbon hydroxylase (AAH) and UDP-glucuronyl transferase. Structural modification of piperine provides selective inhibitors of various cytochrome p450 enzymes. Inhibition of these enzymes by piperine results in enhanced bioavailability of drugs and nutrients like oxytetracyclin, metronidazole, ampicillin, norfloxacin, ciprofloxacin, acefotaxime, amoxicillin trihydrate, curcumin, beta-carotene, carbamazepine, gallic acid, nimesulide, tiferron, nevirapine, pentobarbitone, phenytoin, resveratrol, vasicine and sparteine by different mechanisms. Thus piperine is an absorption enhancer and a potent inhibitor of drug metabolism.

Key words: Piperine, Metabolism inhibitor, Absorption enhancer, Bio-enhancer, bioavailability

Prosopis spicigera Linn. (Family, Fabaceae) is commonly known as ‘Sami’. It is distributed throughout the arid regions of India and other countries. Sami is caducous plant, so in the foliage condition stem and fruits are common.  It is also commonly known as Prosopis cineraria (L.) Druce. It is one of the chief indigenous tree of the plains of the Punjab, Western Rajasthan, Gujarat, Bundelkhand and the neighborhoods of Delhi and Agra. This plant is xerophytic and draught resistant plant, it can survive for long. Tribal people use this plant as fodder and source of wood. Some of the community uses Sami fruits as food. Prosopis cineraria is a moderate sized evergreen thorny tree, with slender branches armed with conical throns and with light yellowish-green foliage. It contains sugars, five flavonones, fatty acids, tannins and alkaloids. The flavone glycoside patulitrin has been isolated from the flowers. Recently a novel variant on the piperidine-3-ol alkaloid is reported, which is spicigerin. Fruits are used as a food for the people in the desert area during scarcity. Fruits are rich source of vitamins. The leaves besides the pods are eaten by camels, goats and cattle as a fodder. Ashes of the wood rubbed over skin to remove hair. The wood is a good fuel for the preparing food in the tribal area. Prosopis cineraria flower is pounded, mixed with sugar and used during pregnancy as safeguard against miscarriage in women. The bark of the tree is dry, acrid, and bitter with a sharp taste and used in leprosy, dysentery, bronchitis, asthma, leucoderma and scorpion sting. The plant is recommended for the treatment of snakebite in rural area. The present review is an effort to emphasize the traditional uses, pharmacognostical, phytochemical and pharmacological information on Prosopis spicigera Linn.

Key Words: Prosopis spicigera, Xerophytic, Caducous, Sami, Fodder

Molecular mechanisms of myocardial remodeling involves rearrangement of normally existing structure of heart include size, geometry, shape, composition and function of the myocardium and heart. Myocardial remodeling occurs mainly due to physical, mechanical stimuli like cardiac overload, ischemia and stretch as well as at chemical level includes misbalancing of atrial natriuretic peptide, renin-angiotensin system, aldosterone, endothelin, nitric oxide production, catecholamine and TNF-α. Myocardial infarction, heart failure and other cardiac diseases are major causes of myocardial remodeling. Myocardial infarction at molecular level involves extracellular matrix (ECM) proteins, elevated peripheral blood mononuclear cell counts, muscle LIM(Lin11, Isl-1, Mec-3) protein-calcineurin signaling; late exercise effects on cardiac remodeling following myocardial infarction, influence of AIN-93(American Institute of Nutrition) diet with myocardial infarction are major factors responsible for pathogenesis of myocardial remodeling.  Heart failure with adaptive versus maladaptive imbalance processes and neuro-hormonal imbalance activation are major causes of myocardial remodeling. Additional factors influence remodeling includes cardiac myocytes, fibroblast proliferation, collagen degradation and apoptosis. This review mainly focuses on pathophysiology involved in myocardial remodeling after myocardial infarction and heart failure as well as various effects of cardiac autocrines.

Keywords: Myocardial Remodeling, Cardiac Autocrines, Myocardial Infarction, Heart Failure, Cardiac myocytes proliferation.

Chronotherapeutic drug delivery system is useful in the treatment of disease, in which drug availability is timed to match rhythm of disease, in order to optimize therapeutic effect and minimize side effects. There is an impact of circadian rhythms in the symptoms of certain diseases like asthma, arthritis, depression, ulcer, allergic rhinitis, sleep disorders etc. The human body follows the solar/ lunar adaptations known as biological clock. The role of circadian rhythms in the mechanisms of disease and the pharmacokinetics and pharmacodynamics of medications constitutes a challenge to drug-discovery and drug-delivery scientists. We must strive to develop intelligent drug-delivery systems that can affect a target cell or organ system at that circadian time when it is possible to optimize desired therapeutic outcomes and minimize or avert adverse effects. The present article covers findings about the effects of biorhythms on various disorders, and their implications for drug therapy are discussed. Here we also reviewed the design of novel chronopharmaceutical drug delivery systems that might be able to release the therapeutic agents at predetermined intervals.

Keywords:Chronotherapy, Circadian rhythm, Chronopharmaceutics, Chronopharmacokinetics.

As an isolated organ, eye is very difficult to study from a drug delivery point of view. Ophthalmic drug delivery is extremely interesting and highly challenging endeavours. In recent scenario, most eye-diseases are treated with topical application of eye-drops. But these conventional eye-drops have two major problems. 1) It needs frequent administration at every 4 hours or 1 hour if the infection is severe and 2) Formation of crystalline deposits on cornea due to its pH-dependent solubility which is very low. In order to provide the solution to above problems many new formulations have been developed, which include nanosuspension, nanoemulsion, inserts, hydrogels, in-situ gel, etc. The poor bioavailability of ophthalmic solution caused by dilution and drainage from the eye can be overcome by using in-situ forming ophthalmic drug delivery system prepared from polymers that exhibit reversible liquid-gel phase transition. The developed formulation provides better drug product effectiveness, reliability, stability, safety, non-irritancy and prolonged release. Thus, it’s a viable alternative to conventional eye-drops by virtue of its ability to enhance bioavailability through its longer pre-corneal residence time & ability to provide prolonged drug release upto 8 hours. The main important factor is the reduced frequency & the ease of installation resulting in better patient acceptance.

Keywords: Ophthalmic delivery, in-situ gel, polymers, liquid-gel phase transition, pre-corneal residence time, prolonged drug release.

Security and safety are two main features desired in pharmaceutical chain supply but to attain the same is a challenging task. With the expectation of improved supply chain visibility for consumer goods, the RFID (Radio Frequency Identification) technology has been attracting considerable attention by manufacturers as well as government procurement agencies. RFID technique showed potential to store and retrieve data using radio waves to automatically identify people or objects. Automatic identification  of product in much shorter time as compared to manual registration and high level of accuracy have attracted channels of distribution to adopt RFID technique as effective tool to counterfeit drugs. The technique is gaining trust with advancement in technology.

Key Words: Counterfeit, supply chain, tracking medication.

It is well known that solid oral dosage forms, particularly tablets, are the most acceptable form of delivering medication. However, some new variations are beginning to emerge such as mini-tablets, which offer formulation flexibility. A multifunctional and multiple unit system for oral use are developed by filling versatile mini-tablets in a hard capsule. Multipulsatile DDS, site-specific DDS, zero-order DDS, slow/quick DDS, and quick/ slow DDS are designed in different ways and are investigated. Mini-tablets are small tablets with a diameter typically equal to or less than 3 mm that are typically filled into a capsule, or occasionally, further compressed into larger tablets. It is possible to incorporate many different mini-tablets, each one formulated individually and programmed to release drug at different sites within the gastrointestinal track, into one capsule. These combinations may include immediate release, delayed release, and/or controlled release mini-tablets. It is also possible to incorporate mini-tablets of different drugs to treat concurrent diseases or combinations of drugs to improve overall therapeutic outcome, while delivering distinct release rates of each according to disease requirements. Mini-tablets combine the advantages of multiparticulate dosage forms with the established manufacturing techniques of tableting. Additional benefits of mini-tablets include excellent size uniformity, regular shape and a smooth surface, thereby offering an excellent substrate for coating with modified release polymeric systems. From this, study it can be concluded that, granules-mini-tablets filled in HPMC capsule systems and coated mini-tablet-in-HPMC capsule system sulphate shows both sustained release as well as immediate release may improve the bioavailability and efficacy of any drugs.

Keywords: Mini-tablets, immediate-release, delayed-release, controlled-release, multiparticulate dosage forms.

Biomarkers and surrogate endpoint largely replaced the clinical trials which are needed to be carried out before drug approval in regular approval process under FDA (Food and Drug Administration), a governing pharma regulatory body in USA and as a result approval process can be accelerated. It can be said that surrogate endpoint and biomarker are substituting the clinical trials and decrease the duration of product development phase as well as decrease the entry time period of novel products in the market. The article enlightens the extent to which the biomarkers and surrogate endpoint have benefited the pharma industry for expediting the entry of their products into the market at the earliest to get the maximum benefit of the product during the patent period. Simultaneously article also throws light on the history of risk factors of surrogate endpoint which are likely to jeopardize the interest of the human beings involved. It may conclude that Biomarkers and surrogate endpoints play pivotal role in accelerating approval process for drug approval in USA and the usage of these parameters to minimize the casualty of human lives who are suffering from serious life threatening diseases by providing recent research products which have caliber to cure or improving the quality of life.

Key words: Clinical trial, Biomarker, Surrogate end point, Accelerated approval, Caliber to cure, Casualty of human lives.

Probiotics are the live microbial feed supplement which benefitted the host when administered in a certain number. Probiotics have been within our domestic use for as long as people have eaten fermented milk, curd, butter milk, but their association with health benefits dates only from the turn of the last century, when Metchnikoff drew attention to the beneficial effects of some gut microflora on the host, and suggested that ingestion of fermented milk products ameliorated this so-called auto-intoxication. Species of Lactobacillus, Bifidobacterium, Bacillus, Streptococcus, Lactococcus and Saccharomyces are used as Probiotics. Probiotics are purposely used for their immunomodulatory, antilipidemic, antitoxin, antimicrobial and anti-allergic properties. There is an endless list of Probiotics properties. In spite of these properties Probiotics are immensely showing fruitful results against diarrhea and stomach disorders like Irritable bowel syndrome, Antibiotic associated diarrhea, Pancreatitis, Clostridium difficle infection, Radiation induced diarrhea, Traveler’s diarrhea etc. It increases IgA level and other immunoglobulins secreted cells in the intestinal mucosa and stimulate local release of interferons. It facilitates antigen transport to underlying lymphoid cells, which serves to increase antigen uptake in Peyer's patches. Present review has been aimed to discuss the role of Probiotics in diarrhea which is very common in developing countries like India.

Keywords: Probiotics, Stomach disorders, Gastroenteritis, Irritable bowel disease

Cyclodextrins, the unique cyclic carbohydrates are successfully utilized as the potential complexing agents which form inclusion complex with insoluble drugs. “Inclusion complex”, this term refers to the dispersion of one or more actives ingredients in an inert carrier or matrix at molecular state. Now a day several drugs molecules are being introduced and many newer techniques have been developed for the formulation of dosage forms but when these drug molecules become more and more complex, sophistication has to find its way in the area of excipients, which are needed to formulate these drug substances optimally. One such versatile adjuvant, tailored with the help of advances in biotechnology and enzyme technology is cyclodextrin. Cyclodextrin are cyclic oligosaccharides which have been recognized as useful pharmaceutical excipients. The molecular structure of these glucose derivatives generates a hydrophilic exterior surface and a non polar cavity interior. Such cyclodextrin can interact with appropriate size drug molecules which lead to the formation of inclusion complexes. A comprehensive literature survey was made collect the rightful utilization of cyclodextrins as complexing, solubility enhancing agents and permeation enhancers.

Key words: Inclusion complexes, Cyclodextrins, Excipients, Complexing agent, Hydrophilic exterior surface

Cancer is an important area of interest in the life sciences because it has been a major killer disease throughout human history. Heterocyclic molecules are well known to play a critical role in health care and pharmaceutical drug design. Currently a number of heterocyclic compounds are available commercially as anticancer drugs and great efforts have been put to the identification of novel anticancer targets for novel anticancer drug discovery.

Key words: Heterocycles, Cancer

Presently pharmaceutical industries are focusing on development of sustained release formulations due to its inherent boons. Sustained release dosage forms are designed to release a drug at a predetermined rate by maintaining a constant drug level for a specific period of time with minimum side effects. The basic rationale of sustained release drug delivery system optimises the biopharmaceutical, pharmacokinetic and pharmacodynamic properties of a drug in such a way that its utility is maximized, side-effects are reduced and cure of the disease is achieved. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilisation of the drug, increased safety margin of potent drug, reduction in healthcare costs through improved therapy and shorter treatment period. Sustained release products are designed to bring the blood level of a drug immediately to therapeutic concentrations by means of an initial dose portion called loading dose and then sustain this level for a certain predetermined time with the maintenance portion. The basic goal of sustained release is provide promising way to decrease the side effect of drug by preventing the fluctuation of the therapeutic concentration of the drug in the body and increase patient compliance by reducing frequency of dose.

Key Words: Oral sustained release system, Matrix tablet, Patient compliance, Half-life

The family of Rutaceae contains extremely wide variety of aromatic plants, mainly in tropical regions. Among them the rich is the genus Ruta. It is now cultivated in many parts of the world. This plant is considered indigenous in South Europe and North Africa and it grows on waste stony ground. Rue (Ruta graveolens) has been used for centuries as a medical preparation and has a variety of roles, probably because of its varied chemical composition. This plant is commonly cultivated in India and is commonly called as sudab or sadab. In traditional system of medicine it is used as stimulant, emmenagogue, diuretic, abortefacient, and resolvent. Detailed and comparative studies from its traditional use especially with reference to Unani system of Medicine, to the modern scientific reports have been evaluated in this paper.

Keywords: Sudab; Ruta graveolens; Unani system of Medicine; Flavonoid.

It’s well established that oxygen is essential for survival and energy generation in all-living organisms and ~5% of its inhaled part is converted into free radicals (either ROS or RNS) as a by-product of aerobic metabolism. Free radicals are also generated on exposure to sun light, X-rays, O₃, tobacco smoke, automobile exhaust, environmental pollutants, and several other physiological processes. These reactive species damage NAs, proteins, lipids, carbohydrate. that consequently affects the immune functions causing degenerative ailments. The initiation steps of oxygen induced oxidation require removal of H-atom which gets accelerated by the presence of certain metals such as Fe and Cu leading to formation of singlet oxygen. In a normal cell there is an appropriate balance between pro-oxidant and antioxidants. Increase in level of pro-oxidant as compared in antioxidant creates oxidative stress. Epidemiological studies provide convincing evidence that a diet rich in antioxidants is associated with a lower incidence of degenerative diseases. Fruits, vegetables and beverages( fruit juices, black-lemon-T, coffee, cocoa, beer & wine) are the potent sources of dietary polyphenols. People relying upon consuming traditional diets rich in soy and tea rarely bear breast, uterus and prostate cancer. Recent advances in biochemistry and molecular biology techniques providing tools for studying the antioxidant enzymes and for elucidating the mechanisms of the actions of antioxidants has been delineated in this manuscript.

Keywords: Aloe Vera, Anti-oxidants, Curry plant, Phytochemicals, Cancerous maladies: Beer, Ginger, Pepper, Coconut, Tea, Tomato

The main anti-acne medicines including retinoids, systemic and topical antibiotics and hormones have several severe side effects. According to the literature, it is expected that Calendula officinalis, Rosa canina, Zataria multiflora and Trigonella foenum graecum which have antibacterial, anti-inflammatory and anti-oxidant effects, and Glycin max that have phytosterogenic property, heal the inflamed lesions of the disease. The purpose of the present study was to formulate and clinically evaluate an anti-acne cream using the extract of the above mentioned plants.A general formula of a cleansing cream containing bees wax, spermaceti, borax, liquid paraffin and water was considered and then corrected. The best formula was chosen according to its physicochemical properties. The stability of the formulation was evaluated. After diagnosis of acne vulgaris, the number of inflamed lesions and severity of the disease were determined. After two weeks of administration of the coded formulations, the process of improvement and possible complications were reviewed. If necessary, the treatment was continued for another two weeks. Finally, the patients were examined for the number of lesions and the severity again. The significance of data was analyzed statistically using SPSS. The final product was water in oil cream with suitable appearance and acceptable physico-chemical stability. Clinical trial results were significantly illustrated the effectiveness of the formulation mainly against papular and pustular lesions; disease severity and acne-induced inflammation, when compared to placebo. Previous researches have shown the presence of steroid saponins in Trigonella foenum graecum that make it a good anti-inflammatory agent. Also, anti-oxidant and anti-microbial effect of the other above mentioned plants are reported. Considering the results of the present study, when compared with placebo, a formulation containing the mixed extract of the plants has a good efficacy in the treatment of acne vulgaris by reduction of the number of lesions and inflamed area.

Key words: Acne vulgaris, Herbal extract, Cream

This study evaluated the dissolution behaviour of a novel amorphous form (Form A) and the commercially preferred crystalline form (Form I) of efavirenz. Generally, amorphous forms tend to achieve a greater extent and rate of dissolution compared to their crystalline counterparts. The results showed that the dissolution of Form A to be significantly lower than that of Form I due to agglomeration. Factors which contributed to the agglomeration behaviour of Form A include: high surface free energy, a lower degree of wetting, and the low glass transition temperature of Form A which caused the sample to convert to the rubber phase which is stickier. The agglomeration increased the relative particle size thereby reducing the exposed surface area of Form A; ultimately reducing the rate and extent of dissolution. The dissolution behaviour of Form A was found to be dependent on sample size and surfactant (SLS) concentration. Scanning Electron Microscopy (SEM) was employed to investigate surface area properties which provided information supporting the powder dissolution results. The solubility and intrinsic behaviour of the two forms were found to be comparable. Upon further investigation it was found that Form A undergoes phase mediated transformation into Form I during the solubility and dissolution experiments and that this too contributed to the apparent dissolution and solubility behaviour of Form A.  It was found the nucleation rate of Form A was potentiated by higher SLS content in the dissolution medium.

Keywords: polymorph, amorph, dissolution, solubility, efavirenz.

In the present study, a series of substituted 2-(1H-benzimidazol-2-ylsulfanyl)-N-phenylacetamide was prepared. The synthesis of titled compounds from starting material unsubstituted 2-mercapto benzimidazoles was prepared from o-phenylenediamine and carbon disulfide in presence of KOH in single step. 2-mercapto Benzimidazole on reacting with N-substituted-α-chloroacetanilides yield different derivatives of Benzimidazole. The structure of new compounds  prepared  during  present  investigation  have  been authentically established by their IR,¹H NMR and Mass spectral studies. The antibacterial and antifungal activities of thiadiazole derivatives also reported. Some of these derivatives exhibit significant antimicrobial activity.

Key words: 2-mercapto benzimidazoles, phenylacetamide, antibacterial, antifungal.

Natural remedies from medicinal plants are considered to be effective and safe alternative treatment for liver toxicity. Our aim was to demonstrate the hepatoprotective effect of petroleum ether, methanol and aqueous extracts of Cassia tora seed with a view to explore its use for the treatment of hepatotoxicity in human. These extracts were used to study the hepatoprotective effect in paracetamol induced hepatotoxic model. In aqueous and methanol extracts treated groups there was statistical significant decrease in the levels of serum bilirubin, serum glutamate oxaloacetate transminase (SGOT), serum glutamate pyruvate transminase (SGPT) and serum alkaline phosphatase (SALP) as compared to the hepatotoxic group. In the histopathological study the hepatotoxic group showed hepatocytic necrosis and inflammation in the centrilobular region with portal triaditis. Aqueous and methanol extracts treated groups showed minimal inflammation with moderate portal triaditis and their lobular architecture was normal. It can be concluded that the aqueous and methanolic extracts of Cassia tora seed were not able to revert completely hepatic injury induced by paracetamol, but it could limit the effect of these drug in liver. The effects of extracts were comparable with standard drug silymarin.

Keywords: Hepatoprotective, cassia tora seed, paracetamol.

To compare the effect of mentat and Donepezil was on working memory in rats. The rats were trained for conditioned avoidance response by using Cook’s pole climbing apparatus. Rats trained for CAR received scopolamine (hydrobromide) in a dose of 0.5mg/kg by intraperitoneal route before administration of study drugs. This is known to produce amnesia which will be used to evaluate the effect on learning and memory of study drugs. Donepezil was given in a dose of 0.32mg/kg by intraperitoneal route and mentat was given in a dose of 200mg/kg by oral route for eight days in the animals after training for conditioned avoidance response. Data was analysed by the chi-square test. Findings show that administration of single dose of scopolamine 20 minutes before the test run on the apparatus causes transient amnesia daily for resulting in disruption of the retention of CAR. Mentat and donepezil significantly increased the retention of condition avoidance response in comparison to scopolamine. However there was no significant statistical difference in the increase in the retention of CAR in mentat or donepezil given alone, but the combination of the two drugs showed statistically significant increase in the retention of CAR than either of these drugs alone. Results from this study provide good platform to conduct clinical studies to assess the benefit of combining mentat with donepezil when given for a longer period of time.

Key Words: Working memory, mentat, donepezil, scopolamine, conditioned avoidance response.

This research paper describes simple analytical method for determination of Camylofin dihydrochloride and Paracetamol in syrup formulation by Gas chromatography method. Benzoic acid was used as internal standard. Validation was carried out in compliance with the International Conference on Harmonization guidelines. The method utilized GC (Agilent Technologies 6890N Network GC system with FID detector), and RTX-5 capillary column (Crossbond 50% diphenyl-95% dimethyl polysiloxane), 30m x 0.53mm, 1.5µm as stationary phase. Helium was used as the carrier gas.  The proposed method was validated for linearity, LOD, LOQ, accuracy, precision, ruggedness and solution stability. It can be conveniently adopted for routine quality control analysis.

Key Words:Validation, Gas chromatography, Pharmaceutical preparations, Camylofin dihydrochloride, Paracetamol.

A simple, fast, and precise reverse phase, gradient HPLC method was developed for the separation and quantification of metformin hydrochloride and its related compounds Cyanoguanidine impurity, Melamine impurity, 1- methylbiguanidine impurity, Monoguanylmelamine impurity, N,N Dimethylmelamine impurity in tablet formulations. Liquid chromatography with using Partisil SCX, 250 X 4.6 mm, 10µm and mobile phase is 17 gms of ammonium Dihydrogen phosphate in 1000 ml water and adjust the pH to 3.0 with phosphoric acid and degassed under sonication. The flow rate was 1.0 ml/min and the effluent was monitored at 218 nm. This new method was validated in accordance with USP requirements for new methods for assay determination, which include accuracy, precision, linearity, range and robustness. The current method demonstrates good linearity over the range of 0.01µg/mL to 10µg/mL for Impurity A and metformin HCl. Remaining all impurities with concentration from 0.02 µg/mL to 15 µg/mL for six levels. The accuracy is carried out with concentrations ranging from 50% to 200% of Target concentration the Mean % recovery for each impurity at each level should be between 85.0 % and 115.0.The precision of this method reflected by relative standard deviation of replicates all metformin Related Substances is NMT 10%. Validation of the same method was also performed according to USP requirements for quantitative determination of impurities which include robustness and limit of quantification (LOQ) and Limit of detection LOD. No significant variation in RRT of Metformin and its substances at flow rate (0.8 to 1.2mL/min.), at pH (2.8 to 3.2), column temperature (23°C to 27°C), hence the method is robust.

Key words: Metformin Hydrochloride, Metformin related substances, HPLC, method validation.

The medicinal plants have been selected for thorough studies from indigenous folk medicines, Ayurvedic, Unani and Siddha systems of medicines. Ficus bengalensis Linn (Moraceae) is a plant that is widely distributed in India. In traditional medicines it is used for healing obstruction of urine flow, diarrhea, dysentery, conjunctivitis, scabies and diabetes. So it has been a subject of chemical, biological and pharmacological interest since a long time. The aqueous or alcoholic extracts of various parts of this plant were found to have various pharmacological activities for example, antidiabetic, hypocholesterolemic, hypolipidemic, anti-inflammatory, anthelmintic, antibacterial, antiallergic and anti-tumor activity. The anti-ulcer activity of a methanolic extract prepared from the stem bark of Ficus bengalensis Linn was evaluated in rats employing the ethanol-acid and Indomethacin models to induce experimental gastric ulcers. Treatments with Ficus bengalensis Linn methanolic extract (100, 200 and 400mg/kg) provided significant anti-ulcer protection in the ethanol-acid and Indomethacin models.

Keywords: Anti-ulcer, ethanol-acid, Indomethacin, Ficus bengalensis Linn, dysentery

A rapid and sensitive UV-Visible spectroscopic method was developed for the estimation of Ranalozine in pure and its Pharmaceutical formulations. The method was validated as per International Conference on Harmonization [ICH] guidelines. The Ranalozine was monitored at 230nm with UV detection and there is interference of diluent at 230nm for Ranalozine. The method was linear (r2 =0.999) at concentration ranging from 12 to 40μg/ml, precise (intra-day relative standard deviation [RSD] and inter-day RSD values < 1.0%), accurate (mean recovery = 100.2%), specific and robust. The results showed that the proposed method is suitable for the precise, accurate and rapid determination of Ranalozine in bulk, its capsule dosage forms.

Key Words: Ranalozine, UV-Visible spectroscopy, Validation, Dosage form.

The present work investigates the formulation and optimization of floating tablets of Domperidone. Formulations were optimized for gas generating agent content, different viscosity grades of HPMC and its concentration. Study revealed that percentage of NaHCO₃ and different grades of HPMC had a major influence on release of drug from hydrophilic matrix tablets and floating properties. Eleven trial batches were undertaken in order to optimize and find out the most suitable formulation and evaluated for various parameters like weight variation, hardness, thickness, friability, floating lag time, total floating time, swelling index, dissolution profile and stability study. The formulation F₁₁ containing 20 mg/ tab. HPMC (K₁₀₀M) was optimized as the best formulation. Optimized formulations were studied for effect of hardness on floating properties and as well as accelerated short term stability study. Hardness of tablets had greater impact on floating lag time which might be due to decreased porosity. Dissolution profiles were subjected to various kinetic drug release equations and found that drug release from hydrophilic matrixes occurred via anomalous transport mechanism (i.e.) follows both diffusion and erosion mechanism. Hence it is evident from this investigation that gas powered matrix tablet could be promising delivery system for Domperidone with sustained release action and improved drug availability.

Keywords: Domperidone. Sustained release. Hydroxyl propyl methyl cellulose. Direct compression. Floating lag time.

The goal of present investigation highlights the formulation and evaluation of mucoadhesive buccal patches of Tramadol hydrochloride. The mucoadhesive buccal patches of Tramadol hydrochloride were prepared by solvent casting technique using various concentrations of Chitosan polymer. The formulated patches were evaluated for their physicochemical parameters like thickness, weight variation, surface pH, content uniformity, folding endurance swelling percentage studies and in vitro residence time. In vitro release studies were performed with pH 6.8 phosphate buffer solution. Good results were obtained both in physicochemical and in vitro studies. The films were exhibited controlled release more than six hours. The in-vitro release datas were fit to different equation and kinetic models to explain release profiles. The best mucoadhesive performance and matrix controlled release was exhibited by the formulation R6. The formulation was found be right and suitable candidate for the formulation of Tramadol HCL mucoadhesive buccal patches for therapeutic use.

Key words: Tramadol HCL, Chitosan, Mucoadhesive buccal patches, PVP K-30.

ABSTRACT

Delonix regia, a well known plant with high medicinal value, reported to have a number of biological activities including antioxidant, and presence of flavonoids in its chemical constituents. Antioxidant property and flavonoids have been associated with wound healing actions of plants. The present study was done to investigate the wound healing properties of Delonix regia in experimental animal models. The ethanolic and aqueous extracts of Delonix regia flowers were prepared to study the effect on wound healing in albino rats using incision and excision wound models. Healing was assessed by the rate of wound contraction, period of epithelialisation, tensile strength (skin breaking strength) and estimation the hydroxyproline content. The extracts significantly promoted the healing process, as evident by an increase in wound breaking strength, percentage of wound contraction, increased hydroxyproline content and decreased epithelialisation period, suggesting the possible utilization of this plant to enhance wound healing.

Key words: Delonix regia, flowers, extract, wound.

ABSTRACT

Asparagus racemosus and Centella asiatica are two very common and well known medicinal plant available in India. Both the plants are traditionally used as antiamoebic drugs. Not only are those, both the drugs used as the herbal treatment of several diseases of human beings. In between them some are really critical disease. Several important phytoconstituents have been already isolated and characterized from both the plants and in between them some are the major active marker for the treatment of above said critical diseases. Instead of all those characters, these two plants have very potent antioxidant property. Here, we have taken an attempt to prepare a formulation of the mixture (50:50) of the aqueous extracts of both the plants and compare the antioxidant property of that formulation and extracts. In this study calcium chloride cross linked alginate microsphere and chitosan coated microsphere have been prepared by using the above said plant extracts and the anti-oxidant property of those formulations were compared with the extracts and also standard drugs. The result therefore reflects that the antioxidant potency of the combined extract entrapped in formulations was almost equivalent to the original extract combinations. This entails despite of the different process control stresses in the manufacturing steps the potency of the polymer entrapped drug substances does not changed. So researchers may look forward in further purification of the extract and then an effective drug loading to get an equivalent potent action from the same quantity of a standard antioxidant.

Keywords: Antioxidant activity, Asparagus racemosus, Centella asiatica, microsphere

ABSTRACT

Oxidative stress caused by free radicals is implicated in the pathogenesis of many diseases.  In order to continue the other plants with potential benefits with free radical scavenging properties, researchers start looking forward for exploring new plants with rich in flavonoids and polyphenolics. These constituents possess not only free radical scavenging properties but also they are highly safe in the treatment of many diseases/disorders. In one of the field survey, it was identified that Sesbania grandiflora(Linn) was extensively used by folklore practitioner for treating many human ailments such as flatulent-colic, astringent, cooling, bitter, tonic, anthelmintic, febrifuge, dyspepsia, diarrhea and gastralgia, pain, nyctalopia, anaemia, emaciation. Even the plant is a rich source of antioxidants such as phenolics and flavonoids. However, scientific information about the plant and concentration of these constituents was not updated. Hence it was planned to undertake the plant of the present study for its spectrophotometric determination of total phenolic and flavonoid contents from 70% alcoholic extract of flowers of Sesbania grandiflora using Catechol and Quercetin as reference standard. It was observed that, 70% alcoholic extract of flowers of Sesbania grandiflora(Linn) showed 64.0mg/G of total phenol equivalent to catechol and 28.80mg/G of flavonoidal content equivalent to quarcetin standard.  Hence it may be concluded that the plant many be potential source of antioxidant principles such as phenolic and flavonoid. Furthermore, the plants possessing these antioxidants can be highly beneficial for the treatment of many common human ailments.

Key-Words: Catechol, Flavonoid, Phenolic, Quercetin, Sesbania grandiflora(Linn).

ABSTRACT

At current 40% of the drugs were poorly soluble and were also called as “brick dust”. And the drugs which were belonging to the BCS CLASS II & IV were most eligible for this Nanosuspension technology. Here by using different methods we are reducing the particle size so the surface area will be increases ultimately it leads to increase in the bio availability. This instance was observed mostly in the case of anti-cancer drugs. Paclitaxel with 25% of Human Serum Albumin (HSA) showed very good results in terms of drug content, particle size, zeta potential and %CDR.

Key words: Nanosuspension, Paclitaxel, Human Serum Albumin (HSA), High pressure homogenization.

ABSTRACT

The anticonvulsant activity of butanol seed extract of Mucuna pruriens was investigated by studying the effects on seizures induced by pentylentetrazole and maximal electroshock convulsive methods in mice. Mucuna pruriens (100 and 200 mg/kg) significantly reduced the duration of convulsion in tonic seizure induced by pentylenetetrazole (80mg/kg, intraperitoneally). Mucuna pruriens (100 and 200 mg/kg orally) significantly reduced the tonic extensor convulsion in both the experimental models and the effects were compared with diphenylhydantoin in maximal electroshock method and Sodium valproate in pentylenetetrazole induced seizures method as standard control respectively. The data obtained suggest that Mucuna pruriens have mild to moderate anticonvulsant property and may be due to involvement of Gamma amino butyric acid.

Keywords: anticonvulsant activity, butanol extract, Mucuna pruriens, pentylenetetrazole. 

ABSTRACT

To assess the use of drugs used in patients of influenza like illness. A Questionnaire was prepared and filled after accessing data from the medical records of patients suffering from influenza like illness including H1N1+ve cases. At the end an evaluation of questionnaires was done and an assessment form was filled. IEC approval was obtained. The H1N1 +ve patients, who received oseltamivir within 36 h, had complete recovery. A higher number of respiratory complications as well as deaths were observed in patients receiving oseltamivir >36h later. An increase in need for antibiotic usage was also observed in those patients who received oseltamivir 36h later. Commonest side effects seen were nausea, vomiting & loose motions. Among the total cases surveyed only 8% did not receive oseltamivir, while more than half the patients receiving oseltamivir turned out to be H1N1 –ve eventually.  The benefits of early use of oseltamivir like rapid clinical recovery & less risk of complications were confirmed. However, more than 50% of these Influenza like illness (ILI) cases received oseltamivir unnecessarily, probably due to phobia of H1N1. The above factors could lead to an increased financial burden on the patient as well as on the already overstretched healthcare system. Early diagnosis of H1N1 infection might be useful to prevent inappropriate use of effective antiviral drugs like oseltamivir

Keywords: H1N1; Influenza like illness; Oseltamivir; (Note: +ve : positive; –ve: negative.)

ABSTRACT

Lignocaine Hydrochloride (LH) is a local anesthetic agent used in the treatment of periodontal and various other dental diseases. It undergoes extensive first pass metabolism with a consequent low bioavailability. Keeping this into account the research work was focused to formulate buccal tablets of LH in an effort to achieve prolonged relief from pain. Buccal tablets were prepared by direct compression method using different bio-adhesive polymers such as chitosan with methocel K15, sodium alginate and methocel K4. Ethyl cellulose (EC) was used as an impermeable backing layer. The optimized formula (F9) was evaluated for in vitro drug release (99.51%±0.59) in phosphate buffer for 6 hrs and bio adhesion strength was found to be 22 gr. The amount of drug permeated through the buccal membrane was found to be 85.03 ±0.21.Stability studies of the F9 indicated no significant changes with respect to drug content, in-vitro release and ex-vivo permeation.

Key Words: Lignocaine hydrochloride, Buccal drug delivery system, First pass hepatic metabolism, Ex vivo permeation studies.

ABSTRACT

The main objective was to evaluate antidepressant effect of diltiazem in rats. Results of numerous pre-clinical studies have demonstrated that calcium channel blockers have an antidepressant activity & a potential for interaction with standard antidepressants. The present study is designed to test this hypothesis in rats .Rats were assigned to six groups,  one group is the control group (distilled water) , three groups are ,imipramine (10 mg/kg), venlafaxine (10 mg/kg), and diltiazem (10mg/kg) alone and other two groups are combination of diltiazem with imipramine, and diltiazem with venlafaxine. To know the antidepressant effect, forced swim model had been used, the immobility period of all the groups are compared with each other  after giving drugs for 7 days Diltiazem produced significant antidepressant effect either alone or in combination with imipramine. The efficacy of diltiazem (10mg/kg) was comparable to that of imipramine (10mg/kg) and venlafaxine (10mg/kg) results of the present study indicate antidepressant like activity of diltiazem

Keywords: Depression, diltiazem, imipramine, venlafaxine, forced swim test

ABSTRACT

In the present scheme, we have an attempt to synthesize some novel benzimidazole derivatives by substituting triazole moiety at N-1 position of benzimidazole by fusion reaction of benzimidazole-1-acetic acid with thiocarbohydrazide. The substituted triazole was refluxed with different aromatic carboxylic acid in the presence of POCl₃ yield different benzimidazole derivatives, respectively. The synthesized compounds were characterized by IR, ¹H-NMR and Mass spectroscopy. The compounds were screened for antibacterial (gram +ve, gram –ve bacteria) activities.

Key words: Benzimidazole, thiocarbohydrazide, substituted benzoic acid, benzimidazole- 1-acetic acid

ABSTRACT

While tomato products supplementation, containing various carotenoids, including lycopene has hypolipidemic and antioxidant effect, the role of purified lycopene for the same remains unclear. Thus we tested the effect of pure lycopene powder for its effect on lipid profile, blood glucose and antioxidant enzyme in hyperlipidemic rabbits.Male New- Zealand White rabbits were used. Blood samples from all the 12 rabbits were taken for the baseline level of lipids, [Serum Total Cholesterol (TC), Low Density Lipoproteins (LDL), Serum Triglycerides (TG), High Density Lipoproteins (HDL)] blood glucose and blood superoxide dismutase(SOD). Same tests were performed in high fat diet fed (control group) and high fat diet + lycopene (10 mg/kg) (test group) after 6 weeks. There was a significant decrease in the level of serum TC, LDL – C and serum TG and an increase in serum HDL – C and antioxidant SOD after addition of lycopene to high fat diet. There was however no change in blood glucose level. Purified lycopene showed significant hypolipidemic and antioxidant activity. However, it did not show significant effect on blood glucose level.

Key Words: Lycopene, Hypolipidemia, Antioxidant Superoxide Dismutase, High fat diet.

ABSTRACT

Mitochondrion plays an important role in cellular metabolism and in energy production. Free radicals contribute damage to mitochondria during various pathological conditions. Tamoxifen is an anti-estrogen drug given to treat breast cancer. Tamoxifen and its metabolites induce varied cellular effects. It was therefore planned to study the impact of tamoxifen on mitochondria to observe its mechanism of action in promoting cell death. Mitochondrion was isolated from sheep liver and different concentrations of tamoxifen were added to study its impact on oxidative stress. Tamoxifen induced swelling of mitochondria which in turn produced lipid peroxides in a dose-dependent manner. Tamoxifen significantly increased the levels of nitrite and nitrate in mitochondria with depletion of glutathione. It was observed that tamoxifen increased NADH oxidation leading to the release of calcium from mitochondria. These changes observed are correlated with the mechanism of action of tamoxifen in treating breast cancer.

Keywords: Mitochondria, Tamoxifen, Swelling, Oxidative Stress, Calcium.

ABSTRACT

Lantana camara L. (Verbenaceae) is a perennial shrub, brought to India some 80 years ago from South America, which has become exotic and spread to different regions of the country. All the parts of this plant are traditionally used for several ailments such as antiseptic, antitumoural and antimicrobial. The current investigation was undertaken to explore the protective effect of methanol extract of Lantana camara L. (MELC) against acetaminophen and Cisplatin induced acute renal toxicity in rats. In each model of nephrotoxicities, thirty adult male Wistar rats were evenly divided into 5 groups. Groups I and II served as untreated and model controls, respectively while groups III–V were the treatment groups which were pretreated with 200, 400 mg/kg/day of MELC and group V was pretreated with Vit-E 1 hr before each dose of the nephrotoxicants (acetaminophen and Cisplatin) for 14 days (acetaminophen induced model) and 5days (Cisplatin induced model). On the 15th day (in acetaminophen) and 6^th day (in Cisplatin), blood samples for serum urea, total protein and creatinine while the rat kidneys for histology were obtained under inhaled diethyl ether anesthesia. In the acetaminophen nephrotoxic rats, 200 and 400 mg/kg/day significantly (p < 0.05, p < 0.01,p < 0.001) attenuated elevations in the serum creatinine, total protein and blood urea nitrogen levels in dose related fashion, as well as, attenuation of acetaminophen induced tubulonephrosis. Similar effects were also recorded in the Cisplatin model of acute renal injury. In the near future, MELC could constitute a lead to discovery of a novel drug for the treatment of drug-induced nephrotoxicity.

Keywords: Lantana camara L. methanolic extract, acetaminophen and Cisplatin induced nephrotoxicities, Protective activities.

ABSTRACT

Conventional drug therapy requires periodic doses of therapeutic agents. These agents are formulated to produce maximum stability, activity and bioavailability.  Floating drug delivery systems (FDDS) have a bulk density less than gastric fluids and so remain buoyant in the stomach without affecting gastric emptying rate for a prolonged period of time. While the system is floating on the gastric contents drug is released slowly at the desired rate from the system. The present study mainly focuses on the development and evaluation effervescent based floating matrix tablet of famotidine. This oral drug delivery offers several advantages over the standard conventional oral dosage forms. Effervescent based floating matrix tablet of famotidine was prepared using sodium bicarbonate as effervescent agent and by incorporating hydrophobic agent stearic acid which retards the drug release and allow the dosage form to float on gastric fluid for several hrs. Then the tablet was evaluated for hardness, friability, drug content and in vitro drug release. On the basis of the preliminary trials, a 3² full factorial design was employed to study the effect of independent variables, HPMC K4M: Carbopol 934P ratio (X₁) and concentration of effervescent agent (X₂) on dependent variables like floating lag time, Q₄ and Q₈. The best batch (F3) exhibited optimum floating lag time (16 sec), drug content (98.94%), Q₄ (54.36 %), Q₈ (93.98%) and similarity factor (83.92). The controlled release of famotidine was observed and good fit to the zero order was demonstrated.

Keywords: Famotidine; floating drug delivery system; Floating lag time; In vitro drug release.

ABSTRACT

In the present work, an attempt has been made to study the sustaining release property of isolated mucilage powder of Plantago ovata by formulating the sustained release tablets of aceclofenac and comparing its efficiency with hydrophilic matrix polymer HPMC K4 M. The drug compatibility with mucilage was checked by FTIR studies and found to be intact and stable. The results of pre-compression studies revealed that they were within prescribed limits that indicate good flowing property. All the formulations were found to be within the acceptable limits of official weight variation test. In all the formulations, friability was less than 1 % indicating good mechanical resistance of tablets. Drug content was found to be within acceptable limits. The formulations were also evaluated for hardness, thickness and dissolution profile. The data of drug dissolution was fitted into kinetic models which revealed that all the formulations followed Peppas release kinetics. The results revealed that the formulation F4 showed sustained drug release up to 12 hours. It also revealed that the isolated mucilage powder of Plantago ovata showed better sustained release over HPMC K4 M. In conclusion, Plantago ovata mucilage, obtained from natural source could be used as a reliable alternative over the synthetic polymers used for sustained release formulations.

Key words: Aceclofenac, Plantago ovata mucilage, HPMC K4 M, Release retardant

ABSTRACT

Chromium is an important non-ferrous metal with high corrosion resistance finding its application in electroplating, tannery, chloral kali industries etc. Out of the two most stable forms of Chromium hexavalent one considered as a serious health hazard and it has attracted attention as a pollutant in natural waters. In view of this the separation and determination of chromium has been receiving considerable attention. Solvent extraction of Chromium (VI) from hydrochloric, sulphuric, and nitric acid solutions with Tri-n-Octyl amine oxide (TOAO) in benzene has been studied. The optimum conditions for extraction were established from the study of the effect of several variables like concentration of extractant, metal ion, acidity etc.  The extractions are nearly quantitative with hydrochloric and sulphuric acid & are partial from nitric acid solutions. The extracted species are also identified. The method has been applied for the recovery and determination of chromium in synthetic as well as stainless steel samples.

Keywords: Chromium (VI) -- Tri-n-Octyl amine oxide (TOAO) -- mineral acid

ABSTRACT

Objective of the present investigation is to evaluate the hepatoprotective activity of combine form of Phylanthus Niruli herbs and Solanum nigrum stem bark extracts against paracetamol-induced hepatotoxicity. Materials and methods: Hepatotoxicity was induced in male Wistar rats by oral solution of paracetamol (500mg/kg for 7 days). Aqueous extracts of combine form of Phylanthus Niruli herbs and Solanum nigrum stem bark were administered to the experimental rats (300 mg/kg/day, p.o. for 7 days). The hepatoprotective effect of these extracts was evaluated by the assay of liver function biochemical parameters (% of body weight changes, total bilirubin count, total protein, total cholesterol, HDL, SGPT and SGOT level) and histopathological studies of the liver. Results: In Aqueous extracts of combine form of Phylanthus Niruli herbs and Solanum nigrum stem bark extract-treated animals, the toxic effect of paracetamol  was controlled significantly by restoration of the levels of serum bilirubin, protein and enzymes as compared to the normal and the standard drug silymarin-treated groups. Histology of the liver sections of the animals treated with the extracts showed the presence of normal hepatic cords, absence of necrosis and fatty infiltration, which further evidenced the hepatoprotective activity. Conclusion: Aqueous extracts of combine form of Phylanthus Niruli herbs and Solanum nigrum stem bark possesses significant hepatoprotective activity.

Key words: Hepatoprotective, SGPT, SGOT, HDL, Solanum nigrum, Phylanthus Niruli

ABSTRACT

The methanolic extract of Alstonia scholaris (L) R.Br. stem bark was screened for hepatoprotective activity against Swiss albino rats with liver damage induced by carbon tetrachloride. The results of hepatoprotective activity revealed that the methanolic extract of Alstonia scholaris significantly decreased the biochemical parameters (SGOT, SGPT, ALP, TP and TB). Silymarin (25 mg/kg), a known hepatoprotective drug, was used for comparison. The extract did not show any mortality up to a dose of 2000 mg/kg body weight. The findings indicated that the methanolic stem bark extract of Alstonia scholaris (L.) R.Br. (200 mg/kg) was effective in bringing the functional improvement of hepatocytes. The hepatoprotective activity was also supported by histopathological studies of liver tissues.

Key words:  Alstonia scholaris, extract, hepatoprotective, carbon tetrachloride.

ABSTRACT

An isocratic reverse phase liquid chromatography (RP-LC) method has been developed and subsequently validated for the determination of Lacosamide in Bulk and its pharmaceutical formulation. Separation was achieved with a Xterra RP-8 ((Make: Waters Corporation; 150 mmx4.6 mm I.D; particle size 5 µm)) Column and Sodium di-hydrogen phosphate monohydrate buffer (pH adjusted to 3.0 with diluted orthophosphoric acid): Acetonitrile (800:200) v/v as eluent at a flow rate of 1.0 ml/min. UV detection was performed at 230nm. The method is simple, rapid, and selective. The described method of Lacosamide is linear over a range of 12.0µg/ml to 37.85 µg/ml. The method precision for the determination of assay was below 1.0%RSD. The percentage recoveries of active pharmaceutical ingredient (API) from dosage forms ranged from 99.3 to 100.9%. The results showed that the proposed method is suitable for the precise, accurate and rapid determination of Lacosamide in bulk, its dosage forms.

Key Words: Lacosamide, RP-LC, Validation, Dosage form.

ABSTRACT

The present study involves preparation and evaluation of floating microsphere of Captopril as model drug for prolongation of gastric residence time. the different gas forming agents are used such as sodium bicarbonate and calcium carbonate. The microsphere were prepared by Ionotropic gelation technique using polymers Sodium alginate along with HPMC (K4M) and Ethyl cellulose. The microsphere was evaluated for angle of repose, bulk density, tapped density, Carr’s index, Hausner's ratio, percent yield and drug entrapment. The shape and surface morphology of prepared microsphere were characterized by optical and scanning electron microscopy, respectively. In-vitro drug release studies were performed by using an USP dissolution test apparatus (type I) at 37±0.5ºC and 50 rpm speed.  To study the release behaviour, kinetic analyses were performed on the optimized formulation. The dissolution data were fitted to zero order, first order, matrix, Hixson-Crowell, Peppas model. The prepared microsphere exhibited prolonged drug release (~ 12 hr) and remained buoyant for > 12 hr.  The optimized formulations H3, H6 were kept for short term stability study. The conditions for stability study were 40ºC and relative humidity of 75% from the study; it was observed that there is no significant change in drug entrapment and drug release rate.

Key-words: Floating microsphere, Captopril, In-vitro release, HPMC (K4M), Ethyl Cellulose

ABSTRACT

A reversed phase high-performance liquid chromatographic method was developed and validated for the quantitative determination of two antiviral drugs viz. lopinavir and ritonavir. Chromatography was carried out by gradient  technique on a reversed-phase C₁₈ Column, Phenomenex (250 x 4.6 mm, 5 µ) with mobile phase mixture of Buffer: Acetonitrile (45:55 v/v) was used as a mobile phase and the pH was adjusted into 4.5 by using with O-phosphoric acid, at a flow rate of 1.2 ml/min. The UV range was detected at 240nm for lopinavir and ritonavir respectively. The different analytical performance parameters such as linearity, precision, accuracy, and specificity, limit of detection (LOD) and limit of quantification (LOQ) were determined according to International Conference on Harmonization ICH Q2B guidelines. The linearity of the calibration curves for each analyte in the desired concentration range is good (r² >0.9). The recovery of the method was between 102.1% and 100.1% for lopinavir and ritonavir respectively. Hence the proposed method is highly sensitive, precise and accurate and it successfully applied for the reliable quantification of API content in the commercial formulations of lopinavir and ritonavir.

Key words: Lopinavir, Ritonavir, UV spectrophotometry, RP-HPLC.

ABSTRACT

The present study was carried out to monitor, estimate the prevalence and consequences of ADRs on treatment of TB and to assess causality, predictability, preventability and severity of the ADRs. A prospective observational and active surveillance study was conducted over a period of 9 months. Each reported ADR was assessed for its causality, severity, predictability and preventability as per standard algorithms. The management and outcome of ADRs were determined. A total of 128 ADRs (in 53 patients) were identified out of which the prevalence of ADRs in female was found to be 31.58% and 29.66% in male patients. The causality assessment by Naranjo’s scale showed that out of 128 ADR’s, 128 (100%) ADR’s were probable and based on WHO probability assessment scale 119(92.97%) were possible where as 9(7.03%) were probable. Preventability assessment showed that 125 (97.66%) were not preventable and 03 (2.34%) were definitely preventable. Severity Assessment by Modified Hartwig and Siegel Scale showed that 82 (64.06%) ADRs were mild and 46(35.94%) ADRs were moderate. 128(100%) were found to be predictable. Majority of the ADRs were recovered without giving symptomatic treatment. The study concluded that there is a need of a system for proper monitoring of ADRs caused by anti-TB drugs in RNTCP centre.  The counselling of patients for timely prevention, detection and management of ADRs will helps in further ADR occurrence minimisation.

Keywords: Adverse drug reactions, Tuberculosis, World health organisation, Directly Observed Treatment-Short course (DOTS), Revised National Tuberculosis Control Programme (RNTCP).

ABSTRACT

Two simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Ibuprofen (IBU) and Famotidine (FAMO) in their combined dosage form. Method A, absorbance correction method involves measurement of amplitudes at 220 nm (for IBU) and 288 nm (for FAMO) in zero derivative spectra. Method B, ratio derivative spectrophotometry, involves division of spectra of IBU by one selected standard spectrum of FAMO and then measuring amplitudes at 234.2 nm in ratio derivative spectra for estimation of IBU. Similarly, spectra of FAMO are divided by one selected standard spectrum of IBU and then amplitudes at 277.8 nm in ratio derivative spectra are measured for estimation of FAMO. Developed methods were validated according to ICH guidelines. The calibration graph follows Beer’s law in the range of 2 to 60 µg/ml for IBU and 3.8 to 4.6 µg/ml for FAMO with R² value greater than 0.999. Accuracy of all methods was determined by recovery studies and showed % recovery between 98 to 102%. Intraday and Interday precision was checked for both the methods and mean %RSD was found to be less than 2 for these methods. The methods were successfully applied for estimation of IBU and FAMO in marketed formulation.

Keywords: Ibuprofen, Famotidine, Absorbance correction method, first order ratio derivative method

ABSTRACT

Gastroretentive dosage forms have potential for use as controlled-release drug delivery systems. The use of floating dosage forms is one method to achieve prolonged gastric residence times, providing opportunity for both local and systemic drug action. The present work was aimed to formulate floating tablets of Itopride hydrochloride using an effervescent approach for gastroretentive drug delivery system. The present investigation concerns the development of floating tablets of Itopride hydrochloride, a novel prokinetic drug, which after oral administration are designed to prolong the gastric residence time and thereby increase drug bioavailability, and drug release rate. This would help in promoting gastrointestinal transit and speed up gastric motility, and thereby it will relieve the symptoms associated with it. Floating tablets were fabricated; using direct compression method; containing Itopride hydrochloride, polymers HPMC K100M, HPMC K15M and HPMC K4M, along with gas generating agent sodium bicarbonate. The floating tablet formulations were evaluated for physical characterization, assay, swelling index, in‐vitro drug release, hardness, friability and weight variation.

Keywords: Itopride Hydrochloride, Gastroretentive drug delivery system, Swelling study, HPMC.

ABSTRACT

Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. Floating Bilayer drug delivery system is combined principle of bilayer tablet as well as floating mechanism. Floating drug delivery system provides advantages local delivery to specific region like stomach and proximal small intestine and it’s also shows better bioavailability and improved therapeutic activity. Floating Bilayer 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 concept of Floating Bilayer drug delivery systems with the recent literature and current technology used in the development of Floating Bilayer drug delivery system as well as summarizes evaluation method and applications of various floating dosage forms.

Key words: - Bilayer Floating drug delivery systems, Gastric residence time, Swelling index, Buoyancy

ABSTRACT

Domperidone is a water insoluble drug exhibiting poor dissolution pattern. Domperidone is an antiemetic and shows gastroprokinetic properties. It is a weak base and shows poor solubility in alkaline pH. Several methods are being employed to enhance the solubility of domperidone irrespective of its pH dependent solubility. The present protocol aim to design Polyethylene glycol (PEG) based solid dispersions of Domperidone to enhance its solubility. PEG 8000 based solid dispersions containing the drug in different mass ratio i.e. 1:1, 1:3, 1:5 and 1:7 were prepared using fusion method. The prepared solid dispersions were characterized for their drug content, phase solubility studies, Fourier-transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), x-ray diffraction, and in-vitro dissolution studies. All the formulations showed marked improvement in the solubility and dissolution rate of drug which may be due to decrease in crystallinity of drug and additives. It was concluded that prepared solid dispersion of the Domperidone with PEG can improve the solubility and dissolution rate of the drug.

Keywords: Domperidone, PEG, Solid dispersion, Solubility 

ABSTRACT

The purpose of this research work was to prepare an extended release formulation of metoprolol succinate using Ion exchange resin. Metoprolol succinate has short half life of 3-7 hours. So it needs to be administered 3-4 times a day. Hence an extended release preparation is desired. Drug-resin complex (DRC) was obtained by loading metoprolol succinate onto a strong cation exchange resin, Indion 244 in the ratio 1.5:1 using batch method. The molecular properties of the complex were investigated by differential scanning calorimetry, X-ray powder diffraction and Infra red spectroscopy which revealed interaction of drug with resin. To achieve the desired release rate, the DRC was initially treated with an impregnating agent, polyethylene glycol (PEG) 4000 and was further treated with hydrophobic polymer ethyl cellulose. Various formulations of tablets using resinate were prepared to achieve desired drug release profile. The formulations were evaluated for hardness, friability, weight variation, in vitro release and assay using HPLC. Formulation (V) shows optimum results in terms of release profile, which were in accordance with the USP specifications. The in vitro release profile showed that complexation of drug with ion exchange resin and use of hydrophobic polymer matrix could retard the initial burst and extend the release of drug up to 24 hours.

Keywords: metoprolol succinate, Indion 244, drug-resin complex, PEG 4000, ethyl cellulose

ABSTRACT

In vitro dissolution studies constitute the mainstay for evaluation of any oral dosage form and more so for a poorly water soluble drugs. Selection of appropriate dissolution medium is critical for these studies as it could have an impact on in vitro - in vivo correlations. Biorelevant media simulate the in vivo conditions in fasting and fed state and are being investigated as novel dissolution media. Telmisartan is a BCS class II drug exhibiting solubility and dissolution rate limited bioavailability. In the present study 03 marketed brands of TEL tablets were subjected to in vitro dissolution studies in biorelevant media. The results were compared with tablets prepared using binary and ternary solid dispersions of TEL with poloxamer 188 and TPGS. The marketed and formulated products displayed widely different release profiles in fasting and fed state simulated intestinal fluid. The results indicated the need to develop dissolution studies and media which will facilitate in vitro in vivo correlation studies.

Key Words: Telmisartan, fasting state simulated intestinal fluid, fed state simulated intestinal fluid

ABSTRACT

Plants are utilized as therapeutic agents since time immemorial in both organized (Ayurveda, Unani) and unorganized (folk, tribal, native) form. The ethanolic fruit extract of Cucumis trigonus Roxb of family Cucurbitaceae was used to treat the urolithiasis induced by ethylene glycol. On this course, the extract also repairs the changes that happened in the mineral constituents like calcium, magnesium, phosphorus and oxalate in serum and urine of the urolithiatic rats. The ethanolic fruit extract (150 mg / kg b.w.) elevated the levels of reduced mineral parameters like calcium, magnesium and phosphorus and reduced the level of oxalate in serum and reduced the levels of calcium, phosphorus and oxalate and elevated the level of magnesium in urine significantly (p<0.05) when compared with the toxic groups. The results shown by the ethanolic fruit extract (150 mg / kg b.w.) was compared to standard thiazide drug treated group, showing no significant difference (p<0.05) and thus it proves that the ethanolic fruit extract of Cucumis trignonus exhibits potent antiurolithiatic activity.

Keywords: Cucumis trigonus, mineral constituents, thiazide, ethylene glycol.

ABSTRACT

The purpose of this study is to investigate the glycoprotein and efficacy of combination of paclitaxel along with Di allyl sulfide against skin cancer in experimental animals. Skin cancer is the most common form of human cancer. It is estimated that over 1 million new cases occur annually. The annual rates of all forms of skin cancer are increasing each year, representing a growing public concern. The most common warning sign of skin cancer is a change in the appearance of the skin, such as a new growth or a sore that will not heal. Skin cancer is caused by chemical carcinogens and Papilloma virus infection. Skin cancer was induced in rats by 7, 12 Di methyl benz(a) anthracene (DMBA) at the dosage of 5 µg was dissolved in 100µl and administered into experimental animals for 28 weeks. In this study, we demonstrated that combination of paclitaxel and Di allyl sulfide protects the rats from a lethal dose of DMBA for 30 days. The levels of glycoprotein in plasma, skin and liver were found to be increased in the cancer bearing animals when compared with control animals. Treatment of Paclitaxel along with Di allyl sulfide to cancer induced animals showed significantly decreased levels of glycoprotein levels when compared with cancer induced animals. The treatment with combination of paclitaxel and Di allyl sulfide effectively reduced glycoprotein levels. So, from the obtained results it is concluded that paclitaxel and Di allyl sulfide is capable of restoring the skin architecture.

Key words: Paclitaxel, Di allyl sulfide, DMBA, Skin cancer.

ABSTRACT

The concept of controlled release tablet can be utilized to provide a long lasting and more reliable release of drug in GIT to ultimately develop a once daily formulation. Thus, they prolong the dosing intervals, but also increase patient compliance beyond the level of existing conventional dosage forms. Erythromycin, macrolide antibiotics is used in the treatment of Mycoplasma pneumoniae infections, Chlamydial infections, etc. It is a drug with short biological half-life 1.5 hrs and dosing frequency more than one per day which makes it an ideal candidate for controlled release. The present investigation was planned to formulate the Erythromycin stearate once daily controlled release tablets. The tablets were prepared by direct compression method and were subjected for in vitro drug release studies. The mechanism of drug release was determined using various kinetic models. The results revealed that all the formulated tablets had acceptable physical properties and showed release up to 24 hrs. The kinetic studies revealed that all the formulations followed Zero order release kinetics. The tablets were prepared by Direct Compression technique and evaluated for various parameters. The optimized formulation contains Erythromycin Stearate as active ingredient, HPMC K15M, Chitosan and Xanthan gum as rate retarding polymers.

Keywords: Erythromycin stearate, Matrix tablets, Controlled release, Chitosan, Hydroxy propyl methyl cellulose, Direct Compression.

ABSTRACT

The study focuses on the behavior of diffusion phenomenon in the normal and stenosed capillary-tissue exchange system where the rheology of flowing blood in the capillary is characterized by the generalized Bingham Plastic fluid model. Assessment of the severity of the disease could be made possible through the variation of a parameter named as retention parameter. The concentration profile and associated physiological diffusion variable involved in the study for normal and diseased state have been analyzed. The model is also employed to study the effect of shape of stenosis on flow characteristics. An extensive quantitative analysis is performed through numerical computations of the desired quantities having physiological relevance through their graphical representations so as to validate the applicability of the present model.

Keywords: Bingham Plastic fluid model, Capillary-tissue exchange, Resistance to flow, Wall shear stress, Stenosis shape parameter.

ABSTRACT

Preliminary characterization and isolation of phytomedicinal components of dried black fruits of xylopia aethiopica in hydro-methanolic (1:4 v/v), hydro-ethanolic (1:4, v/v), methanolic, ethanolic and aqueous solvents has been compared. Results showed variability and significant differences in phytomedicinal compositions and the potency ranked: hydro-methanolic > hydro-ethanolic > methanolic > ethanolic = aqueous and the percentage difference was 75%, 54%, 45.8%, 29% =29% which perhaps validates the efficacy of the therapeutic potentials of xylopia aethiopica for many of the traditional medicinal applications.  Anthraquinone and combined anthraquinone were exclusively found in hydro-methanolic and methanolic concentrates and accounted for 44.4 % and 33.3 % respectively. Glycosides (-terpene, sterols and deoxy-sugar) accounted for 100% in hydro-alcoholic concentrates respectively. Alkaloids and the phenolic compounds flavonoids and tannins with the exception of saponins which was negligible or absence in the solvents were also the phytomedicinial constituents. Results suggest that the ability of hydro-alcoholic to enhance the isolation of useful constituents might be attributed to the differential solubility of the combined hydrophobic and hydrophilic components of the phytomedicinal bioactive ingredients in the solvent which, is still subject to further studies. Hydro-alcoholic, specifically hydro-methanolic, therefore is recommended for isolation and characterization of economically important medicinal plants of medical interest.

Keywords: Xylopia aethiopica, hydro-ethanolic, hydro-methanolic, differential solubility anthraquinone, combined anthraquinone, medicinal plant.