ABSTRACT:

The objective of the present work was to develop and validate a simple, selective, linear, precise, accurate and stability indicating RP-HPLC method for the simultaneous determination of Vildagliptin and Metformin from their combination drug product. 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 Waters C18 250 X 4.6 mm, 5µ column maintained at a temperature of 45˚C. The optimum mobile phase consisted of 0.1M phosphate buffer (pH -7): Acetonitrile (70: 30), mobile phase flow rate of 1mL min^-1 and the effluents were monitored at 263 nm. The pharmaceutical dosage form was exposed to thermal, photolytic, hydrolytic and oxidative stress conditions and the stressed samples were analyzed by the proposed method. The method was validated according to ICH guidelines. It was found to be accurate and reproducible. Linearity was obtained in the concentration range of 50-150 % for both Vildagliptin and Metformin. Mean percent recovery of triplicate samples at each level for both drugs were found in the range of 98% to 102% with RSD of less than 2.0%. The proposed method can be successfully applied in the quality control of bulk manufacturing and pharmaceutical dosage forms.

ABSTRACT

The success of chemotherapy lies in the continuous search for new drugs to counter the challange posed by resistant bacterial strains.The aqueous leaf extract of Clerodendrum serratum Linn. tradionally used in folklore medicine for the treatment of various ailments was investigated for in-vitro  antibacterial activity aganist five bacterial pathogens  namely staphylococcus hominis ATCC27844, Pseudomonas putida ATCC2021, Proteus vulgaris ATCC13315, Bacillus subtilis ATCC2063 and Escherichia coli ATCC2065.The antibacterial activity  of the aqueous extract was determined by employing agar disc diffusion method.Among the various concentrations used ,100mg/ml of aqueous leaf extract was found to be more effective against all tested microorganisms.The highest activity was recorded aganist Proteus vulgaris ATCC2021  with zone of inhibition ranging from  17±0.23mm to 23±0.24mm and the lowest activity was recorded aganist Escherichia coli ATCC2065 at a concentration of 25mg/ml with zone of inhibition  ranging from 10±0.47mm to 20±0.40mm. Therefore, it was found the inhibitory activity of aqueous leaf extract of Clerodendrum serratum Linn. was found to be concentration dependent.The results of this study provides justification  for the use of this plant in folkloric medicine for the treatment of various dreadful ailments.

ABSTRACT: 

A series of novel (E)-N'-(2-chloropyrimidin-4-yl)-N-(5-cyano-2-hydroxy-6-phenylpyrimidin-4-yl) formamidine derivatives were synthesized by the reaction of different aldehydes with 2-chloropyrimidin-4-amine and in vitro antimicrobial activity was evaluated. The synthesized compounds were characterized by elemental analyses, FT-IR, ¹H NMR and LC-MS spectral studies. Antimicrobial data revealed that among all the compounds screened, compounds 7l and 7m were found to have promising antimicrobial activity against all the selected pathogenic bacteria and fungi.

ABSTRACAT:

It could be concluded from the results that some of the vegetables, especially Telfairia occidentalis and Talinum triangulare, can affect the efficacy of Chloroquine and Dihydroartemisinin.

ABSTRACT:

  The drug approval process varies from one country to another. In some countries, only a single body regulates the drugs and responsible for all regulatory task such as approval of new drugs. New drug will not be imported, except under the permission granted by the Licensing Authority. However in some counties all tasks are not performed by a single regulatory authority, such as in India, this responsibility is divided on Centralised and State authorities. Other issues where the difference appears are, time taken for the approval of a CTA application, time taken in evaluation of marketing authorization application, registration fee, registration process and marketing exclusivity. Some countries have two review processes as normal review process and accelerated review process as in USA, China etc. and some countries have only a single review process as in India. Similarly, the format used for the presentation of dossier submitted for approval of drug is also different. In some countries like as in USA, EU, and Japan, it is mandatory that the dossier prepared in CTD format, however, in some countries it is optional such as in India. In order to have easy understanding of all the three CTD, ACTD and Indian Requirement for Dossier Submission in various countries an overview of its differences and similarities is shown in the current article. It gives a clear idea how by some modification in reports one can apply for registration in all countries

ABSTRACT:

Cassia sophera Linn. (Caesalpinaceae), an important drug in Unani medicine, act as a blood purifier, carminative, purgative, digestive and diaphoretic. A number of compounds have been reported from plants belonging to genus Cassia. The chemical analysis of Cassia sophera Linn seed revealed the presence of ascorbic acid, dihydroascorbic acid and β-sitosterol. Novel anthraquinone sopheranin was isolated from the heartwood of Cassia sophera along with β-sitosterol, chrysophenol, physcion and emodin. A new cycloartane triterpene glycoside named cyclosphoroside A was isolated from the seeds of Cassia sophera. The present study aim to identify the constituents present in the Cassia sophera leaves. Seven chemical compounds were isolated from the leaves of Cassia sophera Linn and analysed by GC-MS. The identified compounds are (1) Butanedioic Acid, (2) 1, 2, 4-Butanetriol Triacetate, (3) 7-Hexadecene, (4) E-15-Heptadecenal, (5) 1, 2-Benzenedicarboxylic acid, (6) 3-Eicosene, and (7) 10-Heneicosene with retention time are 15.99, 13.763, 19.93, 18.03, 11.4, 16.70 and 9.54 respectively.

ABSTRACT:

Secondary metabolites are the major constituents of the plants that will protect as from the formation of excess free radical in our body. We therefore decided to check the presence of   secondary metabolites in ethyl acetate leaf extract of Alpinia purpurata by means of High performance thin layer chromatography (HPTLC). From this study A. purpurata showed the presence of 6 terpenoids, 5 steroids, 3 alkaloids and 2 phenols. HPTLC analysis showed that terpenoids are rich in A. purpurata, known for anticancer agents. We hope that the intensive study on the out coming active terpenoid constituents of A. purpurata will lead to the discovery of a novel botanical-drug for chemoprevention.

ABSTRACT:

The objective of the present investigation is to formulate gastroretentive dosage form of Nizatidine, a H₂-receptor antagonist widely prescribed in gastric ulcers, duodenal ulcers. The short biological half-life (1 - 2 hours), maximum absorption in initial part of small intestine, colonic metabolism of Nizatidine favours development of gastro retentive floating dosage form. In the present study Nizatidine floating tablets were prepared by effervescence method using sodium bicarbonate as a gas generating agent. The tablets were formulated using direct compression technology by employing semi synthetic polymers like various grades of HPMC such as HPMC K4M, K15M, K100M and natural polymers like xanthan gum and kondagogu gum. drug-excipient compatable studies  by FTIR and DSC , The FTIR and DSC study revealed that there is no drug-excipient interaction.  The prepared tablets were evaluated for various physicochemical parameters such as flow properties, hardness, weight variation, friability, in vitro buoyancy (floating lag time, total floating time), swelling studies, drug content and in-vitro drug release. The in vitro drug release pattern of Nizatidine floating tablets was fitted to different kinetic models which showed highest regression for zero order kinetics with non fickian diffusion mechanism. Out of all formulations the one prepared with combination of HPMC K4M and K15M was optimised based on desired sustained release time (12hrs) and acceptable floating properties.

Present study was undertaken to compare the effectiveness of venlafaxine, bupropion with amitriptyline in diabetic neuropathic pain. This was an open, parallel, prospective and randomized type study conducted at the outpatient departments of medicine and neurology of Era’s Lucknow Medical College & Hospital, Lucknow and Chhatrapati Shahuji Maharaj Medical University, Lucknow, respectively, to compare the effects of venlafaxine, bupropion and amitriptyline in patients suffering from diabetic neuropathic pain. Present study gives following conclusions: 1). Pain scores improvement (decrease) was highest in amitriptyline followed by venlafaxine followed by bupropion. 2). QOL scores improvement (decrease) was highest in venlafaxine followed by bupropion and least in amitriptyline. 3). NCVs (m/s) improvement (increase) was highest in amitriptyline in all the studied nerves except RCPN. 4). In RCPN, the NCV (m/s) improvement (increase) was highest in venlafaxine followed by bupropion followed by amitriptyline. 

The objective of the present study was to develop once daily sustained release floating dosage form of salbutamol sulfate. The study involves the preparation of floating microspheres of salbutamol sulfate coated with Eudragit L100 using solvent evaporation method and its in vitro characterization. Three batches (F1, F2 & F3) of microspheres were prepared taking three drug: polymer ratios (1:1, 1:2 & 1:3). The entrapment efficiency was increased with the increment in polymer concentration. The microspheres remained buoyant in acidic medium containing surfactant for 8-12 hours in vitro. The mean particle size increased and the drug release rate decreased at higher polymer concentration. The surface morphology of microspheres characterized by SEM showed microspheres with smooth surface. The in vitro drug release studies were carried out for 12 hours both in 0.1N HCl (pH 1.2) and pH 6.8 buffers. The release studies showed the drug release was faster in intestinal pH as compared to gastric pH due to the polymer solubility in pH from 6. 

A novel drug named Tiapride Hydrochloride is used in management of behavioral disorders and in treatment of dyskinesias. Four different simple, accurate, rapid, economical and reproducible spectroscopic methods namely Zero order, First derivative, Second derivative and Area Under Curve(AUC) spectroscopy have been developed and validated for estimation of Tiapride Hydrochloride in physical mixture using distilled water as a solvent according to ICH Guidelines Q2(R1). These methods obey Beer’s law in the range of 20-70 ?g/ml for Tiapride Hydrochloride. Absorbance of each solution was measured at 287.20 nm for zero order spectrophotometry. First derivative spectra are obtained by transformations at ?? of 4 nm and scaling factor 1 and absorbance measured at 301.40 nm. Second derivative spectra are obtained by transformations at ?? of 8 nm and scaling factor 10 and absorbance measured at 307 nm. Peak area is measured between 280.20-294.20 nm for AUC method. The methods showed good reproducibility and recovery with %RSD less than 1. All these four methods were compared statistically. Statistical comparisons by one way ANOVA shows all methods have equal applicability for estimation of Tiapride Hydrochloride in physical mixture. So, the proposed methods were found to be simple, specific, accurate, precise, linear and robust. Hence, all four methods can be equally applied for routine analysis of Tiapride Hydrochloride in pharmaceutical formulations. 

A simple and sensitive kinetic spectrophotometric method has been successfully developed for the determination of Eperisone hydrochloride based on its oxidation using potassium permanganate in alkaline medium. The rate of change of reaction was recorded at 603.5 nm. The different experimental parameters were studied and optimized. 5 minutes and 3 minutes were chosen for the development of initial rate and fixed time method respectively. Calibration curve was found to be linear over the concentration range of 15-35 ?g/ml for initial rate method and 15-30 ?g/ml for fixed time method. The method was applied for estimation of eperisone hydrochloride in RAPISONE (marketed by Abbott, Maharashtra). The assay results were found to be 99.93% ± 0.05 and 99.42% ± 0.05 by initial rate and fixed time method. RSD values were found to be ?2%. The results were validated as per the ICH guidelines. 

Ciprofloxacin HCl has invitro activity against a wide range of gram – negative and gram – positive organisms. The bactericidal action of Ciprofloxacin HCl results from inhibit the enzyme bacterial DNA gyrase (topoisomerase II ).The main objective of this research work was to prepare Ciprofloxacin HCl matrix tablet using HPMC as the polymer and invitro drug release study. In the present study wet granulation method is used for preparing the matrix tablet. Different grades of HPMC were used for the formulation such as, HPMCK 100 LVEP, HPMC K 4M, HPMC E10MCR, HPMC K15M, HPMCK100M. During preparation, all powders were mixed and are then passed through 60# sieve and then granulated using PVP 30 in Isopropyl alcohol and are dried for 2 hours and again passed through 16# sieve. The dried granules were then mixed in poly bag using magnesium stearate and talc. Granules were then punched using rotary tablet machine .The extended release matrix tablet were subjected to in vitro release using USP 2 apparatus. Formulation F14 shows 99.36 % drug release in 24th hour. Stability studies were performed for optimized batch. The optimized formulation F14 showed better stability when stored at 40?c under 75% RH for one month. From similarly factor F2 of F 14 trial batch shows that dissolution profile matches with the marketed product Cifran. Thus it is concluded that HPMC matrix tablet of Ciprofloxacin can be prepared by Wet granulation method and invitro release data is satisfactory. 

Study was undertaken to investigate the Impact of social isolation on various oxidative stress markers and transaminase level in rats. Rats were subjected for short (21 days) and long term (up to 84 days) social isolation; the rats displayed an increase in anxiety on elevated plus maze and open field test relative to control. Various markers of oxidative stress like lipid peroxidation (LPO), reduced glutathione (GSH), Supers oxide dismutase (SOD), catalase (CAT) and biochemical parameters like SGOT and SGPT were determined. There was significant increase in the level of LPO and decrease in the levels of GSH, SOD and CAT after long term isolation in plasma and liver. Biochemical parameters were significantly altered after long term isolation. Results indicate that increase in oxidative stress in anxiety which may leads to alteration of biochemical parameters. 

Oral dissolving films are formulated by incorporating the drug with selected oral cavity absorption enhancers in a specially designed oral dissolving film carriers. This facilitates the rapid absorption in the oral cavity for drugs with low GIT-bioavailability and intensive first-pass effects. This it offers shortening onset time, enhancing bioavailability and reducing the probability of first pass side effect. The current review focuses on the recent development in the oral dissolving film and discusses about its technique for preparation of film as well its evaluation 

Many researchers focused search light on importance of colon specific drug delivery system. These systems proved their efficacy and feasibility to treat various life threatening diseases of colon. The aim of present investigation was to develop more feasible and site specific colon targeted drug delivery system for better patient compliance. In present study the core minitab were designed by using direct compression technique and further coated with different pH dependent polymers like HPMC, Eudragit E-100 and Eudragit L-100 by using pan coating technique. The Ornidazole was used to design colon specific drug delivery system. The dissolution studies were performed at different pH levels in USP dissolution-II apparatus. The core minitab were designed by using drug, citric acid and various additives and evaluated for physicochemical parameters and In-Vitro dissolution study. The core minitabs of Ornidazole showed adequate drug release. The developed core minitabs further coated and evaluated for In-Vitro drug release study and various physicochemical parameters. The optimized formulation consists coating level of HPMC layer was 4%, Eudragit E-100 layer was 12 %, HPMC layer was 2% and Eudragit L-100 layer was 10% respectively. In-Vitro dissolution studies showed that developed system has six hours of lag phase. The enteric coating gives protection up to two hours in acidic condition, Acid soluble coat protects system up to four hours in small intestinal condition. As system switched to pH 7.4 after six hours triggered the release of drug due to solubilization of acid soluble coat by citric acid. In present investigation, Eudragit E-100 is an acid soluble polymer and solubilization of the acid soluble coat is triggered by citric acid. In-Vitro drug release of Ornidazole was markedly found faster when citric acid was included in core minitab. 

Amitriptyline was the first tricyclic used to treat neuropathy and it is still widely prescribed. It is a balanced serotonin and nor adrenaline reuptake inhibitor; Bupropion is an atypical antidepressant that acts as a norepinephrine and dopamine reuptake inhibitor and Venlafaxine, a chemically novel antidepressant, has demonstrated effectiveness in the treatment of pain associated with diabetic peripheral neuropathy in several case reports. Present study was undertaken to compare the effectiveness of venlafaxine, bupropion with amitriptyline in diabetic neuropathic pain. It was an open, parallel, prospective and randomized type study conducted at the outpatient departments of medicine and neurology of Era’s Lucknow Medical College & Hospital, Lucknow and Chhatrapati Shahuji Maharaj Medical University, Lucknow, respectively, to compare the effects of venlafaxine, bupropion and amitriptyline in patients suffering from diabetic neuropathic pain. The present study aimed at evaluating better treatment with efficacy, better safety profile and positive impact in quality of life in patients of diabetic neuropathic pain. The objective of this study was to assess and compare the effects of venlafaxine, bupropion and amitriptyline in patients suffering from diabetic neuropathic pain. 

Reactive oxygen species are oxygen derivative which influence many physiological processes. In normal physiological conditions, ROS are produced in a controlled manner at low concentrations and function as signaling molecules regulating vascular contraction-relaxation and cell growth. Increased ROS bioavailability and altered redox signaling (oxidative stress) have been implicated in chronic diseases including hypertension i.e. imbalance between superoxide and nitric oxide production leading to reduced vasodilation, resulting in development of hypertension. Hypertension caused by angiotensin II is dependent on vascular superoxide (O2-) production. The nicotinamide adenine dinucleotide phosphate (NAD[P]H) oxidase is a major source of vascular O2- and is activated by angiotensin II in- vitro. Activation of oxidative stress may result in vascular injury and in the progression of atherosclerosis. All these effects on the vasculature may explain how increased oxidative stress can cause hypertension. 

Medicinal plants have been the subjects of man’s curiosity since time immemorial. Almost every civilization has a history of medicinal plant use. Approximately 80% of the people in the world’s developing countries rely on traditional medicine for their primary health care needs, and about 85% of traditional medicine involves the use of plant extracts Adhatoda vasica Nees. is an evergreen shrub, distributed from the Punjab in the North and Bengal and Assam in the South-East to the Cylon, Malaya and Singapore in the South. It is one of the most important medicinal plants of this region. The plant is valued for containing bronchodilator alkaloids, mainly vasicine. All parts of the plant are used in herbal medicine and particularly the leaves are credited with insecticidal and parasiticidal properties. The root is useful in strangury, leucorrhoea, bronchitis, asthma, bilious vomiting, sore eyes, fever and gonorrhoea. It is a valuable antiseptic, antiperiodic and anthelmintic. It is well-known in Ayurveda by its Sanskrit name Vasaka& commonly known as Adusa. This paper has been prepared somehow that most of the studies reported on this medicinal has been touched so that much attention will be focused towards this important medicinal plant. 

Helminthiasis is an infection of the human body with parasitic worm such as roundworms, earthworms, hookworms, flukes, tapeworms and pinworms. The worms usually only involve the intestinal tract but sometimes they may invade other organs. The present study was carried out with the aim to formulate, evaluate and In-vitro anthelmintic activity of herbal suspension of Methanolic extract of Musa paradisiaca Linn. The three forms of Suspension (S1, S2 and S3) were evaluated for pH, Specific gravity, sedimentation rate, Stability study in that S2 formulation show better result as well as the anthelmintic activity was carried out using adult earthworms Pheritoma posthuma against Methanolic extract of Musa paradisiaca Linn.( 25.33±0.33to paralysis and 38.33±0.33to death of worms), Albendazole as standard reference (12.03±0.62 to paralysis and 22.94±2.42 to death of worms) and normal saline as control (No change) were S2 formulation shows 12.22±2.12 to paralysis and 22.77±0.33 to death of the worms was determined. 

The term oxidative stress? is defined as a disturbance in the equilibrium between free radicals (FR), reactive oxygen species (ROS), and endogenous antioxidant defense mechanisms. Cells continuously produce free radicals as a part of their normal metabolic processes. Under normal metabolic conditions, 2–5% of the O2 consumed by mitochondria is converted to reactive oxygen species (ROS) which has been implicated in diverse processes in various cancers. The increased ROS in cancer cells is known to play an important role in the initiation and progression of cancer. Lipid peroxidation and DNA damage are two major factors responsible for cancer. Lipid peroxidation is one of the forms of oxidative damage in cell membranes which leads to formation of lipid hydroperoxides (LOOH) that may cause permanent structural changes in DNA such as base-pair mutations, deletions, insertions, rearrangements and sequence amplification. Hence, the prevention of excess free radical formation is a vital step for cell survival. This review article emphasises on the relationship between the increase in cellular reactive oxygen radicals and the pathogenesis of cancer. 

Telmisartan is a biopharmaceutical classification system (BCS) class II drug that has low solubility in biological fluids, which results into poor bioavailability after oral administration.The purpose of this research work was to improve the solubility and therefore the rate of dissolution of telmisartan in pH 1.2, 4.5 and 7.5(FDA recommended) buffers as the dissolution media using spray drying technique. Nanodispersion of telmisartan was prepared by using various proportion of drug: PVP-K30 ratios (1:1 to 1:4). The prepared nanodispersion was subjected to in-vitro dissolution, particle size distribution, FT-IR spectroscopy, and PXRD, DSC and SEM studies. The results indicated that formulation containing drug: PVP-K30 ratio of 1:4, prepared by spray drying technique showed the cumulative release of 99.84% as compared to 9.36% for the pure drug in pH 7.5 phosphate buffers and also significant improvement in pH 1.2, 4.5 and water. Particle size analysis reveals that telmisartan was dispersed in the form of nanoparticles with size 2.5-6.5 r nm in PVP matrix. Absence of significant drug?carrier interaction was confirmed by FTIR and DSC data. XPRD reveals that crystallinity nature of drug was decreased. In conclusion, the prepared nanodispersion telmisartan with PVP-K30 in ratio of 1:4 was shown higher release profile which may contribute to improved bioavailability of telmisartan. 

Some novel 4-(2-amino-3-cyano-4-(substituted-aryl)-5- oxo-5,6,7,8-tetrahydroquinolin-1(4H)-yl)benzene sulfonamide (1a–1u) were were synthesized starting with 4-(3-oxo-cyclohex- 1-enylamino)benzene sulfonamide and 4-(cyclohexenylamino) benzene sulfonamide in the synthesis of some novel 4-(quinolin-1-yl) benzene sulfonamide derivatives. The structures of the synthesized compounds have been elucidated by IR, 1H NMR and elemental analysis. Synthesized compounds were screened for their antimicrobial screened against the E.coli and staphylococcus aureus, Salmonella typhi, Bacillus subtilis, Escherichia coli and antifungal activity against Aspergillus niger, Penecillium crysogenum, Aspergillus flavus, and Candida albicans. 

The benzimidazole nucleus does not appear to occur very widespread in nature. Commonly they are synthesized from o-phenylenediamines hence they are named as derivatives of o-phenylenediamines. Benzimidazoles are regarded as a promising class of bioactive heterocyclic compounds that exhibit a range of biological activities. Specifically, this nucleus is a constituent of vitamin-B12. This ring system is present in numerous antiprotozoal, antihelmintics, anti-HIV, anticonvulsant, antiinflammatory, antihepatic, antineoplastic, and antiulcer, activities. A large number of patents describe benzimidazole derivatives of use in the textile industry as wetting, emulsifying, foaming, or softening agents or as dispersants for use in dyeing. 

The plant Mikania cordata belongs to the family Asteraceae, has been used in different system of traditional medication for the ailments of human diseases. The present study was designed to explore the phytochemical constituents, anthelmintic & anti-emetic activities of methanolic extract of Mikania cordata (Bumr.f.) B.L. Robinson. The phytochemical screening has been done. 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. In antiemetic test (using chick emesis model), the methanolic extract showed antiemetic effect compared with standard reference. 

Telmisartan is a biopharmaceutical classification system (BCS) class II drug that has low solubility in biological fluids, which results into poor bioavailability after oral administration.The purpose of this research work was to improve the solubility and therefore the rate of dissolution of telmisartan in pH 1.2, 4.5 and 7.5(FDA recommended) buffers as the dissolution media using spray drying technique. Nanodispersion of telmisartan was prepared by using various proportion of drug: PVP-K30 ratios (1:1 to 1:4). The prepared nanodispersion was subjected to in-vitro dissolution, particle size distribution, FT-IR spectroscopy, and PXRD, DSC and SEM studies. The results indicated that formulation containing drug: PVP-K30 ratio of 1:4, prepared by spray drying technique showed the cumulative release of 99.84% as compared to 9.36% for the pure drug in pH 7.5 phosphate buffers and also significant improvement in pH 1.2, 4.5 and water. Particle size analysis reveals that telmisartan was dispersed in the form of nanoparticles with size 2.5-6.5 r nm in PVP matrix. Absence of significant drug?carrier interaction was confirmed by FTIR and DSC data. XPRD reveals that crystallinity nature of drug was decreased. In conclusion, the prepared nanodispersion telmisartan with PVP-K30 in ratio of 1:4 was shown higher release profile which may contribute to improved bioavailability of telmisartan.