Abstract

The purpose of this research was to select a suitable drug with negligible side effects and to formulate and evaluate it as fast dispersible tablets and films and to improve and compare the percentage cumulative drug release. Fexofenadine Hydrochloride is a non sedative, no impairing antihistamine used to treat seasonal allergic rhinitis (sneezing, runny nose, itchy nose, palate and throat or watery eyes), and urticaria (hives). Unlike most other antihistamines Fexofenadine Hydrochloride does not cross the blood brain barrier and therefore will not cause any drowsiness which can gradually effect child’s learning ability, drowsiness can also interfere with driving vehicles or operating machinery. During the work, intraoral rapid dispersible tablets were developed using superdisintegrants like Cross Povidone, Cross Carmellose Sodium and Sodium Starch Glycolate each in three different concentrations and in different combinations by direct compression method, these formulated tablets were subjected to pre and post evaluation parameters. All the physical characteristics were within the acceptable limits. A comparison of in vitro drug release of the optimized formulation was compared with the marketed product. Intraoral rapid dispersible films were also formulated using different polymers like HPMC E15 and HPMC 5 cP in different concentrations by Solvent Casting method, these films were evaluated and were within acceptable limits.

Abstract

Saquinavir, an anti-HIV protease inhibitor, is not effective in complete eradication of Human Immunodefeciency virus (HIV), owing to its low oral bioavailability and denied access to viral sanctuary sites like brain. The purpose of this study was to develop saquinavir loaded solid lipid nanoparticles to improve the oral bioavailability and enhance drug distribution in brain tissue. Drug delivery strategy is expected to accomplish the objective. The SLN formulations were developed by solvent emulsion and evaporation method. Drug is entrapped into Glyceryl monostearate made SLNs, stabilized by lecithin and tween. Stearylamine was used as the charge inducer and the effect of charge on brain distribution of drug was studied. The formulations were optimized by Response surface methodology using Box Behnken statistical design. The optimized formulations attained size in the range 70 to 150 nm and entrapped more than 95% of the drug. Zeta potential was found to be in the range -17 to -27 mV. Positive charge induced SLNs showed zeta potential in the range 19.1 to 25 mV. DSC and PXRD patterns displayed uniform distribution of drug in lipid in an amorphous state. The formulations were found to be stable for a period of 3 months, as seen from the stable size and entrapment efficiency at 4 ºC and 25 ºC. The pharmacokinetic and brain distribution studies were conducted in male wistar rats. Higher Cmax and higher AUC values of SLNs in plasma indicate the improved oral bioavailability of SLNs when compared to saquinavir suspension. The AUC of SLNs was increased by 5 fold in brain tissue when compared to control Saquinavir suspension. This report explains the enhanced brain delivery of SLNs when compared to control suspension. The presence of different charges didn’t affect the brain distribution of drug in the present study.  SLN was found to be a potential approach in improving the drug bioavailability and brain distribution.

Abstract

A simple, sensitive, linear, precise and accurate RP-HPLC method for simultaneous estimation of Dextropropoxyphene HCL, Dicyclomine, and Paracetamol in Bulk and Capsule formulation was developed and validated. The chromatographic separation of the two drugs was achieved on Phenominex C18 (250 mm ´ 4.6 mm) 5µ column in an isocratic mode. The mobile phase consisting of NaH₂PO₄ Buffer and acetonitrile in the ratio of 60:40 v/v and pH adjusted to 3.7 using ortho phosphoric acid was delivered at a flow rate of 1ml/ min and effluents were monitored at 231 nm. The retention time of Dextropropoxyphene HCL, Dicyclomine, and Paracetamol was found to be 7.457, 4.400, 3.397 min, respectively. Calibration curves were linear with a correlation coefficient of 0.999  for DEH , 0.998 for DIC and 0.999 for PAR over the concentration range of  19.5-45.5 µg/mL for DEH, 3-7 µg/mL for DIC and 120- 280 µg/mL for PAR respectively and precise with (%RSD<2). The method was validated as per the ICH guidelines and can be employed for routine quality control analysis.

Abstract

Aloe barbadensis a short succulent herb is distributed almost throughout the world. Its use in folk traditional medicine has kept this herb in fashion for over a decade. The remarkable antimicrobial, anti-inflammatory and hypoglycemic potentials of Aloe barbadensis are still exploited by herbal practioners to treat multitudinous ailments. Viewing the previous studies, the research work was carried out utilizing crude methanolic extract of Aloe barbadensis (leaves) for possible antibacterial, antifungal, hemagglutination, phytotoxic and DPPH radical scavenging activity. Antibacterial activity was conducted using well diffusion method. The recorded zone of inhibition exhibited by bacterial species (Bacillus cereus, Escherichia coli, Enterococcus faecalis, Pseudomonas aeruginosa, Proteus mirabilis, Staphylococcus aureus, Salmonella typhi and Klebsiella pneumonia) avered that the crude methanolic extract possess moderate to good antibacterial activity except K. pneumonia. Further antifungal activity proceeding agar tube dilution method against test fungal strains (Alternaria alternata, Fusarium oxysporum, Trichoderma harizanum, Aspergillus niger, Aspergillus flavus, Aspergillus parasitica and Penecillium) manifested good antifungal activity against F. oxysprum only. Absence of phytoglutinins in plant extract displayed negative hemagglutination activity against all blood groups (ABO). Moderate phytotoxic activity was observed at highest 1000 µg/ml concentration against Lemna minor. DPPH radical scavenging activity at different concentration of the test sample unveils less antioxidant activity.

Abstract

The aim of the study was to develop dry powder inhalation dosage form for pulmonary tuberculosis using a combination of drugs Moxifloxacin (MXN) and Ethambutol (ETM) with mannitol as a carrier using spray dryer. The approach was made by preparing powders at six different concentrations i.e. 10% - 60% of mannitol. Prepared powders were uniform in shape, as evidenced by scanning electron microscopy (SEM). The powders were free flowing with good compressibility index. The major outcomes of the work by In vitro drug release studies indicated that F4 as optimized formulation with 90.2 % drug deposition in twin stage liquid impinger (TSLI) and also with low minimum inhibitory concentration (MIC) compared to the pure drugs when tested on Mycobacterium tuberculosis by agar dilution method. By the results obtained it can be concluded that the dry powders prepared by spray drying using mannitol as a carrier has the potential as an inhalation dosage form to target pulmonary tuberculosis

Abstract

Calcium is the fifth most abundant natural element. Calcium is an important part of a healthy diet The rising prevalence of chronic diseases worldwide and the corresponding rise in health care costs is propelling interest among researchers and the public for multiple health benefits related to these food items, including a reduction in cancer risk and modification of tumor behavior. calcium may help reduce the risk of colorectal cancer is unclear, researchers know that, at the biochemical level, calcium binds to bile acids and fatty acids in the gastrointestinal tract to form insoluble complexes known as calcium soaps. In the present paper, role of calcium in cancer prevention was discussed.

Abstract

Nimodipine is a Ca2+ channel blocker. Under normal circumstances, smooth muscle contraction is dependent on the Ca2+ to enter cells, depolarization induced transmembrane current. Nimodipine effectively prevents the Ca2+ to enter cells, inhibits smooth muscle contraction, so as to achieve the purpose of relieving vasospasm. The main objective of present research was focused on preparing Sublingual tablets of Nimodipine to improve its bioavailability, to avoid pre-systemic metabolism in the gastrointestinal tract and hepatic first pass elimination. The Sublingual tablets were prepared by direct compression procedure using different concentration of Starch 1500 and microcrystalline cellulose. Compatibility studies of drug and polymer were performed by FTIR spectroscopy. Preformulation property of API was evaluated. Postcompressional parameters such disintegration time, wetting time, water absorption ratio, in vitro drug release were evaluated. Stability studies was carried out for optimized formulation. FTIR spectroscopy study revealed that there was no possible interaction between drug and polymers. The precompression parameters were in acceptable range of pharmacopoeial specification. The disintegration time of optimized formulation (F3) was up to 46 sec. The in vitro release of Nimodipine was up to 15 min.

Abstract

Diabetes mellitus is the commonest endocrine disorder that affects more than 360 million people worldwide. Use of herbal antidiabetic formulations along with allopathic antidiabetic medicines is increasing in order to achieve efficient treatment. Concurrent administration of herb and drug can lead to pharmacodynamic and pharmacokinetic interactions changing the efficacy. In present study probable interaction between gymnema tea (herbal antidiabetic formulation) and metformin is determined. Interaction study was based on comparison of antidiabetic activity of metformin in presence and absence of gymnema tea in diabetes induced albino rats. For the interaction studies albino rats were divided into four groups. Group I (Normal), Group II (Diabetes induced Control), Group III (Diabetes induced animals treated with metformin alone) and Group IV (Diabetes induced animals treated with combination of metformin and Gymnema Tea). Animals received metformin treatment (50 mg/kg) for a period of 28 days after induction of diabetes. At an interval of 0 min, 30 min, 1 hr, 2 hrs, 4 hrs, 8 hrs, 12 hrs, 24 hrs, 7^th day, 14^th day, 21^st day and 28^th day of drug treatment blood was withdrawn from retro orbital sinus. Metformin was extracted from plasma following liquid – liquid extraction and the plasma concentration of metformin by HPLC and blood glucose level was determined. At different time intervals there was decrease in plasma metformin concentrations and increase in blood glucose levels of group IV rats compared to group III rats indicating a potential drug – herb interaction between metformin and gymnema tea.

Abstract

The oral route of drug administration constitutes the most convenient and preferred means of drug delivery to systemic circulation of the body. Various conventional dosage forms have been employed for this purpose but they lack to provide the desired bioavailability of the drug due to poor residence time and faster clearance resulting in decreased bioavailability. Formulating multiparticulate system with mucoadhesive polymers may provide a significant increase in the residence time. Ranitidine hydrochloride is a H₂-receptor antagonist which inhibits basal and stimulated secretion of gastric acid, reducing both volume and acid and pepsin content of the secretion. It is generally marketed as dosage forms including tablets, capsules, syrup and injections wherein the bioavailability is less. The aim of the present study was to overcome the drawbacks of the conventional dosage forms by formulating mucoadhesive microspheres of Ranitidine hydrochloride with Sodium alginate and copolymers such as Carbopol, CMC and HPMC using ionic gelation method, and to determine its effect on gastric retention. The prepared microspheres were characterized for particle size, surface morphology, degree of swelling, encapsulation efficiency, In-vitro mucoadhesion, drug release and stability studies. Formulations F-VII displayed the best results with Entrapment efficiency 74.6, Mucoadhesion 82 % at the end of first hour and Drug release at the end of 8hr85.7. In-vitro studies concluded that Carbopol and HPMC based microspheres were better than Carbopol and CMC based microspheres for the delivery of Ranitidine. Stability studies indicated that the formulation was stable at 25±2°C.

Abstract

Benzodiazepines and its hydroxylated metabolites were used as hypnotics, in the management of insomnia and anxiety disorders. 1,4-benzodiazepines were widely used in CNS and sleep disturbances as they promote sleep without psychopathology but accompanied by minimal effects of performance. Novel 1,5-benzodiazepines were synthesized, analyzed spectrally and evaluated biologically to prove CNS effects. The synthesized novel 1,5-benzodiazepines derivatives were characterized by the spectral studies and were screened for muscle relaxant action. The results revealed that the derivatives synthesized with acetyl group showed significant effect in the animals at the dose of 4mg/kg, p.o when compared with that of the 1,5-benzodiazepine moieties. All the test compounds were compared with the standard drug diazepam (2mg/kg, p.o). They showed reduced fall of time in the rotarod apparatus, which may be mediated by benzodiazepine chloride channel activation release of GABA neurotransmitter in brain. Hence 1, 5-benzodiazepine derivatives possess significant CNS action and can be safely used for the aggressive mood disorders. Further studies were needed for the exact mechanism and the optimization.

Abstract

Series of new N-(3-chloro-4-substitutedphenyl) guanidines were synthesized and evaluated for their preliminary in vitro antibacterial activity. The synthesized phenylguanidines 4a-h exhibited MIC values in the range of 2-8 and 8-32 µg ml^-1 against Gram-positive and Gram-negative microorganisms, respectively. 4-Methylpiperidinyl derivative 4d was the most active against Gram-positive bacteria Corynebacterium, S. aureus, E. faecelis, S. epidermidis and Bacillus sp. (MIC 2-4 µg ml^-1) and poor to moderate active against Gram-negative bacteria Klebsiella Sp., C. freundi and Proteus Sp. (MIC = 16 µg ml^-1). Cyclic amine substitutions of phenylguanidines resulted in improved antibacterial spectrum of activity against Gram-positive microbes.

Abstract

Cadaba fruticosa leaves are extensively used by the ethnic groups of Kurnool district, Andhra Pradesh, India to cure vitiligo. Biological synthesis of silver nanoparticles was carried out from leaf aqueous extract of Cadaba fruticosa. 10 ml of leaf extract was mixed to 90 ml of 1 mM aqueous of Ag(NO₃)₂ and was heated at 60-80⁰C for 20 min. The color of aqueous solution changes to dark brown color. For characterization using UV-Vis spectrophotometer and AFM are used. AFM, UV-Vis spectrophotometer showed the formation of silver nanoparticles with spherical shape and average size of 35.01 nm. The results indicated that SNPs have good antimicrobial activity against different microorganisms due to the cumulative effect of secondary metabolites or active molecules present in the plant extract.

Abstract

Albuterol Sulphate is indicated for bronchospasm and reversible obstructive air way disease. The objective of the research was to formulate and evaluate Extended-Release (ER) tablets of Albuterol Sulphate which will be simple in design, stable and cost effective to the patients. ER matrix tablets of albuterol sulphate were made by aqueous wet granulation process utilizing Methocel K100M CR as a rate controlling polymer. The prepared ER matrix tablets were 2% seal coated with Opadry Clear YS-1-7006 followed by 4% ER coating with ethyl cellulose as polymer and Hypromellose 3 cps as pore former in the ratio of 8:2. This coating was done to prevent the initial burst release from the core matrix tablets. Over the ER coating, 4% aesthetic coating was given for appeal, appearance and finish with Opadry II White 85F18422. The drug release rate and dissolution profile of prepared ER tablets were comparable to the marketed product VOSPIRE^®. The drug release mechanism of both the prepared ER tablets and the marketed product follows Higuchi’s model of drug release kinetics indicating fickian diffusion. The finalized ER tablets of Albuterol Sulphate were stable at accelerated temperature and humidity.

Abstract

A foam composition mainly comprises of a major amount of water, least quantity of foam stabilizing agent and emulsifying surfactant, water soluble polymer and water immiscible liquefied gas foaming agent. Pharmaceutical foam drug delivery is more successful in dermatology because of ease of application, good spreadability than any other topical dosage form, less dense and no any greasy or sticky residue remaining after application on skin. Surfactant is the key ingredient in development of foam drug delivery system. Foam is used to deliver various categories such as anti-inflammatory, anaesthetics, protectives, antifungal, skin emollients, antiseptics, antipruritics etc. Foam drug delivery system increase the effectiveness of therapy by instant absorption and improving patient compliance hence plays important role in skin care market. In the present article an insight into foam drug delivery system is provided giving emphasis on foam properties, evaluation, and application of foam drug delivery system.

Abstract

The present study explains cocoti sap and wine treated E.coli Nissle 1917grown under stress conditions, isolation of protein by using Trizol protein extraction method. To determine the best method for protein quantification, we followed three different methods for quantification, Lowry’s method, Bradford method and BCA kit method. This report covers, protein extraction methods including sonication, centrifugation to get a better understanding about which methods give better exact quantity and higher amount of proteins and also perform one-way ANOVA for comparison of three method results. Our results indicate that, BCA kit method is fast and easy way to quantify the concentration of proteins. Due to cocoti wine treatment, the protein concentration is decreased when compared to the normal sample and sap treated samples indicating wine is toxic to the probiotic E.coli Nissle 1917.

Abstract

An isocratic reverse phase High Performance liquid chromatography (RP-HPLC) method has been developed, subsequently validated and Stability indicating for the determination of Dasatinib in pharmaceutical formulation. Separation was achieved with a Cosmisil C18 BDS (150mmx4.6 mm I.D; particle size 5 μm) and Tri ethyl amine Buffer (pH adjusted to6.5 with dilute Orthophosporic acid): Methanol: Acetonitrile (55:25:25 v/v) as eluent at flow rate 1.0 ml/min. UV detection was performed at 315nm.The described method of Dasatinib is linear over a range of 5.0 μg/ml was 30.0 μg /ml. The correlation coefficient 0.999 .The method precision for the determination of assay was below 2.0% RSD. The percentage recoveries of active pharmaceutical ingredient (API) from dosage forms ranged from 100.2 to 100.9.The accuracy of method was carried out by recovery studies.the developed method has been validated statistically as per ICH gudielines.The method showed good reproducibility and recovery with % RSD less than 2.So,the proposed methods were found to be simple,specific,precise,accuracy,linear,and rugged.Hence it can be applied for routine analysis of Dasatinib in bulk drug and the Pharmaceutical formulations.

Abstract

Platform technologies are developed to provide therapeutic benefit under similar concept for multiple actives. Currently, the pharmaceutical industry is caught between the downward pressure on price and increasing cost of successful drug discovery and development. The development cost of successful drug discovery is very high comparatively to develop platform drug delivery technology. In the form of platform drug delivery existing molecule can get a new life, thereby increasing its market value and competitiveness, developing a platform technology is driven by identification of actives which can be placed in the technology and can be delivered effectively to target area & therapeutic indication. Most of the time platform technology are conventional but are capable to accommodate different actives having different physicochemical properties. Platform technologies are targeted to deliver drugs through a common drug delivery mechanism. The major limitations of these platform technologies are either patent barrier, complexity of the technology. In our research, our focus is to develop a platform technology for drugs belonging to cardiovascular category, hence a detail review of available technologies was carried out, and primarily it appears that most of the platform technologies are with conventional approach with use of special excipients to control the drug delivery. Hence it is possible to develop cost effective platform technology which can help to deliver drugs of similar physicochemical properties, As a conclusion we could identify numerous platform technologies developed by companies which are commercially available and due to limited application for drugs of cardiovascular category, we have opportunity to investigate different out of scope patent non infringing formulation technique which can result into a cost effective platform technology. In overall all technologies are modification to known art by way of utilizing excipients or by arranging the design of the formulation in more unique way to provide drug delivery at targeted location. Thus in future platform technologies are going to provide a lifecycle extension opportunity to many existing molecules.

Abstract

The main objective of present investigation was to enhance the dissolution rate of water insoluble drug and hence oral bioavailability of Naproxen by using liquisolid compaction technique. Several liquisolid tablets were prepared by using different carrier materials such as microcrystalline cellulose, and dicalcium phosphate (DCP), and coating material such as colloidal silica. Polyethylene glycol (PEG), cremophor EL, Poloxamar 181 and propylene glycol were used as non volatile water miscible liquid vehicles. The ratio of carrier to coating material was kept constant in all formulations at 20 to 1. All the prepared formulations were compressed using 12mm punch after addition of 5 % Sodium starch glycolate to each formulation. In vitro dissolution studies were conducted by using USP six basket dissolution testing apparatus. In vitro intestinal permeation studies were conducted by using goat intestinal membrane and   in vivo oral bioavailability studies were conducted to the optimized formulation, marketed formulation and pure drug sample in healthy rats by balanced block incomplete design. Plasma samples were analyzed by RP-HPLC method. Liquisolid compacts prepared with PEG as solvent, DCP as carrier and colloidal silica as coating material have shown 100 % of drug release with in 10 min and hence have been chosen for in vivo studies. And it has shown 126 % of relative bioavailability when compared with pure drug. FTIR results revealed that there was no interaction between the drug and excipients. Based on all results obtained, it can be concluded that liquisolid compaction technology is one the most promising novel approach to enhance the oral bioavailability of poorly soluble BCS class II drugs.

Abstract

The study was aimed to analyse the prescribing pattern of probiotics and antibiotics in paediatric patients. The study was conducted in the paediatric department of 350 beded multispecialty tertiary care hospital. During the period of 6 months study, 243 prescriptions containing probiotics and antibiotics were collected and analysed using a structured data entry format. The prevalence of diarrhea was seen more in males (62.1%). Out of the 243 prescription reviewed, Bacillus clausii was the most commonly prescribed probiotics, and 16 patients were given combination of probiotics. Antibiotic prescribing pattern was also studied from which shows that Cephalosporin class of antibiotics were mostly prescribed (28.94% in males and 15.43% in females). The results obtained in the study indicate that antibiotic and probiotics were prescribed jointly more than individually.

Abstract

A novel LC-MS-MS method was developed for identification and determination of related substances in paliperidone bulk drug and dosage form. Six related substances of paliperidone API and tablets were identified by the proposed method. The chromatographic system consisted of Zorbax SBCN column (150 × 4.6mm; 5µ).The mobile phase consisted of 0.077 %w/v ammonium acetate buffer and acetonitrile with a nonlinear gradient program at a flow rate of 1.3 ml/min, injection volume of 20 µL and UV detection was carried out at 277 nm. Validation of the developed method was performed. Major impurities have been detected, identified and quantified using two analytical systems HPLC and LC-MS-MS. The newly developed method for quantitative determination of paliperidone and its related substances was found to be specific, accurate, precise and robust. It can therefore be successfully employed for the quality evaluation of impurities in raw material and formulations of paliperidone.This is the first report where one of the impurities marked as keto impurity was identified.

Abstract

The main objective of this article is to summarize recentdata, description results and basic functionality of microneedles Oral bioavailability of molecules is limited due to degradation, low solubility, feed condition of patients etc. In order to administer such drugs, injectable formulations by various routes are available. Due to certain limitations like pain at site of injection, high cost, hemorrhage etc; parenteral route have limited application. With advancement in technology & research, it is possible to avoid needle by reducing the size of needle upto micron size (Microneedle). Recently developmicroneedles manufactured by the silicon etching technology and micro-mechanical system manufacturing (MEMS)technique are very thin , which do not penetrate deep enough into the skin to reach up to the nerve endings and therefore there is no perception of pain during the microneedles insertion into the skin. The use of micron-scale needles in increasing skin permeability of transdermal drug delivery, such as low molecular weight, oligopeptide, protein and peptide, gene and drug release at cellular drug delivery, local delivery and systemic delivery and inactivate influences virus.This paper will discuss what microneedles are, the types and  advantages of microneedles, mechansim of action , Production technique  and applications.

Abstract

Nanodiamonds  drug  delivery  system  is an  new  path  to  the  medical  science.  The unique nanodiamond properties have demonstrated exceptional performance in various fields especially in pharmaceutical as drug delivery system and biotechnology. As compare to other nanoparticle, nanodiamonds have purity, size selectivity, retention of aggregation, colloidal stability and surface functionality. An approach is made herein to review the concept of nanodiamonds, their advantages, and methods of preparation. Also their wide applications in various fields of drug delivery are reported. Nanodiamond  having  a  coat  of  the  drug  and  proteins that  targets  the  cancer  cell  in  body  and  destroy  the cancerous  cells  without  affecting  any  normal  cell  and  they  can  bind  tightly  to  a  variety  of  molecules  and deliver them right into a tumor. This review concludes with an evidence for the future directions and challenges involved in maximizing the potential of these exciting little carbon-based gems in the field of medicine and biotechnology.

Abstract

ADR reporting is a significant attribute of a successful pharmacovigilance program. A number of countries use their particular ADR forms. The review compares similarities and dissimilarities of 15 ADR forms of various countries. The study assessed 89 data elements mentioned in 15 ADR forms. Only 11 elements were common. An ADR form of Food and Drug Administration (FDA) consists of the highest number of data elements which was greater in number, while the ADR form of Nepal falls on the opposite end with less number of data elements. The result of the review highlights 44 data elements for the universal ADR form. The current study illustrates a call for a uniform, brief and instructive ADR form.

Abstract

Cytogenetic damage associated with prallethrin based mosquito repellent use was analyzed by micronuclei (MN) and other nuclear abnormalities (NA) in South Indian human volunteers. The mean MN frequency of exposed subjects showed a significant difference when compared with controls (p<0.05). The presence of other NA such as binucleated cells (BNC), karyorrhexis (KRC) and karyolysis (KLC) were found to be notably higher in exposed individuals (p<0.05). These results show that chronic exposure to prallethrin increases a slight DNA damage. Though the present investigation involving a limited number of human subjects indicates the onset of both protective changes as well as derangement in metabolism, a detailed and rigorous study is greatly warranted to arrive at a definite conclusion about any toxic effects of prallethrin based mosquito repellents.

Abstract

ASEAN (Association of South East Asian nations) was established in 8^th August, 1967 in Bangkok. Presently the association comprises of (Indonesia, Malaysia (Chair), Vietnam, Brunei Darussalam, Democratic republic of Laos, Cambodia, Singapore Philippines and Thailand (Co-Chair)). Labeling as being a very essential part of the Pharmaceutical product and giving an overview to the patient and healthcare professional with respect to the drug’s Administrative information, quality and some other important parameters such as its safety and efficacy. Although many countries in ASEAN region is accepting Harmonized ACTR for drug product registration product for human use, but still variation in the labeling is encountered during registration as per the country specific regulation on the labeling of pharmaceutical product for human use. This review article summarizes the requirement variation with respect to labeling and art-work of pharmaceutical product for human use in ASEAN Region and differences among the  labeling provisions of different countries should be negotiate for further harmonization.

Abstract

Reactive oxygen species are generated as by-products of biological reactions or from exogenous factors, which are involved in a variety of physiological and pathological processes including Cancer, Aging and Alzheimer’s disease. A series of novel P,P-diphenyl phosphinimidic amide derivatives were developed and synthesized by Staudinger reaction in the present study for the control the ROS production. The screening of in vitro antioxidant activity gave good results against DPPH radical, Superoxide anion, ABTS⁺ radical and Nitric oxide radical scavenging activities. The 2D-QSAR descriptors demonstrate that the title compounds possess the prospective drug properties and prompted them as good antioxidant activity. These results are concluding that the title compounds are good antioxidant agents.

Abstract

Plants are potential source of pharmaceutically active compounds. Most of the medicinal herbs are threatened due to over exploitation and also the destruction of their natural habitats. Plant cell culture is an alternative means not only for the elucidation of the lead molecules but also important as an ex situ conservation of the natural resources. Marchantia linearis Lehm & Lindenb. was commonly used in folklore medicine by tribals for curing many diseases. The major objectives of the present study are (i) establishment of cell suspension culture, (ii) elucidation of flavonoids and its fractionation and (iii) analysis of anticancer potentialities against SW 480 colon cancer cell lines in terms of antiproliferation (MTT assay), cell apoptosis, cell cycle and growth kinetics, activities of quinone reductase (QR), glutatione-S- transferase, (GST) and cytochrome P450 (CYP 2E1) correlated with reduced glutathione content (GSH) and lipid peroxidation (LPX). In vitro cell suspension culture of M. linearis yielded remarkable levels of flavonoids. Apigenin, quercetin and luteolin are the major flavonoids identified by RP-HPLC- PAD analysis. Significant decline in proliferation, cell cycle and increased apoptosis in SW 480 cells were noticed. Results of MTT assay showed that 50 µg/mL of flavonoid remark­ably reduced growth kinetics of cells coupled with induced cell apoptosis. The xenobiotic metabolic enzyme CYP 2A1 showed a marginal decrease whereas, QR and GST revealed increased activities. Caspase 3/7, 2, 6, 8 and 9 showed significant level of expressions. The results are statistically significant (p < 0.05). The assay data was further supported by the level of GSH and LPX levels. The present results suggest a positive correlation between flavonoids and their antimetastatic effects. Purification of the principle lead compound and animal studies are warranted to further establish the results.

Abstract

The present research work focused on concurrent process validation for Atorvastatin tablets 10mg. The tablets were manufactured by wet granulation method. Since the dose is 10mg, uniform distribution of the drug in the tablet is critical which can influence the content uniformity, assay and dissolution of the tablets. The critical parameters selected for process validation were drymixing, blending and compression. Uniformity of dry mixing was found to be excellent after 20 minutes because %RSD was less than 1.0%. The content uniformity after 20 minutes of blending was satisfactory since the % RSD was less than 1.0%. Physical parameters and assay at compression stage, i.e different turret speeds (20, 25 and 30 rpm), different hopper levels (Full hopper, half hopper and quarter hopper) and different time intervals (Initial, Middle and End) were within limits. Based on results at each critical stage for the specified parameters, it is concluded that the wet granulation method can ensure uniform distribution of Atorvastatin  and the tablets can be effectively manufactured with the desired specifications & reproducible quality standards.

Abstract

Regulatory involvement in the generic drug development hastens the drug approval process which directly/indirectly accelerated the launching of drug into the market. The regulatory  documents  whether  in-house  of  documents  to  be  submitted  to  regulatory authorities should be carefully reviewed by the skilled personnel to minimise the queries raised  by  the  regulatory  agencies  and  speed  up  the  approval  process. These are few differences in the dossier submission requirements among the three regions i.e., USA, Europe and India which has been clearly represented through succinct comparisons third part of this work. The literature work, the comparison parameters, difference in generic drug approval requirements has been delineated in this work, which gives clear depict where India lies in its generic drug approval process and the challenges that Indian regulatory authority has to overcome in the near future. Regulatory involvement in the generic drug development hastens the drug approval process which directly/indirectly accelerated the launching of drug into the market. The regulatory  documents  whether  in-house  of  documents  to  be  submitted  to  regulatory authorities should be carefully reviewed by the skilled personnel to minimise the queries raised  by  the  regulatory  agencies  and  speed  up  the  approval  process.

Abstract

Clonazepam is a benzodiazepine indicated for seizure disorder, panic disorder and epilepsy. Patients suffering from seizures will have difficulty in swallowing the tablets or will be reluctant to take the tablets or will spit the administered tablet. In such cases, mouth dissolving dosage forms will be an effective solution for patient compliance and efficient medicine regimen. Clonazepam tablets are available in different strengths namely 0.125 mg, 0.25 mg, 0.5 mg, 1 mg and 2 mg. In the present research, mouth dissolving tablet of Clonazepam was made by aqueous wet granulation process. Pearlitol Flash and Microcrystalline Cellulose were used as diluent. Crospovidone was used as disintegrant. Strawberry Flavor and Aspartame were used as flavoring and sweetening agents. Sodium Lauryl Sulphate was used as a wetting agent. Colloidal Silicon Dioxide was used as glidant. Talc and Magnesium Stearate were used as lubricants. The prepared tablets were evaluated for weight, thickness, hardness, friability, disintegration time and dissolution. Prepared tablets showed disintegration time of less than 30 seconds and drug dissolution of about 75% achieved within 30 minutes. After finalizing the composition with 2 mg strength, using the same composition 0.125 mg, 0.25 mg, 0.5 mg and 1 mg strengths were made. The prepared tablets were stability tested at 40°C / 75% RH for 3 months and were found to be stable. Prepared mouth dissolving tablets of Clonazepam 1 mg was found to be bioequivalent under fasting and fed conditions with the marketed product.

Abstract

The industrial and domestic waste water of Faisalabad city, Pakistan is poured into two main drains namely Paharang and Madduana which are discharged in the rivers Chinab and Ravi. A study of heavy metal residues in goat meat was conducted along these drains in winter and summer seasons. Samples were collected from two areas (each consisting of three sites) along the main sewerage drains. Each sample was wet digested and then analyzed for residues of Cd, Cr, Ni and Pb applying atomic absorption spectrophotometry. The range of mean values of heavy metal residues (mg/kg) were found to be: in muscles; arm 0.020-4.704, rib 0.013-4.559, thigh 0.024-8.841, and in organs; liver 0.052-13.089, lung 0.022-12.918, kidney 0.026-14.150. These values were higher than most reported permissible levels. Levels of Cd, Cr, Ni and Pb in meat (muscles and organs) of goat are higher than the most reported values in the literature. Interseasonal variation showed higher heavy metal residues in meat during summer than those present in winter. In view of present investigations, to avoid heavy metal residues entry to food chain through contaminated feed and water, immediate measures must be carried out for the treatment and detoxification of industrial and domestic effluents intended to be used for agricultural purposes.

Abstract

A New extractive methods (A and B) with accuracy, sensitivity and precisely have been developed for the estimation of  telmisartan (TMS) in API and its pharmaceutical dosage form. In Method A, TMS was reacted with Metanil yellow dye, by forming yellow colored chromogen. On further the drug with the dye led to the formation of ion association complexes in acidic phthalate buffer of pH 2.8.This further extracted with chloroform exhibiting λ max at 410 nm .The Method B, TMS was reacted with Methyl Orange dye, by forming light yellow colored chromogen. On further the drug with the dye led to the formation of ion association complexes in acidic phthalate buffer of pH 2.8, followed by their extraction in chloroform, which exhibits λ max at 420 nm. The absorbance-concentration graph is linear and has the range of 5-35 mcg/mL for Method A and 20-45 mcg/mL for Method B. All the analytic parameters as prescribed by ICH guidelines were validated accordingly with statistically interpretation data. The proposed methods are precise, accurate, economical and sensitive for the estimation of TMS in API and its pharmaceutical dosage form.

Abstract

A new series of bis-sulfonyl piperazines were taken up for synthesis by inserting two sulfonyl groups at 1^st and 4^th position of piperazine in search of potent antimicrobial agents. An imperative intermediate 1-tosylpiperazine was accomplished through deprotection of di-tert-butyl dicarbonate group from 4-tosylpiperazine-1-carboxylate by using trifluroacetic acid. Further 1-tosylpiperazine upon electrophilic substitution reaction using appropriate substituted sulfonyl chlorides gave 1-((substituted aryl/alkyl)sulfonyl)-4-tosylpiperazines 8a-k as targeted series of bis-sulfonyl piperazines. The design, synthesis, FT-IR, ¹H NMR, ¹³C NMR, LC-MS spectral characterizations, elemental analysis and their in-vitro antimicrobial potency is discussed in this communication. Compounds 8f, 8j and 8k are proved to be potent antimicrobial agents.

Abstract

The present research work was an attempt to design a formulation to improve the oral therapeutic efficacy with optimal control of plasma drug level which contains two antidiabetic drugs i.e Metformin HCl and Pioglitazone HCl. Metformin HCl sustained release layer and Pioglitazone HCl immediate release layer was optimized separately and constituted in bilayer tablet. Sustained released layer was prepared by wet granulation method using Eudragits (pH dependent and pH independent) as polymers, immediate release layer were prepared by direct compression method using super disintegrates such as sodium starch glycollate. The blend was evaluated for bulk density, tapped density, compressibility index, hausner ratio, angle of repose and content uniformity. All the values were found within limit of standard. In vitro dissolution studies were carried out by USP type II paddle apparatus at 37±0.5°C. The result showed that eudragits in sustained layer can control the release of drug. The in vitro release profile of drug from sustained release layer could be expressed by zero order release as pilot show high linearity R²=0.9924, swelling and diffusion was the dominant mechanism of drug release. The formulation (PM8) having immediate release layer produces immediate effect 99.19±1.36 within 45 minutes followed by sustained release effect (99.53±0.30) up to 12 hours. Bilayer tablet prepared from optimized formula fixed dose combination of sustained release Metformin HCl and immediate release Pioglitazone HCl. It was confirmed from FTIR studies that there was no drug excipients interaction.

Abstract

The drugs today are being synthesised by a variety of modern chemical techniques. The new chemical entities thus designed have a variety of issues which hamper their translation to actual market. These issues are low aqueous solubility, first pass metabolism, low efficacy, potential side effects, pH stability problems, patient non-compliance to name a few. The leaps taken by current medical research prove the benefits of using two drugs simultaneously for effective treatment and management of disorders like hypertension, hyperlipedemia, infections etc. But combining two drugs which would have completely unrelated challenges would prove to be herculean task for any formulator. The present work focuses on this very challenge of combining two commonly prescribed antihypertensive agents’ metoprolol tartrate and hydrochlorothiazide, first of which suffers from extensive first pass metabolism and the latter from poor patient compliance. Thus a bilayered tablet is formulated, wherein the first later is an orodispersible layer of hydrochlorothiazide formulated using Primogel as the superdisintegrant and Galen IQ 720 as the diluent and the second one is the mucoadhesive layer of metoprolol tartrate prepared by using sodium carboxymethylcellulose as the mucoadhesive polymer. Both the layers were evaluated for physical characteristics, in vitro drug release and assay. Additionally, the orodispersible layer was assessed for in vitro wetting time, in vitro disintegration time while the mucoadhesive layer was evaluated for mucoadhesive strength, ex vivo permeation and surface pH.

Abstract

Drug utilization studies are used as a potential tool in the evaluation in the healthcare systems  as well as powerful exploratory tools to ascertain the role of drugs in the society. Irrational use of drugs has laid down the concept of “Rational use of drugs. Inspite of being one of the leading cause of death among Indian population , there is lack of pioneer drug utilization studies in this field. The objective of this study was to assess the pattern of prescribing prescriptions among the patients attending the department of respiratory medicine in  a tertiary care teaching hospital in India. A prospective, observational , cross sectional study was done among the patients attending  the  outpatient department of respiratory medicine with respiratory disease as first diagnosis as confirmed by physicians and laboratory investigations in a tertiary care teaching hospital in India over a period of three months from September 2013 to November 2013. The study was conducted after getting approval from the institutional ethical committee. Total 100 prescriptions were noted from the patients attending respiratory medicine outpatient department after taking written informed consent. Demographic profile, common respiratory diseases, commonly prescribed drugs as per Anatomical Therapeutic Chemical Classification (ATC) and WHO core indicators were assessed from the prescriptions. Data from 100 prescriptions were analyzed. Out of 100 patients, 42 were male patients and 58 were female patients. The most common respiratory condition encountered in the respiratory medicine   outpatient department  was tuberculosis , followed by lobar pneumonia, COPD, bronchitis, asthma, Ca lung, ILD. Most of the patients were in the age group of 41- 60. Most commonly prescribed drugs were antimicrobials followed by bronchodilators, antacids, analgesics, antiallergics, multivitamins, DOTS, i.v. fluids steroids, cough and cold preparations and opioids. The average number of drugs per prescription was 3.72. Out of 372  drugs prescribed, 76 were prescribed by generic names and 296 drugs were  prescribed  by their brand names. Drugs on  WHO EML were only 46%  while  that of  NLEM 2011  was 73%. Dosage forms used in injectable form were 79/372= 21.23%.Complete information about the patient was written in 26 %  patients. Complete diagnosis was written in 78 % patients. More than one diagnosis was present in 34% of prescriptions.82 % of prescriptions were complete in terms of dose, route, frequency, strength and dosage form. Incidence of polypharmacy was present in 52% of prescriptions. Fixed dose combinations were prescribed in 23.9% prescriptions.

Abstract

Tetraethylthiuram disulphide is chemical name of Disulfiram. There are few manufacturers available worldwide involved in the manufacture of Disulfiram Tablets due to its high bio variability from patient to patient. Disulfiram is available as immediate release tablets and effervescent / dispersible tablets. There is a report of high bio variability between the marketed, effervescent / dispersible tablets vis a vis immediate release tablets. Moreover, with respect to manufacturing of disulfiram tablets, the manufacturing process followed worldwide involves dry granulation by roller compaction / slugging method. The tablets thus prepared have very poor mechanical strength; rough edges are observed around the tablet circumference; when the marketed tablets are subjected to friability testing, tablets are failing in friability test owing to capping; some set of tablets show % friability in the range of 0.6-0.85% with severe edge wearing. To overcome this problem, a set of manufacturers perform the blend compression by extending the dwell time to prevent capping of tablets. Another set of manufacturers make the tablets with co-processed excipients. In some of the marketed product, Tween 80 or Myrj 52 is used as wetting agent, which may intervene with the P-gp efflux mechanism precipitating high bio variability of Disulfiram. In the present research, Disulfiram Tablets were manufactured by aqueous wet granulation process. Manufactured tablets showed good morphology and mechanical strength, without tableting issues. In this research apart from robust manufacturing process, influence of milling and micronization of API on the in vivo bio variability of the drug was studied and reported.

Abstract

Nanoparticles have tremendous potential application in drug delivery system. Chitosan nanoparticles have received plenty of attention because of its non-toxicity, biocompatibility, biodegradability and controlled drug release. The objective of the present work was to evaluate the potential of chitosan-tripolyphosphate (TPP) nanoparticles as a carrier in the preparation of Terbinafine loaded nanoparticles in order to enhance the bioavailability of drug and to reduce dose frequency for preventing the side effects of the drug. Ionotropic gelation method was used for preparation of chitosan–TPP nanoparticles loaded with Terbinafine. The cross linking between TPP and chitosan was determined by FTIR studies. The particle size and zeta potential of nanoparticles were studied by dynamic light scattering (DLS) and zeta potential analyzer. Transmission Electron Microscopy (TEM) was used to determine the morphological characteristics of nanoparticles. The particle ranges from 139-200nm in size and have a positive zeta potential +13.6mV.Thevariations in the concentration of chitosan and TPP effects the size and zeta potential of particles. Also, the change in the chitosan and drug ratio changes the physicochemical properties of nanoparticles, particles size increases with the increase in the concentration of Terbinafine while the the zetapotential decreases. These nanoparticles have good encapsulation efficiency of 77.8% for Terbinafine. These studies suggest that chitosan can complex TPP to form terbinafine loaded nanoparticles and appears as a promising system in microbial treatment.

Abstract

Nature has given support for mankind in all means. In the Pharmaceutical novel drug delivery dosage form it plays a important role for developing newer novel and stable dosage form. In this the mucoadhesive buccal delivery is one of the promising field in which so many drugs are designed for the health of nations. In this buccal delivery system to attain good therapeutic and stable polymers is necessary. From the available literatures so many products are formulated with synthetic and semi synthetic polymers .The aim of this article is explain the isolation of polymer from Diospyros pergrina and Dillenia indica which abundantly present in the earth and compare the evaluation parameters with available mucoadhesive polymers. The isolation of natural polymer from Indian Persimmon Fruits and Elephant apple fruit and performed the evaluation parameters for suitability for mucoadhesion and comparing with HPMC, sodium alginate, guar gum.Sodium carboxy methyl cellulose. From the datas the natural mucoadhesive polymers has more compatible and more suitable polymer alone and or with other combinations of polymers for developing optimized formulas and also very much suitable for developing novel drug delivery by buccal delivery especially for low bioavailable drugs.

Abstract

Bioenhancers or biopotentiators are a revolutionary concept in modern medicine. Bose in 1929 reported this for the first time on the antihistaminic effects of Vasaka leaves. Its effect was increased by the addition of long pepper in it. Outcomes: Large number of drug compound has been introduced by the advances in drug designing technologies. By co-administering drugs with naturally occurring compounds from plants which are considered to be simple and safe, can increase the bioavailability of drugs.

With modern medicine, Ayurveda can be combined which can make major contribution to the drug discovery process through reverse pharmacology by identification of active compounds and reduction of drug development costs.

Abstract

A three point geometrical correction method was proposed for the estimation of Hydrochlorothiazide and Clonidine hydrochloride from biological samples. The geometrical correction method was developed which eliminates or reduces the background irrelevant absorption that may be present in samples of biological origin.The method was developed using egg albumin as biological media at three wavelengths 317nm, 269nm and 226nm for Hydrochlorothiazide and 315nm, 280nm and 296nm for Clonidine HCl. The proposed method showed linearity at three wavelengths in the range of 6-14 µg/ml and 2-10µg/ml with regression coefficient of 0.993, 0.999 and 0.995 for Hydrochlorothiazide and 0.992, 0.993 and 0.986 for Clonidine HCl respectively.This proposed method was statistically validated in accordance with ICH guidelines. The method was found to be accurate, precise, rugged and robust as indicated by low values of % RSD. The % RSD for Hydrochlorothiazide at three wavelengths was 0.36, 0.73 and 0.55 and for Clonidine HCl was 0.45, 0.48 and 0.80. For the biological media, corrected absorbance (D value) was calculated and found to be constant for specified concentration. The D value showed linear relationship with concentration showing regression coefficient as 0.996 and 0.991 for Hydrochlorothiazide and Clonidine HCl respectively. A simple three point geometrical correction UV Spectrophotometric method was developed and validated as per ICH guidelines using egg albumin as biological medium for estimation of Hydrochlorothiazide and Clonidine HCl

Abstract

Most of the active pharmaceutical ingredients (APIs) under development are poorly water soluble and have poor bioavailability. Nanotechnology is an approach to overcome the challenges of conventional drug delivery systems. The solubility, in vivo stability, intestinal absorption, route of administration, targeting, effectiveness and side effects are the challenges that push the researchers toward exploring a new drug delivery. Nanoparticles made from solid lipid are alternative novel colloidal drug carrier to alter and improve the pharmacokinetic and pharmacodynamics properties of drug molecules. The present review focused on increasing awareness about nanotechnological field in drug delivery with the emergence of several approaches based on solid lipid like Solid lipid nanoparticles, Nanostructured lipid carriers, Lipid drug conjugates, Polymer lipid hybrid nanoparticles for improving medical therapeutics. Hence, solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and have attracted wide attention of researchers.

Abstract

Most of the floating systems have inherent drawbacks of high variability in the gastro intestinal transit time, invariably affecting the bioavailability of drug. To overcome it, a multiple unit floating system with extended GI transit time, capable of distributing widely throughout the gastrointestinal tract for effective enteric release of the drug has sought. Microballoons loaded with drug in their outer polymer shells were prepared by novel emulsion solvent diffusion method. The ethanol: dichloromethane solution of drug and polymers (HPMC, Eudragit S100, Carbapol 934) each with a ratio of 1:1, 1:2 and 1:3 respectively were poured into the solution of heavy liquid paraffin containing 1.5% span 80. The flowability of resulting microballoons improved when compared to that of the pure drug. The formulations were evaluated for percentage practical yield, particle size analysis, percentage drug loading, drug entrapment efficiency, floating behavior, Scanning Electron Micrography, FTIR, DSC, dissolution study and the drug release kinetics. The enhanced floatability of the formulations and their retention in GIT may attribute for the increased bioavailability and decrease in frequency of administration. Of all the three polymers used it was observed that HPMC to be a suitable candidate for sustained release of the drug from that of the floating microspheres (microballoons). Among the three formulations prepared with HPMC, formulation F1 (drug: polymer 1:1) was found to be an optimized one with particle size of 32.96µm, 40.46% drug entrapment efficiency, 91.03 percentage yield, 69.88% buoyancy and 20.74% of drug loading. At the end of 12^th hr the drug release rate was found to be 96.42%.

Abstract

The investigation is aimed to study the effect of different viscosity grades of Hydroxypropyl methylcellulose (HPMC K4M, K15M, K100M) at different concentration on the release rate of two drugs with different aqueous solubility, that is freely water soluble drug Propranolol hydrochloride and practically water insoluble drug Valsartan. Hydrophilic matrix tablets containing 80 mg of drug and 10%, 15% 30%, 45% and 60% w/w of each of the three grades of the polymer were fabricated for both the drugs respectively. Formulations were evaluated with respect to drug release studies for 24 hours and rate kinetics study was done on each formulations. The result indicated that of the various viscosity grades of HPMC, HPMC K15 was able to better control the release for both water soluble and insoluble drug at desired rate for 24 hrs. For water soluble Propranolol hydrochloride HPMC K15M concentration required to give desired release profile is 45% of tablet weight and for the insoluble drug Valsartan the HPMC K15M concentration needed to get desired release profile is 15%. The Peppas release kinetic model defined the drug release for the optimized Propranolol HCl controlled release formulation indicating non Fickian diffusion. For Valsartan, the Hixon Crowell model best defined the release rate kinetics.

Abstract

Cycas beddomei (Cycadaceae) is reported as traditional medicinal plant used against rheumatism, skin diseases, aphrodisiac, arthritis and ulcers. C.beddomei is also reported Critically Endangered Globally (CR) under IUCN Red listed species. Different plant parts are screened for their phytochemical constituents and reported alkaloids, flavonoids, phenols, terpenoids, saponins, tannins, glycosides and lignins in leaf, bark, pith, male, female cones and in roots. And also reported antibacterial and anthelmintic activities equally to that of Ampicillin and Albendazole the respective standard drugs. Hence the present study emphasized on the qualitative analysis of phenols, flavonoids and anthocyanidin compounds the major secondary metabolites as per the standard methods. The results revealed the presence of 23 phenolic compounds, 7 flavonoids and 5 anthocyanidin compounds in all parts which supports the herbal uses and the biological activities as antimicrobial against human pathogenic bacteria and fungi mainly which causes skin diseases, rheumatism and ulcers.

Abstract

An accurate and precise RP-HPLC method was developed and for the simultaneous determination of Emtricitabine and Tenofovir in Pharmaceutical dosage form and was validated as per ICH guidelines. The separation was achieved on an Inertsil ODS Column (250 x 4.6 mm, 5 micron) as a stationary phase and Methanol: Water (80:20) v/v as mobile phase, with at a flow rate of 1 ml/min and separation was monitored by UV detector, at a detection wavelength of 260 nm. Retention time of Emtricitabine and Tenofovir was obtained at 2.893 and 3.932 min. respectively. Validation was performed as per ICH guidelines which include accuracy, precision, linearity, specificity, ruggedness and robustness. The linearity was found to lie between 20-100 µg/ml for Emtricitabine and 30-150 µg/ml for Tenofovir disoproxil fumarate. The Percentage recovery of Emtricitabine and Tenofovir was found to lie in the range of 98.0 – 102.0 %. Hence the proposed method was found to be fast, precise and accurate, since the run time is less than 5 minutes and the mobile phase preparation does not require an elaborative procedure. Hence the proposed method can be applied for the routine quality control of pharmaceutical preparations in combined dosage form.

Abstract

Radioprotective agents are the compounds which are used for the protection of normal tissues during accidental and therapeutical exposure to ionizing radiation. Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) is a pyrazolone derivative known for its radioprotective and neuroprotective efficacy. The present work describes the evaluation of radioprotective efficacy of edaravone derivative with trifluoromethyl moiety, 3-methyl-1- (4-(trifluoromethyl)phenyl) -1,2-dihydropyrazol-5-one (MTMPP). The in vitro antioxidant activities namely DPPH radical scavenging, nitric oxide radical scavenging and reducing power activity assay of MTMPP showed a comparable activities with that of standard edaravone. The MTMPP pretreated flies on 3Gy electron beam irradiation exhibited a considerable radioprotective ability towards radiation induced oxidative stress damage by diminishing lipid peroxidation, elevating glutathione level and by restoring the activities of  antioxidant enzymes  SOD and CAT to near basal level.

Abstract

This review article presents a survey covering the synthetic strategies leading to benzoxazole derivatives that have shown various considerable biological activities such as Antimicrobial, Anti inflammatory, Analgesic, Antifungal, Herbicidal, Antiplatelets, Anticonvulsants, Antitumor, Anticancer,Anti alzheimer's actions, Antihyperglycemic Potentiating Activity, Melatoninergic Ligands, Antitubercular ,Photophysical Properties, Anti HIV agents Anthelmintic agents. This review may help medicinal chemists to develop newer compounds possessing benzoxazole moiety that could be better agents in term of efficacy and safety.

Abstract

Telmisartan is a well-known and widely used anti-hypertensive agent and it belongs to bio-pharmaceutical classification system (BCS) class II drug with low solubility and high permeability. The present study was aimed to enhance the solubility of Telmisartan by solid-dispersion techniques (physical mixing and solvent evaporation methods) using carriers like Micro crystalline cellulose, Sodium Starch Glycolate, Cross-povidone and Cross-caramellose sodium. The prepared formulations were characterized for percentage practical yield, drug content and in-vitro drug release studies. Amongst the formulations prepared (F1-F5), F5 formulation consisting of Telmisartan and Crospovidone in the ratio 1:4was considered as optimized formulation in which percentage drug release was found to be 98.82% within 60 minutes in comparison with that of pure drug dissolution of only 65.46% within 60 minutes. Solubility and drug release rate of Telmisartan was enhanced in all the formulations (F1-F5) by this technique. The order of enhancement of the drug release rate with various carriers was found to be CP>SSG > CCS > MCC.

Abstract

The Chitosan is obtained by the alkaline deacetylation of chitin, which is the major component of protective cuticles of various crustaceans like crabs, shrimps, prawns, lobsters etc. A lot of work is done on the chitosan to explore its clinical, biomedical, food, agricultural and horticultural use. The chitosan is Biodegradable, non-toxic, Bacteriostatic, fungistatic hence it have wide application in the pharmaceutical field. The current review gives the detailed information about chitosan properties, application and its future applications in pharmaceutical field.

Abstract

Aim of the present study was to determine the sensitivity, specificity, positive and negative predictive values of anti-tissue trans-glutaminase immunoglobulin A in celiac disease. It is a comparative cross sectional study conducted in Department of Pediatric Medicine, Services Hospital Lahore, which is a tertiary care hospital.Fifty suspected cases of celiac disease were included in this study.  The study included 50 patients (age range 1-12 years) who visited the hospital during one year time, with mean age of 5.7±3.0 years. Out of these patients 54% were girls and 46% boys. Anti-tissue trans-glutaminase was positive in 40 patients and 10 patients were negative while in 37 patients histopathology was consistent with Celiac Disease (CD) and 13 patients had normal histopathology. 32 patients were true positive, 8 patients false positive, 5 patients’ false negative and 5 patients were true negative. Anti-tissue trans-glutaminase IgA proved sensitivity 86.5% and specificity 38.4%. The diagnostic accuracy of the test was 74.0% with positive predictive value of 80.0% and negative predictive value 50.0%. Positive anti-tissue trans-glutaminase antibody titers may give suspicion of Celiac disease in children but can’t replace Small Bowel Biopsy (SBB) which is still Gold standard. Hence, histological confirmation is mandatory for its diagnosis. Serological tests may be more significant if they are combined instead of using single one for diagnosis of Celiac disease.

Abstract

The anti-ulcer effect of aqueous extract of Aerva lanata stem was tested against ulcers induced by ethanol, pyloric ligation, indomethacin and cysteamine in wistar albino rats. The anti-ulcer activity was assessed by determining and comparing the ulcer index in the test group (250,500 mg/kg) with that of the control group and omeprazole 20mg/kg was used as a reference standard. Aerva lanata significantly decreased free-acidity, total-acidity, ulcer index and increased the pH in pylorus ligated model where as ulcer index decreased in ethanol, indomethacin and cysteamine induced models. One of the more significant findings to emerge from this study is that aqueous extract of Aerva lanata stem possess antiulcer properties in a dose dependent manner which could be either due to cytoprotective action, anti secretory or anti oxidant mechanism of the drug. The antiulcer properties of the extract may be attributed to the presence of phyto chemicals like flavonoids, alkaloids and tannins present in the plant extract with various biological activitiesDepartment Of Pharmaceutical chemistry: Mallareddy College of Pharmacy, Medchal.

Abstract

Combination therapy has gained a lot of importance nowadays due to greater patient acceptability, increased potency, action at different sites, fewer side effects and quicker relief.  Literature survey revealed that various methods like UV, HPLC, and HPTLC have been reported for the analysis of Olmesartan and Indapamide individually and combined with other drugs but there was no HPTLC method for their simultaneous estimation. As HPTLC methods offer advantages in being simple, faster and cost effective, an accurate, precise, and specific HPTLC method has been developed for the simultaneous estimation of Olmesartan and Indapamide. Chromatographic separation was performed on HPTLC Aluminium plates coated with Silica gel 60 F₂₅₄ adsorbent. The mobile phase optimised for the separation was Toluene: Chloroform: Ethanol (4:4:1 v/v). The separated components gave R_f values of 0.15 and 0.47 for Olmesartan medoxomil and Indapamide, respectively. The linear regression analysis data for the calibration plots showed good linear relationship with r value 0.99930 and 0.99660 for Olmesartan medoxomil and Indapamide respectively, in the concentration range of 100 to 700 ng/spot for Olmesartan and 100 to 600 ng/spot for Indapamide. The method was validated according to the ICH guidelines with respect to accuracy, precision, specificity and robustness. The LOD and LOQ were 100 and 300 ng/spot respectively for Olmesartan and 100 and 300 ng/spot respectively for Indapamide. The proposed, developed and validated HPTLC method can be used as an important tool for identification and quantitative determination of Olmesartan medoxomil and Indapamide in bulk drugs and pharmaceutical formulations.

Abstract

Free radicals are the atomic and molecular varieties of oxygen that are collectively known as reactive oxygen species that initiates oxidative stress, an imbalance between the formation and neutralization of the pro-oxidants. The free radicals seek stability by stealing electrons from the biological macromolecules such as proteins, lipids and DNA in healthy human cells that in turn leads to the damage of proteins and DNA along with lipid peroxidation. Cellular constituents act as antioxidants play an important role in scavenging the free radicals formed and any disturbances can lead to various disease conditions that include cancer, neurodegenerative disorders, atherosclerosis, cardiovascular disease, ageing etc. Several researches have shown plant extracts and different classes of phytochemicals to have a prominent antioxidant activity. The free radical scavenging activities of the methanolic extract of leaves of Artemisia vulgaris was assessed in different concentrations ranging from 0.125mg to 1.0mg against in vitro generated radicals like DPPH, ABTS, Hydrogen peroxide and Hydroxyl. The results were compared with a standard antioxidant trolox at the same concentrations. Methanolic extract of A. vulgaris showed considerable scavenging activity against the radicals generated in vitro in a dose-dependent manner. Hence, the extracts can be used for the treatment of diseases where free radicals play a major role.

Abstract

A single high performance liquid chromatography (HPLC) method has been developed and validated for the quantitative estimation of Oxcarbazepine and its impurities (assays dissolution and related substances) in different type of dosage form. The chromatographic separation was performed on a Hypersil BDS C18 column with a particle size of 5µ (250X4.6 mm) and a mixture of 0.05M phosphate buffer adjusted to pH 6.0, methanol and acetonitrile in the ratio of 62:22:16 v/v/v as mobile phase at flow rate of 2.0 mL/minutes, Calibration showed that the response of impurity and drug substance was a linear function of concentration over the range 0.02–2.43 μgmL−1 (r2 ≥ 0.999) and the method was validated over this range for precision, intermediate precision, accuracy, linearity and specificity. For precision study, RSD of each impurity and drug substance was <5% and <2% respectively. The method was found to be precise, accurate, linear and specific. The proposed method was successfully employed for assay, dissolution and related substances analysis of Oxcarbazepine immediate release (IR), extended release (ER) tablets and suspension. A simple isocratic method with 35 minutes run time for determination of all three critical parameters is an added advantage of getting product quality in one shot.

Abstract

The main objective of the present investigation was to develop sustained release tablets of Lornoxicam a highly potent nonsteroidal anti-inflammatory drug with short half-life, that are characterized by initial burst drug release in the stomach and comply with the release requirements of sustained-release products using polymer and hydrophilic wax viz. HPMC K-15 M, PEG 6000. Sustained release tablets were prepared by melt granulation technique in which PEG 6000 used as a binder. This technique is better than a conventional granulation due to no water or organic solvents is needed. The process is less time consuming and uses less energy than wet granulation. Melt granulation is a useful technique to enhance the solubility and dissolution rate of poorly water-soluble drug.  The tablets were evaluated for physical characteristics like hardness, weight variation, friability and drug content. All the physical characters of the fabricated tablet were within acceptable limits. In-vitro release of drug was performed in 0.1 N HCl and phosphate buffer pH 6.8 for 12 hr. employing USP Type –II (paddle) at 50 rpm. The FTIR study revealed that there was no chemical interaction between drug and excipients. The drug release profile of the best formulation was well controlled and uniform throughout the dissolution studies. The drug release of optimized formulation follows the Higuchi kinetic model.

Abstract

The simple and cost effective approach to synthesis of stable silver nanoparticle was achieved from the methanolic extract of Gloriosa superba rhizome. Research work has summarized as green synthesis of nanomaterial, identification of size and characterization of synthesized nanoparticle by SEM analysis, UV-visible spectrophotometer, Infrared spectroscopy, and X-ray diffraction.  The synthesized nanoparticle revealed their antibacterial efficacy against Staphylococcus aureus, Bacillus subtilis and Salmonella typhi. The results found to be potent antibacterial activity at the different dosage level (25, 50, 75 and 100 µg/ml) among the concentration level, the 100 µg/ml was found  effective and zone of inhibition 16.2±0.76, 13.3 ± 0.91 and 11.1 ± 0.94 mm against Staphylococcus aureus, Bacillus subtilis and Salmonella typhi respectively compared to the ciprofloxacin. 

Abstract

The research objective is to formulate modified-release tablets of Prednisone which will be stable and bioequivalent to the marketed product RAYOS^® manufactured by Horizon Pharma USA, Inc. Present research involves design of a simple reservoir type drug delivery system that releases the drug as a single pulse after a definite time lag. RAYOS^® involves Skye Pharma’s patented GEOCLOCK™ technology which is a press coated tablet design where the inner immediate release core tablet is housed in a barrier tablet containing Dibasic Calcium Phosphate Dihydrate, Glyceryl Behenate and Polyvinylpyrrolidone. This outer barrier tablet delays the disintegration and dissolution for about 4 hours after which it breaks to expose the inner core tablet to release the drug as a single pulse. In USA, RAYOS^® and in Europe LODOTRA^® is available in 3 strengths namely 1 mg, 2 mg and 5 mg which are pseudo dose proportional to each other. Like marketed product, a look-alike approach was followed in the design of drug delivery system, where immediate release tablets of prednisone were modified-release coated to about 21% w/w build-up of Ethyl Cellulose and Hypromellose 3 cps in the ratio of 8:2. The prepared tablets were stable; showed comparative disintegration, dissolution and promising bio equivalence profile to that of RAYOS^®.

Abstract

The objective of the present study was to formulate and characterize the poorly soluble drug simvastatin in order to enhance the solubility and dissolution characteristics. Simvastatin is a Biopharmaceutical classification system (BCS) Class II drug having very less solubility and therefore low oral bioavailability (5%). In the present study, simvastatin nanosuspensions were prepared by homogenization technique by using poloxamer 188 and poloxamer 407 with different ratios. The Lyophilized nanosuspensions were characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (pXRD), scanning electron microscopy (SEM) and infra red spectroscopy (FTIR). The nanosuspension was evaluated for drug content, saturation solubility and in-vitro dissolution studies. The pXRD profile of nanosuspension suggests that transformation of crystalline drug into amorphous form. DSC studies revealed that there was no interaction between drug and carrier. The effect of particle size was found to be significant on the saturation solubility of the drug and in-vitro drug release studies showed significant increase in the dissolution rate of nanosuspensions as compared with pure drug. This study has shown that initial crystalline state is changed to amorphous form due to particle size reduction. Saturation solubility with poloxamer 188 and poloxamer 407 was found to be 317.7 µg/ml and 218 µg/ml respectively when compared with pure drug. The dissolution profile with poloxamer 188 was better than with poloxamer 407, with former releasing   99.14 % drug in 60 minutes. In conclusion the results indicated nanosuspension technique by using poloxamer successfully used for enhancing the solubility of simvastatin. nanosuspension with poloxamer 188 showed suitability, as a stabilizer in the formulation of nanosuspension.

Abstract

In the present study, we evaluated the preventive effect of methanolic extract of  Momordica cochinchinensis(MEMC) fruit on renal function in alloxan-induced diabetic rats. In addition, we examined (MEMC) extract could prevent diabetic nephropathy and insulin sensitisation action. Initially we kept rats for acclimatisation along with high fat diet for 20days and then, Diabetes was induced in Wistar albino rats with a single intraperitoneal injection of alloxan (120 mg/kg). Two days after alloxan injection diabetic rats were selected and divided into groups, MEMC preparations (200 mg/kg per day), (400 mg/kg per day) were given orally for 28 days to diabetic rats. Survival analysis as well as biochemical parameters were measured. Administration of MCC extract to diabetic rats resulted in a significant decrease of Proteinuria and serum parameters(creatinine, uric acid, urea, triglycerides, cholesterol, LDL ) in Standard, Test1 and Test2 when compared to Toxic group(only alloxan 120mg/kg and high fat diet) treated group. Insulin resistance action was measured by glucose tolerance test and there is remarkable decreased blood glucose levels of Standard, Test1 and Test2 compared to Toxic group at different time intervals. MCC treatment improve the impairment of fatty acid metabolism in diabetes. From the results we can conclude that MCC preparations are able to attenuate diabetic renal damage, probably by its anti-oxidative action and its anti diabetic activity. The protective role on diabetic nephropathy and insulin resistance by  MCC against the high fat diet and along with Alloxan induced damages in diabetic rats gives a hope that they may have similar protective action in humans.

Abstract

Flavonoids are polyphenolic compounds found to have enormous pharmacological activity, Naringin, a molecule with a wide spectrum of pharmacological activity still has not been used for treatment of any diseases due to its lacking potency. The present study was focused to synthesize various derivatives of naringin and to evaluate their antioxidant activity. Compounds, N.a, N.l, N.k, N.l have shown very potent antioxidant activity. Many literatures have claimed that many free radicals are responsible for carcinogenesis, and these compounds have very good scavenging properties. Thus these compounds can further be studied for their anticancer property and these compounds could be useful in discovering a new lead moiety for cancer.

Abstract

Metoprolol tartrate is effective β-blocker which is having antianginal properties and used in the treatment of myocardial infarction. Oral bioavailability of metoprolol tartrate is around 40%. In present work an attempt has been made to prepare fast dissolving tablets of metoprolol tartrate to enhance the dissolution rate. Sublimation method . The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. In all the formulations, friability is less than 1%, indicated that tablets had a good mechanical resistance. Drug content was found to be in the range of 98 to 102%, which is within acceptable limits. In sublimation method, camphor is used as subliming agent. All the tablets of metoprolol tartrate were subjected to weight variation, hardness, friability, in vitro dispersion, drug polymer interaction, drug content uniformity, and in vitro drug release The drug release from tablets of metoprolol tartrate prepared by sublimation methods were found to be S1 showed 98.20% drug release within 10 minute. It  is  concluded  that  Metoprolol  Tartrate  mouth   dissolving  tablets  could  be  prepared using  sublimation technique with improved bioavailability and rapid onset of action.

Abstract

Assessment of liver can be made by estimating the activities of ASAT, ALAT, ALP and LDH, which are enzymes originally present in higher concentration in cytoplasm. When there is hepatopathy, these enzymes leak into the blood stream in conformity with the extent of liver damage. Many toxins target the liver and cause hepatotoxic effects that can be observed through some biochemical parameters. Impairment of the liver generally occurs from excessive exposure to xenobiotics, alcohol, chemotherapeutic agents, virus and protozoan infections. Depending upon the severity of toxicant insult, hepatic cell injury can lead from acute to chronic hepatitis, which if left untreated can result in cirrhosis or malignant lesions. In this paper we study of the effect of selected drugs against each toxicant by estimating the biochemical parameters using hepatocytes.

Abstract

The present study is an attempt to investigate the pharmacodynamic and pharmacokinetic interactions of Cassia auriculata with Metfornin. Though Cassia auriculata’s antihyperglycemic activity has been proved but no work till date has been done to study its Pharmacodynamics and Pharmacokinetic interactions with other oral Hypoglycemics (OH). A single dose of 55 mg/kg streptozotocin prepared in citrate buffer (pH 4.4, 0.1 M) was injected intraperitoneally to overnight fasted animals to induce diabetes. The control rats received an equal volume of citrate buffer and used along with diabetic animals. The One Touch Glucometer AccuCheck is used for quantitative in vitro determination of glucose in various samples.  Each day after administering drug to the animals after 3 hours a drop of blood was applied on the AccuCheck strip and the blood glucose reading was measured.  Diabetes was confirmed after 48 hr of streptozotocin injection, the blood sample were collected through retro-orbital puncture and plasma glucose levels were estimated by one touch Glucometer. The rats having fasting plasma glucose levels more than 250 mg/dL were selected and used for the present study. Cassia auriculata extract was administered for 21 days at single dose level 500 mg/kg made in aqueous and given orally along with the standard drug combinations. The Blood was collected by terminal tail vein puncture and retro orbital puncture. Blood glucose levels were measured using one touch glucometer. Blood was centrifuged at 4000 rpm for 7 minutes. Body weight and blood glucose levels was analyzed every day were analyzed after 21 days.  Pharmacokinetically Cassia auriculata and 90 mg/kg Metformin combination increased the t_1/2, t_max of Metformin, decreased the C_max and AUC_0-t was similar to Metformin control. These results suggest that Cassia auriculata and 90 mg/kg Metformin combination is potentiating Metformin’s action by decreasing its elimination, but this may lead to Metformins toxicity. As Cassia auriculata extract itself has antidiabetic activity, it may be a reason why this combination is showing potentiating effect (supra additive).  Pharmacokinetically Cassia auriculata and 45 mg/kg Metformin combination is increasing t_max, decreasing t_1/2, increasing C_max and increasing AUC_0-t of Metformin.

Abstract

Attenuation of postprandial glycemia is hypothesized to reduce the risk of progression from impaired glucose tolerance to diabetes. It is also thought to reduce the number of complications associated with diabetes. The marketed α- gliucosidase inhibitor like Acarbose, Miglitol and Voglibose are wide used for treatment of DM, apart from these drugs Salacia Oblonga and Salacia reticulata are plants native to India and Sri Lanka these are widely used for thousands of years in Ayurvedic medicine for the oral treatment of diabetes a chronic disorder in metabolism of carbohydrates, proteins and fat due to absolute or relative deficiency of insulin secretion with/without varying degree of insulin resistance.  A clinical trial conducted to assess the comparison of outcome of marketed drugs and their combination with salacia species,  found significant effect on weight and HbA1C value of patients of Type II DM.