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  • PREPARATION AND CHARACTERIZATION OF NIOSOMES CONTAINING ACECLOFENAC

    About Author:
    Patel Sanjay P
    Sanjeevan College Of Pharmacy,
    Behind Shyam Sarovar Township,
    Jaipur-Agra Highway,Dausa-303303,Rajasthan
    sanonly4frdz@gmail.com,sanjay_411987@yahoo.com

    1.Abstract
    Aceclofenac is a drug with narrow therapeutic index and short biological half-life, so can achieve steady state concentration rapidly. This study was aimed at developing and optimizing niosomal formulation of aceclofenac in order to improve its bioavailability as compare to liposomes.This niosome is prepared by modified ether injection technique. In this span 60 & span 20 is used as non ionic surfactants. Different 6 formulation are prepared, In this NFS-1 to 3 formulation are prepared using the span 60 & NFS-4 to 6 are prepared using span 20 along with different proportion of cholesterols. Because of the presence of nonionic surfactant with the lipid, there is better targeting of drugs to tumor, liver and brain. In evaluation study, the effect of the varying composition of non ionic surfactant and cholesterol on the properties such as drug entrapment efficiency, drug content, particle size & shape and drug release were studied. Moreover, the release of the drug was also modified and extended over a period of 72 h in all formulations. NSF-3 emerged as the most satisfactory formulation. Further, release of the drug from the most satisfactory formulation NSF-6 was evaluated through dialysis membrane to get the idea of drug release. The mechanism of dug release was governed by K- Peppas model. In all the niosomes prepared with spans, as the concentration of surfactant increased drug entrapment efficiency increased. Among the spans, span 60 having high phase transition temperature (gel to liquid transformation) and having critical packing parameter (CPP) ranging from 0.5 to 1 entrap drug molecule without any cholesterol. The only drawback of span 60 vesicles was rapid leakage of drug from the vesicle because of high phase transition temperature. In all the cases the best fit model was found to be Peppas with ‘n’ value between 0.65 to 0.73 suggesting the non fickian (anomalous) release mechanism for the drug i.e., erosion followed by diffusion controlled. Formulation NSF-6 showed high entrapment efficiency (96.07%±0.35), particle size (4.22±0.47μm) and drug release (87.21%) over 72 h. Hence it was considered to be good niosomal formulation with greater bioavailability.

  • FORMULATION AND EVALUATION MULTIPARTICULATE SYSTEM OF RABEPRAZOLE SODIUM

    About Authors:
    Sriharsha Vardhan
    SRM College of Pharmacy,
    Chennai, Tamil Nadu

    sriharshavardhan.51@gmail.com

    ABSTRACT
    The present study is formulating Rabeprazole modified release beads (Immediate and Time, Pulsatile Release) and to target the release of the drug in intestine and to avoid stability related problems. Preparation of immediate release (IR) Rabeprazole beads has done by drug layering process and barrier coated beads by providing an enteric coating membrane on IR beads. Timed release beads has done by providing a Film coating for IR and lag time coating for TPR (Timed, Pulsatile Release)  on enteric coated beads. Encapsulation Process and evaluation of enteric coated IR and TPR beads has done by physical evaluation and chemical evaluation. Stability studies have done for best quality Rabeprazole IR and TPR enteric coated beads formulations. Based on the results Formulation 3 and Formulation 9 were selected as the best formulation developed for Rabeprazole Dual Drug Release Capsules.

  • Synthesis and Antimicrobial activity of Bulky molecules comprising Benzothiazole and Sulphonamide moieties

    About Authors:
    Pritesh R. Patel*, Priyank Patel, Jagath Pillai, Nilesh Darji, Bhagirath Patel
    Department of Pharmaceutical Chemistry,
    Sat Kaival College of Pharmacy, Sarsa,
    Ta & Dist: Anand (Gujarat), India-388365

    *prit.pharma@gmail.com

    ABSTRACT
    As part of ongoing studies in developing new antimicrobials, a novel series of 4-acetamido-N-(substituted 1, 3-benzothiazol-2-yl) benzenesulphonamide and N-(substituted 1, 3-benzothiazol-2-yl)-4-(substituted aryl diazenyl) benzenesulphonamide were synthesized in order to determine their antibacterial and antifungal activity. The synthesized compounds were tested in vitro against two Gram-positive bacteria like Staphylococcus aureus, Bacillus subtilis; two Gram-negative bacteria like Escherichia coli, Pseudomonas aeruginosaand one fungal strain Candida albicans in comparison with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial and antifungal activity against the tested microorganisms. The compounds with a 6-chloro (SK5b), 7-chloro-6-fluoro(SK5d) and 6-nitro (SK5e) on 2-amino benzothiazole ring possessing azo linkage showed better antimicrobial activity; almost similar or less to that of standard drugs thus they could be promising candidates for novel drugs. The novel heterocyclic derivatives were characterized by Physical characterization (Melting point, TLC) and different Spectroscopy techniques (IR, 1H NMR and Mass spectroscopy).

  • A REVIEW ON ROLE OF MOLECULAR DESCRIPTORS IN QSAR: A COMPUTATIONAL METHODS APPROACH

    About Authors:
    Rakesh Bhatia*
    School of Pharmaceutical Sciences,
    Department of Pharmaceutical Chemistry,
    Jaipur National University,
    Jaipur-302025 (Rajasthan), India

    *rakesh.mpharm1304@yahoo.com

    Abstract
    Chemical synthesis data and their biological screening have provided a vast amount of experimental data. As a result of that, availability of large amount of biological data information through molecular biology has made drug discovery and development a more complex method. To combat these problems, Quantitative structure-activity relationships (QSAR) emerged as a very useful tool in drug design. QSAR has been applied extensively and successfully over several decades to find predictive models for activity of bioactive agents. QSAR have brought revolution in drug discovery process by thedevelopment of mathematicalrelationships linking chemical structures and pharmacological activity in quantitative manner of series of compounds. Description of the molecular structure, electronic orbital reactivity and the role of structural and steric components has been the subject of mathematical and statistical analysis. Computational drug design method in QSAR is a rapidly growing field which is now a very important component in the discipline of medicinal chemistry. Virtual filtering and screening of combinatorial libraries have recently gained attention as methods complimenting the high-throughput screening and combinatorial chemistry. These chemoinformatic techniques rely heavily on quantitative structure-activity relationships (QSAR) analysis, a field with established methodology and successful history.By characterize a specific aspect of a molecule that is numbers containing structural information derived from the structural representation used for molecules under study called “Molecular descriptors” to find appropriate representations of the molecular structure of drug compoundsto obtain the structure-activity relationships in which these theoretical and computational methods are based, the ability to predict physicochemical, pharmacokinetic and toxicological properties of these leads are becoming increasingly important in reducing the number of expensive methods and late development failures. Thus thereby, QSAR certainly decreases the number of compounds to be synthesized by easing the selection of the most promising candidates. This review seeks to provide a review on role of molecular descriptors in the drug design in QSAR.

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  • BULLOUS PEMPHIGOID

    About Authors:
    Patel Punita s*, Patel Brilina M, Arora Bhoomi
    Institute of clinical research India
    ahmedabad, Gujarat
    *
    punitapatel_icri@ymail.com

    Abstract:
    Bullous Pemphigoid (BP) is an autoimmune subepidermal blistering disease appearing predominantly in the elderly. Bullous Pemphigoidcharacterized by an autoimmune response to 2 hemidesmosomal proteins within the dermal–epidermal junction, These proteins, called BP antigen 1 (BPAG1 or AgBP230), and BPAG2 (or AgBP180 or collagen XVII) have respective molecular masses of 230 and 180. While BP180 is a transmembrane glycoprotein with an extracellular domain BP230 localizes intracellularly and associates with the hemidesmosomal plaque. The disease is characterized clinically by tight bullae, with clear content, often large, developing primarily on the edge of erythematous plaques. Intense itching is common. The disease is primarily treated with systemic corticosteroids. Now,The increased knowledge of the development of noveltherapeutic strategies for Bullous Pemphigoids.

  • FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF CHLORPHENIRAMINE MALEATE.

    About Authors:
    H.S.Sawwalakhe*, J.M.Maidankar, M.A.Channawar, Dr.A.V. Chandewar

    P. W. College of Pharmacy, Yavatmal,
    Amravati university

    *hemant_11sep@rediffmail.com

    ABSTRACT:
    The demand for mouth dissolving tablets has been growing during the last decade especially for elderly and children who have swallowing difficulties. Chlorpheniramine maleate is a non-steroidal anti-inflammatory drug (NSAID) histamine H1 antagonist with antihistamine drug it is commonly used  in allergic reactions, hay fever, rhinitis, urticaria, and asthma. The main criteria for mouth dissolving tablets are to disintegrate or dissolve rapidly in oral cavity with saliva in 15sec to 60sec with need of water. The disintegrants used should fulfill the criteria by disintegrating the tablets in specified time limit.in the present investigation variety of super disintegrants Crospovidone, sodium starch glycolate,kyron t-314 , were selected and tablets were prepared by direct compression method in different concentration like 3%,6% and 8%. The prepared tablets were evaluated for weight variation, hardness, friability, in vitro disintegration time, wetting time, in vitro dissolution study, etc.formulation f-9 shows the lowest disintegration time (29sec) and wetting time (37sec). In vitro dissolutionstudies revealed that formulation F-9 containning 9% t-314  showed 98% drug release at the end of 10 min.

  • SELECTIVE ESTROGEN RECEPTOR MODULATORS: ANTIBREAST CANCER AGENTS

    About Authors:
    Rawat Pinki1*, Rawat Preeti2, Kumar Piyush3 Kanoujia Jovita3, Singh Sangeeta 1
    1. Institute of Pharmaceutical Science and Research, Unnao, U.P., India.
    2.  L.T.R. College Of Technology, Meerut, U.P., India.
    3. Curadev Pharmaceuticals Ltd., Kanpur, U.P., India.

    *pnkrawat@gmail.com

    Abstract:
    Selective estrogen receptor modulators, called SERMs for short, blocks the naturally circulating estrogen in breast tissues and other estrogen-sensitive tissues in the body. Each estrogen receptor has a slightly different structure, depending on the kind of cell it is in. If a SERM binds to a estrogen receptor, there is no site available for estrogen to bind and it can't attach to the cell. SERMs are called "selective" because they bind to particular estrogen receptors. This selective binding action is sometimes called estrogen inhibition, or estrogen suppression.

  • A REVIEW ON: BIOAVAILABILITY AND BIOEQUILANCE

    ABOUT AUTHORS:
    1 Shashi Kant*,Satinder Kumar, Rajender Kumar,
    Research scholar department of pharmacy.
    2 Dr. Bharat Prashar
    HOD & Associate professor  Department of Pharmaceutical Sciences, Manav Bharti University, Solan (H.P)

    * shashi_ranaute@yahoo.in

    ABSTRACT:-
    In this review article, we discussed about Bioavailability and bioequilance study, bioavailability means rate and extent to which active ingredients absorbed from a drug product and become available at site of action. This article provides the information about important aspect involved in bioequivalence and regulatory requirement for bioequivalence study. The rate or rapidity at which drug is absorbed is important consideration in treatment of acute conditions such as asthma attack in pain. Extent of absorption is of special significance in treatment of chronic conditions like hypertension, epilepsy. In this review we discussed all the factors affecting bioavailability from its dosage form, objective/purpose of bioavailability study, design and evaluation of bioequilance study, methods of assessing of bioavailability and bioequilance etc.

  • REVIEW ARTICLE: Solid Dispersions

    ABOUT AUTHORS:
    D.PRAVEEN KUMAR*, Vandana Arora
     M.Pharm (Pharmaceutics)
    Lloyd Institute of Management & Technology,
    Greater Noida,
    U.P., India

    * praveen_73a@yahoo.co.in

    ABSTRACT
    The solubility behaviour of drugs remains one of the most challenging aspects in formulation development. Currently only 8% of the new drug molecules have high solubility and permeability. The solubility behaviour of a drug is key determinant to its oral bioavailability and it is the rate limiting step to absorption of drugs from the gastrointestinal tract. This results in important products not reaching the market or not achieving their full potential. Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and bioavailability of a range of hydrophobic drugs. This article reviews the various preparation techniques for solid dispersion, types of solid dispersions based on molecular arrangement and other aspects such as selection of carriers and methods of characterization and their applications have been discussed.

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  • Anti-inflammatory activity oflic extract of R Methanooot of Cissampelos pareira on Carragenin induced rat paw edema

    About authors:
    Gourab Saha*1, Pankaja Senapati1, Narahari Sahu2, Dr. Sambit Parida3
    1. Department of Pharmaceutics, College of Pharmaceutical Sciences, Mohuda, Berhampur – 2, Orissa, India.
    2. Department of Pharmacology, College of Pharmaceutical Sciences, Mohuda, Berhampur – 2, Orissa, India.
    3. Department of Pharma analysis, College of Pharmaceutical Sciences, Mohuda, Berhampur–2, Orissa, India.

    *gourab.pharma2012@gmail.com

    Abstract
    This study investigated the anti-inflammatory activity of the methanolic extract of Cissampelos pareira (Abuta) in male albino rats after intramuscular administration. This was done using the carragenin-induced paw edema method. Methanolic extract of Cissampelos pareira showed significant anti-inflammatory activity similar to ibuprofen and indomethacin.

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