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INFLUENCE OF STABILIZERS IN MELOXICAM NANOCRYSTAL FORMATION AND ITS APPLICATION ON SUSPENSION ORAL DOSAGE FORM
Get PDFMeloxicam is a non steroid anti inflammatory drug that is classified as Biopharmaceutics Classification System (BCS) class II. Meloxicam is poorly soluble in water, therefore its solubility would be the rate limiting step for drug absorption. This study was conducted to improve meloxicam solubility using nanotechnology approach. Meloxicam nanocrystal was prepared using high pressure homogenization technique. Several stabilizers were investigated for suitable nanocrystal production. Formulation of suspension on the meloxicam nanocrystal was developed. Short physical stability was performed to assess the potential use of the stabilizer. Nanocrystal containing 10% meloxicam and 5% PVP K25 was formed faster with better physical stability compared to other stabilizers (xanthan gum, HPMC 2910 type 603 dan 645). Meloxicam nanocyrstal suspension containing meloxicam nanocrystal with stabilizer 5% or 10% of PVP K25 showed excellent particle size stability (with particle size 466.6nm and 486.9nm) and dissolution rate compared to reference product (without nanonization). Particle size and dissolution rate of meloxicam nanocrystal suspensions (containing 5% or 10% of PVP K25) were stable after storage for 30 days at room temperature. Kinetic solubility of meloxicam nanocrystal was three times higher than that of meloxicam. According to XRD profile, there was no differences in crystallinity between meloxicam and meloxicam nanocrystal.Key words: meloxicam, high pressure homogenizer, nanocrystal,dissolution rate, kinetic solubilit
FORMULATION AND EVALUATION OF BILAYER SUSTAINED RELEASE TABLET OF ZOLPIDEM TARTRATE
Get PDFThe purpose of the present study was to develop a bilayer tablet of zolpidem tartrate (ZT) using sodium starch glycolate (SSG) as superdisintegrant in the immediate release (IR) layer and hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC K4M), metalose 90 SH 4000, carbapol 974 PNF in sustained release (SR) layer. Both the IR and SR granules of ZT were evaluated for bulk density, tapped density, angle of repose, Carr’s index, Hausner ratio and loss on drying. All the values were found to be satisfactoy. The prepared bilayer tablets were evaluated for weight variation, hardness, friability, drug content, in vitro drug release, FT-IR studies, similarity factor and stability studies. In vitro dissolution studies were carried out in a USP dissolution apparatus I using 500mL of 0.01N HCl as dissolution medium. The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 4 h. The data obtained were fitted to Zero order, First order, Higuchi’s model and Korsmeyer-Peppas equations. The release exponent (n) values for all the formulations were less than 0.45 indicating Fickian diffusion was the drug release mechanism. FT-IR studies indicated that there are no drug-excipient interactions. The similarity factor (f2) was calculated by comparing dissolution data of all the formulations with that of marketed bilayer tablet of ZT (Ambien CR). The f2 value was highest (70) for the formulation SF8 and was selected as promising formulation among all the developed formulations. The stability study was performed on the formulation SF8 at 25oC/60% RH, 30oC/75% RH and 40oC/75% RH (accelerated condition) for 3 months. The results indicated that there were no significant changes in aforesaid tablet properties.Key words: bilayer tablets, zolpidem tartrate, sustained release, higuchi’s equation, similarity facto
SYNTHESIS AND ANTIMICROBIAL ACTIVITY EVALUATION OF SOME SCHIFF BASES DERIVED FROM 2-AMINOTHIAZOLE DERIVATIVES
Get PDFVarious substituted acetophenones (1-5) on treatment with iodine and thiourea yielded 2-amino-4-(substituted-phenyl)-thiazole (1a-5a), which on further treatment with various substituted aldehydes to get N-(substitutedbenzylidene)-4-(substitutedphenyl) thiazol-2-amine (1b-5b). All the synthesized compounds were characterized by their respective FTIR, 1H NMR and mass data. Synthesized compounds (1b-5b) were subjected to investigation for their antibacterial and antifungal studies against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Asperigillus flavus and Asperigillus fumigatus by disk diffusion method. Compound 5b was found to be most effective with largest zone of inhibition.Key words: thiazole, acetophenones, antibacterial, antifungal, substituted aldehydes
A REVIEW ON SUPRAMOLECULAR CHEMISTRY IN DRUG DESIGN AND FORMULATION RESEARCH
Get PDFSupramolecular chemistry, other way called as intermolecular chemistry disclose the relationship of molecules with environment. It exploits while exposing the physicochemical phenomina that happens when two like or unlike molecules/ions/systems contact each other. Drug action involve the target recognition process and response triggered by the intermolecular complex of drug and target. Drug design therefore require in depth study of intermolecular forces that exist between drug and target. Formulation of the drug or Active Pharmaceutical Ingredient (API) is also regulated by these forces. Compatibility and incompatibility in formulations are nothing but of the effect of the intermolecular forces on physical behavior of systems. Therefore review of intermolecular chemistry in general and its role particularly in pharmaceutical research is presented here for the benefit of the students and research scholars who aspire to work on interdisciplinary projects in the field of pharmacy. Key words: intermolecular forces, hydrogen bond, drug design, active pharmaceutical ingredient (API), crystal
STUDY OF ANALGESIC AND ANTIDIARRHOEAL ACTIVITIES OF Sonneratia caseolaris (LINN.) LEAF AND STEM USING DIFFERENT SOLVENT SYSTEM.
Get PDFThe different fractions of crude ethanol extract of leaf and stem of S. caseolaris (Linn.) (Sonneratiaceae) were screened for its analgesic and antidiarrhoeal activities. The different fraction of crude extract was obtained by using four different solvent systems. The different fractions of crude extract produced significant writhing inhibition in acetic acid induced writhing in mice at dose of 250 and 500mg/kg BW comparable to the standard drug diclofenac sodium at the dose of 25mg/kg BW. When tested for its antidiarrhoeal effects on castor oil induced diarrhea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the dose of 250 and 500mg/kg BW comparable to the standard drug loperamide at the dose of 50mg/kg BW. The overall results tend to suggest the analgesic and antidiarrhoeal activities of the different fractions of crude extract. Both ethyl acetate fraction of stem and chloroform fraction of leaf have significant analgesic activity. Again between the two fractions of crude ethanol extract ethyl acetate fraction of S.caseolaris stem have most significant antidiarrhoeal activity.Key words: analgesic, antidiarrhoeal, S.caseolaris, diclofenac sodium, loperamide
CRYSTAL FORMS OF LOMEFLOXACIN: PREPARATION, CHARACTERIZATION AND DISSOLUTION PROFILE
Get PDFThe present work was undertaken with the synthesis of crystal forms of Lomefloxacin from solvents of varying polarity (polar, protic solvents). The purpose of the present investigation was to employ crystallization techniques in order to improve the solubility and dissolution studies of Lomefloxacin. The experimental methods involved the preparation of lomefloxacin crystals by crystallization from single solvent technique. Crystals were prepared from solvents like distilled water, ethanol and methanol. Prepared crystals were undergone various studies in terms of crystal yield, melting point, true density, solubility and in vitro drug release study as well as characterized by technique viz: FT-IR, differential scanning calorimetry (DSC) and Powder X-ray Diffractometry(PXRD). Photomicrographs of the crystals shows that the crystals obtained from different solvents existed in different shape. Among all the crystals, LOME-I belongs to Type-1 and LOME–II belongs to Type-2 based on instrumental techniques. Highest crystal yield (88%) and maximum density (1.2021g/mL) was observed with LOME-I. Maximum solubility and dissolution rate was observed in LOME-III followed by LOME-II and LOME-I. However all prepared crystal forms showed higher solubility and dissolution profile when compare with commercial Lomefloxacin. It is concluded that the study has indicated the existence of two polymorphic forms of Lomefloxacin which was having better solubility and in vitro release than that of commercial Lomefloxacin.Key words: Polymorphism, Solubility, Dissolution rate, DSC, FT-IR, PXR
EFFECT OF WATER MELON SEEDS EXTRACTS (Citrullus vulgaris) ON SPERMS IN DIABETIC RAT.
Get PDFCitrullus vulgaris is an antioxidant and has been shown to reduce oxidative stress. Previous studies confirmed that antioxidants have essential effect on infertility through participating in reactive oxygen’s species. Chronic hyperglycemia is known to cause infertility in diabetes disease. Wistar male rats (n=40) were allocated into three groups: control group(n=10), Citrullus vulgaris seeds extract (CVE) group that received 55mg/kg by gavage method (n=10), and Diabetic group that received 55mg/kg (IP) streptozotocin (STZ) (n=20). The last group was subdivided into two groups of 10. STZ group and treatment group. Treatment group received 55mg/kg (IP) STZ plus 55mg/kg CVE, daily for 4weeks; however, the control group just received an equal volume of (0.9% NaCl) daily (gavage). Diabetes was induced by a single (IP) injection of streptozotocin (55mg/kg). Animals were kept in standard condition. In 28th day, 5cc bloodn sample was taken from every rat for biochemical analysis. Collecting epididymis tissues, they were prepared for sperm analysis by WHO method. In comparison to other groups, sperm parameters were significantly increased in groups that received 55mg/kg (CVE) (
POLYMERIC MICELLES: POTENTIAL DRUG DELIVERY DEVICES
Get PDFPolymeric micelles (PMs) have been the most popular and promising topic of many researches in the field of drug delivery and targeting for the past two decades. Polymeric micelles are the selfassembled nano-sized colloidal particles which are made up of amphiphilic block copolymers i.e. polymers consisting of hydrophobic block and hydrophilic block. In this highlight, we give an overview of the structure of micelles and polymeric micelles followed by a summary of the methods used for their preparation. We then focus on several kinds of PMs based on intermolecular forces such as polyion complex micelles (PICMs), non-covalently connected micelles (NCCMs) and recently developed smart polymeric assemblies which can respond to the application of external stimuli such as a change in temperature, pH, redox and light to afford novel nanomaterials. The types of polymers used in the preparation of PMs have also been highlighted so as to facilitate its use in drug delivery and targeting. These polymeric micelles nanocarriers have applications in drug delivery primarily such as anticancer therapy, to the brain to treat neurodegenerative diseases, antifungal agents, stimuli-responsive nanocarriers for drug and gene delivery, ocular drug delivery. Targeted drugs will hopefully reduce adverse reactions by limiting their action to cancer tissue only. Finally, this review broadly presents the basic aspects of PMs which help in delivery and targeting of actives with its recent advancements and applications.Key words: micelles, polymeric micelles, block copolymer, stimuli sensitivit
ANTIHEPATOTOXIC ACTIVITY OF TWO NEW QUERCETIN DERIVATIVES IN CARBON TETRACHLORIDE INDUCED HEPATOXICITY IN RATS
Get PDFQuercetin, a bioflavonol is widely found in nature and possesses diverse pharmacological properties. A heterocyclic 1,4 dioxane nucleus was incorporated in Quercetin structure to obtain two structural analogues of silybin. The aim of the study was to antihepatotoxic potential of Quercetin derivatives containing 1,4 dioxane heterocyclic ring in Carbon tetrachloride (CCl4) induced hepatotoxicity in female Wistar Albino rats. Two Quercetin derivatives (QD) were synthesized by reported method. QD were administered orally at dose of 10 mg/kg, once daily for 7 days to Wistar Albino rats. A single dose of CCl4(1mL/kg) was used for inducing liver damage. Antihepatotoxic activity was evaluated by measuring levels of total proteins (TP), total albumin (TA), alkaline phosphatase (ALKP) and liver enzymes such as serum glutamate oxaloacetate (SGOT) and serum glutamate pyruvate transaminase (SGPT).QD exhibited potent antihepatotoxic activity with respect to standard drug silybon-70. However, it was observed that the Quercetin derivative having –CH2OH group in the dioxane ring exhibited better activity in comparision to unsubstituted 1,4 dixoane ring derivative.The exact mechanism by which QD protects the liver is unknown however the observed effects could be attributed to presence of 1,4 dioxane ring and due to the significant antioxidant activity of Quercetin flavone. Key words: Antihepatotoxic activity, Quercetin; Silymarin, 1,4 dioxanering, CCl
Formulation of nanoparticles from short chain chitosan as gene delivery system and transfection against T47D cell line
Get PDFRecently numerous prototype DNA-based biopharmaceuticals can be used to control disease progression by induction and inhibitin the overexpression of genes. Since there are poor cellular uptake and rapid in vivo degradation of DNA-based therapeutics therefore the use of delivery systems to facilitate cellular internalization and preserve their activity is necessary. Cationic polymers commonly used as carriers to delivery gene because of easy to form complexes and higher stability compared to that lipoplexs. Chitosan, a cationic, are polymer most widely used in gene delivery systems because of the low toxicity, and biocompatible. The aim of this study was to formulate nanoparticles of short chain chitosan-pEGFP-C1 and short chain chitosan/TPP-pEGFP-C1 by coaservation complex method. Stability test of the formula was performed by incubating the nanoparticles complex with DNase I and Artificial Intestinal Fluid. Cytotoxicity and transfection studies were evaluated against T47D cell line. The diameter of Chitosan-pEGFP-C1 and chitosan/TPP-pEGFP-C1 nanoparticles were on the range of 56–282.8 nm. The zeta potential wasdetermined to be +14.03 - +16.6 mV. Stability studies showed that chitosan-pEGFP-C1 and chitosan/TPPpEGFP-C1 nanoparticles were stable, undegradable by DNase I and artificial intestinal fluid. Cytotoxic Assay of Chitosan-pEGFP-C1 and chitosan/TPP-pEGFPC1 nanoparticles (pH 4.0) showed that the viability of cell was > 90% for all formulas. EGFP-C1 plasmid gene delivered by chitosan nanoparticles can be expressed in T47D cell culture. According to these results chitosan and chitosan/TPP nanoparticles had potentially to be used as a non-viral vector system delivery for gene therapy.Key words:Chitosan, Nanoparticles, Plasmid EGFP-C1, Cell culture T47D