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CONTROLLED RELEASE OF GABAPENTIN THROUGH RETICULATED CHITOSAN AND HYDROXYETHYL CELLULOSE HYDROGEL MATRIX TABLETS
Get PDFThe aim of the present work was to prepare hydrogel matrix tablets using crosslinked chitosan and hydroxyethyl cellulose (HEC) for controlled release of gabapentin. The chitosan was crosslinked with acetaldehyde and used for the preparation of hydrogel matrix tablets along with hydroxylethyl cellulose by wet granulation method. The samples were characterized by FTIR, DSC, TGA, XRD, SEM and evaluated drug content, swelling pattern and drug release. The matrix tablets were capable of releasing the drug for 24h depending upon the formulation variables. It was observed that as the concentration of HEC increased in the tablets, the drug release was also increased. On the other hand, as the crosslinking of chitosan was increased, the drug release was decreased. Drug release mechanism followed non-Fickian transport. This study demonstrated that the blend hydrogel matrix tablets of crosslinked chitosan and HEC could be a versatile drug delivery system for controlled release of gabapentin
ISOLATION OF SULPHATE POLYGALACTAN FROM Eucheuma alvarezii Doty AND ITS ANTICOAGULANT ACTIVITY
Get PDFA sulphate polygalactan carrageenan was isolated from Euchema alvarezii Doty with yield 54.36%. The sulphate polygalactan was fractionated with KCl (aq) 2.5% result of a sulphate polygalactan of soluble fraction with the yield 60.34% and a sulphate polygalactanof insoluble fraction with the yield 34.53%. Based on the properties and supported by IR spectrum, the sulphate polygalactan of soluble fraction is k-carrageenan, whilethe sulphate polygalactan of insoluble fraction is l-carrageenan. Anticoagulant activitiy of the carrageenans were based on their prolongation effects on Activated Partial Thromboplastine Time (APTT) and Prothrombine Time (PT) of sodium citrate. On the assays, the carrageenans exhibited promising anticoagulant activities.Key words: Eucheumaalvarezii Doty, k-carrageenan, l-carrageenan, anticoagulant activity, APTT and P
OPTIMIZATION AND IN VIVO EVALUATION OF MESALAMINE pH DEPENDENT COATED PELLETS FOR PROMISING ILEOCECAL TARGETING
Get PDFThe present research is a challenge to design, optimized and evaluates mesalamine loaded burst release pH dependent coated pellets for possible ileo-cecal targeting to treat effectively Crohn’s disease. The novelty of this formulation is to release drug specifically and instantly in ileo-cecal region where the chances of Crohn’s disease is more frequent, without being released in upper gastrointestinal tract. Preliminary experimental batches are studied for micromeritic properties and in-vitro drug release. Formulation showed desirable lag time of 5h and dissolution profile were further optimized by applying 32 full factorial design to study the effect of extent of coating (% w/w) Eudragit S100 and croscarmellose sodium over drug layered pellets. The regression equation generated for Q300 (lag time of 5h) = +5.72-31.97*A+0.82*B-0.49*A*B+26.36*A2-0.15*B2 and for Q390 (90% of drug release at pH7.2 within 90 minutes after lag time) = +84.63- 40.09*A+4.62*B. The drug release data of optimized formulation were close to that predicted by the model. Various kinetic models were applied to the all optimized batches. In vivo evaluation of optimized formulations was performed to assess macroscopic, microscopic and biochemical parameters in rats and performed. The present study demonstrates that the mesalamine enteric coated pellets successfully targeted at ileo-cecal region.Key words: Mesalamine, pulsatile, ileo-cecal targeting, celpheres, Croscarmellose sodium, eudragit S10
IN VITRO ABSORPTION STUDY OF CARBAMAZEPINE SOLID DISPERSION USING EVERTED GUT SAC METHOD
Get PDFThe oral Bioavailability of BCS (Bio Pharmaceutical Classification System) class II drug with poor solubility and reasonable permeability is limited by drug dissolution. In order to improve the aqueous solubility of the drug and dissolution of thedrug, the solid dispersion was prepared and evaluated for its absorption in intestine using modified everted gut sac method. The solid dispersion of carbamezepine (CBZ) was prepared using polaxomer and guargum by kneading method. The CBZ and CBZSD (Solid Disposisi) shows 2.329% and 3.948% drug absorption, respectively. The data show that solid dispersion increase the absorption of the CBZ in CBZ-SD is more than 70% in comparison to pure CBZ. The increase in CBZ solubility of the SD could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction. Key words: Everted gut sac method, solid dispersion, absorption, solubilit
THE EVALUATION OF SINGLET OXYGEN QUENCHING AND SUNSCREEN ACTIVITY OF CORN COB EXTRACT
Get PDFThe corn cob waste has been reported to have antioxidant activity. Active compound such as antioxidant has been considered as potential sunscreen resources. The objectives of this research were to determine singlet oxygen quenching and sunscreen activity of corn cob. Corn cob was extracted using ethanol 20, 40, 60 and 80% by reflux for 2h at 78oC. The singlet oxygen quenching activity was evaluated by photooxidation of linoleic acid. Singlet oxygen quenching activity was conducted using linoleic acid as substrate containing erythrosine as a sensitizer and exposed under continuous illumination (4000 lux) with the fluorescent light for up to 5h. The sunscreen activity was evaluated by sun protection factor (SPF) using spectrophotometry UV-Vis. Ethanol extract 80% (E80) shows the highest total phenolic content followed with E60, E40 and E20. The result shows that the lowest singlet oxygen quenching activity was E20 (15.63%), and the highest was E80 by 65.63% percentage of inhibition. SPF value of E20, E40, E60, and E80 at concentration 200μg/mL were 7.52; 12.24; 15.81 and 17.78, respectively. SPF value increase with the increasing of concentration, total phenolic content and singlet oxygen quenching activity. The conclusion of this research was corn cob extract possess phytochemical compound having potency as singlet oxygen quencher and sunscreen active compound.Keywords: corn cob, phenolic phytochemical, singlet oxygen quenching, sunscreen
FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLET OF DOMPERIDONE MALEATE
Get PDFThe objective of the present study was to develop and evaluate mucoadhesive dosage form of Domperidone maleate. It is an antiemetic synthetic benzimidazole compound that acts as a dopamine D2 receptor antagonist. Mucoadhesive Domperidone maleate tablet formulation was prepared by direct compression method. The formulation F3 containing (Carbopol 940 + sodium alginate) was found to be best among all the formulation batches because of its consistent release rate for 7 h and extent of drug release was 94.44%. Graphical treatment of the formulation F3 to Higuchi’s equation showed that the drug release was diffusion mediated. In-vitro permeability study for formulation F3 for 7 h had shown 76.69% drug release. FTIR studies showed no evidence on interaction between drug and polymers. Key words: Domperidone maleate, Mucoadhesive tablet, antiemeti
EVALUATION OF ANTIMICROBIAL POTENTIALS OF Cardiospermum halicacabum Linn.
Get PDFAntimicrobial activity of Cardiospermum halicacabum shoot extracts were studied on gram-positive bacteria such as Staphylococcus aureus, Bacillus substilis, and gram-negative bacteria such as E.coli, Proteus vulgaris, and fungus Candida albicans. Disc diffusion method was used to study the antimicrobial activity of aqueous, ethanol, chloroform and ether extracts of C. halicacabum. Ampicillin was used as reference standard at 10 mg/disc concentration. Extracts of C. halicacabum exhibited a significant antibacterial activity except the aqueous extract. Ethanolic extract was found to be very effective with maximum activity index (0.84). The ethanolic extract exhibited minimum inhibitory concentration (MIC of 0.25 mg/mL against Staphylococcus aureus, Bacillus substilis, E. coli and Proteus vulgaris and 0.125 mg/mL against Candida albicans. The MIC of chloroform and ether extracts ranged between 0.25 and 1.0 mg/ml against the test organisms. All the extracts showed antifungal activity against Candida albicans. Key words: antimicrobial activity, Cardiospermum halicacabum shoot system, solvent extraction,
SUPER POROUS HYDROGELS: A RECENT ADVANCEMENT IN GASTRORETENTIVE DRUG DELIVERY SYSTEM
Get PDFSuper porous hydrogels (SPHs) were originally developed as a controlled drug delivery system to retain drugs in gastic medium. Super porous hydrogels (SPHs) are recent advancement in gastro retentive drug delivery system (GRDDS) which also includes intragastric floating system (low density system), mucoadhesive system, high density system and swellable system. Super porous hydrogels should instantly swell in the stomach and maintain their integrity in the harsh environment and release the pharmaceutical active ingredient. SPH swell fast, within minutes, the fast swelling property is based on water absorption through open porous structure by capillary force. This review discusses about the GRDDS, difference between gels and hydrogels and comparison between SAP vs. SPH. It also includes types of SPH, different generations, general synthesis, methods of preparations, gastric emptying, advantages, characterization, applications and salient features of SPH. Key words: Superabsorbent polymers (SAP), Super porous hydrogel (SPH), Gastro retentive drug delivery syste
IN–VITRO PHARMACEUTICAL EVALUATION OF TWO BRANDS OF DISPERSIBLE ACETYL SALICYLIC ACID TABLETS AVAILABLE IN OMAN
Get PDFAcetyl salicylic acid (ASA), a non-steroidal anti-inflammatory drug (NSAID) is widely used for its analgesic, antipyretic, antiinflammatory and anti-thrombotic action. The aim of the present study was to investigate the pharmaceutical equivalence of two brands of dispersible ASA tablets marketed in Oman. Two different brands of dispersible ASA tablets (300mg) were purchased from the retail pharmacy outlets and their pharmaceutical quality were assessed by using in-vitro tests as per the British Pharmacopoeia (BP) and unofficial standards as recommended by the manufacturers. The assessment of tablets included the evaluation of uniformity of weight and diameter, friability, crushing strength, disintegration and chemical assay by volumetric titration and colorimetric methods to determine the content of active pharmaceutical ingredient (API). Both brands of the ASA tablets passed the BP standards for uniformity of weight and diameter, disintegration, friability and crushing strength. However one of the two brands did not comply with the standard assay of content of active ingredient. Thus based on these results it can be concluded that these two brands of ASA are not pharmaceutically equivalent.Key words: ASA tablets, pharmaceutical equivalence, disintegration, volumetric method
ANTIMICROBIAL METABOLITES FROM A MARINE-DERIVED FUNGUS
Get PDFA marine fungus was separated from the surface of a marine red algae. Ethyl acetate extract of the cultivated marine fungus inhibited the growth of the pathogenic bacteria E.coli and S.aureus, and the phytopathogenic fungus C. cucurbitarum. Separation of the EtOAc extract gave four compounds, which were identified as new anthraquinonederivatives 3 and 4, and the known chrysophanol (1) and rubelin A (2) by the extensive analysis of NMR data. Compounds 1-4 inhibited the growth of the gram negative bacteria E. coli and gram positive bacteria S. aureus. Compound 3 also inhibited the fungus C. cucurbitarum.Key words: marine-derived fungus, structure elucidation, anthraquinone, antimicrobial activit