Current Issue : April - June Volume : 2018 Issue Number : 2 Articles : 6 Articles
Venlafaxine controlled drug delivery systems using different matrixes have been tested to\nreduce undesirable side effects in the treatment of depression. The legal status of chitosan (Cs) in\nPharmacy has dramatically improved after its acceptance as excipient in several Pharmacopeias\nand, therefore, there is great interest in pharmaceutical formulations based on this polymer.\nIn this paper, chitosan microcapsules cross-linked with sodium tripolyphosphate (TPP) for oral\ndelivery of venlafaxine were formulated using the spray drying technique. The effect of chitosan\nphysico-chemical properties, TPP concentration and TPP/Cs ratio on drug release was evaluated.\nThe microcapsules were characterized in terms of size, zeta potential and morphology. The physical\nstate of the drug was determined by X-ray diffraction (XRD) and the drug release from the\nmicrocapsules was studied in simulated gastric and intestinal fluids. The release pattern fitted\nwell to the Peppas-Koersmeyer model with n exponents indicating anomalous transport....
Aripiprazole is a new antipsychotic drug used in schizophrenia. It acts on serotonin 5-HT2A receptors. Drug undergoes extensive first pass metabolism. Oral dose was practically insoluble in water and sparingly soluble in 0.1 N HCl. In psychotic patients, unpredictable symptoms are observed any time mainly in schizophrenia, Parkinson’s disease and migraine. Thus, it requires immediate action to minimize the symptoms. Moreover, patients are also not in condition to take dosage form by themselves and have difficulty in swallowing. Gelucire 44/14 was used as a carrier for improving solubility of aripiprazole by melt granulation technique. Different ratio of drug to gelucire were tried and depending upon DSC, FTIR and solubility studies 1:2 ratio of aripiprazole to gelucire was considered as significant proportion. Optimized ratio was used to prepared oral dispersible tablet using calcium silicate (FM1000) as dispersing agent and orocell and MCC burst as novel diluent. Prepared tablets were evaluated for various parameters like disintegration, dissolution study, hardness, friability etc. optimized batch showed friability 0.4±0.04, hardness 3±0.2 kg/cm2, wetting time 28±3 sec and disintegration time 32±3 sec. Thus, optimized tablet was sufficiently capable of delivering rapid drug release of such practically insoluble drug using novel excipients....
This study was aimed at evaluating chitosan-microcrystalline cellulose blends as direct compression excipients. Crab shell chitosan,\n...
Purpose: Hydrophobic drugs are facing a major challenge in dissolution rate enhancement and\nsolubility in aqueous solutions; therefore, a variety of methods have been used to improve dissolution\nrate and/or solubility of bendroflumethiazide as a model hydrophobic drug. Methods: In this study,\ntwo main methods (physical mixing and lyophilisation) were used with gluconolactone, hydroxyl propyl\n�³-ccyclodextrin, and trehalose to explore this challenge. Bendroflumethiazide, practically insoluble\nin water, was mixed with one of the three excipients gluconolactone, hydroxyl propyl �³-cyclodextrin,\nand trehalose in three different ratios 1:1, 1:2, 1:5. To the best of our knowledge, the dissolution of the\ndrug has not been previously enhanced by using either these methods or any of the used excipients.\nSamples containing drug and each of the excipients were characterized via dissolution testing,\nFourier Transform infra-red spectroscopy, differential scanning calorimetry, and scanning electron\nmicroscopy. Results: The used methods showed a significant enhancement in dug dissolution\nrate; physical mixing significantly, p < 0.05, increased the percentage of the drug released with\ntime; for example, bendroflumethiazide dissolution in distilled water was improved from less than\n20% to 99.79% within 90 min for physically mixed drug-cyclodextrin 1:5. The lyophilisation process\nwas enhanced and the drug dissolution rate and the highest drug dissolution was achieved for\n(drug-gluconolactone 1:1) with 98.98% drug release within 90 min. Conclusions: the physical mixing\nand freeze drying processes significantly increased the percentage of drug release with time....
Nanoparticles or microparticles created by physical complexation between two\npolyelectrolytes may have a prospective use as an excipient for oral insulin administration. Natural\npolymers such as tragacanth, alginate, dextran, pullulan, hyaluronic acid, gelatin and chitosan\ncan be potential candidates for this purpose. In this research, insulin particles were prepared\nby the inclusion of insulin into a tragacanth hydrogel. The effect of the pH and concentration\nrelationship involving polyelectrolytes offering individual particle size and zeta potential was\nassessed by zetasizer and scanning electron microscopy (SEM). Insulinââ?¬â??tragacanth interactions\nat varying pH (3.7, 4.3, 4.6, or 6), and concentration (0.1%, 0.5%, or 1% w/w) were evaluated by\ndifferential scanning calorimetry (DSC) and ATR Fourier transform infrared (ATR-FTIR) analysis.\nIndividual and smaller particles, approximately 800 nm, were acquired at pH 4.6 with 0.5% of\ntragacanth. The acid gelation test indicated that insulin could be entrapped in the physical hydrogel of\ntragacanth. DSC thermograms of insulinââ?¬â??tragacanth showed shifts on the same unloaded tragacanth\npeaks and suggested polyelectrolyteââ?¬â??protein interactions at a pH close to 4.3ââ?¬â??4.6. FTIR spectra of\ntragacanthââ?¬â??insulin complexes exhibited amide absorption bands featuring in the protein spectra and\nrevealed the creation of a new chemical substance....
Present study deals with the study of okra mucilage as sustain release excipient in transdermal formulation. Mucilage was extracted using water based extraction method, the yield of mucilage was found to be 9.83 gm/kg. Characterization of the extracted mucilage was done by various parameters such as micromeritic studies, flow behaviour, solubility, pH and organoleptic properties. Various transdermal patches of itraconazole were prepared by solvent evaporation technique using different proportions of okra mucilage and glycerin as plasticizer and polyethylene glycol-400 as permeation enhancer. The compatibility studies between itraconazole and okra mucilage revealed that there were no negative interactions between itraconazole and okra mucilage. Formulated transdermal films were physically evaluated with regard to thickness, physical appearance, weight variation, drug content, folding endurance, percentage of moisture content and elongation break. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. The experimental results shows that the drug release from the patches delayed in controlled manner as the proportion of okra mucilage increased. The stability studies proved that the formulated patches were stable at stressed storage conditions. It was concluded that okra mucilage can be used as polymer for making transdermal patches....
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