Current Issue : July - September Volume : 2012 Issue Number : 3 Articles : 12 Articles
Orotransmucosal drug delivery is an alternative approach to the systemic and enteral drug delivery. It avoids presystemic elimination and gastric acid hydrolysis of drugs resulting in increase in the oral bioavailability. The permeability when compared through different oral mucosa, sublingual route is greater than buccal route and buccal route is greater than palatal. The permeability of buccal mucosa is 4-4000 times greater than that of skin. It provides rich blood supply for absorption. Mucoadhesion is an important phenomenon in which two material one of which is biological in nature are held together for extended period of time by interfacial forces. Adhesion is occurring due to presence of hydroxyl, carboxyl or amine group on the molecule. The mechanism of mucoadhesion is generally divided into two steps contact stage and consolidation stage. Low molecular weight, Non- ionised species, and lipid soluble substances are most easily diffusible material across the oral epithelium. Drug diffuses more efficiently across the oral mucosa if it having high pKa value. Sometime buccal drug delivery system has required permeation enhancer to overcome problem associated with drug absorption. The permeation enhancer should have reversible effect on the epithelium it should recover its barrier properties after the drug has been absorbed. This review explains the details on buccal mucosa, mucoadhesion theories and its mechanism, and evaluations for the buccal mucoadhesive tablets....
Corticosteroids were found to be most helpful to speed healing and relieve symptoms in the management of aphthous ulcers. For improved patient compliance a long lasting action and a targeted treatment are required. The aim of the present study was to design and evaluate triamcinolone acetonide controlled release mucoadhesive films for the topical treatment of aphthous ulcers. Radiation-induced crosslinked polyvinyl pyrrolidone hydrogel membranes as well as polyvinyl pyrrolidone/hydroxypropyl methylcellulose and polyvinyl pyrrolidone/sodium carboxymethylcellulose hydrogel copolymer blends were prepared. The films were evaluated before and after crosslinking for water uptake, bioadhesion, mechanical properties as well as in vitro drug release. In addition, the rheological characteristics of radiated and non-radiated polymer solutions were investigated. The obtained results revealed that, radiation with the subsequent formation of crosslinked hydrogels was accompanied by an obvious sustainment in drug release, change in the release mechanism from anomalous to Fickian, an apparent increase in swelling behavior of the hydrogel films as well as a great increase in viscosity of the polymeric solutions. In addition, the crosslinking of the polymer chains improved the tensile strength but reduced elasticity and mucoadhesive properties of the films. Furthermore, results showed that the introduction of hydroxypropyl methylcellulose and sodium carboxymethylcellulose to polyvinyl pyrrolidone membranes affected greatly the characteristics of both the crosslinked and uncrosslinked films. Polyvinyl pyrrolidone/hydroxypropyl methylcellulose hydrogels demonstrated the highest acceptability by the volunteers, easiest handling and greatest sustainment of drug release. This formula also relieved pain and produced complete healing of aphthous ulcers within 2-5 days....
The aim of the present study was to evaluate and compare the influence of accelerated-aging conditions on the drug content and in vitro dissolution stability of two different piroxicam non aqueous emulsions. Emulsions can be formulated without an aqueous phase to produce anhydrous, non-aqueous or oil-in-oil emulsions. Such systems, which can replace conventional emulsions where the presence of water is to be avoided, have been used for the preparation of nanoparticles or as templates in the formation of silicate microstructures. Dissolution efficiency (DE) was calculated from dissolution profiles that were performed according to the United State Pharmacopoeia monograph. This determination was performed at time zero, three and six months of storage; according to ICH accelerated-aging conditions (40°C/75% RH). Each formulation was compared with the reference at the specified times, using ANOVA in terms of DE and similarity factor f2. Furthermore, ANOVA for DE values was used to evaluate the effect of aging conditions on the dissolution stability within each formulation. Although the storage conditions examined in the study affected the dissolution behavior of all formulations, they did not have a significant effect on chemical stability, with the exception of one formulation that showed undesirable performance in both chemical and dissolution stability....
During last few years mucoadhesive dosage forms have promoted an area of drug delivery system that renders the treatment more effective and safe, not only for topical disorders but also for systemic problems. Bioadhesive formulations have a wide scope of application for both systemic and local effects of drugs. Timolol maleate is a non-selective beta-adrenergic blocker, and having short biological half-life, approximate 4.1 h, and low oral bioavailability.The aim of the present study was to design formulation and evaluate the mucoadhesive buccal patches containing the timolol maleate drug using the different ratios of hydrophilic polymers like carbopol 934P, PVA, PVP by using the solvent casting technique.The patches which were prepared by the solvent casting method, were smooth and elegant in appearance. prepared films were evaluated for weight, thickness, surface pH ,swelling index(SI), folding endurance, drug content uniformity, in vitro drug realese studies.Thermal analysis by DSC show no intreaction between drug and polymers. In vitro drug release studies were performed using USP apparatus-II at 50 rpm.A faster drug release rate was observed for patches prepared with the low concentration of PVPK30. It was also observed that patches prepared with high concentration of PVP K30 show highest swelling index and increasing concentration of PVA shows high tensile strength of mucoadhesive patches.kinetic study mainly revealed that the drug releases from the patches follow zero order kinetics....
Amlodipine besylate is a drug that is used for treating high blood pressure, certain types of angina, and coronary heart failure. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. The purpose of the present investigation was to increase the solubility and dissolution rate of amlodipine besylate by the preparation of its solid dispersion with polyethylene glycol 4000, polyethylene glycol 6000 & polyvinyl pyrrolidine k30 by using solvent evaporation method in the 1:1, 1:3 and 1:5 ratios of drug and carrier respectively. The prepared solid dispersions were characterized by IR spectroscopy & DSC suggested no interaction of drug with carriers. The solid dispersions were evaluated for physical appearance, % practical yield, drug entrapment efficiency, solubility & in-vitro dissolution. All the Solid Dispersions Prepared Were Found to be Fine Free Flowing Powder. The drug entrapment efficiency of the prepared Solid dispersions were in the range of 89.3% - 97% indicated that the drug is uniformly dispersed in the powder formulation. The solubility of amlodipine besylate was increased with increase in conc. of carrier for all the solid dispersions. Among the carriers used, PVP K-30 showed highest solubility in the range of 2.21 to 2.69 mg/ml. Dissolution rate of solid dispersion was determined in 0.01 N HCl at 75 rpm. At the end of 60 min, formulation F2 gave the highest drug release that is 95.02%. Kinetic study mainly revealed that the drug releases from the solid dispersions follow zero order kinetics....
The purpose of present investigation is to formulate and optimize the sustained release matrix tablet containing Trimetazidine dihydrochloride as a model drug. A 32 full factorial design were applied to carry out systematic studies. The concentration of HPMC K 100 (X1) and Eudragit RSPO (X2) were chosen as independent variables while percentage drug release at 2 hrs, 6 hrs and 12 hrs (Q2, Q6 and Q12) was taken as dependent variables. The dissolution profile of all nine factorial formulations was fitted to zero-order, first-order, Higuchi and Korsemeyer-Peppas models to ascertain the kinetic modeling of drug release. A response surface plot is presented to show the effects of X1 and X2 on % drug releases after 2 hrs, after 6 % and at the end of 12 hrs. The drug was released by diffusion of anomalous type. A model was validated for accurate prediction of drug release profile. Acceptable batches were identified in the experimental design with constraints on percentage drug released in 2, 6 and 12 hrs. From this study, it was observed that the concentration of HPMC K 100 and Eudragit RSPO have distinct effect on in-vitro drug release profile. The release rate of Trimetazidine dihydrochloride decreased proportionally with increased polymer concentration. Also the concentration of pH independent polymer Eudragit RSPO increases resulted decrease in initial burst release. The study helped in finding the optimum formulation with excellent sustained drug release....
The objective of this work was to develop piroxicam non aqueous emulsion and to understand the kinetics of drug release by applying mathematical and model-dependent approaches. Four formulations of non aqueous emulsions were prepared by the hand mixing method using PEG 200 and PEG 400 polar phases and olive oil, Liquid paraffin and MCT as a non polar phases. The in vitro drug release was studied in pH 7.2 Phosphate buffer using Franz diffusion cell. Zero-order, first-order, Higuchi, Hixson-Crowell, and Korsmeyer et al. models were used to estimate the kinetics of drug release. The criteria for selecting the most appropriate model were based on the goodness-of-fit test. Furthermore, experimentally, we assessed the in vitro transfer of the prepared piroxicam non aqueous emulsion for steady state flux and permeability coefficient through an artificial cellulose acetate membrane....
The goal of ionic cocrystals is to increase the number of crystal forms available for selection of the optimal crystal form for pharmaceutical applications and to enhance the drug aqueous solubility....
New innovation through research is becoming more and more expensive, mostly in case of pharmaceutical industries. If after investing lots on money and efforts, one cannot commercialize their invention due to unforeseen problems with third party patents, then it is a high loss. Thus to ease the commercialization of new research innovations, most innovative and research-driven companies have started outsourcing patent landscaping studies for their future research plans. Patent landscaping is the art of analyzing and communicating information about a patent technology space in or patent maps give the detailed overview of the merging of the different technologies to give rise to break-through technologies. A visual and informative way allowing for easy interpretation of trends and patterns. Patent landscapes patent landscape reveals past and present activities of various top and small players in a given broad-spectrum of technology. It includes the white space analysis, which results in identification of problematic and safest research areas. It can also give insight to new potential areas, where there is a possibility of improvement. It provides additional insights, including trends in the IP activity over the time and who and what the technological progress had been made during a defined period of time. The geographical distribution information the patent families, will reveals market trends over a time duration and results in forecasting future potential market....
Cellulose was modified by using 2-(Trifluromethyl) benzoylchloride by base catalyzed reaction. Modification of cellulose was confirmed by IR studies. The biodegradable composite films were developed by film casting method using modified cellulose with Polypyrrolidone in different compositions. Better barrier and mechanical properties showed by film composites as the percentage of modified cellulose increased. Film composites showed good biodegradability. This indicates the importance of modified cellulose as a reinforcing agent. After evaluating these properties of film composites we came to the conclusion that, these biocomposites can use to membrane and packaging applications....
Solubility is one of the most important parameter to achieve desired concentration of the drug in systemic circulation for pharmacological response to be shown. Poorly water soluble drug often require high dose in order to reach therapeutic plasma concentration after oral administration. To the aqueous solubility can help to increase the efficacy and reduce the side effects of the drug. For improving the oral bioavailability of the drug various technique are used. This review article thus begins with discussion regarding the traditional approaches to drug solubilization include solid dispersion, Complexation, and physical mixture....
Mesalamine pellets, prepared by an extrusion process and coated with varying concentrations of different pH independent polymers (Ethyl cellulose, Eudragit RLPO and Eudragit RSPO) either alone or in combination were compressed into tablets and their dissolution was compared with a reference product. Morphology of pellets and tablets were studied using SEM and solid state characterized using DSC. SEM studies showed that the coating was smooth and pellets after compression were not fragmented and DSC indicated lack of interaction. Drug release from tablets was inversely proportional to polymer concentration and predominantly followed diffusion kinetics. Composition containing 2% Ethyl cellulose and 3% Eudragit RSPO was able to modulate the release of drug to the desired extent....
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