Repaglinide has the half life of 1 hour, and bioavailability in the body is 56% due to first-pass metabolism. The total daily dose of Repaglinide is 16 mg (e.g., 4 mg four times daily depending on meal patterns); hence, it required frequent dosing. Transdermal patch of Repaglinide was prepared to sustain the release and improve bioavailability of drug and patient compliance. Different formulations were prepared by varying the grades of HPMC and concentration of PVP K30 by solvent casting method. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in vitro drug release, in vitro permeation, and drug excipient compatibility. A 32 full factorial design was applied to check the effect of varying the grades of HPMC (X 1) and PVP concentration (X 2) on the responses, that is, tensile strength, percentage drug released in 1 hr (Q 1), 9 hr (Q 9), and diffusion coefficient as a dependent variables. In vitro release data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. The results of the F2 statistics between factorial design batches and theoretical profile were used to select optimized batch. Batch F6 was considered optimum batch which contained HPMC K100 and PVP (1.5%), showed release 92.343% up to 12 hr, and was more similar to the theoretical predicted dissolution profile (f 2 = 69.187).

Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

The real challenge in the development of a controlled drug delivery system is not just to sustain the drug release but also to prolong the presence of the dosage form in the stomach or the upper small intestine until all the drug is completely released in the desired period of time (1-2). The residence of a drug delivery system in the upper part of the gastrointestinal tract (GIT) can be accomplished by several drug delivery systems, such as intragastric floating systems (3), swelling and expandable systems (4), bioadhesive systems (5), modified shape systems (6), high density systems (7), delayed gastric emptying systems (8) and low density super porous systems (9).Domperidone is a synthetic benzimidazole compound that acts as a dopamine D2 receptor antagonist. Domperidone is also used as a prokinetic agent for treatment of up- The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X 1 ), Carbopol 934P (X 2 ) and sodium alginate (X 3 ), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t 50 ) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties.

Nowadays, in situ gel forming systems are of great importance, having the combined advantage being patient convenient with favorable residence time for enhancing ocular bioavailability and for reducing systemic side effects (1, 2). The sol-gel transition can be induced by a shift in the pH (Carbomer) (3), temperature (poloxamer) or by the presence of deacetylated gellan gum cations (Gelrite) (4).Poloxamer is a triblock copolymer made of polyethylene oxide (PEO) and polypropylene oxide (PPO) units. Formation of highly ordered structures such as cubic crystalline phase and intramolecular hydrogen bonds might promote gelation (6). The mucomimetic property of poloxamers is proposed to be due to their hydrophobic and hydrophilic sequences simulating mucin action by adsorption of the aqueous layer of tears on the hydrophobic epithelium. This makes them suitable for use as a drug delivery system. The purpose of the study was to develop an optimized thermoreversible in situ gelling ophthalmic drug delivery system based on Pluronic F 127, containing moxifloxacin hydrochloride as a model drug. A 3 2 full factorial design was employed with two polymers: Pluronic F 68 and Gelrite as independent variables used in combination with Pluronic F 127. Gelation temperature, gel strength, bioadhesion force, viscosity and in vitro drug release after 1 and 10 h were selected as dependent variables. Pluronic F 68 loading with Pluronic F 127 was found to have a significant effect on gelation temperature of the formulation and to be of importance for gel formation at temperatures 33-36°C. Gelrite loading showed a positive effect on bioadhesion force and gel strength and was also found helpful in controling the release rate of the drug. The quadratic mathematical model developed is applicable to predicting formulations with desired gelation temperature, gel strength, bioadhesion force and drug release properties.Keywords: moxifloxacin, in situ gel, ophthalmic drug delivery, mucoadhesive polymers, 3 2 full factorial design * Correspondence; e-mail: divyeshshastri@gmail.com Unauthenticated Download Date | 5/8/18 7:32 AM Poloxamer 407 gives a colorless and transparent gel but requires higher concentration of about 25 to 30 % (m/V) to exhibit sol-gel phase transition at 37°C when used alone (7). Gelation temperature can be adjusted within the range of 33-36°C by modifying cross-linking agents (8), by mixing the different series of poloxamers (9), by changing the weight of poloxamers (10), or by changing the pH and ionic strength (11). However, studies have been focused on modulating only gelation temperatures of poloxamer solutions. There is lack of knowledge of the strength and bioadhesive force of gelled poloxamers.In the present study, an attempt was made to solve this problem by combining two poloxamers, i.e., Pluronic F 127 (PF 127) and Pluronic F 68 (PF 68), and developing a series of combinations with gelation temperature ranging from 30 to 36°C (12). They were found suitable for formulating an in situ gelling ophthalmic drug delivery ...

Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly water-soluble drug with absolute bioavailability of 26%. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate. Liquisolid compacts were prepared using Acrysol El 135 as a solvent, Avicel PH 102, Fujicalin and Neusilin as carrier materials, and Aerosil as coating material in different ratios. The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial limits. The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets. Amongst carriers used Fujicalin and Neusilin were found to be more effective carrier materials for liquid adsorption.