Design, preparation, and evaluation of gastroretentive floating matrix tablet of mitiglinide.

The present research is focused on developing floating matrix tablets of mitiglinide to prolong its gastric residence time for better absorption. Gastroretentive tablets were prepared using a direct compression technique with hydroxypropyl methylcellulose K15M (HPMC K15M) and sodium alginate as matrix-forming polymers and sodium bicarbonate as the gas-forming agent. A 3 full factorial design was adopted to optimize the flotation and release profile of the drug.

Melt Dispersion Adsorbed onto Porous Carriers: An Effective Method to Enhance the Dissolution and Flow Properties of Raloxifene Hydrochloride.

The objective of the present investigation is to enhance the dissolution and flow properties of raloxifene hydrochloride (RXH), a biopharmaceutical classification system class II drug. Melt dispersion of RXH with polyethylene glycol (PEG) 6000 was prepared by the fusion method. The melt dispersion was then adsorbed onto a porous adsorbent, Neusilin, by the melt adsorption method.

Spray dried solid dispersion of repaglinide using hypromellose acetate succinate: and characterization.

Objective: This research study attempted to develop spray-dried solid dispersion, to enhance the solubility of repaglinide, an antidiabetic drug.

Significance: Aqueous solubility plays a major role in drug delivery because any chemical entity has to be in a dissolved state at the site of absorption, in order to get absorbed. Solid dispersion (SD) is one of the widely used techniques to enhance solubility and hence dissolution rate of poorly soluble drugs.

Solid dispersion adsorbate technique for improved dissolution and flow properties of lurasidone hydrochloride: characterization using 3 factorial design.

The aim of the present study was to improve the dissolution and flow properties of lurasidone hydrochloride (LH) by solid dispersion adsorbate (SDA) technique. Solid dispersions (SDs) of LH were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate).

Liquisolid Tablets for Dissolution Enhancement of a Hypolipidemic Drug.

This investigation was aimed to improve the dissolution rate of the poorly soluble drug lovastatin, by formulating it as a liquisolid compact. Different liquisolid compacts were prepared using mathematical formulae to calculate the required quantities of powder and liquid ingredients to produce acceptably flowable and compressible admixture. Avicel PH 200, Cab-O-Sil, sodium starch glycolate and PEG 400 were employed as carrier, coating material, disintegrant and non-volatile liquid vehicle, respectively.

Preparation and optimization of microemulsion of rosuvastatin calcium.

Due to very less bioavailability (20%) of Rosuvastatin calcium, an attempt was made to develop and optimize microemulsion formulation. Capmul MCM, Tween 20 and PEG 400 were selected as oil, surfactant and cosurfactant respectively as the drug is having higher solubility in them. 3:1% w/w S:CoS was selected as it gave higher microemulsion area.

Chronopharmaceutics based modern colon specific drug delivery systems.

Colon-targeted delivery of bioactives has recently gained importance in addressing specific needs in the therapy of colon based diseases. Many approaches have been attempted for the development of colon-specific delivery systems, with not much success in the past. With the advancement in the field of chronobiology, modern drug delivery approaches have elevated to a new concept of chronopharmacology i.

Development of microemulsion for solubility enhancement of clopidogrel.

Clopidogrel, an inhibitor of platelet aggregation, selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation. Oral bioavailability of clopidogrel is very low (less than 50%), due to its poor water solubility. The aim of this investigation was to design and develop a microemulsion formulation of clopidogrel for enhancing its solubility, and hence its oral bioavailability.

Intracellular delivery of nanoparticles of an antiasthmatic drug.

The aim of the investigation was to prepare and characterize wheat germ agglutinin(WGA)-conjugated poly(D: ,L-lactic-co-glycolic) acid nanoparticles encapsulating mometasone furoate (MF) as a model drug and assess changes in its fate in terms of cellular interactions. MF loaded nanoparticles were prepared using emulsion-solvent evaporation technique. WGA-conjugation was done by carbodiimide coupling method.

Wheat germ agglutinin-conjugated nanoparticles for sustained cellular and lung delivery of budesonide.

The purpose of our studies was to assess in vitro nanoparticles cellular uptake and cellular budesonide levels after treatment of alveolar epithelial cell lines with wheat germ agglutinin (WGA)-conjugated budesonide nanoparticles and pharmacokinetic evaluation of drug after intratracheal instillation of nanoparticles in rats. Confocal microscopy was used to study the cellular uptake of nanoparticles, and the cellular and lung tissue drug levels were estimated by HPLC. Higher amount of fluorescence observed in the cells treated with WGA nanoparticles, higher and sustained cellular drug levels, and better bioavailability in lungs of WGA-conjugated nanoparticles indicate superiority of WGA-conjugated nanoparticles over unconjugated nanoparticles.