Development of a new single unit dosage form of propranolol HCl extended release non-effervescent floating matrix tablets: In vitro and in vivo evaluation.

The objective of the present investigation was to develop extended release non-effervescent floating matrix tablets of Propranolol Hydrochloride (PPH) to extend the gastric residence time (GRT) and prolong the drug release after oral administration. Different viscosity grades of Hydroxypropyl methylcellulose (HPMC) polymers such as HPMC K4M, HPMC K15M and HPMC K100M were used as drug release retardants. Glyceryl behinate (Compritol 888 ATO) and Glyceryl monosterate (Precirol ATO 5) were used as low density lipids in order to get the desired buoyancy over a prolonged period of time. The drug excipients compatibility study was carried out by using Differential Scanning Calorimetry (DSC). All the formulations were prepared by direct compression technique. The prepared tablets were evaluated for their physical characters, in vitro drug release and in vitro buoyancy. The release and floating property depends on the polymer type, polymer proportion, lipid type and lipid proportions. The drug release profiles of all the formulations were subjected to Zero order, First order, Higuchi and Peppas kinetic models, and the optimized formulation (F7) followed the Peppas model (R2= 0.987) with non-Fickian diffusion mechanism(n>0.5). The optimized formulation was subjected for in vivo radiographic studies in healthy human volunteers (n=3). These studies revealed a mean gastric residence time of 5±1.73 h (n=3).

Development of pioglitazone hydrochloride lipospheres by melt dispersion technique: Optimization and evaluation.

The objective of the present study was to develop and evaluate pioglitazone hydrochloride loaded lipospheres for treatment of diabetes. Pioglitazone hydrochloride lipospheres were formulated by using melt dispersion (homogenization) technique using compritol®888 ATO as lipid matrix and Phospholipon 90G (P 90G), PVA, Poloxamer 188 as surfactants. Formulation was optimized by using 32 full factorial design where entrapment efficiency and particle size were dependent variables and lipid and surfactant concentration were independent variables. Optimized formulation of pioglitazone hydrochloride (PLS 5) shows 79.69± 1.35% entrapment efficiency, 94.63± 2.10% drug content and particle size was found to be 23.74± 0.35μm with spherical shaped free flowing particles. In vitro release was carried out using dissolution apparatus in 0.1N HCl and optimized formulation shows 96.06 ± 0.54 % drug release within 8 hrs. which follows quasi-fickian type of transport and was characterized by the Korsmeyer- Peppas model. Formulation was stable at 5 oC ± 3 oC for two months. Developed liposphere formulation was able to sustain the drug release and entrap the pioglitazone hydrochloride drug at high level.