Abstract
ABSTRACT 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 h (n=3). Key words: Propranolol HCl, Compritol 888 ATO, Precirol ATO 5, Non-effervescent, Floating drug delivery system and Gastric residence time.
Highlights
The oral route remains the preferred route for the administration of therapeutic agents because of the low cost of therapy and ease of administration leading to high levels of patient compliance
Different viscosity grades of Hydroxypropyl methylcellulose (HPMC) polymers such as HPMC K4M, HPMC K15M and HPMC K100M were used as drug release retardants
Drugs having site-specific absorption are difficult to design as oral Controlled-release drug delivery systems (CRDDS) because only the drug released in the region preceding and in close vicinity to the absorption window is available for absorption (Drewe et al, 1992)
Summary
The oral route remains the preferred route for the administration of therapeutic agents because of the low cost of therapy and ease of administration leading to high levels of patient compliance. Conventional oral dosage forms provide a specific drug concentration in systemic circulation without offering any control over drug delivery. An important requisite for the successful performance of oral CRDDS is that the drug should have good absorption throughout. Such drugs are said to have an absorption window. After crossing the absorption window, the released drug goes to waste with negligible or no absorption. This phenomenon drastically decreases the time available for drug absorption after its release and jeopardizes the success of the delivery system
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