Sustained release drug delivery system

Abstract

The invention discloses a controlled release dosage form comprising a therapeutically effective amount of a pharmaceutically active agent, illustrated by Acyclovir, that would release in about 12 hours not more than about 90% of the said active agent in a simulated gastric juice in a first order rate of release in a USP type 1 dissolution test, and not containing a solubilizer or a swelling enhancer or both, comprising (a) a tablet made from polymer matrix of at least two biocompatible polymers, illustrated by Carbopol 974P and polyethylene oxide, the said pharmaceutically active agent and pharmaceutically permitted excipients; the said tablet capable of rapid swelling without disintegration in the said simulated gastric juice to a size that shall result in its gastric retention in the stomach and start controlled release of the said active agent by starting controlled erosion as well as diffusion immediately after coming into contact with the said gastric juice, or (b) microspheres of ungrafted chitosan or a chitosan derivative illustrated by thiolated chitosan and trimethyl chitosan, or Carbopol incorporating the said active agent, wherein the said pharmaceutically active agent is not a polymeric molecule and after administration in stomach, the said microspheres adhare to the gastric mucosa for a long time releasing the active agent in a controlled way.

Description

technical field [0001] The present invention describes a delayed / controlled drug delivery system that can improve drug bioavailability, using mucoadhesives, swelling polymers and their derivatives as carriers to achieve delayed / controlled drug delivery, especially for acyclovir and mucoadhesive swelling polymers like carbomer, PEO, sodium alginate, hypromellose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, acrylic resin (Eudragits), chitosan and Administration of its derivatives. Background technique [0002] Some drugs and macromolecules are poorly absorbed across the mucosa, or those that are sparingly / slowly soluble are caused by the fact that, for a limited time, they remain in the gastrointestinal tract, mostly not released or absorbed, most Excreted without absorption. One of the biggest challenges for scientists is the administration of such poorly bioavailable molecules, where only limited doses reach plasma over a given period of time. Low bioavailabi...

AI Technical Summary

Problems solved by technology

[0014] The in vivo studies described in the references cited above do not specify exactly how the drug works in the in vivo environment

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