US 2002/0119195 A1 · Rapidly disintegrating sustained release cefuroxime axetil composition

Abstract

A fast disintegrating controlled release oral composition comprising a core material containing cefuroxime axetil present as controlled release form, the cefuroxime axetil being provided with an outer coating of a copolymer selected from aqueous dispersions of enteric methacrylic acid and methacrylic acid esters anionic copolymers having carboxyl group as the functional group or mixtures thereof and an inner coating of a sustained-release copolymer selected from aqueous dispersions of acrylate and methacrylate pH independent copolymers having quaternary ammonium group as a functional group or mixtures thereof, and optionally probenecid. Additionally, the coating composition may contain plasticizers. The composition is suitable for once daily administration.

Claims47

Dependent claims

A fast disintegrating controlled release oral composition comprising a core material containing cefuroxime axetil present as controlled release form, and optionally probenecid, said controlled release form comprising:

a) an outer coating of a copolymer selected from aqueous dispersions of enteric methacrylic acid and methacrylic acid esters anionic copolymers having carboxyl group as the functional group or mixtures thereof and;
b) an inner coating of a sustained-release copolymer selected from aqueous dispersions of acrylate and methacrylate pH independent, neutral copolymers having quaternary ammonium group as a functional group or mixtures thereof.

A process for preparing a fast disintegrating controlled release oral composition containing cefuroxime axetil as controlled release form, which comprises spraying onto a fluidized bed of cefuroxime axetil core material an aqueous dispersion of an inner polymeric coating, retrieving and drying the coated core material and applying to a fluidized bed of the dried material an aqueous dispersion of an outer polymeric coating material and drying the coated particles wherein the inner polymeric coating is a mixture of a first copolymer, poly(ethylacrylate, methylmethacrylate, trimethylammonioethyl methacrylate chloride) with a molar ratio of 1:2:0.2 and a molecular weight of 150,000 and a second copolymer, a poly(ethylacrylate, methylmethacrylate, trimethylammonioethyl methacrylate chloride) with a molar ratio of 1:2:0.1 and a molecular weight of 150,000;

and the outer polymeric coating is a poly(ethylacrylate, methacrylic acid) with a molar ratio of 1:1 and average molecular weight around 250,000, wherein the first copolymer of inner coating is present in amount of about 1% to about 8%, the second copolymer of inner coating is present in amount of about 0.1% to about 5% and outer coating is present in amount of about 2% to about 10% by weight of controlled release form, respectively.

Dependencies are inferred from the claim text.

Facts

Application

09/928,466Filed 13 Aug 2001

Priority

30 Oct 2000

Published

29 Aug 2002

Term ends

Not estimatedThe source records don’t support an estimate.

Classification5 codes

A61K 9/5026
Organic macromolecular compounds: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, polyacrylates
A61K 9/2077
Characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets;…: tablets…
A61K 9/2081
Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets: with microcapsules or…
A61K 9/5073
Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated…:…

Rapidly disintegrating sustained release cefuroxime axetil composition

Life of this patent

Rapidly disintegrating sustained release cefuroxime axetil composition

Life of this patent

Abstract

Claims47