Extended release, film-coated tablet of astemizole and pseudoeph

Details Extended release, film-coated tablet of astemizole and pseudoeph Extended release, film-coated tablet of astemizole and pseudoeph

1995-11-08

1997-10-28

Krass, Frederick

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424469, 424470, 424472, 424474, 424480, 424476, A61K 920

Patent

active

056815824

DESCRIPTION:

BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATIONS

This application is based upon PCT Application Serial No. PCT/EP 94/01878, filed Jun. 7, 1994, which claims priority from European Patent Application Ser. No. 93.201.697.5, filed on Jun. 14, 1993.
The present invention is concerned with an extended release, film coated tablet comprising as active ingredients the antihistaminic, antiallergic agent astemizole and the adrenergic, decongestant agent pseudoephedrine hydrochloride and also with a process of preparing such tablets.
The antihistaminic antiallergic agent astemizole, its preparation and activity are known from U.S. Pat. No. 4,219,559. The pharmacokinetics of astemizole in man, in particular its rapid distribution to tissues and its terminal half-life of about 1 day, are known from Drug Dev. Res., 8 (1-4), 71-78, 1986. Pseudoephedrine, and especially its hydrochloride salt is a known decongestant having a half-life of several hours, typically about 6 to 8 hours. It is therefore usually employed in divided doses of 60 mg three or four times daily or in sustained release preparations, usually in doses of about 120 mg every 12 hours.
An effective treatment of patients suffering from allergic disorders such as allergic rhinitis, perennial rhinitis and the like, calls for a composition that upon adminstration releases an antihistaminic agent and a decongestant in such a manner that effective plasma levels of both active ingredients are maintained throughout the next 24 hours, i.e. until the next administration.
The present invention deals with such a composition that comprises (i) astemizole which has a terminal half-life of about 24 hours and a rapid distribution and thus does not need any special precautions, together with (ii) pseudoephedrine hydrochloride that has too short a half-life to attain effective plasma levels for the desired 24 hours and therefore requires special technical measures.
In particular the composition of the present invention concerns a tablet comprising hydrochloride as the active ingredient, a highly viscous hydrophilic polymer as matrix material, a solid diluent and optitionally other formulating agents known in the art such as, for example, granulating agents, glidants, tablet binding agents, solvents, anticaking agents, preservatives or lubricants; as active ingredients, a hydrophilic polymer and optionally other formulating agents known in the art such as surfactants, plasticizers, lubricants; and
Said tablets preferably comprise about 75% of the available pseudoephedrine hydrochloride in the core from which it will be released over an extended period, and the remaining 25% in the drug coating which will be released and taken up together with the antihistaminic astemizole immediately following digestion.
The tablets comprise from 60 mg to 240 mg pseudoephedrine hydrochloride in the core, from 20 mg to 80 mg pseudoephedrine hydrochloride in the drug coating as well as 5 mg to 20 mg astemizole in said drug coating. Tablets for adult humans preferably comprise about 180 mg pseudoephedrine hydrochloride in the core, about 60 mg pseudoephedrine hydrochloride in the drug coating, and about 10 mg astemizole in the drug coating. Tablets for humans having a lower bodyweight, e.g. children are preferably only half as large and thus comprise about 90 mg pseudoephedrine hydrochloride in the core, about 30 mg pseudoephedrine hydrochloride in the drug coating, and about 5 mg astemizole in the drug coating.
The highly viscous hydrophilic polymer in the core of the tablet should release the active ingredient therein gradually, preferably with zero order release kinetics. Suitable highly viscous polymers have a viscosity ranging from about 3.500 mPa.cndot.s to about 100.000 mPa.cndot.s, in particular ranging from about 4.000 mPa.cndot.s to about 20.000 mPa.cndot.s. Examples of such polymers are hydroxypropyl methylcellulose, hydroxypropyl cellulose and hydroxyethyl cellulose. For the active ingredient pseudoephedrine hydrochloride this can conveniently be achieved using a hydroxypropyl methylcellulos

REFERENCES:
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patent: 4829064 (1989-05-01), Sunshine et al.
patent: 4975426 (1990-12-01), Sunshine et al.
patent: 4996061 (1991-02-01), Webb et al.
patent: 4999226 (1991-03-01), Schock et al.

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