Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-10-28
1999-02-02
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514458, 514474, A61K 31445, A61K 31355, A61K 3134
Patent
active
058665900
DESCRIPTION:
BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a 35 U.S.C. 371 national application of PCT/DK96/00192 filed Apr. 29, 1996 and claims priority under 35 U.S.C. 119 of Danish application 0523/95 filed May 5, 1995, the contents of which are fully incorporated herein by reference.
The subject-matter of the present invention is a new pharmaceutical composition containing tiagabine hydrochloride as active ingredient and the process for its preparation.
In the present invention the R.isomer of N-(4,4-di(3-methylthien-2-yl)but-3-enyl-nipecotic acid is referred to by its generic name (INN): tiagabine, which is a well tolerated medication, having antiepileptic activity.
The compound N-(4,4-di(3-methylthien-2-yl)but-3-enyl-nipecotic acid is disclosed in USP 5,010,090.
Various solutions have been proposed for the preparation of medications based on tiagabine hydrochloride.
The aim of the present invention is to supply a new composition intended for the preparation of tiagabine hydrochloride with improved stability, in particular solid dosage forms thereof.
It has been found in fact that tiagabine hydrochloride decomposes in the presence of and in contact with oxygen and water.
Thus, from a first aspect, the subject-matter of the present invention is a pharmaceutical composition intended for the preparation of dosage forms and in particular solid dosage forms containing an efficacious quantity of tiagabine hydrochloride or of one of its pharmaceutically acceptable salts as active ingredient and characterised in that it contains at least one pharmaceutically acceptable antioxidant agent, in a sufficient quantity to stabilise the active ingredient.
Thus the present invention is based on the surprising discovery of the fact that the stability of tiagabine hydrochloride, or of one of its pharmaceutically acceptable salts, can be considerably improved in preparations containing tiagabine hydrochloride or of its pharmaceutically acceptable salts and antioxidant agent.
Tiagabine hydrochloride, together with a conventional adjuvant, antioxidant carrier, or diluent, and if desired a pharmaceutically acceptable acid addition salt thereof, may be placed into the form of pharmaceutical compositions and unit dosages thereof, and in such form may be employed as solids, such as tablets or filled capsules, or liquids such as solutions, suspensions, emulsions, elixirs, or capsules filled with the same, all for oral use, in the form of suppositories for rectal administration; or as pessaries for vaginal use; or in the form of sterile injectable solutions for parenteral (including subcutaneous) use.
Within the framework of the present description and of the claims, by powders is meant any mixture of components, granulated or not, intended to be placed in solution and/or in suspension in water, or again to be ingested directly or by any other appropriate means as for example in a mixture with a food product.
In accordance with a particular characteristic of the invention, the granulation is carried out as a melt-granulation.
In accordance with another particular characteristic, this composition also contains pharmaceutically acceptable diluents.
In accordance with a particular characteristic of the invention, the antioxidant agent cited above is selected from among .alpha.-tocopherol, .gamma.-tocopherol, .delta.-tocopheral, extracts of natural origin rich in tocopherol, L-ascorbic acid and its sodium or calcium salts, ascorbyl palmitate, propyl gallate (PG), octyl gallate, dodecyl gallate, butylated hydroxy anisole (BHA) and butylated hydroxy toluene (BHT).
In accordance with a currently preferred embodiment, the antioxidant agent will be .alpha.-tocopherol.
In accordance with another particular characteristic of the invention, the diluent is lactose and/or polyethylenglycol.
However, any other pharmaceutically acceptable diluents could be used.
The quantities of diluents can be easily determined by a person skilled in the art and depend of course on the final pharmaceutical form required.
Generally speaking, a composition wh
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Weibel, H., et al., Proc. 1st World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology -Budapest, pp. 951-952, (1995).
Andersen Tina Meinertz
Hjorth Thyge Borup
Nygaard Lars
Svensson J.o slashed.rgen Ryhl
Weibel Helle
Agris, Esq. Cheryl H.
Henley III Raymond
Novo Nordisk A S
Zelson Esq. Steve T.
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