Gelatine capsule containing selegiline or derivative and paraffi

Details Gelatine capsule containing selegiline or derivative and paraffi Gelatine capsule containing selegiline or derivative and paraffi

1997-06-12

1999-07-06

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Capsules

424451, 424452, 424455, 514789, A61K 948

Patent

active

059194820

DESCRIPTION:

BRIEF SUMMARY
The invention relates to a gelatine capsule containing selegiline, or a structurally related compound or pharmaceutically acceptable salt thereof and paraffin as a carrier.
Selegiline ((-)N-(1-phenyl isopropyl)-N-methyl-N-propionyl amine) is a MAO-B inhibitor. It has been available in tablet form for more than ten years in the treatment of Parkinson's disease and for a few years as an aqueous mixture.
Gelatine capsules provide an alternative to the present compositions of selegiline worthy of consideration because the pharmaceutical availability of drugs formulated for this kind of dosage form may be regulated more efficiently. Furthermore, the accuracy and uniformity of dosage are usually better in formulations having liquid contents than in entirely dry formulations.
Different problems to those connected with the preparation of conventional solid oral formulations are encountered when a gelatine capsule, especially a soft gelatine capsule, of a new drug is prepared. In soft gelatine capsules, the active drug is usually dissolved or suspended in a suitable liquid, e.g. vegetable oil. Hard gelatine capsules are usually prepared using principally the same technology as in conventional solid oral formulations (i.e. tablets, granules etc.). However, it is also possible to prepare hard gelatine capsules having liquid or semi-solid contents. If liquid contents are to be used in hard gelatine capsules then a special sealing technology of the capsules is needed.
According to U.S. Pat. No. 4,812,481 selegiline and amantadine act together synergistically in the treatment of Parkinsonism. The active ingredients may be administered either sequentially or in a single formulation. Numerous formulation agents are mentioned and several types of preparation are mentioned. The examples illustrate a suspension of amantadine hydrochloride and selegiline in water for injection, and capsules of amantadine hydrochloride and selegiline hydrochloride granulated with gelatin, corn starch, magnesium stearate and silicon dioxide, which mixture is used to fill hard gelatin capsules.
When the stability of selegiline hydrochloride was tested in vegetable oil suspensions which are typically used in gelatine capsules having liquid contents the active ingredient was degraded within a few weeks. However, in liquid paraffin suspension no degradation of selegiline hydrochloride was detected even after a storage period of 11 weeks at 45.degree. C.
It is therefore the object of the invention to provide a gelatine capsule of selegiline, a structurally related compound or pharmaceutically acceptable salt thereof.
It is a further object of the invention to provide the use of a paraffin carrier, especially a paraffin oil carrier, in gelatine capsules of selegiline, a structurally related compound or pharmaceutically acceptable salt thereof.
It is a still further object of the invention to provide a liquid carrier which may be used in gelatine capsules of selegiline, a structurally related compound or pharmaceutically acceptable salt thereof.
By the definition "structurally related compound" it is meant that especially the side chain of the compound is structurally similar to that of selegiline i.e. said compound is isopropylpropynylamine derivative.
The gelatine capsules according to the invention may be prepared using conventional techniques (see eg. The Theory and Practice of Industrial Pharmacy, Ed. Lachman L. et al, Third Edition, Lea & Febiger, 1986, Philadelphia, pp. 398-412). The amount of selegiline, a structurally related compound or pharmaceutically acceptable salt thereof, may be about from 2.5 to 60 mg per unit dosage, the amount of paraffin being from 2 to 250, preferably from about 5 to about 50 parts by weight relative to 1 part by weight of selegiline. A substantial part of paraffin, i.e. preferably at least 50% by weight and (especially in soft gelatine capsules) most preferably at least 80% by weight, is added in liquid form (paraffin oil). However, especially in hard gelatine capsules up to 85 weight % solid paraffin may also be

REFERENCES:
patent: 4812481 (1989-03-01), Reischig et al.
J. P. Stanley, Soft Gelatin Capsules, The Theory and Practice of Industrial Pharmacy, Ed. Lachman et al., Third Edition, Lea & Febiger, 1986, 398-412.
P.A. Veronesi, "Unit Dosage Delivery System for Hydrophobic Drugs", AN 96-051911, Database WPI, Week 9606, Jan. 1996, Derwent Publications Ltd., London, GB.

Affiliated with

Also associated with

Rating

Gelatine capsule containing selegiline or derivative and paraffi does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Gelatine capsule containing selegiline or derivative and paraffi, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Gelatine capsule containing selegiline or derivative and paraffi will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-897401