Tetrahydrolipstatin containing compositions

• US 6,004,996 A
• Filed: 01/06/1998
• Issued: 12/21/1999
• Est. Priority Date: 02/05/1997
• Status: Expired due to Term

• Current Assignee: Cheplapharm Arzneimittel GmbH
• Original Assignee: Hoffmann-La Roche Incorporated (Roche Holding AG)
• Inventors: Zeller, Max, Shah, Navnit Hargovindas
• Primary Examiner(s): Moezie, M.
• Application Number:
  US09/003,137
• Time in Patent Office: 714 Days
• Field of Search: 514/449, 424/452, 424/465
• US Class Current: 514/449
• CPC Class Codes: A61K 31/365 Lactones
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics

Abstract

Product containing tetrahydrolipstatin as the active ingredient and pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter of 0.25 to 2 mm; and pharmaceutical preparation s or compositions for oral administration containing the product.

Claims

1. A pharmaceutical composition comprising a plurality of pellets having a diameter in the range of from about 0.25 mm to about 2 mm, and at most only a trace amount of pellets outside this range, each pellet comprising about 50% by weight tetrahydrolipstatin;

polyvinylpyrrolidone;

microcrystalline cellulose; and

at least one pharmaceutically acceptable excipient.

2. The composition of claim 1, wherein the pellets have a diameter of from about 0.5 mm to about 1.5 mm.

3. The composition of claim 1, wherein at least 5% by weight of the composition is polyvinylpyrrolidone.

4. The composition of claim 1, wherein the pharmaceutically acceptable excipient is a surfactant, diluent, or disintegrant.

5. The composition of claim 4, wherein the pharmaceutically acceptable excipient is a surfactant.

6. The composition of claim 5, wherein the surfactant is sodium lauryl sulfate or sodium dioctylsulfosuccinate.

7. The composition of claim 4, wherein the pharmaceutically acceptable excipient is a diluent.

8. The composition of claim 7, wherein the diluent is sucrose or corn starch.

9. The composition of claim 4, wherein the excipient is a disintegrant.

10. The composition of claim 9, wherein the disintegrant is sodium starch glycolate, cross-linked polyvinyl pyrrolidone, cross-carmolose sodium, or a hydroxypropyl cellulose.

11. The composition of claim 1 which comprises about 50% by weight tetrahydrolipstatin;

about 39% by weight microcrystalline cellulose;

about 3% by weight sodium starch glycolate;

about 3% by weight sodium lauryl sulfate;

about 5% by weight polyvinylpyrrolidone; and

about 0.1% by weight talc.

12. The composition of claim 1 which is in unit dosage form.

13. The composition of claim 11 which is in unit dosage form.

14. The composition of claim 1 which comprises about 120 mg of tetrahydrolipstatin;

about 93.6 mg of microcrystalline cellulose;

about 7.2 mg of sodium starch glycolate;

about 7.2 mg of sodium lauryl sulfate;

about 12 mg of polyvinylpyrrolidone; and

about 0.24 mg of talc.

15. The composition of claim 14 which is in unit dosage form.