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Patent Searching and Data


Title:
SOLID LIPID FORMULATIONS COMPRISING AN INHIBITOR OF LIPASES AND A FATTY ACID ESTER OF POLYOLS
Document Type and Number:
WIPO Patent Application WO/2001/019378
Kind Code:
A2
Abstract:
The present invention refers to a pharmaceutical composition comprising at least one inhibitor of lipases and at least one fatty acid ester of polyols, characterized in that the fatty acid ester has a melting point above the body temperature and the polyols are chosen from the group consisting of sugars, sugar derivatives and mixtures thereof.

Inventors:
DE SMIDT PASSCHIER CHRISTIAAN
HADVARY PAUL
LENGSFELD HANS
SCHMID MARCEL
SMALL DAVID MACFARLAND
STEFFEN HANS
TARDIO JOSEPH
Application Number:
PCT/EP2000/008857
Publication Date:
March 22, 2001
Filing Date:
September 11, 2000
Export Citation:
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Assignee:
HOFFMANN LA ROCHE (CH)
International Classes:
A61K9/00; A61K47/14; A61K9/20; A61K9/46; A61K9/48; A61K9/68; A61K31/365; A61K35/00; A61K45/00; A61K45/08; A61K47/24; A61K47/26; A61K47/36; A61P3/04; A61P3/06; (IPC1-7): A61K35/00
Domestic Patent References:
WO1998034607A11998-08-13
WO2000009123A12000-02-24
Foreign References:
US5741496A1998-04-21
Attorney, Agent or Firm:
Witte, Hubert (124 Grenzacherstrasse Basle, CH)
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Claims:
CLAIMS
1. A pharmaceutical composition comprising at least one inhibitor of lipases and at least one fatty acid ester of polyols, characterized in that the fatty acid ester has a melting point above the body temperature and the polyols are chosen from the group consisting of glycerol, sugars, sugar derivatives and mixtures thereof.
2. The pharmaceutical composition according to claim 1, wherein the polyols are chosen, independently from each other, from the group consisting of sucrose, glycerol, and sugar alcohols.
3. The pharmaceutical composition according to claim 1 or 2, wherein the polyol is glycerol.
4. The pharmaceutical composition according to any of claims 1 to 3, wherein the fatty acid ester is a glyceride ester and is chosen from the group consisting of one or more triglycerides, one or more monoglycerides, one or more phospholipids and mixtures thereof.
5. The pharmaceutical composition according to any of claims 1 to 4, wherein the fatty acid moieties in the fatty acid ester of the polyol have, independently from each other, twelve or more carbon atoms and the fatty acid moieties in the fatty acid ester of the polyol are saturated.
6. The pharmaceutical composition according to claim D, wherein the fatty acid moieties in the fatty acid ester of the polyol have, independently from each other, twelve to twenty carbon atoms.
7. The pharmaceutical composition according to any of claims 4 to 6, wherein the triglycerides are chosen from the group consisting of trilaurin, trimyristin, tripalmitin, tristearin and mixtures thereof.
8. The pharmaceutical composition according to claim 7, wherein the triglyceride is trimyristin or trilaurin or mixtures thereof.
9. The pharmaceutical composition according to any of claims 4 to 6, wherein the monoglycerides are chosen from the group consisting of monocaprin, monolaurin, monomyristin, monopalmitin and mixtures thereof.
10. The pharmaceutical composition according to any of claims 4 to 6, wherein the phospholipid is a lecithin.
11. The pharmaceutical composition according to claim 10, wherein the phospholipid is a non, partially or fully hydrogenated lecithin and mixtures thereof.
12. The pharmaceutical composition according to claim 10 or 11, wherein the phospholipids are chosen from the group consisting of natural lecithin, synthetic lecithin, sojalecithin, egglecithin, synthetic dipalmitoyllecithin, partially or fully. hydrogenated lecithin and mixtures thereof.
13. The pharmaceutical composition according to any of claims 1 to 12, wherein the fatty acid ester of polyols is present in an amount varying between 0.5 % and 90 % of the total weight of the composition.
14. The pharmaceutical composition according to any of claims 1 to 13, further comprising at least one pharmaceutically acceptable excipient.
15. The pharmaceutical composition according to claim 14, wherein the excipient is selected from the group consisting of carbohydrates, starch and/or its derivatives, maltodextrines, cellulose, cellulose derivatives, sugars, fillers, disintegrants, effervescents, antioxidants, anionic surfactants, nonionic surfactants and mixtures thereof.
16. The pharmaceutical composition according to claim 15, wherein the surfactant is selected from the group consisting of sodium dodecylsulfate, fatty acid salts, polyoxyethylene alkyl esters and polyoxyethylene alkyl ethers and mixtures thereof.
17. The pharmaceutical composition according to any of claims 14 to 16, comprising an excipient selected from the group consisting of glucose, lactose, sorbitol, maltodextrin, talcum, magnesium stearate, mannitol, sodium bicarbonate, Crospovidone, glycofurol, tartaric acid and mixtures thereof.
18. The pharmaceutical composition according to any of claims 1 to 17, wherein the inhibitor of lipases is an inhibitor of gastrointestinal lipases.
19. The pharmaceutical composition according to claim 18, wherein the inhibitor of gastrointestinal lipases is orlistat.
20. The pharmaceutical composition according to any of claims 1 to 19, wherein the lipase inhibitor is present in an amount varying from 1 to 50% of the total weight of the composition.
21. The pharmaceutical composition according to claim 20, wherein the lipase inhibitor is present in an amount varying from 5 to 30'Yo of the total weight of the composition.
22. The pharmaceutical composition according to any of claims 1 to 21, wherein a) 1 to 50% of the total weight of the composition is at least one lipase inhibitor; b) 0.5 to 90% of the total weight of the composition is at least one fatty acid ester of polyols; and optionally c) the composition comprises one or more pharmaceutically acceptable 'excipient (s).
23. A process for preparing a pharmaceutical composition according to any one of claim 1 to 22, comprising mixing at least one inhibitor of lipases with at least one fatty acid ester of polyols, wherein the fatty acid ester of polyols has a melting point above the body temperature and the polyols are chosen from the group consisting of glycerol, sugars, sugar derivatives and mixtures thereof.
24. Use of a pharmaceutical composition as defined in any one of claim 1 to 22 for controlling or preventing obesity.
25. A method for controlling or preventing obesity comprising the step of administering to a patient a pharmaceutical composition as defined in any one of claims 1 to 22.
26. Use of a composition as defined in any of claims 1 to 22 for the preparation of a medicament for the prevention and treatment of obesity.
27. The invention as hereinbefore described.
Description:
INTERNATIONAL SEARCH REPORT Inte ional Application No Information on patent family members PCT/EP 00/08857 PCT/EP 00/08857 Patent document Publication Patent Publication cited in search report date member (s) date WO 9834607 A 13-08-1998 US 6004996 A 21-12-1999 AU 713192 B 25-11-1999 AU 6097298 A 26-08-1998 CA 2258095 A 13-08-1998 CN 1220600 A 23-06-1999 CN 1220600 T 23-06-1999 CZ 9803528 A 17-02-1999 EP 0921796 A 16-06-1999 HR 980057 A 31-12-1998 NO 985337 A 16-11-1998 PL 330972 A 21-06-1999 ZA 9800746 A 05-08-1998 HU 0001468 A 28-09-2000 JP 3059149 B 04-07-2000 JP 11255645 A 21-09-1999 US 5741496 A 21-04-1998 FR 2710264 A 31-03-1995 AT 186834 T 15-12-1999 BR 9403783 A 23-05-1995 CA 2132369 A, C 22-03-1995 CN 1109740 A 11-10-1995 DE 69421778 D 30-12-1999 DE 69421778 T 21-06-2000 EP 0643960 A 22-03-1995 ES 2141208 T 16-03-2000 GR 3032673 T 30-06-2000 JP 7196469 A 01-08-1995 PT 643960 T 28-04-2000 WO 0009123 A 24-02-2000 AU 5420599 A 06-03-2000 US 6030953 A 29-02-2000 US 6030953 A 29-02-2000