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Title:
PHARMACEUTICAL COMPOSITION COMPRISING A SALT OF PAROXETINE
Document Type and Number:
WIPO Patent Application WO/2000/078290
Kind Code:
A2
Abstract:
Pharmaceutical compositions comprising water soluble salts of paroxetine are described.

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Inventors:
AL-GHAZAWI AHMAD KHALAF AL-DEE (GB)
ELDER DAVID PHILIP (GB)
MENEAUD PADMA (GB)
Application Number:
PCT/EP2000/005638
Publication Date:
December 28, 2000
Filing Date:
June 16, 2000
Export Citation:
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Assignee:
SMITHKLINE BEECHAM PLC (GB)
AL GHAZAWI AHMAD KHALAF AL DEE (GB)
ELDER DAVID PHILIP (GB)
MENEAUD PADMA (GB)
International Classes:
A61K9/20; A61K31/445; (IPC1-7): A61K9/20; A61K31/445
Domestic Patent References:
WO1999040084A11999-08-12
WO2000008016A12000-02-17
WO1998056787A11998-12-17
WO1997003670A11997-02-06
WO1995016448A11995-06-22
Foreign References:
EP0970955A12000-01-12
US5371092A1994-12-06
Other References:
SUCKER H ET AL: "PHARMAZEUTISCHE TECHNOLOGIE" , DE,STUTTGART, THIEME VERLAG, PAGE(S) 259-260 XP002060945 page 259 -page 260
Attorney, Agent or Firm:
Thompson, Clive Beresford (Middlesex TW8 9EP, GB)
Giddings, Peter John (SmithKline Beecham Corporate Intellectual Property Two New Horizons Court Brentford Middlesex TW8 9EP, GB)
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Claims:
Claims
1. A pharmaceutical composition comprising a salt of paroxetine which is more watersoluble than paroxetine hydrochloride hemihydrate and a pharmaceutically acceptable carrier wherein the carrier comprises a watersoluble and/or hydrophilic diluent, excluding the following tablet compositions consisting of: INGREDIENTS 20 mg Tablet 30mg Tablet More watersoluble paroxetine 20.00 mg 30.0 mg salt as hereinbefore defined (calc. as free base) (calc. as free base) Dicalcium Phosphate (DCP) 83.34 mg 125.0 mg Microcrystalline Cellulose 50.67 mg 76.0 mg Sodium Starch Glycollate 8.34 mg 12.5 mg Magnesium Stearate 1.67 mg 2.5 mg.
2. A composition according to claim 1 in which the salt of paroxetine is selected from glutamate, succinate, propionate, gluconate, 4hydroxybutyrate, aspartate, formate, benzenesulfonate, toluenesulfonate or methanesulfonate.
3. A composition according to claim 1 or 2 in which the salt of paroxetine is paroxetine methanesulfonate.
4. A composition according to any one of claims 1 to 3 wherein the diluent has a water solubility at 20°C of at least 0.005 mg/ml.
5. A composition according to claim 4 wherein the diluent has a water solubility at 20°C of at least 0.01 mg/ml.
6. A composition according to claim 5 wherein the diluent has a water solubility at 20°C of at least O. 1 mg/ml.
7. A composition according to any one of claims 1 to 3 wherein the water soluble and/or hydrophilic diluent is a carbohydrate diluent.
8. A composition according to claim 7 wherein the carbohydrate diluent is selected from compressible sugar, confectioner's sugar, a dextrate, dextrin, dextrose, fructose, microcrystalline cellulose, silicified microcrystalline cellulose, pregelatinised starch, powdered cellulose, lactose, maltodextrin, mannitol, sorbitol, sucrose, sugar spheres, lactitol, maltitol, or xylitol or a mixture thereof.
9. A composition according to claim 8 wherein the carbohydrate diluent is selected from lactose, microcrystalline cellulose or mannitol or a mixture thereof.
10. A composition according to any one of claims 1 to 9 wherein the diluent is present in an amount ranging from 1 to 99% w/w of the composition.
11. A composition according to claim 10 wherein the diluent is present in an amount ranging from 20 to 95% w/w of the composition.
12. A composition according to claim 11 wherein the diluent is present in an amount ranging from 40 to 95% w/w of the composition.
13. A composition according to claim 12 wherein the diluent is present in an amount ranging from 80 to 90% w/w of the composition.
14. A composition according to any one of claims 1 to 13 further comprising an additional diluent selected from calcium carbonate, calcium sulfate, dibasic calcium phosphate dihydrate or dibasic calcium phosphate or a mixture thereof.
15. A composition according to claim 14 which does not contain dicalcium phosphate in combination with microcrystalline cellulose.
16. A composition according to claim 14 which does not contain dicalcium phosphate.
17. A composition according to any one of claims 14 to 16 wherein the diluent admixture comprises at least 20 % by weight thereof of the watersoluble and/ or hydrophilic diluent.
18. A composition according to any one of claims 14 to 16 wherein the diluent admixture comprises at least 40 % by weight thereof of the watersoluble and/ or hydrophilic diluent.
19. A composition according to any one of claims 14 to 16 wherein the diluent admixture comprises at least 60 % by weight thereof of the watersoluble and/ or hydrophilic diluent.
20. A composition according to any one of claims 14 to 16 wherein the diluent admixture comprises at least 80 % by weight thereof of the watersoluble and/ or hydrophilic diluent.
21. A composition according to any one of claims 1 to 13 wherein the water soluble and/or hydrophilic diluent is present as the sole diluent.
22. A composition according to any one of claims 1 to 21 further comprising a disintegrant.
23. A composition according to claim 22 wherein the disintegrant is selected from starch, methylcellulose, crospovidone, croscarmellose sodium or sodium starch glycollate or a mixture thereof.
24. A composition according to claim 23 wherein the disintegrant is sodium starch glycollate.
25. A composition according to any one of claims 22 to 24 wherein the disintegrant is present in an amount up to 30% w/w of the composition.
26. A composition according to claim 25 wherein the disintegrant is present from 1 to 20% w/w of the composition.
27. A composition according to claim 26 wherein the disintegrant is present from 2 to 10% w/w of the composition.
28. A composition according to any one of claims 1 to 27 wherein said more water soluble salt of paroxetine is in crystalline form.
29. A composition according to claim 28 wherein paroxetine methanesulfonate is in crystalline form.
30. A composition according to claim 29 wherein the paroxetine methanesulfonate has inter alia the following characteristic IR peaks: 1208,1169,1038,962, 931,838 and 546 t 2 cmi'.
31. A composition according to claim 29 wherein the paroxetine methanesulfonate has inter the following characteristic IR peaks: 1604,1194,1045,946, 830,601,554 and 539 2 cri'.
32. A composition according to any one of claims 1 to 31 comprising 1 to 200mg of said more water soluble salt of paroxetine per unit dose, calculated on a free base basis.
33. A composition according to claim 32 comprising 10 to 50mg of said more water soluble salt of paroxetine per unit dose, calculated on a free base basis.
34. A composition according to claim 33 comprising 10,12.5,15,20,25,30 or 40mg of said more water soluble salt of paroxetine methanesulfonate per unit dose, calculated on a free base basis.
35. A composition according to any one of claims 32 to 34 wherein said more water soluble salt of paroxetine is paroxetine methanesulfonate.
36. A composition according to any one of claims 1 to 35 adapted for oral administration.
37. A composition according to claim 36 which is a tablet or capsule.
Description:
INTERNATIONALSEARCH REPORT Int tional Application No PCT/EP 00/05638 C. (Continuation) DOCUMENTS CONSIDERED TO BE RELEVANT Cate, gory ° Citation of document, with indication. where appropriate, of the relevant passages Relevant to claim No. P, X EP 0 970 955 A (SMITHKLINE BEECHAM PLC) 1-3, 12 January 2000 (2000-01-12) 10-13, 22-26, 28,29, 32-37 page 23; example 55 X WO 98 56787 A (SYNTHON B V) 1-3,36, 17 December 1998 (1998-12-17) 37 cited in the application page 2, line 36-page 3, line 37 page 9, line 6-line 26 A SUCKER H ET AL:"PHARMAZEUTISCHE 1 TECHNOLOGIE", DE, STUTTGART, THIEME VERLAG, PAGE (S) 259-260 XP002060945 page 259-page 260 X US 5 371 092 A (JOHNSON ANTHONY M) 1,4-9, 6 December 1994 (1994-12-06) 22-24, 32-34, 36,37 column 1, line 32-line 36 A WO 97 03670 A (EDLER DAVID PHILIP; LEONARD 1 GRAHAM STANLEY (GB); SMITHKLINE BEECHA) 6 February 1997 (1997-02-06) page 4-page 5; example 1 A WO 95 16448 A (SMITHKLINE BEECHAM PLC 1 ; PATHAK RAM DUTTA (GB); DOUGHTY DAVID GEORG) 22 June 1995 (1995-06-22) page 3; example 1 1 FURTHER INFORMATION CONTINUED FROM PCTASS 210 Continuation of Box 1. 2 Claims Nos.: 1 Present claim 1 relate to an extremely large number of possible compounds encompassed by the terms"a salt of paroxetine which is more soluble than parpxetine hydrochloride hemihydrate"and"a water soluble and/or hydrophilic diluent". Support within the meaning of Article 6 PCT and disclosure within the meaning of Article 5 PCT is to be found, however, for only a very small proportion of the compounds claimed. In the present case, the claims so lack support, and the application so lacks disclosure, that a meaningful search over the whole of the claimed scope is impossible. Consequently, the search has been carried out for those parts of the claims which appear to be supported and disclosed, namely those parts relating to the compounds claimed in claim 2 of the present application, and in claims 7,8 of the present applicatoion as well as the compounds which are disclosed in examples 1-15 of the present application. * The applicant's attention is drawn to the fact that claims, or parts of claims, relating to inventions in respect of which no international search report has been established need not be the subject of an international preliminary examination (Rule 66.1 (e) PCT). The applicant is advised that the EPO policy when acting as an International Preliminary Examining Authority is normally not to carry out a preliminary examination on matter which has not been searched. This is the case irrespective of whether or not the claims are amended following receipt of the search report or during any Chapter II procedure. INTERNATIONAL SEARCH REPORT Int : ional Application No Information on patent family members PC T/EP 00/05638 PCT/EP 00/05638 Patent document Publication Patent family Publication cited in search report date member (s) date WO 9940084 A 12-08-1999 AU 2528899 A 23-08-1999 EP 1053234 A 22-11-2000 NO 20003960 A 25-09-2000 AU 2528699 A 23-08-1999 WO 0008016 A 17-02-2000 AU 5294899 A 28-02-2000 AU 5294799 A 28-02-2000 EP 0970955 A 12-01-2000 AT 3185 U 25-11-1999 AT 195121 T 15-08-2000 AU 2392899 A 20-01-2000 AU 713131 A 25-11-1999 AU 713877 A 09-12-1999 AU 3619199 A 24-01-2000 AU 4903999 A 24-01-2000 BE 1012403 A 03-10-2000 BE 1011664 A 09-11-1999 BE 1012420 A 03-10-2000 CH 689805 A 30-11-1999 DE 19918588 A 27-01-2000 DE 29907248 U 09-09-1999 DE 69900007 D 07-09-2000 DK 9900176 U 13-08-1999 WO 0001692 A 13-01-2000 EP 1020463 A 19-07-2000 EP 1020464 A 19-07-2000 ES 2149044 T 16-10-2000 FI 4209 U 10-11-1999 FI 990922 A 03-01-2000 FR 2780728 A 07-01-2000 WO 0001694 A 13-01-2000 GB 2336364 A, B 20-10-1999 GB 2339428 A 26-01-2000 GR 99100140 A 31-03-2000 IE 81166 B 31-05-2000 NL 1011874 C 12-07-1999 NL 1011875 C 24-03-2000 NL 1011875 A 07-01-2000 NL 1012271 C 23-09-1999 NL 1012271 A 12-07-1999 NL 1012272 C 12-07-1999 NO 991944 A 03-01-2000 PT 102291 A 31-05-2000 PT 970955 T 30-11-2000 US 6063927 A 16-05-2000 WO 9856787 A 17-12-1998 US 5874447 A 23-02-1999 AU 3108097 A 30-12-1998 BG 103980 A 31-07-2000 BR 9714787 A 18-07-2000 EP 0994872 A 26-04-2000 NO 995455 A 09-02-2000 PL 336895 A 17-07-2000 US 5371092 A 06-12-1994 AU 658155 B 06-04-1995 AU 8915391 A 25-06-1992 CA 2096853 A 25-05-1992 EP 0558679 A 08-09-1993 INTERNATIONAL SEARCH REPORT Int tional Application No Information on patent family members PCT/EP 00/05638 PCT/EP 00/05638 Patent document Publication Patent family Publication cited in search report date member (s) date US 5371092 A WO 9209281 A 11-06-1992 JP 6502854 T 31-03-1994 MX 9102180 A 08-07-1992 ZA 9109247 A 28-10-1992 WO 9703670 A 06-02-1997 AU 6659196 A 18-02-1997 BG 102259 A 30-09-1998 BR 9609857 A 16-03-1999 CN 1195986 A 14-10-1998 CZ 9800183 A 17-06-1998 EA 980140 A 29-10-1998 EP 0839039 A 06-05-1998 HU 9900299 A 28-09-1999 JP 11509539 T 24-08-1999 NO 980240 A 20-01-1998 PL 324553 A 08-06-1998 SK 5398 A 08-07-1998 WO 9516448 A 22-06-1995 AP 540 A 20-09-1996 AT 180973 T 15-06-1999 AU 697982 B 22-10-1998 AU 1314595 A 03-07-1995 BG 62755 B 31-07-2000 BG 100648 A 28-02-1997 BR 9408219 A 26-08-1997 CA 2178637 A, C 22-06-1995 CA 2214575 A 22-06-1995 CN 1137236 A 04-12-1996 CZ 9601763 A 11-09-1996 DE 69419033 D 15-07-1999 DE 69419033 T 25-11-1999 DK 734260 T 15-11-1999 EP 0734260 A 02-10-1996 ES 2132610 T 16-08-1999 FI 962445 A 12-06-1996 GR 3031047 T 31-12-1999 HU 75880 A 28-05-1997 JP 9506602 T 30-06-1997 NO 962547 A 14-06-1996 NZ 277790 A 26-02-1998 PL 314980 A 30-09-1996 RO 115413 B 28-02-2000 SI 734260 T 31-08-1999 SK 75696 A 06-11-1996 US 6007842 A 28-12-1999 US 6113944 A 05-09-2000 ZA 9409900 A 10-10-1995



 
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