Compositions comprising sibutramine metabolites in combination with phosphodiesterase inhibitors
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/135
A61K-031/496
출원번호
US-0278097
(2002-10-23)
발명자
/ 주소
Jerussi, Thomas P.
Senanayake, Chrisantha H.
Fang, Qun K.
출원인 / 주소
Sepracor Inc.
대리인 / 주소
Jones Day
인용정보
피인용 횟수 :
1인용 특허 :
32
초록
Pharmaceutical compositions and dosage forms are disclosed that comprise a racemic or optically pure sibutramine metabolite and a phosphodiesterase inhibitor.
대표청구항▼
1. A pharmaceutical composition comprising a sibutramine metabolite, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, or prodrug thereof, and a phosphodiesterase inhibitor, wherein the sibutramine metabolite is (R/S)-desmethylsibutramine, (R)-desmethylsibutramine, (S)-desmethylsib
1. A pharmaceutical composition comprising a sibutramine metabolite, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, or prodrug thereof, and a phosphodiesterase inhibitor, wherein the sibutramine metabolite is (R/S)-desmethylsibutramine, (R)-desmethylsibutramine, (S)-desmethylsibutramine, (R/S)-didesmethylsibutramine, (R)-didesmethylsibutramine, or (S)-didesmethylsibutramine.2. The pharmaceutical composition of claim 1 wherein the sibutramine metabolite is optically pure (R)-desmethylsibutramine, (S)-desmethylsibutramine, (R)-didesmethylsibutramine, or (S)-didesmethylsibutramine.3. The pharmaceutical composition of claim 1, wherein the phosphodiesterase inhibitor is sildenophil, desmethylsildenophil, vinopocetine, milrinone, amrinone, pimobendan, cilostamide, enoximone, peroximone, vesnarinone, rolipram, R020-1724, zaprinast, dipyridamole, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, prodrug, optically and pharmacologically active stereoisomer, or a pharmacologically active metabolite thereof.4. The pharmaceutical composition of claim 1 wherein the sibutramine metabolite is in an amount of from about 0.1 mg to about 60 mg.5. The pharmaceutical composition of claim 4 wherein the sibutramine metabolite is in an amount of from about 2 mg to about 30 mg.6. The pharmaceutical composition of claim 5 wherein the sibutramine metabolite is in an amount of from about 5 mg to about 15 mg.7. The pharmaceutical composition of claim 1 wherein the phosphodiesterase inhibitor is in an amount of from about 0.5 mg to about 500 mg.8. The pharmaceutical composition of claim 7 wherein the phosphodiesterase inhibitor is in an amount of from about 1 mg to about 350 mg.9. The pharmaceutical composition of claim 8 wherein the phosphodiesterase inhibitor is in an amount of from about 2 mg to about 250 mg.10. The pharmaceutical composition of claim 1 wherein the pharmaceutical composition is adapted for oral, mucosal, rectal, parenteral, transdermal, or subcutaneous administration.11. The pharmaceutical composition of claim 10 wherein the pharmaceutical composition is adapted for oral, mucosal, or transdermal administration.12. A lactose free pharmaceutical composition which comprises a sibutramine metabolite, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, a phosphodiesterase inhibitor, and a pharmaceutically acceptable excipient, wherein the sibutramine metabolite is (R/S)-desmethylsibutramine, (R)-desmethylsibutramine, (S)-desmethylsibutrarnine, (R/S)-didesmethylsibutramine, (R)-didesmethylsibutramine, or (S)-didesmethylsibutramine.13. The pharmaceutical composition of claim 12 wherein the excipient is croscarmellous sodium, microcrystalline cellulose, pre-gelatinized starch, or magnesium stearate.14. The pharmaceutical composition of claim 13 wherein said pharmaceutical composition is substantially free of mono- or di-saccharides.15. The pharmaceutical composition of claim 12 wherein the sibutramine metabolite is optically pure (R)-desmethylsibutramine, (S)-desmethylsibutramine, (R)-didesmethylsibutramine, or (S)-didesmethylsibutramine.
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