Semi-solid delivery vehicle and pharmaceutical compositions for delivery of granisetron
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/435
A61K-031/439
A61K-031/53
A61K-047/30
C07D-319/04
출원번호
US-0564881
(2009-09-22)
등록번호
US-8252304
(2012-08-28)
발명자
/ 주소
Ng, Steven Y.
Shen, Hui Rong
Heller, Jorge
출원인 / 주소
A. P. Pharma, Inc.
대리인 / 주소
Lowenstein Sandler PC
인용정보
피인용 횟수 :
11인용 특허 :
37
초록▼
A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the a
A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
대표청구항▼
1. A pharmaceutical composition comprising: (A) semi-solid delivery vehicle, comprising: (i) a polyorthoester consisting of formula I where:R* is ethyl;n is an integer of 5 to 1000; andA is R1 or R3 whereR1 is: where:p is an integer of 1 to 20;R5 is hydrogen; andR6 is: where:s is an integer of 0 to
1. A pharmaceutical composition comprising: (A) semi-solid delivery vehicle, comprising: (i) a polyorthoester consisting of formula I where:R* is ethyl;n is an integer of 5 to 1000; andA is R1 or R3 whereR1 is: where:p is an integer of 1 to 20;R5 is hydrogen; andR6 is: where:s is an integer of 0 to 10;R3 is: where:x is an integer of 0 to 30;in which about 0.05-30 mol percent of the A units are of the formula R1; and(ii) polyethylene glycol monomethyl ether; and(B) granisetron in an amount of 1-5 weight % of the composition. 2. The pharmaceutical composition of claim 1, wherein the polyethylene glycol monomethyl ether has a molecular weight between 200 and 4000. 3. The pharmaceutical composition of claim 2, comprising polyethylene glycol monomethyl ether 550. 4. The pharmaceutical composition of claim 1, wherein the total concentration of the polyethylene glycol monomethyl ether is 5-60 weight % of the composition. 5. The pharmaceutical composition of claim 1, comprising 78.4 weight % polyorthoester, 19.6 weight % polyethylene glycol monomethyl ether and 2 weight % granisetron. 6. The pharmaceutical composition of claim 1, which provides a controlled release of the granisetron. 7. The pharmaceutical composition of claim 1, which is suitable for injection. 8. The pharmaceutical composition of claim 7, which is suitable for subcutaneous injection. 9. The pharmaceutical composition of claim 1, which is filled into a syringe with a 16-25 gauge needle. 10. The pharmaceutical composition of claim 1, wherein p is an integer of 1 to 7 in a portion of the units of formula I. 11. The pharmaceutical composition of claim 1, wherein x is 2 in a portion of the units of formula I. 12. The pharmaceutical composition of claim 1, wherein s is 2 in a portion of the units of formula I. 13. A pharmaceutical composition comprising (a) a reaction product of 3,9-di(ethylidene)-2,4,8,10-tetraoxaspiro[5.5]undecane (DETOSU), triethylene glycol (TEG) and triethylene glycol diglycolide (TEG-diGL) wherein the reaction comprises TEG-diGL in an amount of about 0.05-30 mol percent of total diols; (b) polyethylene glycol monomethyl ether 550 and (c) granisetron in an amount of 1-5 weight % of the composition. 14. A pharmaceutical composition consisting essentially of (a) a reaction product of 3,9-di(ethylidene)-2,4,8,10-tetraoxaspiro[5.5]undecane (DETOSU), triethylene glycol (TEG) and triethylene glycol diglycolide (TEG-diGL) wherein the reaction comprises TEG-diGL in an amount of about 0.05-30 mol percent of total diols; (b) polyethylene glycol monomethyl ether 550 and (c) granisetron in an amount of 1-5 weight % of the composition. 15. A pharmaceutical composition comprising: (A) semi-solid delivery vehicle, comprising: (i) a polyorthoester which is a reaction product of reagents comprising 3,9-di(ethylidene)-2,4,8,10-tetraoxaspiro[5.5]undecane (DETOSU), triethylene glycol (TEG) and triethylene glycol diglycolide (TEG-diGL) wherein the reaction comprises TEG-diGL in an amount of about 0.05-30 mol percent of total diols;(ii) polyethylene glycol monomethyl ether; and(B) granisetron in an amount of 1-5 weight % of the composition. 16. The pharmaceutical composition of claim 1, wherein about 0.1-25 mol percent of the A units are of the formula R1. 17. The pharmaceutical composition of claim 13, wherein the reaction comprises TEG-diGL in an amount of about 0.1-25 mol percent of total diols. 18. The pharmaceutical composition of claim 14, wherein the reaction comprises TEG-diGL in an amount of about 0.1-25 mol percent of total diols. 19. The pharmaceutical composition of claim 15, wherein the reaction comprises TEG-diGL in an amount of about 0.1-25 mol percent of total diols.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (37)
Churchill Jeffrey R. (Northwich GBX) Hutchinson Francis G. (Lymm GBX), Biodegradable amphipathic copolymers.
Chandrashekar Bhagya L. ; Zhou Mingxing ; Jarr Eileen M. ; Dunn Richard L., Controlled release liquid delivery compositions with low initial drug burst.
Domb Abraham J.,ILX ; Gref Ruxandra,FRX ; Minamitake Yoshiharu,JPX ; Peracchia Maria Teresa,ITX ; Langer Robert S., Nanoparticles and microparticles of non-linear hydrophilic-hydrophobic multiblock copolymers.
Heller Jorge (Woodside CA) Ng Steve Y. W. (San Francisco CA) Penhale Donald W. H. (Menlo Park CA), Polymers containing carboxy-ortho ester and ortho ester linkages.
Heller Jorge (Palo Alto CA) Helwing Robert F. (Sunnyvale CA) Penhale Donald W. (Cupertino CA), Polymers of di- (and higher functionality) ketene acetals and polyols.
Cohen Edward M. (Beaumont PA FRX) Grim Wayne M. (Doylestown PA) Harwood Richard J. (Philadelphia PA) Mehta Gunvant N. (Lansdale PA), Solid state ophthalmic medication.
Berger Jacob (Los Altos Hills) Clark Robin D. (Palo Alto) Eglen Richard M. (Mountain View) Smith William L. (Sunnyvale) Weinhardt Klaus K. (San Francisco CA), Tricyclic 5-HT3receptor antagonists.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.