Process for preparing a semi-solid delivery vehicle comprising granisetron
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/439
A61K-031/435
A61K-031/46
A61K-031/416
A61K-047/30
A61P-001/08
C07D-319/04
출원번호
US-0279949
(2011-10-24)
등록번호
US-8252306
(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 :
2인용 특허 :
35
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 process for the preparation of a pharmaceutical composition comprising: (A) 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
1. A process for the preparation of a pharmaceutical composition comprising: (A) 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; the process comprising mixing the components (A)(i) and (A)(ii) and (B) to form the composition. 2. The process of claim 1, wherein the process comprises: (1) warming the polyorthoester;(2) dissolving the granisetron in the polyethylene glycol monomethyl ether to form a solution; and(3) mixing the polyorthoester and the solution to obtain a homogeneous mixture. 3. The process of claim 1, wherein the polyethylene glycol monomethyl ether has a molecular weight between 200 and 4000. 4. The process of claim 3, wherein the polyethylene glycol monomethyl ether comprises polyethylene glycol monomethyl ether 550. 5. The process of claim 4, wherein the total concentration of the polyethylene glycol monomethyl ether is 5-60 weight % of the composition. 6. The process of claim 1, wherein the polyorthoester is 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). 7. The process of claim 1, wherein the composition comprises 78.4 weight % polyorthoester, 19.6 weight % polyethylene glycol monomethyl ether and 2 weight % granisetron. 8. The process of claim 1, wherein p is an integer of 1 to 7 in a portion of the units of formula I. 9. The process of claim 1, wherein x is 2 in a portion of the units of formula I. 10. The process of claim 1, wherein s is 2 in a portion of the units of formula I. 11. The process of claim 1, wherein the total concentration of the polyethylene glycol monomethyl ether is 5% to 80% weight percent of the composition. 12. The process of claim 1, wherein the mixing is performed at a temperature between about 5° C. and 200° C. 13. The process of claim 1, wherein: the polyorthoester is 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); andthe polyethylene glycol monomethyl ether has a molecular weight between 200 and 4000. 14. The process of claim 1, wherein about 0.1-25 mol percent of the A units are of the formula R1.
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