Details for Patent: 8,252,304
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Title: | Semi-solid delivery vehicle and pharmaceutical compositions for delivery of granisetron |
Abstract: | 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. |
Inventor(s): | Ng; Steven Y. (San Francisco, CA), Shen; Hui Rong (Fremont, CA), Heller; Jorge (Ashland, OR) |
Assignee: | A. P. Pharma, Inc. (Redwood City, CA) |
Filing Date: | Sep 22, 2009 |
Application Number: | 12/564,881 |
Claims: | 1. A pharmaceutical composition comprising: (A) semi-solid delivery vehicle, comprising: (i) a polyorthoester consisting of formula I ##STR00023## where: R* is ethyl; n is an integer of 5 to 1000; and A is R.sup.1 or R.sup.3 where R.sup.1 is: ##STR00024## where: p is an integer of 1 to 20; R.sup.5 is hydrogen; and R.sup.6 is: ##STR00025## where: s is an integer of 0 to 10; R.sup.3 is: ##STR00026## 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 R.sup.1; 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 R.sup.1. 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. |