Details for Patent: 8,715,710
✉ Email this page to a colleague
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: | Heron Therapeutics, Inc. (Redwood City, CA) |
Filing Date: | Jul 18, 2012 |
Application Number: | 13/552,083 |
Claims: | 1. A semi-solid pharmaceutical composition comprising a polyorthoester, 10-50 weight percent polyethylene glycol monomethyl ether having a molecular weight in a range of 200 to 4,000, and about 1-5 weight percent granisetron, the polyorthoester comprising subunits selected from: ##STR00023## where x is an integer from 1-4, the total amount of p is an integer from 1-20, s is an integer from 1-4, the mole percentage of .alpha.-hydroxyacid containing subunits in the polyorthoester is from about 0.1 to about 25 mole percent, and the polyorthoester has a molecular weight in a range of 1000 to 10,000. 2. A semi-solid pharmaceutical composition comprising a polyorthoester, 10-50 weight percent polyethylene glycol monomethyl ether having a molecular weight in a range of 200 to 4,000, and 1-5 weight percent granisetron, where the polyorthoester comprises alternating residues of 3,9 -diethyl-3,9-2,4,8,10-tetraoxaspiro[5.5] undecane-3,9-diyl: ##STR00024## and a diol-ate residue of triethylene glycol or of triethylene glycol diglycolide prepared by reacting triethylene glycol with from 0.5 to 10 molar equivalents of glycolide at 100-200.degree. C. for about 12 hours to 48 hours, where the mole percentage of glycolide-containing subunits in the polyorthoester is from about 0.1 to about 25 mole percent, and the polyorthoester has a molecular weight of 1000 to 10,000. 3. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the polyethylene glycol monomethyl ether has a molecular weight of about 550. 4. The semi-solid pharmaceutical composition of claim 1 or claim 2, comprising from 2-3 weight percent granisetron. 5. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the granisetron is in the form of a free base. 6. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the granisetron is in the form of an acid addition salt. 7. The semi-solid pharmaceutical composition of claim 1 or claim 2, comprising 78.4 weight percent polyorthoester, 19.6 weight percent polyethylene glycol monomethyl ether and 2 weight percent granisetron. 8. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the polyorthoester has a molecular weight of about 6,500. 9. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the composition is stable upon irradiation. 10. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the composition is stable upon sterilization. 11. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the granisetron is in the form of a solid having a particle size of less than 100 microns. 12. The semi-solid pharmaceutical composition of claim 1 or claim 2, wherein the composition is capable of being dispensed from a 16-25 gauge needle. 13. The semi-solid pharmaceutical composition of claim 1 or claim 2, effective to release the granisetron in a sustained and controlled manner after administration. |