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US 7,115,565 B2Granted
Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability
AssigneePharmacia & Upjohn Company
InventorsPing Gao, Walter Morozowich
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Abstract
Pharmaceutical compositions suitable for oral administration comprising paclitaxel, a solvent, a surfactant, a substituted cellulosic polymer, and optionally but preferably a P-glycoprotein inhibitor. The composition may further comprise a diglyceride or mixture of diglyceride and monoglyceride. The composition generates a supersaturated paclitaxel microemulsion upon contact with water resulting in improved oral bioavailability of paclitaxel.
Claims61
A composition for administering paclitaxel, wherein:
- the composition is self-emulsifying;
- the composition comprises:
- (a) a paclitaxel or an analog thereof;
- (b) a pharmaceutically acceptable surfactant;
- (c) a pharmaceutically acceptable solvent;
- and
- (d) a substituted cellulosic polymer;
- the paclitaxel and surfactant are present in a ratio of from about 1:3 to about 1:20 by weight;
- and
- the substituted cellulosic polymer and paclitaxel are present in a ratio of from about 50:1 to about 0.1:1 by weight.
7 more elements
A method of treating a patient suffering from cancer and in need of treatment, wherein:
- the method comprises administering a self-emulsifying composition to the patient;
- the composition comprises:
- a) a chemotherapeutically effective amount of paclitaxel,
- b) a pharmaceutically acceptable surfactant,
- c) a pharmaceutically acceptable solvent, and
- d) a substituted cellulosic polymer;
- the paclitaxel and surfactant are present in a ratio of from about 1:3 to about 1:20 by weight;
- and
- the substituted cellulosic polymer and paclitaxel are present in a ratio of from about 50:1 to about 0.1:1 by weight.
6 more elements
Dependencies are inferred from the claim text.