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US 2003/0212148 A1Published application
Pharmaceutical compositions using semi-solid delivery vehicle
AssigneeA.P. Pharma, Inc.
InventorsSteven Y. Ng, Hui-Rong Shen, Jorge Heller
Life of this patent
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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.
Claims24
A pharmaceutical composition, comprising:
- (a) an active agent;
- and
- (b) a semi-solid delivery vehicle comprising:
- (i) a polyorthoester of formula I or formula II
- 16
- where:
- R is a bond, —(CH2)a—, or —(CH2)b—O—(CH2)c—;
- where a is an integer of 1 to 10, and b and c are independently integers of 1 to 5;
- R* is a C1-4 alkyl;
- n is an integer of at least 5;
- and
- A is R1, R2, R3, or R4, where
- R1 is:
- 17
- where:
- p is an integer of 1 to 20;
- R5 is hydrogen or C1-4 alkyl;
- and
- R6 is:
- 18
- where:
- s is an integer of 0 to 30;
- t is an integer of 2 to 200;
- and
- R7 is hydrogen or C1-4 alkyl;
- R2 is:
- 19
- R3 is:
- 20
- where:
- x is an integer of 0 to 30;
- y is an integer of 2 to 200;
- R8 is hydrogen or C1-4 alkyl;
- R9 and R10 are independently C1-12 alkylene;
- R11 is hydrogen or C1-6 alkyl and R12 is C1-6 alkyl;
- or R11 and R12 together are C3-10 alkylene;
- and
- R4 is a diol containing at least one functional group independently selected from amide, imide, urea, and urethane groups;
- in which at least 0.1 mol percent of the A units are of the formula R1, and
- (ii) a pharmaceutically acceptable, polyorthoester-compatible liquid excipient selected from polyethylene glycol ether derivatives having a molecular weight between 200 and 4000, polyethylene glycol copolymers having a molecular weight between 400 and 4000, mono-, di-, or tri-glycerides of a C2-19 aliphatic carboxylic acid or a mixture of such acids, alkoxylated tetrahydrofurfuryl alcohols and their C1-4 alkyl ethers and C2-19 aliphatic carboxylic acid esters, and biocompatible oils.
37 more elements
Dependencies are inferred from the claim text.