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US 2014/0371187 A1Published application
Semi-solid delivery vehicle and pharmaceutical compositions
AssigneeHeron Therapeutics, Inc.
InventorsSteven Y. Ng, Hui-Rong Shen, Jorge Heller
Life of this patent
Estimating the term…
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.
Claims25
A pharmaceutical composition comprising:
- (A) semi-solid delivery vehicle, comprising:
- (i) a polyorthoester of formula I or formula II
- 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:
- where:
- p is an integer of 1 to 20;
- R5 is hydrogen or C1-4 alkyl;
- and
- R6 is:
- 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:
- R3 is:
- 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-C12 alkylene;
- R11 is hydrogen or C1-6 alkyl and R12 is C1-C6 alkyl;
- or R11 and R12 together are C3-10 alkylene;
- and
- R4 is the residue of a diol containing at least one functional group independently selected from amide, imide, urea, and urethane groups;
- in which at least 0.01 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;
- and
- (B) an anesthetic agent.
33 more elements
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Dependencies are inferred from the claim text.