# US 10,500,281 B2 · Injectable long-acting local anesthetic semi-solid formulations and its compositions

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- Number: US 10,500,281 B2
- Document ID: US10500281B2
- Status: Granted
- Kind: B2
- Application number: 14/839,352
- Filed: 2015-08-28
- Published: 2015-12-24
- Granted: 2019-12-10
- Earliest claimed: 2013-02-28
- Assignees: Mira Pharma Corporation
- Applicants: Mira Pharma Corporation
- Inventors: Hui Rong Shen; Na Gan
- Web page: https://patentgrep.com/patent/US10500281B2

## CPC

- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61P 23/02: Local anaesthetics
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

What is disclosed is a semi-solid controlled release pharmaceutical composition containing biocompatible and bioerodible semi-solid lipid matrix incorporating local anesthetics agents to form a semi-solid solution, a method of using the pharmaceutical composition to treat, and a method of making the pharmaceutical composition.

## Claims

### Claim 1

A pharmaceutical composition consisting of
5-14% bupivacaine,
63-76% a mixture of ricinoleic acid partial glycerides (S701), and
17-27% a mixture of C12-C18 fatty acids (G39/01);
wherein the pharmaceutical composition consists of a biocompatible, bioerodible, homogeneous, semi-solid gel; and wherein the semi-solid gel consists of a soft paste with a viscosity of 408-1095 cPs at 30° C., and forms a depot in an aqueous buffer that releases less than 80% of the bupivacaine in five days when measured in vitro at 37° C.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1 consisting of
72% S701,
18% G39/01, and
10% bupivacaine.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1 consisting of
63% S701,
27% G39/01, and
10% bupivacaine.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1 consisting of
76% S701,
19% G39/01, and
5% bupivacaine.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1 consisting of
69% S701,
17% G39/01, and
14% bupivacaine.