# US 2014/0155434 A1 · Thermogelling anaesthetic compositions

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- Number: US 2014/0155434 A1
- Document ID: US20140155434A1
- Status: Published application
- Kind: A1
- Application number: 14/172,794
- Filed: 2014-02-04
- Published: 2014-06-05
- Earliest claimed: 2010-04-01
- Assignees: Pharmanest AB
- Applicants: Pharmanest AB
- Inventors: Mark Sundberg; Arne Brodin; Nils Kallberg
- Web page: https://patentgrep.com/patent/US20140155434A1

## CPC

- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- 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 9/0034: {Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61L 15/44: Medicaments
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 23/02: Local anaesthetics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61L 2300/402: Anaestetics, analgesics, e.g. lidocaine
- 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)
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a thermogelling pharmaceutical composition comprising local anaesthetics in base form and which is suitable for topical administration. The compositions further comprise a polyoxyethylene castor oil and one or more surfactants to obtain thermogelling characteristics.

## Claims

### Claim 1

A method of treating pain during an obstetric or gynaecological procedure which method comprises:
(i) application to a mucosal surface of a patient in need of such pain treatment of a composition comprising:
1 to 10% by weight of one or more local anaesthetics in base form selected from the group lidocaine, prilocaine and mepivacaine,
said one or more local anaesthetics being solubilized in 10 to 30% by weight of a polyoxyethylene castor oil,
15 to 30% by weight of one or more non-ionic block copolymers of poly(oxyethylene) and poly(oxypropylene) type, and
water,
wherein the pH of the composition is at least the value of the pKa of said one or more local anaesthetics;
wherein said application is carried out by intravaginal, intracervical, pericervical or intrauteral administration of said composition, and
(ii) formation of a thermogel on said mucosal surface.

### Claim 2 (depends on 1)

The method according to claim 1 wherein said application is carried out during an obstetric procedure.

### Claim 3 (depends on 2)

The method according to claim 2 wherein the obstetric procedure is labour.

### Claim 4 (depends on 1)

The method according to claim 1 wherein said application is carried out during a gynaecological procedure.

### Claim 5 (depends on 4)

The method according to claim 4 wherein the gynaecological procedure is an abortion, application of an intrauterine device, a hysteroscopy, in vitro fertilization or a general vaginal examination.

### Claim 6 (depends on 1)

The method according to claim 1 wherein the composition further comprises an additional solubilizer in an amount of 1 to 5% by weight.

### Claim 7 (depends on 6)

The method according to claim 6 wherein the additional solubilizer is a lower alcohol.

### Claim 8 (depends on 6)

The method according to claim 6 wherein the additional solubilizer is selected from the group consisting of glycerol formal, glycofural, polysorbate 80, and ethyl acetate.

### Claim 9 (depends on 1)

The method according to claim 1 wherein the one or more local anaesthetics is lidocaine.

### Claim 10 (depends on 9)

The method according to claim 9 wherein the amount of lidocaine is 1 to 7% by weight.

### Claim 11 (depends on 9)

The method according to claim 9 wherein the amount of lidocaine is 3 to 5% by weight.

### Claim 12 (depends on 1)

The method according to claim 1 wherein the polyoxyethylene castor oil is polyoxyethylene 35 castor oil.

### Claim 13 (depends on 1)

The method according to claim 1 wherein the block copolymers comprise a higher molecular weight poloxamer and a lower molecular weight poloxamer, wherein the higher molecular weight poloxamer and the lower molecular weight poloxamer are present in about equal amounts.

### Claim 14 (depends on 1)

The method according to claim 1 wherein the block copolymers are poloxamer 188 and poloxamer 407.

### Claim 15 (depends on 1)

The method according to claim 1 wherein the composition has an elasticity modulus (G′) below 20 Pa at room temperature and an elasticity modulus (G′) in the range of 50 to 10000 Pa at body temperature.