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Topical film-forming spray

A topical, film-forming polymer technology, applied in the direction of aerosol delivery, non-active ingredient medical preparations, active ingredient-containing medical preparations, etc., can solve skin irritation, occlusion and other problems

Active Publication Date: 2018-11-02
GRACE THERAPEUTICS LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, conventional topical spray formulations tend to remain at the site of application for only a short time, so active agents absorbed through the skin are only temporarily effective
Additionally, known topical spray formulations may cause skin irritation or occlusion problems

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0123] In certain preferred embodiments, the topical spray formulations of the present invention include a local anesthetic as an active agent. In certain embodiments, it is especially preferred that the local anesthetic is bupivacaine hydrochloride. It was surprisingly found that the topical spray formulations were only dose proportional when using the bupivacaine salt; the bupivacaine base incorporated into the topical spray compositions of the present invention was not dose proportional.

[0124] In certain preferred embodiments, the bupivacaine hydrochloride topical spray formulation includes a sufficient concentration of bupivacaine such that a dose of about 0.1 mg to about 50 mg is applied to the desired location on the patient's skin. In certain preferred embodiments, the dose of bupivacaine is about 10 mg based on bupivacaine hydrochloride. The dosage regimen may be, for example, 5 sprays (each containing 10 mg of bupivacaine hydrochloride) in 5 different areas. In o...

Embodiment 1

[0129] In Example 1, a Bupivacaine HCl topical spray formulation was prepared using the ingredients listed in Table 1.

[0130]Film-forming sprays are prepared by adding the drug of interest, a non-volatile solvent, and a penetration enhancer to a solvent while stirring the solution to ensure complete dissolution of the drug and other excipients. The solvent used was ethanol (95%). After obtaining a clear solution, polymer and other optional excipients are added. After all excipients have been added, the solution is stirred to ensure complete dissolution and / or hydration of the polymer prior to use. Store the formulation in glass vials tightly sealed with caps or spray pumps.

[0131] Table 1

[0132]

[0133]

[0134] The process of preparing the formulation is as follows:

[0135] Mix the drug, propylene glycol, (highly purified diethylene glycol monoethyl ether commercially available from Gattefosse; it is a highly purified hydrophilic solvent for pharmaceutical...

Embodiment 2- Embodiment 5

[0140] In Examples 2-5, Bupivacaine HCl topical spray formulations were prepared using the ingredients listed in Table 3 and the hydrophilic polymer Avicel RC-591 in the presence of water and / or ethanol as solvent (CMC sodium and MCC) and povidone K-30 (PVP) for additional studies.

[0141] table 3

[0142]

[0143] The process of preparing the formulation is as follows:

[0144] While stirring the RC591 (microcrystalline cellulose and sodium carboxymethylcellulose NF, Ph. Eur. commercially available from FMC Biopolymer) (except Example 5) and povidone K30 (polyvinylpyrrolidone) were added to purified water and mixed until The polymer is fully hydrated. Drug, propylene glycol, transcutol (except Example 4), penetration enhancer and menthol were added in ethanol or purified water with stirring and mixed until a clear solution formed. The clear solution with drug was added to the polymer dispersion while stirring until the drug solution was uniformly dispersed with the t...

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PUM

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Abstract

A polymeric bio-adhesive film forming topical spray formulation providing a modified, pulsatile (e.g., biphasic) release of the active agent(s) once the solvent evaporates and the film sets, e.g., onhuman skin is disclosed. In certain embodiments, the active agent is bupivacaine hydrochloride.

Description

technical field [0001] The present invention relates to a film-forming composition that forms a stable film when applied (eg sprayed) on a surface (eg skin). A stable film is formed by evaporating the solvent and adheres to the surface. Background technique [0002] Topical films containing therapeutic agents have been developed for various purposes in the pharmaceutical field. For example, Tipton et al. (U.S. Pat. Nos. 5,632,727 and 5,792,469) describe formulations of biodegradable film dressings with or without additional therapeutic agents, composed of at least one biodegradable / biodegradable membrane dressing in a pharmaceutically acceptable solvent. A liquid composition of an erodable thermoplastic polymer is formed. The film is formed by dispensing, preferably by spraying, a liquid composition onto the tissue site and contacting the liquid composition with an aqueous-based fluid to coagulate or solidify the film onto the human or animal tissue. Biodegradable films c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K9/70A61K31/16A61K31/167A61K31/44A61K47/10A61K47/32A61K47/36A61K47/40
CPCA61K47/08A61K47/10A61K47/12A61K47/14A61K47/26A61K47/38A61K31/4458A61K31/7036A61K9/7015A61K31/135A61K31/167A61K31/445A61K31/4468A61K31/566A61K31/568A61K31/7048A61K47/32A61K45/06A61P23/02A61K2300/00A61K9/0014A61K47/22A61K47/34
Inventor S·乔治·科塔伊尔安雷什·库马尔普拉桑纳·松森卡维马尔·卡武鲁
Owner GRACE THERAPEUTICS LLC
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