Topical transdermal dexmedetomidine compositions and methods of use thereof

A technology of dexmedetomidine and its composition, which is applied in the field of external transdermal dexmedetomidine composition and its application, and can solve the problem of unsuitable analgesics, no sedative effect, analgesic preparations, etc. question

Inactive Publication Date: 2012-10-24
RECRO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite the analgesic properties of dexmedetomidine, formulations for use as an analgesic are not commercially available
And for a number of reasons, commercially available injectable formulations are not suitable for self-administered analgesics
Thus, there is a continuing unmet need for dexmedetomidine-based analgesics that, for example, can be administered autonomously to produce analgesia (or otherwise treat or prevent pain), while no sedation

Method used

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  • Topical transdermal dexmedetomidine compositions and methods of use thereof
  • Topical transdermal dexmedetomidine compositions and methods of use thereof
  • Topical transdermal dexmedetomidine compositions and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1a

[0046] Example 1a - Placebo Transdermal Gel Formulation (Vehicle)

[0047] Exemplary ingredients and methods used to prepare 50 g of Methyl Salicylate / Menthol Hydroalcoholic Clear Gel.

[0048] Table A: 50 g methyl salicylate / menth hydroalcoholic clear gel (RECRO1-45)

[0049]

[0050] Table B: Preparation of 50 g methyl salicylate / menth hydroalcoholic clear gel (RECRO1-45)

[0051]

[0052]

[0053] In this example, the inventors commented as follows: 1) pH = 0.592g, and a large amount of white mass (white mass) was produced after adding water; and 2) Adding water to rehydrate or reconstitute the gel also produced precipitation . The precipitation effect is thought to result from the insolubility of methyl salicylate after more water is added. Furthermore, the occurrence of precipitation is at least partly pH dependent.

Embodiment 1b

[0054] Example 1b - Transdermal Dexmedetomidine Gel Formulation

[0055] Table C: 50 g gel formulation (RECRO1-53) at a concentration of [0.5 mg / g Dex HCl]

[0056] Component No.

[0057] Table D: Preparation of 50 g gel formulation (RECRO1-53) at a concentration of [0.5 mg / g Dex HCl]

[0058] steps

[0059] In the method of this example, several observations were made on step B (before adding component No. 2 dexmedetomidine hydrochloride): 1) the gel preparation became cloudy; The viscosity of the gel obtained in step B is reduced compared to the gel. To resolve the turbidity that occurred in 1, triethanolamine was added and this worked. In this example, triethanolamine was added at a ratio of 0.463 g of triethanolamine (identified as batch number XT0007) to 32.532 g of the gel obtained in step C.

Embodiment 2、3 and 4-De

[0060] Example 2, 3 and 4 - Dex HCl (dexmedetomidine hydrochloride) topical (topical) cream formulation

[0061] The use of a base placebo cream formulation to prepare an active dexmedetomidine hydrochloride transdermal formulation is further described herein.

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PUM

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Abstract

Analgesic topical formulations of dexmedetomidine and methods of use thereof in the treatment and management of pain and other conditions.

Description

[0001] References to related applications [0002] This application claims priority to US Provisional Patent Application 61 / 293,440, filed January 8, 2010, which is hereby incorporated by reference in its entirety. [0003] Not applicable. Background technique [0004] Dexmedetomidine, 5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, is a non-narcotic drug with sedative and analgesic properties alpha 2 - Adrenoceptor agonists. [0005] [0006] Dexmedetomidine [0007] Currently, dexmedetomidine is only commercially available as an injectable formulation for sedation and can only be administered intravenously by a healthcare professional. Despite the analgesic properties of dexmedetomidine, formulations for use as an analgesic are not commercially available. And for a number of reasons, commercially available injectable formulations are not suitable for self-administered analgesics. Thus, there is a continuing unmet need for dexmedetomidine-based analgesics that, fo...

Claims

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Application Information

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IPC IPC(8): A61K31/415A61K9/06A61P35/00A61P25/06A61P25/00
CPCA61K47/20A61K9/08A61K9/0014A61K31/415A61P25/00A61P25/04A61P25/06A61P29/00A61P35/00
Inventor 杰拉尔丁·A·亨伍德兰德尔·J·马克克里斯托弗·T·萨尔小约翰·J·科伦格
Owner RECRO PHARMA
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