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Preparations for external use on the skin containing bupivacaine or a pharmaceutically acceptable salt thereof

A technology of bupivacaine and external preparations, which is applied in the field of pharmaceutical preparations, and can solve the problems of reducing the peeling strength of patches, inconvenient industrial production, and reduced stability of patches.

Active Publication Date: 2020-05-12
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent literature (Patent No. US6224857 B1) discloses a transdermal drug delivery system containing bupivacaine free base. The bupivacaine patch reported in this literature uses polybutylene pressure-sensitive adhesive as the adhesive material, and simultaneously adds A special auxiliary material, sucrose acetate isobutyrate, is used to reduce the peel strength of the patch. The polybutene pressure-sensitive adhesive patch is easy to crystallize, which reduces the content of active ingredients in the effective drug and reduces the stability of the patch. Inconvenience is brought in the use process, and sucrose acetate isobutyrate auxiliary material is difficult for obtaining simultaneously, has improved production cost, has brought great inconvenience for suitability for industrialized production

Method used

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  • Preparations for external use on the skin containing bupivacaine or a pharmaceutically acceptable salt thereof
  • Preparations for external use on the skin containing bupivacaine or a pharmaceutically acceptable salt thereof
  • Preparations for external use on the skin containing bupivacaine or a pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]

[0025] Preparation method: add the prescribed amount of bupivacaine into an appropriate amount of ethyl acetate, and mix to obtain the main drug mixture; mix the prescribed amount of colloid evenly, add the main drug solution into the colloid, stir, and mix evenly; The prepared paste is evenly spread on the anti-adhesive layer, covered with a backing layer, and cut to the required size after the ethyl acetate volatilizes.

Embodiment 2

[0027]

[0028] Note: The volume ratio of ethyl acetate and ethanol is 1:1 to prepare a mixed solution.

[0029] Preparation method: add the prescribed amount of terpene resin into a certain amount of mixed solution of ethyl acetate and ethanol, and stir evenly; add the prescribed amount of bupivacaine into a certain amount of mixed solution of ethyl acetate and ethanol, and stir evenly , to obtain the main drug solution; add the mixed solution obtained above into a container with colloid, continue to stir, and after stirring evenly, apply the prepared paste evenly on the anti-adhesive layer, cover the backing layer, and wait for ethyl acetate After the ester and ethanol volatilize, it is cut to the required size.

Embodiment 3

[0031]

[0032] Note: The volume ratio of ethyl acetate and ethanol is 1:1 to prepare a mixed solution.

[0033] Preparation method: add the prescribed amount of terpene resin into a certain amount of mixed solution of ethyl acetate and ethanol, and stir evenly; add the prescribed amount of bupivacaine into a certain amount of mixed solution of ethyl acetate and ethanol, and stir evenly , to obtain the main drug solution; add the mixed solution obtained above into a container with colloid, and continue to stir. After stirring evenly, apply the prepared paste evenly on the anti-adhesive layer, cover the backing layer, and wait for ethyl acetate After the ester and ethanol volatilize, it is cut to the required size.

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PUM

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Abstract

The invention discloses a skin topical preparation containing bupivacaine or pharmaceutical salt thereof, and provides an external preparation for local administration. The preparation contains active pharmaceutical ingredients, a pressure-sensitive adhesive binder, a diluent and other pharmaceutically acceptable excipients. The adopted pressure-sensitive adhesive binder is an acrylic acid pressure-sensitive adhesive containing hydroxyl, or a silicone pressure-sensitive adhesive or a mixture of the two. The pressure-sensitive adhesive enables the active pharmaceutical ingredients to exist stably and does not chemically react with the active pharmaceutical ingredients, so that drug stability is improved, and clinical application of the preparation is safer and more reliable. Meanwhile, the pressure-sensitive adhesive material can effectively avoid crystallization of a patch, and can also control the viscosity of the patch on the basis of certain content, so that the patch does not fall off easily in use, skin can not be injured when the patch is peeled off, no residue is left on skin, pollution is avoided, and great convenience is brought to patients in use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an external skin preparation containing long-acting local anesthetic bupivacaine or a medicinal salt thereof and a preparation method thereof. Background technique [0002] Pain is an unavoidable reaction of patients during surgical wound healing, which usually lasts for 3-7 days. Most of the existing postoperative pain relief methods are oral analgesic drugs or the use of pain relief pumps, although the above methods can relieve the pain of patients to a certain extent However, after the administration of oral analgesics, the drugs are distributed throughout the body, and only a small amount of drugs reach the wound, which not only has poor analgesic effect, but also causes unnecessary toxicity to other organs and tissues. In addition, patients need to spend more time during wound healing. Taking painkillers every time, using an analgesic pump is not only costly, but als...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K47/32A61K47/34A61K31/445A61P23/02
CPCA61K9/7061A61K9/7069A61K31/445
Inventor 赵焰平纪明文申桂芬杨娜齐连权刘亚男
Owner BEIJING TIDE PHARMA
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