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Loperamide hydrochloride patch

A loperamide hydrochloride patch, loperamide hydrochloride technology, applied in the direction of anti-inflammatory agents, non-central analgesics, medical preparations of non-active ingredients, etc., can solve the problems of product stability and performance decline, and achieve High transdermal rate and efficiency, high bioavailability

Inactive Publication Date: 2018-03-23
广州市桐晖药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the preparation prepared by this method has higher requirements on the environment and packaging materials during storage. For example, when the air humidity is high, the moisture in the air can react with the sodium bicarbonate in the preparation to generate carbon dioxide, resulting in the stability of the product. decline

Method used

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  • Loperamide hydrochloride patch
  • Loperamide hydrochloride patch

Examples

Experimental program
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Effect test

Embodiment

[0027] Table 1

[0028]

[0029] All examples, comparative examples and comparative examples all contain the same amount of loperamide hydrochloride to ensure the comparability of the tests.

[0030] The above-mentioned examples and comparative examples were prepared according to conventional patch preparation methods.

[0031] The comparative example is prepared by adopting the prescription and method of CN101224206.

experiment example

[0032] Experimental example: Determination of release amount of loperamide hydrochloride in patch

[0033] The above patch was carried out in vitro transdermal test according to the experimental method introduced in "Transdermal Drug Delivery Preparation" (Liang Bingwen, China Medical Science and Technology Press, published in September 1992, page 252).

[0034] Experimental equipment: FRANZ transdermal diffusion instrument (model TK-60B, Shanghai Kaikai Technology Trading Co., Ltd.)

[0035] Experimental carrier: freshly prepared guinea pig rib-back full-thickness skin (preparation method refers to "transdermal drug delivery preparation" Liang Bingwen, China Medical Science and Technology Press, published in September 1992, page 252)

[0036] Number of samples: 5 (select 5 samples in parallel for the test product of each embodiment or comparative example patch)

[0037] Patch surface area: 10cm 2

[0038] Diffusion medium: pH6.2 phosphate buffer

[0039] Determination met...

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Abstract

The invention discloses a loperamide hydrochloride patch, and belongs to the technical field of preparations. The loperamide hydrochloride patch sequentially comprises a backing layer, at least one medicament-containing adhesive layer and a release gasket layer, wherein the medicament-containing adhesive layer comprises polyisobutylene substrate containing loperamide hydrochloride and other pharmaceutically acceptable components, and the amount of the loperamide hydrochloride is 0.5 to 2.5 percent (w / w) of the weight of the medicament-containing adhesive layer. The transdermal patch has a unique advantage in the percutaneous penetration rate of the loperamide hydrochloride, as well as higher sustained and uniform medicament release performance.

Description

technical field [0001] The invention relates to the technical field of preparations, in particular to a loperamide hydrochloride patch. Background technique [0002] Loperamide, chemical name N,N-dimethyl-α,α-diphenyl-4-(p-chlorophenyl)-4-hydroxy-1-piperidine butyramide, molecular formula C 29 h 33 ClN 2 o 2 . Loperamide is an opioid receptor agonist, which antagonizes smooth muscle contraction by stimulating the mu-opioid receptors on the intestinal wall and preventing the release of acetylcholine and prostaglandins, thereby reducing intestinal peristalsis and secretion and prolonging the retention time of intestinal contents. Purpose. [0003] In recent years, studies have found that loperamide hydrochloride has neurokinin 2 (NK 2 ) and neurokinin 3 (NK 3 ) antagonist-like effect (Michael J Keiser, Bryan L Roth, Blaine N Armbruster, et al.Relating protein pharmacology by ligand chemistry, NATURE BIOTECHNOLOGY, 2007, 25: 197-206), can be used to treat acute trauma ca...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/22A61K31/451A61P29/00A61P17/00A61P17/04A61P1/08A61P25/00
CPCA61K9/7023A61K31/451A61K47/22
Inventor 张彤丽
Owner 广州市桐晖药业有限公司
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