Indapamide bisoprolol percutaneous patch and preparation method thereof

A technology of bisoprolol and indapamide, applied in the field of medicine, can solve problems such as lack of and hindering the research and development of transdermal patches

Active Publication Date: 2014-11-19
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has been difficult to find an enhancer that can specifically increase the permeability of one drug without affecting the transdermal permeability of another drug.
[0007] The development of many transdermal patches has undoubtedly been hampered by the lack of satisfactory methods for modulating the transdermal permeability of drugs

Method used

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  • Indapamide bisoprolol percutaneous patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 2 g of bisoprolol fumarate was dissolved in 5 ml of distilled water, and 20% (w / v) sodium carbonate aqueous solution was added dropwise until no oily liquid was produced. Use 240ml of ethyl acetate to extract three times, combine the extracts, add an appropriate amount of anhydrous sodium sulfate for dehydration, and then dry by rotary evaporation to obtain bisoprolol free base.

Embodiment 2

[0024] Dissolve 0.1 mol of bisoprolol free base in 40 ml of acetone, add 0.05 mol of maleic acid under stirring, continue to stir for 2 hours, and dry the solvent by rotary evaporation to obtain the bisoprolol maleate ion-pair complex.

Embodiment 3

[0026] Dissolve 0.1 mol of bisoprolol free base in 40 ml of acetone, add 0.05 mol of fumaric acid under stirring, continue to stir for 2 hours, and spin evaporate to dry the solvent to obtain the bisoprolol fumarate ion-pair complex.

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Abstract

The invention belongs to the technical field of medicine and relates to an indapamide bisoprolol percutaneous patch and a preparation method thereof. The indapamide bisoprolol percutaneous patch is composed of a back liner layer, a medicine-carrying pressure-sensitive adhesive layer and an anti-bonding layer. The medicine-carrying pressure-sensitive adhesive layer includes indapamide, bisoprolol free alkali or a organic acid ion pair compound thereof, a pressure-sensitive adhesive and a percutaneous absorption promoter, wherein a total medicine amount of the indapamide, bisoprolol free alkali or the organic acid ion pair compound thereof accounts for 0.5-5.5 wt% of the total weight of the medicine-carrying pressure-sensitive adhesive layer and a molar ratio of the indapamide to the bisoprolol free alkali or the organic acid ion pair compound thereof is 0.5:1-2:1. According to the invention, two-way regulation of a percutaneous penetrating capability of indapamide and bisoprolol in the percutaneous patch can be achieved and equal-speed penetration of the indapamide and the bisoprolol from the percutaneous patch is achieved.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to an indapamide bisoprolol transdermal patch and a preparation method thereof. Background technique: [0002] In the clinical treatment of hypertension, at least 75% of patients need to use combination therapy to achieve the target blood pressure. Combination therapy for hypertension is composed of drugs with different antihypertensive mechanisms, and usually has a better antihypertensive effect than monotherapy. For this reason, a wide variety of antihypertensive preparations have appeared on the market. Given that hypertension is a chronic disease, patient compliance with medication is particularly important. Therefore, it is an ideal choice to prepare a transdermal patch that not only has a good antihypertensive effect, but also can improve patients' medication compliance. [0003] Indapamide, a thiazide diuretic, is prescribed by JNCⅧ as the first-line drug for the treatment...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61K9/70A61P9/12A61K31/138
Inventor 方亮宋文婷权鹏
Owner SHENYANG PHARMA UNIVERSITY
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