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Preparation for percutaneous administration and preparation method and application thereof

A technology for drug delivery and preparation, applied in the field of transdermal drug delivery preparations and preparations containing paeoniflorin, can solve the problems of preparation stability, bioavailability difficult to meet requirements, unclear active ingredients, and difficulty in recovering viscosity, etc. The effect of lasting and stable drug concentration, improving bioavailability and convenient administration

Active Publication Date: 2012-08-15
北大世佳科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the ingredients contained in traditional Chinese medicine are complex and the active ingredients are not clear. Most of the transdermal drug preparations of traditional Chinese medicine are used as crude extracts. The preparation process is simple, and the stability and bioavailability of the preparations are difficult to meet the requirements.
Moreover, some commercially available adhesive plasters for external use are too viscous, so they tend to stick to body hair when used, and it is difficult to restore the viscosity to continue to use, and long-term use may cause irritation or allergies such as skin whitening, itching, and erythema.

Method used

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  • Preparation for percutaneous administration and preparation method and application thereof
  • Preparation for percutaneous administration and preparation method and application thereof
  • Preparation for percutaneous administration and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 preferred paeoniflorin patch and preparation method thereof

[0047] Prescription: the following components are parts by weight

[0048] Paeoniflorin 1.5 parts

[0049] Carbomer (U10) 0.2 parts

[0050] Sodium polyacrylate (7S) 1.0 parts

[0051] Aluminum chloride 0.2 parts

[0052] Citric acid 0.015 parts

[0053] Glycerin 2.26 parts

[0054] Azone 0.5 parts

[0055] Propylene glycol 4 parts

[0056] 7 parts water

[0057] Ethylparaben 0.0021 parts

[0058] Preparation:

[0059] According to the prescription, ethylparaben is fully dissolved in distilled water and used as the water phase for later use; carbomer, paeoniflorin and appropriate amount of water phase are fully swollen and dispersed uniformly to obtain mixture I; sodium polyacrylate, glycerin, azone, propylene glycol and An appropriate amount of water was mixed uniformly to obtain mixture II; citric acid, aluminum chloride and the remaining water were mixed and dissolved to obtain mixtu...

Embodiment 2

[0062] Preferred paeoniflorin patch of embodiment 2 and preparation method thereof

[0063] Prescription: the following components are parts by weight

[0064] Paeoniflorin 1.0 part

[0065] Carbomer (980) 0.25 parts

[0066] Sodium polyacrylate (7M) 0.8 parts

[0067] Aluminum hydroxide 0.018 parts

[0068] Tartaric acid 0.02 parts

[0069] Glycerin 2.5 parts

[0070] Azone 0.5 parts

[0071] 1 part propylene glycol

[0072] 7.5 parts of water

[0073] Methylparaben 0.002 parts

[0074] Preparation:

[0075] Take methylparaben according to the prescription and fully dissolve it in distilled water for later use; prepare according to the preparation method of Example 1, and obtain paeoniflorin-containing 15.7mg / cm 2 The patch has a water content of about 8.9%, just pack it.

Embodiment 3

[0076] Embodiment 3 preferred paeoniflorin patch and preparation method thereof

[0077] prescription:

[0078] Paeoniflorin 0.8 parts

[0079] 0.1 parts of polyvinyl alcohol

[0080] Cross-linked sodium polyacrylate (NP-700) 0.8 parts

[0081] Magnesium hydroxide 0.025 parts

[0082] Tartaric acid 0.02 parts

[0083] Sorbitol 2.8 parts

[0084] 0.7 parts of 1-methyl-2-pyrrolidine

[0085] 6.8 parts of water

[0086] Preparation:

[0087] Prepared according to the preparation method of Example 1, the difference is that there is no preservative, that is, 12.5 mg / cm of paeoniflorin is obtained. 2 The patch can be packaged.

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Abstract

The invention relates to a paeoniflorin preparation for percutaneous administration and a preparation method. The paeoniflorin preparation percutaneous administration is prepared by mixing paeoniflorin, skeleton materials, polyacrylate and a percutaneous absorption enhancer in certain proportion. The preparation for percutaneous administration has high drug-loading rate, can effectively maintain blood concentration of a medicament in a body, can significantly improve the bioavailability of the paeoniflorin, is convenient to use, improves the adaptability of a patient, and has significant effect of preventing and treating cardiovascular and cerebrovascular diseases, particularly coronary heart disease.

Description

technical field [0001] The invention relates to a transdermal preparation containing a single active ingredient and its preparation method and use, in particular to a paeoniflorin-containing transdermal preparation, its preparation method and use. Background technique [0002] Paeoniflorin is a hygroscopic, amorphous powder extracted from Radix Paeoniae Rubra, Radix Paeoniae Alba, and Cortex Moutan. It can be used to treat acute myocardial ischemia, dilate coronary arteries, increase coronary blood flow, and improve myocardial tolerance to hypoxia. It is especially suitable for the treatment of coronary heart disease (application number: CN200310121025.9, a paeoniflorin injection and its preparation method and application). In addition, paeoniflorin can also be used for: 1) prevention and treatment of nervous system diseases such as Parkinson's disease (ZL200410025717.8, medicinal use of paeoniflorin), 2) prevention of postoperative intestinal adhesion (CN200510042410.3, ne...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K9/00A61K9/70A61P9/10A61P9/00
Inventor 周亚伟
Owner 北大世佳科技开发有限公司
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