Compositions for transdermal administration of streoid drugs

A technology for steroid drug and transdermal drug delivery, which can be applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. low cost effect

Inactive Publication Date: 2000-02-16
LG CHEM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has the following disadvantages: the drug release rate is high at the beginning and then decreases significantly
To alleviate this problem, crystal formation inhibitors such as polyvinylpyrrolidone and polyvinylpyrrolidone-vinyl acetate copolymers have been used, but very limited effects have been observed (Ma, X. et al., supra, 142, 115-119 (1996)

Method used

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  • Compositions for transdermal administration of streoid drugs
  • Compositions for transdermal administration of streoid drugs
  • Compositions for transdermal administration of streoid drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 4 and comparative example 7-10

[0046] Five transdermal compositions were prepared and tested according to the method of Reference Example 1, but human cadaver skin was used, and 3.5% by weight of testosterone was used together with the absorption enhancers listed in Table 4.

[0047] serial number

[0048] As can be seen from the results in Table 4, compared with using TC or SML alone (comparative examples 8 and 9), the present invention contains diethylene glycol monoethyl ether (TC) and sorbitan monolaurate (SML) The composition in which the mixture acts as an absorption enhancer (Example 4) has a significantly higher permeation rate. Embodiment 5-7 and comparative example 11-12

Embodiment 5-7 and comparative example 11-12

[0049] Five transdermal compositions were prepared and tested according to the method of Reference Example 1, but human cadaver skin was used, and 0.8% by weight of estradiol was used together with the absorption enhancers listed in Table 5.

[0050] serial number

[0051] As can be seen from the results in Table 5, the present invention comprises diethylene glycol monoethyl ether (TC) and sorbitan monolaurate (SML) mixture and the combination of TC and SML weight ratio in the range of 1-4 The compounds (Examples 5, 6 and 7) had significantly higher penetration rates of estradiol through human cadaver skin.

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Abstract

A composition for the transdermal administration of a steroid drug containing a therapeutically effective amount of the drug; an absorption promoter consisting essentially of a diethylene glycol ether and a sorbitan ester; and a pharmaceutically acceptable adhesive matrix.

Description

field of invention [0001] The present invention relates to compositions for the transdermal administration of steroidal drugs, wherein mixtures of diethylene glycol ethers and sorbitan esters are used as absorption enhancers; and transdermal preparations comprising the compositions. Background of the invention [0002] Transdermal drug delivery has advantages over conventional oral drug delivery, which is plagued by unpredictable drug absorption rates, metabolic degradation of the drug, and other side effects such as gastrointestinal irritation from the drug itself or its metabolites. That is, transdermal administration can alleviate the above-mentioned problems due to increased bioavailability decreased by the digestive tract, and can release the drug at a controlled rate over a longer predetermined period of time. [0003] In transdermal drug delivery, the stratum corneum of the skin acts as a barrier to the penetration of the drug into the systemic circulatory system. Ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/14A61K9/70A61K31/56A61K31/565A61K31/568A61K47/08A61K47/10A61K47/26
CPCA61K47/26A61K47/10A61K9/7061A61K31/575A61K31/569A61K31/568A61K9/70
Inventor 文哲柳济弼崔美淑崔钟根
Owner LG CHEM LTD
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