Compound contraceptive patch containing drospirenone and estrogen, preparation method and application

A drospirenone and compound technology, applied in the field of compound contraceptive patch and its preparation, can solve the problems of poor compliance, frequent use and the like

Active Publication Date: 2021-05-18
SHANGHAI CHANGHAI HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Overcome the shortcomings of frequent use and poor compliance of compound drospirenone oral contraceptives

Method used

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  • Compound contraceptive patch containing drospirenone and estrogen, preparation method and application
  • Compound contraceptive patch containing drospirenone and estrogen, preparation method and application
  • Compound contraceptive patch containing drospirenone and estrogen, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Such as figure 1 As shown, the compound contraceptive patch 10 is composed of a backing layer 11 , an anti-adhesive layer 13 and a drug-loaded layer 12 . The drug-loaded layer 12 is coated on the backing layer 11, the anti-adhesive layer 13 is covered on the drug-loaded layer 12, and the anti-adhesive layer 13 is peeled off during use. Ketones and estrogen act as a synergistic contraceptive. The specific formulation of the drug on the drug-loaded layer 12 is shown in Example 2-Example 5.

Embodiment 2

[0043] Prescription: drospirenone 0.3g, ethinylestradiol 6mg, azone 0.15g, polyacrylate pressure-sensitive adhesive 6g.

[0044] Preparation method: Add drospirenone and ethinyl estradiol to 4 g of ethyl acetate, stir to dissolve, and obtain a liquid medicine for later use. Add polyacrylate pressure-sensitive adhesive and azone into the drug solution, stir at 800 rpm / min for 30 minutes, and place to degas to obtain drug-containing glue. Apply the drug-containing glue on the release layer, dry at 50°C for 30 minutes, and cover the backing layer to obtain the product. The anti-adhesive layer adopts the 9744 type release film of the American 3M Company, and the backing layer adopts the 9680 type backing film of the American 3M Company. Prepared to contain drospirenone 1.14mg / cm 2 , ethinyl estradiol 0.023mg / cm 2 patch.

[0045]Measurement of permeation rate in vitro: Using a Franz vertical diffusion cell, the patch was attached to the horny layer of nude mouse skin, sandwiche...

Embodiment 3

[0047] Prescription: drospirenone 1g, ethinylestradiol 10mg, menthol 0.1g, isopropyl myristate, polyisobutylene pressure-sensitive adhesive 10g.

[0048] Preparation method: Add drospirenone and ethinyl estradiol to 8 g of acetone, stir to dissolve, and obtain a medicinal solution for later use. Add polyisobutylene pressure-sensitive adhesive, menthol and isopropyl myristate to the liquid medicine, stir at a speed of 600 rpm / min for 40 minutes, place to degas, and obtain the liquid glue containing the medicine. Apply the drug-containing glue on the release layer, dry at 70°C for 30 minutes, and cover the backing layer to obtain the product. The anti-adhesive layer adopts the 9748 type release film of the 3M Company of the United States, and the backing layer adopts the 9718 type backing film of the 3M Company of the United States. Prepared to contain drospirenone 0.73mg / cm 2 , ethinyl estradiol 0.042mg / cm 2 patch.

[0049] Measurement of permeation rate in vitro: Using a F...

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Abstract

The invention relates to the technical field of medicine, in particular to a compound contraceptive patch containing drospirenone and estrogen, a preparation method and application thereof. The compound contraceptive patch provided by the present invention is composed of a backing layer, an anti-adhesive layer and a drug-loaded layer, the drug-loaded layer is coated on the backing layer, the anti-adhesive layer is covered on the drug-loaded layer, and the anti-adhesive layer is peeled off during use The contraceptive drug in the drug-loaded layer includes drospirenone as a contraceptive active ingredient and estrogen as a synergistic contraceptive effect, and also includes a penetration enhancer and a drug-loaded material. The contraceptive patch of the present invention is easy to use, reduces the frequency of administration, improves the compliance of users, avoids gastrointestinal tract irritation and liver first-pass effect caused by oral administration, and can maintain the stability of the drug for a long time Compared with the marketed compound drospirenone oral contraceptives, it has obvious advantages.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound contraceptive patch containing drospirenone and estrogen, a preparation method and application thereof. Background technique [0002] Combined hormonal contraceptives, which combine progestin and estrogen, are currently the most widely used form of contraception worldwide. Most of the first, second, and third-generation progestogens currently in clinical use are testosterone derivatives. These compounds have no receptor selectivity, and in addition to progesterone activity, they also have other side effects. [0003] Drospirenone is an aldosterone derivative that binds to progesterone receptors more selectively and specifically, and acts more like natural progesterone. Compared with the 1st to 3rd generation progestogens, these progestogens have no androgenic, estrogenic or glucocorticoid activity, so they are safer. [0004] The combined oral contraceptive of drosp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/585A61K31/565A61K31/567A61K31/566A61P15/16
CPCA61K9/7023A61K31/565A61K31/566A61K31/567A61K31/585A61K2300/00
Inventor 高申强磊宫春爱夏清明李艳李国瑞张丽娟
Owner SHANGHAI CHANGHAI HOSPITAL
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