Compound contraceptive composition, contraceptive transdermal patch containing composition and preparation method

A technology of a composition and a transdermal penetration enhancer, which is applied in the field of contraceptive transdermal patches and its preparation, can solve the problems of no drug delivery system, poor compliance of users, and high contraceptive failure rate, so as to avoid the first-pass effect, High bioavailability, effect of reducing frequency of dosing

Inactive Publication Date: 2010-05-05
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The composition of desogestrel and estrogen is administered orally once a day, and there are many cases of missed doses, and the compliance of users is poor, so the contraceptive failure rate is high; at the same time, due to oral administration of desogestrel, it cannot Completely metabolized to etonogestrel, so its bioavailability is low
[0003] Chinese patent CN1190351A discloses a transdermal patch and method for administration of progestin alone or in combination with estrogen, but the progestin claimed is 17-deacetyl norgestimate; Chinese patent CN1692122 discloses a novel relying on Pregnenyl ester and its use, but there is no drug delivery system related to the transdermal delivery route; European Patent EP1941866A1 discloses an oral contraceptive spray whose active ingredient contains etonogestrel, but it is in the form of a spray for oral route

Method used

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  • Compound contraceptive composition, contraceptive transdermal patch containing composition and preparation method
  • Compound contraceptive composition, contraceptive transdermal patch containing composition and preparation method
  • Compound contraceptive composition, contraceptive transdermal patch containing composition and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] [Prescription] (based on 1000 tablets)

[0070] Etonogestrel 0.6g, ethinylestradiol 0.6g, polyacrylate pressure-sensitive adhesive 100g, sodium alginate 20g, lauric acid 1g, Eudragit RL (10% trimethylamine chloride methacrylic acid, Rohm, Germany) 3g;

[0071] Preparation:

[0072] Add the drug and sodium alginate to 20g of ethanol to dissolve, and stir at 5000rpm for 0.5 hours to obtain a skeleton storage system;

[0073] In addition, lauric acid and Eudragit RL were added to 5 g of acetone to dissolve, then polyacrylate pressure-sensitive adhesive was added, mixed evenly, and degassed to obtain a pressure-sensitive adhesive solution.

[0074] Then, mix the skeleton-type reservoir system obtained above with the pressure-sensitive adhesive solution, stir at 10,000 rpm for 1 hour, mix and disperse, and degas to obtain the drug-containing adhesive solution.

[0075] Apply the above-mentioned drug-containing viscose solution on the release layer, dry at 80°C for 1 hour, ...

Embodiment 2

[0080] [Prescription] (based on 1000 tablets)

[0081] Etonogestrel 3g, ethinyl estradiol 1g, silicone pressure sensitive adhesive 30g, hydroxypropyl cellulose 10g, azone 3g, β-cyclodextrin 1g;

[0082] Preparation method: Add drug and hydroxypropyl cellulose to 20g ethanol to dissolve, stir at 8000rpm for 1 hour to obtain a skeleton storage system;

[0083] In addition, add azone and β-cyclodextrin to 10 g of ethanol to dissolve, then add silicone pressure-sensitive adhesive, mix well, and degas to obtain a pressure-sensitive adhesive solution.

[0084] Then, mix the skeleton-type reservoir system obtained above with the pressure-sensitive adhesive solution, stir at 8000 rpm for 1 hour, mix and disperse, and degas to obtain the drug-containing adhesive solution.

[0085] Apply the above-mentioned drug-containing viscose solution on the release layer, dry at 90°C for 1 hour, and finally cover the adhesive surface with a backing layer to obtain the product.

[0086] The above...

Embodiment 3

[0090] [Prescription] (based on 1000 tablets)

[0091] Etonogestrel 10g, ethinyl estradiol 2g, polybutylene pressure-sensitive adhesive 30g, cross-linked polyvinylpyrrolidone 20g, oleic acid 3g, dimethyl sulfoxide 6g;

[0092] Preparation method: Add drug, dimethyl sulfoxide, and cross-linked polyvinylpyrrolidone to 50 g of dichloromethane to dissolve, stir at 5000 rpm for 0.5 hour, and obtain a skeleton storage system;

[0093] In addition, oleic acid is added to the polybutylene pressure-sensitive adhesive, mixed evenly, and degassed to obtain a pressure-sensitive adhesive solution.

[0094] Then, mix the skeleton-type storage system obtained above with the pressure-sensitive adhesive solution, stir at 12000 rpm for 1.5 hours, mix and disperse, and degas to obtain the drug-containing adhesive solution.

[0095] Apply the above-mentioned drug-containing viscose solution on the release layer, dry at 90°C for 1 hour, and finally cover the adhesive surface with a backing layer ...

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Abstract

The invention provides a compound contraceptive composition, a contraceptive transdermal patch containing the composition and a preparation method. The compound contraceptive composition comprises effective contraceptive quantity of active components dispersed in a skeleton polymer substrate: etonogestrel and estrogen with a contraceptive cooperative function. Drugs are carried out bidirectional regulation by distribution and dispersal in two phases of the skeleton polymer substrate and a pressure sensitive adhesive substrate for drug transdermal release; and a crystallization inhibiting agent is added to a drug warehouse or the pressure sensitive adhesive substrate in order to effectively inhibit the drugs from crystallizing and maintain the long-time continuous transdermal high activity and power of the drugs in the substrates. The contraceptive transdermal patch prepared from the compound contraceptive composition maintains longer (1 to 7 days) stable drug release and blood drug concentration, has better effect, reduces administration frequency, adds user compliance and has obvious advantages in medical application.

Description

technical field [0001] The invention relates to a contraceptive transdermal patch with etonogestrel and its composition as active substances and a preparation method thereof. Background technique [0002] The third-generation progestogens, such as desogestrel, gestodene and norethisterone, have strong physiological activity. At present, third-generation progestogens have been widely used in the world either alone or in combination with estrogen. Among them, desogestrel is metabolized into physiologically active etonogestrel (3-ketone-desogestrel) in the body through oral administration. The composition of desogestrel and estrogen is administered orally once a day, and there are many cases of missed doses, and the compliance of users is poor, so the contraceptive failure rate is high; at the same time, due to oral administration of desogestrel, it cannot Complete metabolic conversion to etonogestrel, therefore its bioavailability is low. [0003] Chinese patent CN1190351A ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61K9/70A61P15/18
Inventor 罗华菲王浩侯惠民陈纯尹栩颖郑炎贺颖
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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