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Independently controllable contraceptive transdermal patch containing progestogen and estrogen and preparation method thereof

An independently controlled, transdermal patch technology, which is applied in the direction of medical preparations containing active ingredients, medical preparations with inactive ingredients, polymer compounds with inactive ingredients, etc., can solve the problem of increasing skin irritation and the mixing effects of hormones and drugs , pressure-sensitive adhesiveness and reduced strength, to achieve the effects of ensuring safety and effectiveness, improving patient compliance, and reducing drug doses

Active Publication Date: 2010-04-21
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 temperature is high during the process operation, which is easy to cause the degradation of the drug
Existing transdermal technology is still unsatisfactory for the release rate of contraceptives, especially the transdermal rate of gestodene. Chinese patents CN1633995A, CN1835722A, and CN1399533A disclose one or several steroidal hormone contraceptive transdermal delivery systems. In order to increase the transdermal flow rate and rate of progesterone in the system, various transdermal penetration enhancers are added, and the dosage is high (the optimal dosage is at least 45% by weight distributed in the base material composition in a molecularly dispersed form), Although it can effectively improve the skin penetration of drugs, the addition of a large amount of penetration enhancers will cause the viscosity and strength of the pressure-sensitive adhesive to be greatly reduced, and at the same time increase the irritation to the skin
Chinese patent CN101229144A discloses a transdermal absorption patch containing gestodene and / or estrogen. In order to meet the hormone transdermal and adhesion performance for 7 days, more drug-loaded materials (drug and drug-loaded material weight Ratio is 1:80~300), which is more than 2 times of the drug-carrying material used in the invention, so the patch coating is thick, sticking to the skin for a long time is prone to allergies, skin irritation, etc.
All of the above patents mixed one or several hormones into the pressure-sensitive adhesive for coating, but due to the different solubility, distribution coefficient and diffusion capacity of estrogen and progesterone in different drug-loaded materials, their transdermal rate There are differences in the transdermal behavior of hormones and progesterone, and it is difficult to meet the levels of estrogen and progesterone required by the human body at the same time; and the mixing of hormones and drugs may affect each other, which brings great difficulty to the design of the prescription, and eventually leads to the transdermal drug in the patch. And the release is not easy to control
For example, in the Chinese patent CN1835722A, the system meets the requirement that progesterone is released into the body at a rate of 20 μg / d, but the rate of estrogen fluctuates in the range of 10-50 μg / d

Method used

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  • Independently controllable contraceptive transdermal patch containing progestogen and estrogen and preparation method thereof
  • Independently controllable contraceptive transdermal patch containing progestogen and estrogen and preparation method thereof
  • Independently controllable contraceptive transdermal patch containing progestogen and estrogen and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] [Prescription] (based on 1000 tablets)

[0054] System 1: 0.6g of ethinyl estradiol, 0.6g of isopropyl myristate, 1.2g of silicone pressure-sensitive adhesive;

[0055] System 2: Gestodene 1.0g, polyvinylpyrrolidone / vinyl acetate copolymer (S-630) 3.0g;

[0056] Preparation method: add the drug in system 1 to 0.5 g of ethyl acetate to dissolve, add isopropyl myristate, silicone pressure-sensitive adhesive, mix well, and degas;

[0057] Add the drug and S-630 in system two to 40g ethanol to dissolve, mix well, and degas.

[0058] First, apply the above-mentioned system 1 drug solution on the anti-adhesive layer, and dry it at 60°C for 1 hour to obtain the estrogen drug storage layer 2;

[0059] Then apply the above-mentioned system two drug solution prepared with the material on the backing layer, and dry at 60°C for 1 hour to obtain the progesterone skeleton polymer drug storage layer 3;

[0060] Utilize the stickiness of drug storage layer 2 at last, by adjustable p...

Embodiment 2

[0067] [Prescription] (based on 1000 tablets)

[0068] System 1: 0.8g ethinyl estradiol, 8g oleic acid, 12g polyacrylate pressure sensitive adhesive;

[0069] System 2: Gestodene 1.2g, polyvinylpyrrolidone (K-90) 12g;

[0070] Process: Add the drug in system 1 to 0.5g ethyl acetate to dissolve, add oleic acid and polyacrylate pressure-sensitive adhesive, mix well, and degas;

[0071] Add the drug and K-90 in system two to 40g ethanol to dissolve, mix well, and degas.

[0072] First, apply the above-mentioned system 1 drug solution on the anti-adhesive layer, and dry it at 100°C for 0.5 hours to obtain the estrogen drug storage layer 2;

[0073] Then apply the above-mentioned system two drug solution prepared with the material on the backing layer, and dry at 100°C for 0.5 hour to obtain the progesterone drug storage layer 3;

[0074] Utilize the stickiness of drug storage layer 2 at last, pass through adjustable pressing roller (pressure 20N / cm 2 ), at 30°C, compound the d...

Embodiment 3

[0081] [Prescription] (based on 1000 tablets)

[0082] System 1: 1.0 g of ethinyl estradiol, 20 g of lauric acid, and 30 g of polyisoprene rubber pressure-sensitive adhesive;

[0083] System 2: Gestodene 1.8g, ethylene-vinyl acetate copolymer (EVA) 54g;

[0084] The above-mentioned backing layer material adopts 9723 backing film of 3M Company, with a thickness of 43.2 μm; the material of the anti-adhesive layer adopts silicone oil-coated anti-adhesive film of Shanghai People’s Sanitary Materials Co., Ltd., with a thickness of 70 μm.

[0085] The preparation method is the same as in Example 1.

[0086] The in vitro skin penetration rate is shown in Table 1.

[0087] For the cumulative in vitro skin penetration rate of ethinyl estradiol within 7 days, see figure 2 .

[0088] For the cumulative in vitro skin penetration rate of gestodene within 7 days, see image 3 .

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Abstract

The invention discloses an independently controllable contraceptive transdermal patch containing progestogen and estrogen and a preparation method thereof. The contraceptive transdermal patch comprises an estrogen drug storage layer and a progestogen drug storage layer, wherein the estrogen drug storage layer is dispersed over a pressure sensitive adhesive and has the active ingredient with useful quantity of contraception of the estrogen, the progestogen drug storage layer is dispersed over a membrane-forming framework polymer had has the active ingredient with useful quantity of contraception of the progestogen, and the estrogen drug storage layer and the progestogen drug storage layer are compounded. Each component is transdermal and released according to respective transdermal transferring rule without interference on each other and can be independently controlled and freely adjusted. In the invention, the transdermal patch adopts a transdermal controlled-release drug administration method, the drug effect can maintain for seven days, the dosage of the drug is reduced, the blood drug level is stable, the poison and side reactions are reduced, and compared with the normal oral administration, the transdermal patch has remarkable advantages; meantime, with respect to subdermal implants, intrauterine implants and the like, the administration of the transdermal patch is convenient and flexible, and the patient compliance is greatly improved.

Description

technical field [0001] The invention relates to a contraceptive transdermal patch with progesterone and estrogen as active substances and a preparation method thereof. Background technique [0002] Traditionally, the combination of estrogen and progesterone has been used orally. Although this combination of hormones can effectively inhibit ovulation, this oral contraceptive still has certain defects. For example, oral contraceptives generally have a large dose, so the incidence of blood clots, stroke, myocardial infarction and other related vascular diseases among users is relatively high; at the same time, oral contraceptives need to be taken once a day, and users often miss or take wrong doses , resulting in a higher rate of contraceptive failure. In addition, if a woman continues to take it after pregnancy, it may cause fetal abnormalities. [0003] In recent years, people have begun to develop subcutaneous implants, vaginal contraceptive rings or other slow-release del...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K45/06A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P15/18
Inventor 罗华菲尹栩颖王浩侯惠民陈凯栋王雅珍胡婧
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT