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Long-acting composite contraception microspheres and preparation method thereof

A microsphere and compound technology, which is applied in the field of long-acting compound contraceptive microspheres and its preparation, can solve problems such as affecting liver and kidney functions, large side effects, and complicated use of long-acting contraceptive implants

Active Publication Date: 2013-05-01
CHINA RESOURCES ZIZHU PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] An object of the present invention is to solve the problems in the above-mentioned prior art that oral contraceptives have large side effects, affect liver and kidney functions, and long-acting contraceptive implants have complicated usage methods or large side effects, and provide a contraceptive with good contraceptive effect and small side effects. , a simple and convenient long-acting compound contraceptive microsphere and its preparation

Method used

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  • Long-acting composite contraception microspheres and preparation method thereof
  • Long-acting composite contraception microspheres and preparation method thereof
  • Long-acting composite contraception microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation of Gestodene / Ethinyl Estradiol Microspheres

[0059] Under room temperature conditions, weigh 250mg polylactic acid-glycolic acid (50:50, Mw=10000) and 5mg gestodene and 2mg ethinyl estradiol, dissolve with organic solvent 2ml dichloromethane, will contain PLGA and medicine The organic solution was quickly added to 60ml of 1% PVA solution, emulsified in an electric stirrer (1200rpm) for 10min, then poured into 160ml of 1%PVA solution, evaporated at 25°C for about 6 hours, and stood to separate the solidified PLGA microspheres , and freeze-dried after washing with double distilled water, the diameter of the microspheres is 40-80 microns.

[0060] The determination results of microsphere drug encapsulation efficiency are as follows: the encapsulation efficiencies of gestodene and ethinylestradiol were 77.61% and 69.38%, respectively.

Embodiment 2

[0061] Example 2 Preparation of Gestodene / Estradiol Microspheres

[0062] Under room temperature, weigh 250mg of polylactic acid (Mw=20000), 5mg of gestodene and 2mg of estradiol, dissolve it with 3ml of ethyl acetate as an organic solvent, and quickly add the organic solution containing polylactic acid and drugs to 100ml In 0.2% PVA solution, emulsify in electric stirrer (2000rpm) for 2min, then pour into 150ml 1%PVA solution, evaporate for about 6 hours at 25°C, stand to separate the solidified PLGA microspheres, and wash with distilled water After freeze-drying, the microspheres have a diameter of 20-60 microns.

[0063] The experimental results showed that the encapsulation efficiencies of gestodene and estradiol were 86.32% and 74.86%, respectively.

Embodiment 3

[0064] Example 3 Preparation of Gestodene / Ethinyl Estradiol Microspheres

[0065] At room temperature, weigh 250mg of polylactide-glycolide (75:25, Mw=10000), 5mg of gestodene and 2mg of ethinylestradiol, and dissolve them in 5ml of dichloromethane as an organic solvent. Add the drug organically to 200ml of 0.2% sodium carboxymethylcellulose solution, emulsify in an electric stirrer (1000rpm) for 5min, reduce the stirring speed to 300rpm, evaporate at 25°C for about 6 hours, and stand to separate the solidified PLGA The microspheres are obtained by washing with double distilled water and freeze-drying. The diameter of the microspheres is 60-120 microns.

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Abstract

The present invention relates to a contraception medicament and pharmacy field. The compound contraceptive medicament is prepared to a biological degradation type long-effect microsphere preparation for injection. The invention settles the problems of large side effect, inferior compliance property and liver-kidney function effect of prior oral contraceptive medicament, and complicated using method, large side effect, etc. of traditional unilateral abiotic degradation type long-effect contraception implantation agent. The invention provides a long-term compound contraception microsphere injection which has the advantages of good contraception effect, small side effect and easy use, and a preparing method thereof. The microsphere comprises gestodene, estrogen and biological degradation polymer. The detailed content is in the instruction book. The product of the invention can stably and synchronously release two effective components in a long time. The inside and outside relativity of effective component is excellent.

Description

technical field [0001] The invention relates to the field of contraceptive drugs, and relates to a long-acting compound contraceptive microsphere and its preparation. Background technique [0002] Family planning is a long-term basic national policy to control the population and improve the quality of the population. Therefore, the development of safe, effective and convenient new contraceptives has been widely valued at home and abroad. [0003] The use of synthetic steroid hormones as contraceptives has a history of more than 40 years. In 1960, the FDA approved the production and marketing of norethindrone-10. It is a compound oral contraceptive containing progesterone and estrogen. Due to its efficacy Satisfied, it will soon be used worldwide. In the history of the use of progestins, norethindrone developed by Djerassi is generally considered to be the first-generation progestin, and 18-methyl norethindrone, which came out in 1963, is considered to be one of the second-g...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K45/00A61K31/56A61P15/18
Inventor 张强孙毅周敏冯磊尹栩颖张志军任辉郑炎
Owner CHINA RESOURCES ZIZHU PHARMA