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Long-acting composite contraception microspheres and preparation method thereof

A technology of microspheres and compound prescriptions is applied in the field of long-acting compound contraceptive microspheres and their preparation, and can solve the problems of large side effects, complicated use methods of long-acting contraceptive implants, affecting liver and kidney functions, and the like.

Active Publication Date: 2009-06-17
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] At room temperature, weigh out 250mg of polylactic acid-glycolic acid (50:50, Mw=10000), 5mg of gestodene and 2mg of ethinyl estradiol, and dissolve them with 2ml of dichloromethane as an organic solvent. The organic solution was quickly added to 60ml of 1% PVA solution, emulsified in an electric stirrer (1200rpm) for 10 minutes, and then poured into 160ml of 1% PVA solution, evaporated at 25°C for about 6 hours, and left to stand to separate the solidified PLGA microspheres , And washed with distilled water and freeze-dried to obtain, the diameter of the microspheres is 40-80 microns.

[0060] The measurement results of the drug encapsulation efficiency of microspheres are as follows: the encapsulation efficiency of gestodene and ethinyl estradiol are 77.61% and 69.38%, respectively.

Embodiment 2

[0061] Example 2 Preparation of gestodene / estradiol microspheres

[0062] At room temperature, weigh out 250mg of polylactic acid (Mw=20000), 5mg of gestodene and 2mg of estradiol, dissolve in 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 an electric stirrer (2000rpm) for 2 minutes, then pour it into 150ml 1% PVA solution, evaporate at 25°C for about 6 hours, stand still to separate and solidify PLGA microspheres, and wash with re-distilled water It is obtained after freeze-drying, and the diameter of the microspheres is 20-60 microns.

[0063] The experimental results showed that the encapsulation rates 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 polylactide-glycolide (75:25, Mw=10000), 5mg gestodene and 2mg ethinyl estradiol, and dissolve them with 5ml dichloromethane as an organic solvent to dissolve the PLGA and Add the organic medicine dropwise to 200ml 0.2% sodium carboxymethyl cellulose solution, emulsify in an electric mixer (1000rpm) for 5 minutes, reduce the stirring speed to 300rpm, evaporate at 25°C for about 6 hours, and stand still to separate the solidified PLGA The microspheres are washed with re-distilled water and then freeze-dried to obtain the microspheres with a diameter of 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 is a long-acting compound contraceptive microsphere and its preparation. Background technique [0002] Family planning is a long-term basic national policy for my country 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] Synthetic steroid hormones have been used as contraceptives for more than 40 years. In 1960, the FDA approved the production and marketing of norethindrone-10, which is a compound oral contraceptive containing progesterone and estrogen. Satisfied, it will be promoted and used worldwide soon. In the history of progesterone use, norethindrone developed by Djerassi is usually considered to be the first-generation progesterone, and then 18-methyl norethindrone, which came out in 1963, is considered to be one of the second-generation p...

Claims

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Application Information

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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
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