Biodegradation type long-acting contraception microsphere and preparation method and application thereof

A biodegradable, microsphere technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc. Avoiding the effects of contraceptive failure

Inactive Publication Date: 2011-06-08
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report on enorgestrel acetate microspheres coated with biodegradable polymer materials at home and abroad

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve 100 mg of PLGA (the weight ratio of lactide:glycolide is 50:50) and 2 mg of enorgestrel acetate into 2 mL of dichloromethane, and fully dissolve under ultrasonic vibration. Inject this solution into 20 mL of 0.5% PVA solution under high-speed stirring, emulsify for 10 min to form an O / W emulsion, and then gently stir for 1 h to evaporate the solvent and solidify the microspheres. The microspheres in the obtained suspension were collected by centrifugation, washed several times with distilled water, and dried to obtain drug microspheres. The content of the enorgestrel acetate in the microsphere is 5-8%, and the particle diameter of the microsphere is in the range of 10-50 μm. The drug release amounts of the obtained microspheres on the 1st, 3rd, 7th, 14th and 30th day were 8%, 22% and 40% respectively. 72% and 95%.

Embodiment 2

[0029] Dissolve 120 mg of PLGA (lactide:glycolide weight ratio: 65:35) and 6 mg of enorgestrel acetate in 2 mL of dichloromethane, and fully dissolve under ultrasonic vibration. The solution was injected into 30 mL of 2% PVA solution under high-speed stirring, emulsified for 8 minutes to form an O / W emulsion, and stirred gently for 3 hours to evaporate the solvent and solidify the microspheres. The microspheres in the obtained suspension were collected by centrifugation, washed several times with distilled water, and dried to obtain drug microspheres. The content of the enorgestrel acetate in the microsphere is 5-8%, and the particle diameter of the microsphere is in the range of 10-50 μm. The drug release amounts of the obtained microspheres on the 7th, 14th, 28th, 56th, 70th and 90th days were 8%, 18%, 32%, 55%, 78% and 96%, respectively.

Embodiment 3

[0031] Dissolve 140 mg of PLGA (lactide:glycolide weight ratio: 85:15) and 10 mg of enorgestrel acetate in 4 mL of dichloromethane, and fully dissolve under ultrasonic vibration. Inject this solution into 80 mL of 4% PVA solution under high-speed stirring, emulsify for 5 minutes to form an O / W emulsion, and then gently stir for 5 hours to evaporate the solvent and solidify the microspheres. The microspheres in the obtained suspension were collected by centrifugation, washed several times with distilled water, and dried to obtain drug microspheres. The content of the enorgestrel acetate in the microsphere is 5-8%, and the particle diameter of the microsphere is in the range of 10-50 μm. The drug release amounts of the obtained microspheres on the 7th, 14th, 28th, 56th, 70th, 96th and 120th day were 8%, 18%, 28%, 45%, 72%, 86% and 96%, respectively.

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Abstract

The present invention discloses a biodegradation type long-acting contraception microsphere and a preparation method and an application thereof, belonging to a pharmacy technology field. The biodegradation type long-acting contraception microsphere is taken a biodegradable manpower synthetic polymer as a carrier and a Nestorone as a basic remedy, wherein a weight shares of the carrier is from 100to 140 shares, the weight share of the basic remedy is from 2 to 10 shares. The preparation method includes dissolving the basic remedy and the carrier in an organic solvent to obtain a solution containing the basic remedy and the carrier, adding the solution containing the basic remedy and the carrier into a stabiliser water solution of 10-20 shares by weight as well as agitating, agitating to emulsify thoroughly, remixing to volatilize the organic solvent, solidifying to obtain a microsphere. The invention also provides an application of the microsphere, that is the microsphere is prepared into an injecting heeling-in agent by a preparation method of a conventional medicinal preparation. The long-acting Nestorone microsphere of the invention has an integral modality, the microsphere dimension is from 10 to 50 [Mu]m, the diameter is distributed well, and a vitro release time is from 1 to 12 weeks.

Description

technical field [0001] The invention relates to a biodegradable long-acting contraceptive microsphere and a preparation method and application thereof, belonging to the technical field of pharmacy. Background technique [0002] Breastfeeding women are very cautious about the choice of contraceptive drugs out of consideration for the safety of their babies. Norgestrel acetate is a synthetic progestin compound, which has strong progesterone activity and no androgen, estrogen and adrenal cortex hormone activity. Even if it is secreted from breast milk, it has no effect on the baby. In clinical trials, the contraceptive rate is high and the side effects are small. However, it is ineffective orally and must be administered parenterally. [0003] It is reported in the literature that the existing enorgestrel acetate silicone rubber implants and vaginal rings are inconvenient to use. The long-acting silicone rubber implants need to be surgically implanted and the drug carrier mat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/573A61K47/34A61P15/18A61K31/57A61K47/10
Inventor 张蜀邓红林华庆白海芬廖清江
Owner GUANGDONG PHARMA UNIV
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