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
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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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