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Sustained release microsphere of finasteride and its analogue, preparation process and use thereof

A technology of sustained-release microspheres and finasteride, which is applied to medical preparations containing active ingredients, drug combinations, and pharmaceutical formulas, and can solve problems such as compliance and low bioavailability

Inactive Publication Date: 2007-05-23
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This has compliance problems for patients, especially elderly patients. In addition, oral preparations often have the defect of low bioavailability due to the first-pass effect of the liver

Method used

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  • Sustained release microsphere of finasteride and its analogue, preparation process and use thereof
  • Sustained release microsphere of finasteride and its analogue, preparation process and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Dissolve 100mg of polylactide in 0.6ml of dichloromethane, add 100mg of finasteride, stir and dissolve to form a clear solution. Add 0.5% PVA (05-88) aqueous solution into a flat-bottomed beaker equipped with a stirring paddle, keep the temperature (25°C), then drop the above polymer solution into it under stirring, stir at 2000rpm to form an emulsion, then add a large amount of distilled water, Maintain 200rpm to gradually evaporate the organic solvent in the o / w emulsion to dryness. Sampling and microscopic inspection were carried out continuously during the whole process to observe the multi-stage microsphere formation process.

[0029] The above solution is centrifuged, the supernatant is poured off, the microspheres are collected under reduced pressure on a filter membrane, washed with a small amount of distilled water several times, and dried under reduced pressure at room temperature.

Embodiment 2

[0031] Dissolve 160mg of poly-DL-lactide-glycolide in ethyl acetate, add 40mg of finasteride, and stir to form a clear solution. Add a 1% PVPk-30 aqueous solution of 10 times the volume of the dispersed phase into a flat-bottomed beaker equipped with a stirring paddle. After constant temperature (25°C), drop the above polymer solution into it under stirring, stir at 2000rpm to form an emulsion, and then add a large amount of distilled water, and kept stirring at 200 rpm for 4 hours, so that the organic solvent in the o / w emulsion was gradually evaporated to dryness. Sampling and microscopic inspection were carried out continuously during the whole process to observe the multi-stage microsphere formation process.

[0032] The above solution is centrifuged, the supernatant is poured off, the microspheres are collected under reduced pressure on a filter membrane, washed with a small amount of distilled water several times, and dried under reduced pressure at room temperature.

Embodiment 3

[0034] Dissolve 800 mg of polylactic-glycolic acid in 2.5 ml of acetonitrile, and add 200 mg of finasteride. Stir to dissolve. As O1 phase; in 30ml liquid paraffin, add 1.5% Span85, mix well as O2 phase. At 3000rpm, drop O1 into O2 to make O1 / O2 emulsion. Control the temperature of the system, keep the constant temperature at 30°C, and gradually evaporate the organic solvent in the dispersed phase to dryness. The suspension is centrifuged, and the supernatant is removed. The microspheres are washed with a small amount of hexane several times, and dried under reduced pressure at room temperature. .

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Abstract

The invention relates to an injection slow-release micro ball of Finasteride and similar component, wherein said micro ball contains 5-80% Finasteride and biological degradable polymer at 95-20%. The production comprises emulsion disperse (oil / water or oil / oil method), liquid drying method, or atomization drying method. The inventive agent can prolong function time and improve drug utilization.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to sustained-release microspheres for injection of finasteride and its analogues, a preparation method and application thereof. Background technique [0002] Finasteride is a 4-nitrogen steroid hormone that is a specific inhibitor of 5-alpha reductase. 5-alpha reductase metabolizes testosterone into the more potent androgen dihydrotestosterone, which the prostate gland depends on for growth. Finasteride can inhibit the synthesis of dihydrotestosterone and reduce the swelling of the prostate. Clinically used for the treatment of benign prostatic hyperplasia. [0003] [0004] The oral bioavailability of finasteride is 63-80%. (Edited by Zhang Shige, Sun Dingren, New Drug Clinical Pharmacology and Application Manual, Chemical Industry Publishing, Beijing, 2001, p421) A foreign source reported that 895 patients with benign prostatic hyperplasia took this product orally,...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K9/16A61P13/08
Inventor 肖莉莉陈庆华包泳初潘峰曹霖朱焰谢淑武
Owner SHANGHAI INST OF PHARMA IND
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