Finasteride lyotropic liquid crystal gel preparation precursor and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a finasteride lyotropic liquid crystal gel preparation precursor. The finasteride lyotropic liquid crystal gel preparation precursor comprises the following raw materials in percentage by mass: 45-80% of phospholipid, 10-50% of glyceride, 5-9% of a cosolvent and 0.1-6% of finasteride. The finasteride in the finasteridelyotropic liquid crystal gel preparation precursor disclosed by the invention is uniformly dispersed; the precursor is low in viscosity and can be used for injection; after entering a human body, theprecursor can act with water to form the lyotropic liquid crystal with an excellent drug sustained release effect; the biocompatibility is excellent, no systemic inflammatory response is caused, andtoxic and side effects of the medicine are avoided; the drug administration frequency can be decreased; the precursor is low in cost, simple in preparation method and capable of easily realizing industrialization; the precursor can be used for treating male hair loss and benign prostatic hyperplasia, so that an enlarged prostate is shrunk, and symptoms brought by urine flow and benign prostatic hyperplasia are improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a finasteride lyotropic liquid crystal gel preparation precursor and a preparation method thereof. Background technique [0002] Finasteride is a 4-azasteroid that is a specific inhibitor of type II 5α-reductase, an intracellular enzyme involved in the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia depends on the conversion of testosterone to dihydrotestosterone in the prostate. Finasteride is very effective in reducing DHT in the blood and in the prostate. Contain type II 5α-reductase in the hair follicle, and the hair follicle becomes less in the bald area scalp of male baldness patient, and dihydrotestosterone increases. Administration of finasteride can reduce the concentration of dihydrotestosterone in the scalp and serum of these patients. Men who are congenitally deficient in type II 5α-reductase do not...

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Problems solved by technology

[0005] In the patent CN101327192A, a soft capsule of finasteride was prepared, which can speed up the dissolution rate of the drug and improve the bioavailability to a certain extent, but the bioavailability is still low due to the strong first-pass effect of the liver

[0006] In view of the defects of oral finasteride preparations, the patent CN200510110382.4 discloses the preparation method of finasteride sustained-release microspheres for injection. This dosage form prolongs the drug action time and reduces the number of administrations, but the preparation process The organic solvent cannot be completely removed, and the degradation product CO 2 May cause increased local acidity of the tissue, resulting in sterile inflammation

[0007] At present, liquid crystal gel preparation precursor injections made of finasteride have not been reported yet.

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