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Phenasteroid gel preparation

A finasteride gel preparation technology, applied in the field of finasteride plastid gel preparations, to achieve the effects of promoting transdermal transport, improving transdermal transport, and improving drug efficacy

Inactive Publication Date: 2004-12-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are currently no dosage forms on the market other than finasteride oral tablets

Method used

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  • Phenasteroid gel preparation
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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 Several compositions of the preparation of the present invention

[0030] Prescription 1 Prescription 2 Prescription 3 Prescription 4 Prescription 5

[0031] Finasteride 0.010 0.020 0.020 0.040 0.040

[0032] Phospholipids 0.15 0.15 0.30 0.50 0.60

[0033] Low molecular weight alcohols 3.0 6.0 6.0 6.0 9.0

[0034] Carbomer 0.10 0.20 0.24 0.24 0.24

[0035] Glycerin 0.20 0.50 0.50 0.50 0.50

[0036] Antioxidant (vitamin E) 0 0.10 0.20 0.20 0.20

[0037] Triethanolamine 0.025 0.050 0.050 0.050 0.050

[0038] Water 16.0 13.0 13.0 13.0 10.0

[0039] The above is the ratio of the 20g gel prescription, and the units are grams. The low-molecular-weight alcohols in prescriptions 1, 2, and 3 are ethanol, and the low-molecular-weight alcohols in prescriptions 4 and 5 are propylene glycol.

Embodiment 2

[0040] Embodiment 2 Other several compositions of preparation of the present invention

[0041] Prescription 6 Prescription 7 Prescription 8 Prescription 9 Prescription 10

[0042] Finasteride 0.080 0.08 0.080 0.1 0.2

[0043] Phospholipids 0.15 0.15 0.30 0.50 0.60

[0044] Low molecular weight alcohols 3.0 6.0 6.0 6.0 9.0

[0045] Carbomer 0.10 0.20 0.24 0.24 0.24

[0046] Glycerin 0.50 0.50 0.50 0.50 0.8

[0047] Antioxidant (vitamin E) 0.20 0.20 0.20 0.20 0.50

[0048] Triethanolamine 0.050 0.050 0.050 0.050 0.10

[0049] Water 16.0 13.0 13.0 13.0 10.0

[0050] The above is the ratio of the 20g gel prescription, and the units are grams. The low-molecular-weight alcohols in prescriptions 6, 7, and 8 are ethanol, and the low-molecular-weight alcohols in prescriptions 9 and 10 are propylene glycol.

Embodiment 3

[0051] Embodiment 3 A kind of preparation method of the present invention

[0052]Get 300mg of soybean lecithin, 25mg of finasteride, 3.8ml of ethanol, 6.8ml of solvent, dissolve finasteride and soybean lecithin in ethanol, inject buffer solution or water to 10g under airtight conditions at room temperature, and obtain finasteride Steroidal ethosome suspension, controlled ethosome particle size by probe-type ultrasound (400-500w, 30-60 times), passing through microporous membrane (0.1 micron or 0.22 micron), etc., to obtain finasteride The finished product of the plastid, observe the shape of the finasteride ethosome sample through a transmission electron microscope, the ethosome particle size is about 150nm, and the appearance is a regular circle or oval.

[0053] The finasteride plastid prepared by the above method is prepared into a gel, and the method is as follows: in addition, carbomer (0.5-1.5%) is swelled with an appropriate amount of water, and 1-5% glycerin, 15%- 45...

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Abstract

An alcoholic gel of phenasteroamine is prepard from phenasteroamine, phosphatide, low-molecular alcohol, glycerine, carbomer, antioxidizing agent, triethanolamine and solvent. Its advantags are endermism with high target, high and durable curative effect and low by-effect.

Description

Technical field [0001] The invention belongs to pharmaceutical preparations, and relates to gel preparations for transdermal administration of medicines, mainly related to finasteride elastosome gel preparations, which can improve the transdermal transport of finasteride and increase the retention of medicines in the skin. Improve the percutaneous absorption of drugs and improve the curative effect. Background technique [0002] Transdermal drug delivery systems (TDDSs) have been a hot spot in pharmaceutical research since the first marketed transdermal drug delivery agent-scopolamine came out in the early 1980s. Regardless of whether percutaneous absorption produces systemic effects or local effects, drugs must pass through the stratum corneum of the skin. However, due to the good natural barrier function of the stratum corneum, the curative effects of many drugs cannot be well exerted. [0003] Ethosomes are a new type of vesicle drug delivery carrier with a lipid bilaye...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06A61K9/127A61K31/56A61M37/00A61P13/08A61P17/14
Inventor 梁文权饶跃峰
Owner ZHEJIANG UNIV