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5-hydroxymethyl tolterodine gel preparation and preparation method thereof

A technology of hydroxymethyl tolterol and hydroxymethyl torterol, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve low bioavailability, many adverse reactions, etc. problem, to achieve the effect of good air permeability, smooth gel, and good percutaneous absorption effect

Inactive Publication Date: 2010-09-29
李又欣 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides a 5-hydroxymethyl tolterodine gel preparation, which is applied externally and administered through the skin, which overcomes the shortcomings of low bioavailability and many adverse reactions of oral preparations

Method used

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  • 5-hydroxymethyl tolterodine gel preparation and preparation method thereof
  • 5-hydroxymethyl tolterodine gel preparation and preparation method thereof
  • 5-hydroxymethyl tolterodine gel preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0028] 5-Hydroxymethyltolterodine gel preparation

[0029] Gel was prepared according to the following prescription (according to 100g): 5-hydroxymethyl tolterodine 1g, carbomer 9801.5g, azone 5g, glycerin 10g, sodium hydroxide 2.5g, ethanol 30ml, and the balance was distilled water.

[0030] Add 5-hydroxymethyl tolterodine into ethanol, vortex to dissolve it fully, then add glycerin, azone and distilled water to make a solution; take the prescribed amount of Carbomer 980 and sprinkle it into the above The solution was mechanically stirred at 100rpm for 24h until it swelled completely, and sodium hydroxide was added to adjust the pH value to 7 to obtain the solution.

Embodiment 2

[0032] 5-Hydroxymethyltolterodine gel preparation

[0033] Prepare the gel (by 100 g) according to the following prescription: 3 g of 5-hydroxymethyl tolterodine, 3 g of hydroxypropyl cellulose, 5 g of linoleic acid, 10 g of propylene glycol, 10 ml of ethanol, and the remainder is distilled water.

[0034] Add 5-hydroxymethyl tolterodine into ethanol, vortex to dissolve it fully, then add propylene glycol, linoleic acid and distilled water to make a solution; weigh the prescribed amount of hydroxypropyl cellulose, sprinkle it Put it into the above solution, stir it mechanically at 100rpm for 24h until it swells completely.

Embodiment 3

[0036] 5-Hydroxymethyltolterodine gel preparation

[0037] Prepare the gel (by 100g) according to the following prescription: 5-hydroxymethyltolterodine 3g, hydroxypropyl cellulose 1.5g, carbomer 9801g, silicone elastomer (Pharmat, Guangzhou Biaomei Pharmaceutical Excipients Co., Ltd. company) 0.5g, N-methylpyrrolidone 5g, glycerol 10g, triethanolamine 2g, ethanol 10ml, and the balance is distilled water.

[0038] Add 5-hydroxymethyl tolterodine into ethanol, vortex to dissolve it fully, then add glycerin, N-methylpyrrolidone and distilled water to make a solution; Boomer 980 and silicone elastomer are mixed and sprinkled into the above solution together, mechanically stirred at 100rpm for 24h until completely swollen, and triethanolamine is added dropwise to adjust the pH value to obtain the product.

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PUM

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Abstract

The invention provides a 5-hydroxymethyl Tolterodine gel preparation. The 5-hydroxymethyl Tolterodine gel preparation is in external use through being applied and has the transdermal medication effect, and the defects of low bioavailability and many untoward effects of an oral preparation are overcome. The 5-hydroxymethyl Tolterodine gel preparation is mainly prepared from 5-hydroxymethyl Tolterodine, a gel substrate, a filming substrate, an organic silicon elastic body, a transdermal penetration promoting agent, a pH regulating agent, a moisture preserving agent and the like. When the 5-hydroxymethyl Tolterodine gel preparation is in use, the gel preparation contains the filming substrate capable of forming flexible films after being dried, the 5-hydroxymethyl Tolterodine gel preparation is in external use to be applied on the parts of the thigh, the abdomen, the upper arm or the shoulder and the like, can fast form flexible and wear-resistance films on the selected skin regions, and can prevent the gel from being brought away by clothes, at the same time, the medication parts are in a non-sealed state, and the ventilation effect is good. The contained organic silicon elastic body can obviously improve the performance such as the dispersivity, the softness, the wettability, the lustrousness and the like of the gel system, the prepared gel is smooth, translucent and exquisite, the skin has no foreign body sensation after use, the medicine is perpetually and slowly released, the transdermal absorption effect is good, the use is convenient, and the adaptability of the patients can be improved.

Description

technical field [0001] The present invention is the improvement to the dosage form of the precursor compound 5-hydroxymethyl tolterodine of tolterodine medicine, furthermore discloses a kind of 5-hydroxymethyl tolterodine gel preparation, the present invention also provides the described The preparation method of the preparation belongs to the technical field of medical pharmacy. Background technique [0002] The drug tolterodine (R)-N, N-diisopropyl-3-(2-hydroxy-5-methylphenyl) 3-phenylpropylamine involved in the present invention is a muscarinic receptor antagonist, available To treat overactive bladder. Clinical studies have proved that tolterodine is converted into different metabolites by the enzyme CYP2D6 in the liver after oral administration, among which 5-hydroxymethyl tolterodine plays a major role in pharmacodynamics. Due to the differences in liver metabolic enzymes among individuals, oral administration of tolterodine will cause differences in the composition ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/137A61K47/34A61P13/10
Inventor 李又欣顾景凯孙凤英睢诚刘喜明孟庆繁滕利荣
Owner 李又欣
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