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Tolterodine gel preparation and preparation method thereof

A preparation and gel matrix technology, applied in pharmaceutical formulations, urinary system diseases, drug combinations, etc., can solve the problems of many adverse reactions and low bioavailability, and achieve smooth gel, good air permeability, and improved dispersibility. Effect

Inactive Publication Date: 2010-08-25
李又欣 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention provides a 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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  • Tolterodine gel preparation and preparation method thereof
  • Tolterodine gel preparation and preparation method thereof
  • Tolterodine gel preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Tolterodine Gel Preparation

[0029] Prepare the gel (according to 100g) according to the following prescription:

[0030] Free base tolterodine 1g, carbomer 980 1.5g, azone 5g, glycerin 10g, sodium hydroxide 2.5g, ethanol 30ml, and distilled water as the balance.

[0031] Add the free base tolterodine into ethanol, vortex to fully dissolve it, then add glycerin, azone and distilled water to make a solution; take the prescribed amount of Carbomer 980, sprinkle it into the above solution, Stir mechanically at a speed of 100rpm for 24h until it swells completely, add sodium hydroxide to adjust the pH value to 7, and obtain the product.

Embodiment 2

[0033] Tolterodine Gel Preparation

[0034] Prepare the gel (according to 100g) according to the following prescription:

[0035] Free base tolterodine 3g, hydroxypropyl cellulose 3g, linoleic acid 5g, propylene glycol 10g, ethanol 10ml, the balance is distilled water.

[0036] Add the free base tolterodine into ethanol, vortex to dissolve it fully, then add propylene glycol, linoleic acid and distilled water to make a solution; take the prescribed amount of hydroxypropyl cellulose and sprinkle it into the above solution , mechanically stirred at 100rpm for 24h until it swelled completely.

Embodiment 3

[0038] Tolterodine Gel Preparation

[0039] Prepare the gel (according to 100g) according to the following prescription:

[0040] Free base tolterodine 3g, hydroxypropyl cellulose 1.5g, carbomer 980 1g, silicone elastomer (Pharmat, Guangzhou Biaomei Pharmaceutical Excipients Co., Ltd.) 0.5g, N-methylpyrrolidone 5g, glycerin 10g , 2 g of triethanolamine, 10 ml of ethanol, and the balance is distilled water.

[0041] Add the free base tolterodine into ethanol, vortex to dissolve it fully, then add glycerin, N-methylpyrrolidone and distilled water to make a solution; weigh the prescribed amount of hydroxypropyl cellulose, carbomer 980 and silicone elastomer, mix well and sprinkle into the above solution together, mechanically stir at 100rpm for 24h until completely swollen, add triethanolamine dropwise to adjust the pH value, and obtain.

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Abstract

The invention discloses a tolterodine gel preparation, which is mainly prepared from free alkali tolterodine, gel matrix, film-forming matrix, organosilicon elastic body, percutaneous penetration accelerators, pH regulators, humectants, and the like. During use, the gel preparation contains the film-forming matrix which can form a flexible film after being dried, and can be externally coated on the thigh, the belly, the upper arm or shoulder, and other parts; flexible and wear-resistant thin film can be rapidly formed in the selected skin region; the gel is prevented from being taken away by the clothes; and meanwhile, the application site is in an unsealed state and has good air permeability. The contained organosilicon elastic body can obviously improve the dispersibility, flexibility, wettability, glossiness, and other performances of the gel system. The prepared gel is smooth, crystal clear and fine, has no foreign body sensation on the skin after use, durable medicament and slow release, good percutaneous absorption effect, convenient use, and improves the patient compliance.

Description

technical field [0001] The invention is an improvement to the dosage form of tolterodine, and further discloses a tolterodine gel preparation. The invention also provides a preparation method of the preparation, which belongs to the technical field of medicine and pharmacy. Background technique [0002] The drug tolterodine (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine is a muscarinic receptor antagonist and can be used 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. Due to differences in liver metabolic enzymes between individuals, the composition and content of metabolites in the body are different, resulting in differences in drug efficacy for different patients. Very large, not conducive to dose control, and cause dry mouth, constipation and other adverse reactions. If a common injection is used for administration, as a ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/137A61K47/34A61K47/38A61P13/10
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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