Tolterodine film-forming hydrogel preparation and preparation method thereof

A kind of technology of gel preparation, regulator, be applied in [0010] The present invention also provides tolterodine into, tolterodine film-forming hydrogel preparation, the field of improvement of tolterodine pharmaceutical dosage form, achieves good compatibility, The effect of smooth drug release and ease of use

Inactive Publication Date: 2013-06-12
南京锐利施生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention provides a kind of tolterodine film-forming hydrogel preparation, which is externally smeared and transdermally administered, which solves the difficulty in quality control of free base tolterodine in industrial production. , individual differences in metabolism in the body, and tolterodine tartrate is not easy to prepare hydrogels and gel preparations are easily taken away by clothes after application

Method used

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  • Tolterodine film-forming hydrogel preparation and preparation method thereof
  • Tolterodine film-forming hydrogel preparation and preparation method thereof
  • Tolterodine film-forming hydrogel preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Prepare the gel (according to 10g) according to the following prescription:

[0046] Tolterodine Tartrate 0.5844g, Carbomer 980 0.1g, Hydroxypropylcellulose (HPC) 0.05g, Triethanolamine 0.5997g, Hypromellose (HPMC) 0.1g, Ethanol 4ml, Tween 0.1g , and the balance is distilled water.

[0047] Weigh tolterodine tartrate, carbomer 980, HPC, and HPMC and add them into a beaker, add ethanol, triethanolamine, and Tween 80, stir, add water to 10g, stir until the gel is uniform and transparent, and put it into a vial Store sealed at room temperature. In vitro transdermal cumulative release rate-time curve see figure 1 .

Embodiment 2

[0049] Prepare the gel (according to 10g) according to the following prescription:

[0050] Tolterodine Tartrate 0.5844g, Carbomer 980 0.1g, Hydroxypropylcellulose (HPC) 0.05g, Triethanolamine 0.5997g, Hypromellose (HPMC) 0.15g, Ethanol 3.2g, Tween 0.1 g, the balance is distilled water.

[0051] Weigh tolterodine tartrate, carbomer 980, HPC, and HPMC and add them to a beaker, add ethanol, triethanolamine, and Tween 80, stir, add water to 10g, stir until the gel is uniform and transparent, and put it into a vial Store sealed at room temperature. In vitro transdermal cumulative release rate-time curve see figure 2 .

Embodiment 3

[0052] Example 3 Tolterodine tartrate gel preparation

[0053] Prepare the gel (according to 10g) according to the following prescription:

[0054] Tolterodine Tartrate 0.8767g, Carbomer 980 0.1g, Hydroxypropylcellulose (HPC) 0.05g, Triethanolamine 0.783g, Hypromellose (HPMC) 0.1g, Ethanol 3.2g, Tween 0.1 g, the balance is distilled water.

[0055] Weigh tolterodine tartrate, carbomer 980, HPC, and HPMC and add them into a beaker, add ethanol, triethanolamine, and Tween 80, stir, add water to 10g, stir until the gel is uniform and transparent, and put it into a vial Store sealed at room temperature. In vitro transdermal cumulative release rate-time curve see image 3 .

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Abstract

The invention discloses a tolterodine film-forming hydrogel preparation. A preparation method comprises the following steps of: directly adopting tolterodine tartrate to prepare the tolterodine film formation hydrogel preparation which utilizes carbomer 980 and hydroxypropyl cellulose as a mixed gel, water and ethanol as a solvent, methyl cellulose as a film-forming agent, polysorbate 80 as a film mechanical strength modifier and triethanolamine as a pH modifier and a drug transforming agent. The preparation has the drug-loading rate of 4-10%, the gel is transparent, the drug is uniformly dispersed, a transparent drug film is formed after the preparation is applied, and the application volume of the preparation is less than 0.5ml. The preparation can be stably released for 24 hours after being applied, and the bioavailability of the preparation is more than 20%. The prepared gel is smooth, crystal and fine, does not generate a foreign body sensation to skin after being applied, is slow in drug sustainable release, has a good percutaneous absorption effect and is convenient to use, and the compliance of patients is improved.

Description

[0001] [0002] Technical field: [0003] The invention is an improvement to the dosage form of tolterodine, and further discloses a film-forming hydrogel preparation of tolterodine. The invention also provides a preparation method of the preparation, which belongs to the technical field of medicine and pharmacy. [0004] Background technique: [0005] Tolterodine belongs to 3,3 diphenylpropylamine muscarinic receptor antagonists, and the drug concentration in the blood in the body fluctuates greatly after oral administration, resulting in low drug efficacy and increased side effects, such as dry mouth, constipation, indigestion, headache, dizziness , dry eyes, urinary retention. The unabsorbed part will produce systemic side effects or interactions (EP1077912), and the hepatic first-pass effect also leads to decreased drug efficacy and increased side effects. Although it can be administered by ordinary injection, for the long-term treatment of urinary incontinence patient...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/137A61K47/18
Inventor 李又欣刘喜明付璐代文文孙凤英縢乐生
Owner 南京锐利施生物技术有限公司
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