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Free alkali tolterodine filming hydrogel preparation and preparation method thereof through later drug loading

A gel preparation and gel technology are applied in the improvement of tolterodine pharmaceutical dosage forms, the preparation of tolterodine film-forming hydrogels, and the field of free-base tolterodine film-forming hydrogel preparations. Improve physical properties and fine texture

Inactive Publication Date: 2014-02-05
JILIN UNIV
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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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  • Free alkali tolterodine filming hydrogel preparation and preparation method thereof through later drug loading
  • Free alkali tolterodine filming hydrogel preparation and preparation method thereof through later drug loading
  • Free alkali tolterodine filming hydrogel preparation and preparation method thereof through later drug loading

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Prepare the gel (according to 10g) according to the following prescription:

[0034] Tolterodine tartrate 0.584g, Carbomer 980 0.1g, hydroxypropylcellulose (HPC) 0.05g, ethyl acetate 200μl, hydroxypropylmethylcellulose (HPMC) 0.2g, ethanol 4ml, Tween 80 0.1 g, the balance is distilled water.

[0035] Treat tolterodine tartrate lye as KOH. Carbomer 980, HPC, and HPMC were weighed and added to a beaker, swelled with 6ml of water for 12 hours, added Tween 80, ethyl acetate and the rest of ethanol, stirred, added water to 10g, stirred until the gel was uniform and transparent, and put into a vial Store sealed at room temperature. In vitro transdermal cumulative release rate-time curve see figure 1 .

Embodiment 2

[0037] Prepare the gel (according to 10g) according to the following prescription:

[0038] Tolterodine tartrate 0.584g, Carbomer 980 0.1g, hydroxypropylcellulose (HPC) 0.05g, ethyl acetate 500μl, hydroxypropylmethylcellulose (HPMC) 0.15g, ethanol 4ml, Tween 80 0.1 g, the balance is distilled water.

[0039] Treat tolterodine tartrate lye as KOH. Carbomer 980, HPC, and HPMC were weighed and added to a beaker, swelled with 6ml of water for 12 hours, added Tween 80, ethyl acetate and the rest of ethanol, stirred, added water to 10g, stirred until the gel was uniform and transparent, and put into a vial Store sealed at room temperature. In vitro transdermal cumulative release rate-time curve see figure 2 .

Embodiment 3

[0040] Example 3 Tolterodine tartrate gel preparation

[0041] Prepare the gel (according to 10g) according to the following prescription:

[0042] Tolterodine tartrate 0.584g, Carbomer 980 0.1g, hydroxypropylcellulose (HPC) 0.05g, ethyl acetate 100μl, hydroxypropylmethylcellulose (HPMC) 0.25g, ethanol 4ml, Tween 80 0.15 g, the balance is distilled water.

[0043] Treat tolterodine tartrate lye as KOH. Carbomer 980, HPC, and HPMC were weighed and added to a beaker, swelled with 6ml of water for 12 hours, added Tween 80, ethyl acetate and the rest of ethanol, stirred, added water to 10g, stirred until the gel was uniform and transparent, and put 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 free alkali tolterodine filming hydrogel preparation. Ethyl alcohol and alkali liquor are used for converting tolterodine tartarate so as to prepare the free alkali tolterodine filming hydrogel preparation by taking carbomer 980 and hydroxy propyl cellulose (HPC) as a mixed gel, water and ethyl alcohol as solvents, hydroxypropyl methyl cellulose (HPMC) as a film-forming agent, and Tween 80 and ethyl acetate as solubilizers. The drug loading capacity is 0.5-5%, the gel is transparent, the drug is dispersed uniformly and the gel becomes a transparent drug membrane after being applied; when the free alkali tolterodine filming hydrogel preparation is used, ethyl alcohol in the substrate of the gel is volatilized rapidly in 1-3 minutes, the membrane formed on the surface is not adhered to clothes, the drug is dispersed uniformly, a large quantity of moisture is volatilized in 30 minutes, the membrane becomes transparent, the drug can be released stably and slowly for 24 hours, and the bioavailability is greater than 20%. The free alkali tolterodine filming hydrogel preparation can be applied on a thigh, a belly, an upper arm, and a shoulder, and the parts applied with the drug are not at an airtight state and have good air permeability.

Description

[0001] Technical field: [0002] The invention is an improvement to the dosage form of tolterodine, and further discloses a free base tolterodine film-forming hydrogel preparation. The invention also provides a preparation method of the preparation, which belongs to the technical field of medical pharmacy. Background technique: [0003] 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 patients, one or more...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/137A61K47/38A61K47/34A61K47/14
Inventor 刘喜明付璐代文文李又欣孙凤英縢乐生武毅
Owner JILIN UNIV
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