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Tolterodine tartrate sustained-release dropping pill and preparation method thereof

A technology of tolterol tartrate and skeleton materials, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of many times of taking medicine, long dissolution time limit, poor absorption, etc.

Inactive Publication Date: 2008-09-24
北京博智绿洲医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0040] Due to preparation technology and other reasons, most oral preparations of drugs have long dissolution time, low dissolution rate, poor absorption, many times of taking medicine, uncontrollable drug release time, poor intestinal first-pass effect and bioavailability after taking. Low-level problems, which affect the efficacy of the drug and directly affect the therapeutic effect
In addition, conventional oral dosage forms, such as tablets, capsules, granules (infusions), etc., due to the granulation process in the preparation process, will generate relatively large dust pollution, which will cause health problems to the staff to a certain extent. harm, and also cause some pollution to the environment
Furthermore, the production process of conventional oral preparations is complicated and the production cost is high, so that the cost of medication for patients is also increased, which is not conducive to improving the ability of patients to seek medical treatment, and is also not conducive to improving the overall health level of society.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0064] Now with several groups of specific examples, the preparation method of tolterodine tartrate sustained-release dropping pills of the present invention is further described.

[0065] First group:

[0066] Based on a total weight of 100g, take by weighing substrate PEG400040%, PEG600010%, PEG150010%, stearic acid 11%, glyceryl monostearate 17%, stabilizer vitamin A 2%, raw material tolterodine tartrate 10%; The matrix is ​​placed in a heating container and heated and stirred to melt, then add the corresponding proportion of tolterodine tartrate, stir well, then add the stabilizer vitamin A and stir evenly, under the condition of heat preservation, melt or mix the liquid medicine Drop it into a condensation column filled with simethicone, where the temperature when heated and melted is 55°C, the temperature of the upper part of the condensate is 20°C, and the temperature of the bottom is -4°C; take it out after forming.

[0067] The obtained product has a 2-hour cumulativ...

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PUM

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Abstract

The invention discloses a drug compound for treating urinary incontinence, frequency of micturition and urgency of micturition due to bladder stimulation and particularly relates to a prepared sustained-release tolterodine tartrate dropping pill adopting tolterodine tartrate as the ingredient. The drug compound aims to supplement the deficiency of the prior art and provide a sustained-release tolterodine tartrate dropping pill formulation. The sustained-release tolterodine tartrate dropping pill is prepared by adding stabilize Vitamin A and hydrophobic framework ingredients to the ingredients adopted by the prior art, thereby overcoming the defects in the prior art effectively, guaranteeing no occurrence of an obvious change related to the substance content for the drug during the effective storage period and having the advantages of full release, controllable release time and high bioavailability simultaneously. The sustained-release tolterodine tartrate dropping pill is suitable for clinical and family use.

Description

technical field [0001] The invention belongs to the technical field of sustained-release pharmaceuticals, in particular to a pharmaceutical composition for urinary incontinence, urinary frequency and urgency caused by bladder stimulation, in particular to a trolterodine tartrate prepared from tolterodine tartrate Terodine sustained-release drop pill drug. Background technique [0002] Tolterodine L-tartrate, the chemical name is (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine L(+ )-tartrate. It is a new type of muscarinic receptor antagonist with good tissue selectivity, and it is clinically used to treat urinary urgency, frequency and urge urinary incontinence. Clinical studies have shown that tolterodine tartrate can significantly reduce the frequency of urination and the number of episodes of urinary incontinence, and has the characteristics of quick onset, long duration of action, and small side effects. [0003] The following is the content of th...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/135A61K47/34A61P13/00A61K47/10
Inventor 曲韵智
Owner 北京博智绿洲医药科技有限公司
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