Tolterodine sustained release microsphere preparation containing small molecular additive and preparation method thereof

A technology of tolterodine and slow-release microspheres, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, and pharmaceutical formulas, which can solve the problems of increased side effects, decreased drug efficacy, increased patient pain and Discomfort and other problems, to achieve the effect of reducing toxic and side effects, relieving pain, and increasing drug loading

Inactive Publication Date: 2016-10-12
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its unabsorbed part will produce pre-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 patients with urinary incontinence, one or more injections per day will increase the pain and discomfort of patients

Method used

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  • Tolterodine sustained release microsphere preparation containing small molecular additive and preparation method thereof
  • Tolterodine sustained release microsphere preparation containing small molecular additive and preparation method thereof
  • Tolterodine sustained release microsphere preparation containing small molecular additive and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 52.9 mg of tolterodine and 300.0 mg of 7525 7E PLGA, add the above weighed substances into 0.5 ml of dichloromethane and dissolve them, and inject them into 50 ml of 0.5% PVA ( w / w) in the aqueous solution, keep the above homogeneous condition for 5 minutes, then volatile the solvent by stirring at 1000rpm for 4 hours, filter with 25μm and 125μm sieves, wash the microspheres with distilled water three times, and lyophilize. The microspheres containing 8.6% drug were prepared, the embedding rate was 57%, and the measured particle size was 50-300 μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 2 .

Embodiment 2

[0027] Weigh 52.9 mg tolterodine, 300.0 mg 7525 7E PLGA, 0.3 mg stearic acid, add the above weighed substances into 0.5 ml dichloromethane to dissolve, and inject it into In 50 ml of 0.5% PVA (w / w) aqueous solution, keep the above homogeneous conditions for 5 minutes, then stir at 1000rpm to evaporate the solvent for 4 hours, filter with 25μm and 125μm sieves, wash the microspheres with distilled water three times, and freeze-dry. The microspheres containing 9.4% drug were prepared, the embedding rate was 63%, and the measured particle size was 50-300μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 2 .

Embodiment 3

[0029] Weigh 52.9 mg tolterodine, 300.0 mg 7525 7E PLGA, 1.5 mg butyl stearate, add the above weighed substances into 0.5 ml dichloromethane to dissolve, and dissolve them under homogeneous (6000-8000rpm) conditions Inject into 50 ml of 0.5% PVA (w / w) aqueous solution, keep the above homogeneous condition for 5 minutes, then volatile solvent with stirring at 1000rpm for 4 hours, filter with 25μm and 125μm sieves, wash the microspheres with distilled water three times, freeze-dry . The microspheres containing 10.3% drug were prepared, the embedding rate was 68.7%, and the measured particle size was 50-300μm. The line graph of the cumulative release rate of the sustained-release microspheres in the simulated release solution is shown in figure 2 .

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Abstract

The invention provides a tolterodine sustained release microsphere preparation containing a small molecular additive and a preparation method thereof. The method consists of: weighing tolterodine, the small molecular additive and polylactide-glycolide, dissolving them in 0.2-5ml of dichloromethane, under a homogeneous condition, injecting the mixture into an aqueous solution, maintaining the homogeneous condition for 5min, then conducting 1000rpm stirring to volatilize the solvent for 4h, performing filtering with sieves with a pore diameter of 25 micrometers and 125 micrometers respectively, washing the microspheres with distilled water three times, and performing freeze-drying. The invention utilizes fatty acid or fatty acid ester as the additive of the biological sustained release microsphere preparation, the drug release can last for nearly one month, thus greatly reducing the medication frequency, improving the drug bioavailability and therapeutic efficacy, reduce the toxic and side effect, and greatly alleviating the suffering of patients, and improving the quality of life. Encapsulation of tolterodine with polylactide-glycolide can delay the release of tolterodine and reach a sustained release effect. Adding of the small molecular additive changes the existence and distribution form of tolterodine in microspheres, further delays the release of tolterodine, and improves the drug loading capacity.

Description

technical field [0001] The invention provides a tolterodine sustained-release microsphere preparation containing a small molecular additive, and also provides a preparation method thereof, which belongs to the technical field of pharmaceutical preparation. Background technique [0002] Tolterodine belongs to 3,3-diphenylpropylamine muscarinic receptor antagonists, and its oral efficacy is low and its side effects are large, such as dry mouth, constipation, indigestion, headache, dizziness, dry eyes, and 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 injections per day will increase the pain and discomfort of the patient. Contents of the invention [0003] The invention provides a tolterodine ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/137A61K47/12A61K47/14A61K47/34A61P13/00
Inventor 李又欣赵金龙孙凤英刘喜明王晨晖余昌会
Owner JILIN UNIV
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