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Medicinal composition containing fesoterodine and preparation method thereof

A technology of fesoterodine and its composition, which is applied in the field of medicinal chemistry, can solve the problems of shortened shelf life, gastrointestinal irritation, osmotic diarrhea, etc., and achieve the effects of enhancing stability, slowing down oxidative degradation, and prolonging storage time

Active Publication Date: 2019-12-17
合肥信风科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although xylitol can effectively slow down the degradation of fesoterodine, since the absorption rate of xylitol in the intestine is less than 20%, it is not easy to be decomposed by gastric enzymes after entering the stomach, and has a certain stimulating effect on the stomach
Because patients with this disease generally need to take medicine for a long time, taking the pharmaceutical composition for a long time can cause gastrointestinal diseases such as abdominal pain, abdominal distension, borborygmus, etc., and in severe cases, osmotic diarrhea can also be caused.
[0005] In addition, even if excipients are used to excipient the active ingredients of the drug, the degradation of fesoterodine can only be relatively slowed down, and it cannot be well prevented from decomposing over time, and in the pharmaceutical process due to Improper technology often leads to inactivation of fesoterodine efficacy
Therefore these shortcomings all shorten the shelf life of this class of drugs, therefore, how to further improve the stability of fesoterodine pharmaceutical composition is a topic worthy of scientific research workers' study

Method used

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  • Medicinal composition containing fesoterodine and preparation method thereof
  • Medicinal composition containing fesoterodine and preparation method thereof
  • Medicinal composition containing fesoterodine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] (1) Preparation of Fesoterodine oily suspension product

[0072] Put 300mL soybean oil into a reaction container, put it in a vacuum drying oven for 5 minutes, take it out, seal it, and ultrasonicate it at room temperature for 5 minutes for pre-dispersion. Ultrasonic pre-dispersion of soybean oil can make the coated oily film more uniform and fine , can improve the stability of the follow-up fesoterodine fumarate oily suspension product and can also reduce the amount of surfactant used. Keep filling with nitrogen in the reaction vessel that soybean oil is housed, cut off air and enter, add 10g fesoterodine fumarate and 1g monoglyceride diacetyl tartrate in reaction vessel, make fesoterodine fumarate and diacetyl tartrate The weight ratio of acetyl tartrate monoglyceride is 10:1, and then stir and disperse at 500 rpm for 10 hours to obtain the semi-finished product of fesoterodine fumarate oily suspension, and then mix the obtained fesoterodine fumarate oily suspension ...

Embodiment 2

[0079] (1) prepare fesoterodine oily suspension product

[0080] Put 300mL of olive oil into a reaction vessel, put it in a vacuum drying oven for 30 minutes, take it out, seal it and ultrasonicate it at room temperature for 10 minutes for pre-dispersion, and keep filling nitrogen in the reaction vessel with olive oil. Add 5g of fesoterodine fumarate and 0.1g of propylene glycol fatty acid ester to the container, so that the weight ratio of fesoterodine fumarate and propylene glycol fatty acid ester is 5:0.1, then stir and disperse at a speed of 3000rpm for 3h, Obtain the semi-finished product of fesoterodine fumarate oily suspension, then centrifuge the semi-finished product of fesoterodine fumarate oily suspension obtained at 5000rpm, remove the clarified oil layer after centrifugation, then wash 2 times with ethanol, wash with Afterwards, the semi-finished product of fesoterodine oily suspension was obtained and vacuum-dried at 25°C to finally obtain the fesoterodine oily s...

Embodiment 3

[0086] (1) prepare fesoterodine oily suspension product

[0087] Put 300mL of a mixture of linseed oil and soybean oil into a reaction vessel, wherein the weight ratio of linseed oil and soybean oil is 2:0.8, then add 0.6g of soybean lecithin, put it in a vacuum drying oven for 30 minutes, and take it out Seal and ultrasonicate at room temperature for 5min to carry out pre-dispersion, keep filling with nitrogen in the reaction vessel equipped with linseed oil and soybean oil, add 10g fesoterodine fumarate and 0.3g citrate monoglycerol in the reaction vessel ester, so that the weight ratio of fesoterodine fumarate and monoglyceride citrate is 10:0.3, then stir and disperse for 5h at a rotating speed of 3000rpm to obtain the semi-finished product of fesoterodine fumarate oily suspension, and then Obtain the fesoterodine fumarate oily suspension semi-finished product and carry out centrifugation under 5000rpm, remove the clarified oil layer after centrifugation, then wash 2 times...

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Abstract

The invention belongs to the technical field of medical chemistry and particularly relates to a pharmaceutical composition and a preparation method thereof. According to the provided pharmaceutical composition containing fesoterodine and the preparation method of the pharmaceutical composition, dextrin, maltodextrin, mannitol, cyclodextrin and / or sucrose are selected as stabilizers, and the stability of the pharmaceutical composition containing fesoterodine is greatly improved by optimizing the compatibility of components and improving process conditions. In addition, by pretreating a main drug of fesoterodine, not only are the problems solved that fesoterodine is likely to be hydrolyzed and oxidized under high-temperature and high-humidity conditions, but also the problem is solved that pharmaceutically acceptable excipients used in existing fesoterodine pharmaceutical compositions cause gastrointestinal side effects; the pharmaceutical composition has application properties in a wider range.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a pharmaceutical composition containing fesoterodine and a preparation method thereof. Background technique [0002] Overactive bladder syndrome is the sudden, abnormal need to void, usually accompanied by frequency and nocturia, with or without symptoms of urinary urge incontinence, clinically manifested by noninhibited bladder contractions. Among them, overactive bladder is the most common cause of urinary incontinence in the elderly, but the pathogenesis of the disease has not yet been clarified. As my country's population aging becomes more and more serious, the number of patients suffering from this disease is also on the rise. Studies have shown that the prevalence of overactive bladder is as high as 17%, and the incidence rate among the elderly over 75 years old is 30% to 40%. Once it occurs, it is relatively difficult to treat. Although the curre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/28A61K47/36A61K31/222A61P13/10
CPCA61K9/2059A61K9/2095A61K9/28A61K31/222A61P13/10
Inventor 高嵩宗国军章晓玲查大俊
Owner 合肥信风科技开发有限公司
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