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Composite aminophylline slow-release capsule and preparation method thereof

The technology of compound aminophylline and sustained-release capsules is applied in pharmaceutical formulations, medical preparations with non-active ingredients, respiratory system diseases, etc. Narrow distribution of effects

Inactive Publication Date: 2018-03-23
HUAYI PHARMA ANHUI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is just to solve problems such as headache, nausea, vomiting, abdominal discomfort and central nervous excitement caused by excessive dosage of traditional theophylline drugs or too fast intravenous administration. Determine the dose according to your own body weight to achieve personalized drug administration, making the drug intake more accurate and safer; at the same time, the active ingredients of the drug are highly soluble in the dispersant in the form of nanometers, which is conducive to full absorption and bioavailability higher

Method used

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  • Composite aminophylline slow-release capsule and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0021] A compound aminophylline sustained-release capsule, the preparation method comprising the following steps:

[0022] 1) Preparation of clathrate: In a stainless steel ceramic reaction kettle, under the conditions of jacketed water bath temperature 50°C-70°C and stirrer speed 120-180 rpm, 8-12 parts by weight of β-cyclopaste Refining into a saturated aqueous solution, then gradually adding 2.8 parts by weight of aminophylline and cholophylline extract hot water solution, stirring and mixing for 2-3 hours, standing at room temperature for 8-15 hours, filtering, and concentrating the filtrate to 1 / 3 volume , dried under reduced pressure and vacuum at 50°C to 70°C, and crushed to obtain compound aminophylline inclusion compound;

[0023] 2) Preparation of sustained-release granules: 20-50 parts by weight of ethylcellulose, 0.87-2.3 parts by weight of hydroxypropylmethylcellulose and 8-23 parts by weight of the clathrate prepared in step 1) were placed in Mix in a dry contai...

Embodiment 2

[0026] A compound aminophylline sustained-release capsule, the preparation method comprising the following steps:

[0027] 1) Preparation of clathrate: In a stainless steel ceramic reaction kettle, under the conditions of jacketed water bath temperature 50°C-70°C and stirrer speed 120-180 rpm, 8-12 parts by weight of β-cyclopaste Refined into a saturated aqueous solution, then gradually add 3.5 parts by weight of the hot aqueous solution of aminophylline and cholophylline extract, stir and mix for 2-3 hours, let stand at room temperature for 8-15 hours, filter, and concentrate the filtrate to 1 / 3 volume , dried under reduced pressure and vacuum at 50°C to 70°C, and crushed to obtain compound aminophylline inclusion compound;

[0028] 2) Preparation of sustained-release granules: 20-50 parts by weight of ethylcellulose, 0.87-2.3 parts by weight of hydroxypropylmethylcellulose and 8-23 parts by weight of the clathrate prepared in step 1) were placed in Mix in a dry container, a...

Embodiment 3

[0031] A compound aminophylline sustained-release capsule, the preparation method comprising the following steps:

[0032] 1) Preparation of clathrate: In a stainless steel ceramic reaction kettle, under the conditions of jacketed water bath temperature 50°C-70°C and stirrer speed 120-180 rpm, 8-12 parts by weight of β-cyclopaste Refined into a saturated aqueous solution, then gradually add 4.2 parts by weight of the hot aqueous solution of aminophylline and cholophylline extract, stir and mix for 2-3 hours, let stand at room temperature for 8-15 hours, filter, and concentrate the filtrate to 1 / 3 volume , 50 ℃ ~ 70 ℃ vacuum drying under reduced pressure, solid pulverization to obtain compound aminophylline inclusion compound;

[0033] 2) Preparation of sustained-release granules: 20-50 parts by weight of ethylcellulose, 0.87-2.3 parts by weight of hydroxypropylmethylcellulose and 8-23 parts by weight of the clathrate prepared in step 1) were placed in Mix in a dry container, ...

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Abstract

The invention discloses a compound aminophylline sustained-release capsule and a preparation method thereof. The inclusion compound is prepared by adopting the method of the β-cyclodextrin inclusion compound sustained-release capsule, and 8-12 parts by weight of the β-cyclodextrin Make a saturated aqueous solution, then gradually add 2.8 to 4.2 parts by weight of aminophylline and hot water solution of cholophylline extract, dry under reduced pressure and vacuum, and crush the solid to obtain clathrates; prepare slow-release granules: 20 to 50 parts by weight ethyl cellulose, 0.87 to 2.3 parts by weight of hydroxypropylmethylcellulose and 8 to 23 parts by weight of the prepared clathrate are mixed in a dry container, added with ethanol solution, stirred to a solid state, dried, pulverized, Obtaining granules; filling of sustained-release capsules: filling empty capsules with the prepared granules to obtain β-cyclodextrin aminophylline inclusion compound sustained-release capsules. The sustained-release capsule of the present invention has good taste, stable quality, can accurately calculate the dose, and reduces the occurrence of adverse reactions that may be caused by inaccurate doses. Moreover, the preparation method is simple to operate, does not require a sterilization step, does not require special equipment, has a short preparation cycle, and is low in cost.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a compound aminophylline sustained-release capsule and a preparation method thereof. Background technique [0002] Due to the deteriorating environmental quality, air pollution has become a major public hazard that endangers human life. Smoking and drug abuse are becoming more and more common. At the same time, various new viruses, bacteria, chlamydia and other pathogenic microorganisms are complicated. The incidence of respiratory diseases has greatly increased, seriously affecting the quality of life of the public. Aminophylline, as a commonly used drug for respiratory diseases, not only requires the standardization and standardization of clinical use, but also needs to be further developed and researched to improve its safety and curative effect, thereby contributing to the treatment of diseases. [0003] Theophylline has been used to treat bronchial asthma for decad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/38A61K31/522A61K47/69A61P11/06
CPCA61K9/1652A61K31/522
Inventor 操铖高煜
Owner HUAYI PHARMA ANHUI CO LTD
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