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Aminophylline slow-release capsules and preparation method thereof

A technology of sustained-release capsules and aminophylline, which is applied in the field of medicine, can solve the problems of poor oral absorption and low bioavailability, and achieve the effects of improving poor taste, good reproducibility, and good curative effect

Active Publication Date: 2012-11-14
YANGZHOU ZHONGBAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to provide a sustained-release capsule of aminophylline to improve the defects of poor oral absorption and low bioavailability

Method used

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  • Aminophylline slow-release capsules and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0031] A kind of aminophylline sustained-release capsule comprises the following components by weight percentage:

[0032] Aminophylline 50%,

[0033] Sodium Carboxymethyl Cellulose 18%,

[0034] Magnesium Stearate 0.5%,

[0035] Ethyl Cellulose 20%,

[0036] Polyethylene glycol (PEG1540) 11.5%.

[0037] The production method is as follows:

[0038] (1) Weigh aminophylline and sodium carboxymethylcellulose, add water with a total weight of 10% (w / w), mix them evenly to make a soft material, granulate with a 20-mesh sieve, and dry at 60°C;

[0039] (2) After adding magnesium stearate and mixing, press into a medicine chip with a diameter of 2mm;

[0040] (3) Take ethyl cellulose and polyethylene glycol, add its gross weight 5% (w / w) acetone to dissolve as coating solution;

[0041] (4) Carry out fluidized bed coating to the aminophylline drug chip obtained in step (2) using the coating solution obtained in step (3), the air inlet temperature is 50°C, the air inlet volume ...

Embodiment 2

[0044] A kind of aminophylline sustained-release capsule comprises the following components by weight percentage:

[0045] Aminophylline 48%,

[0046] Hydroxypropyl Methyl Cellulose 17%,

[0047] Talc 0.5%,

[0048] Eudragit RS 100 25%,

[0049] Polysorbate 20 9.5%.

[0050] The production method is as follows:

[0051] (1) Weigh aminophylline and hydroxypropyl methylcellulose, add water with a total weight of 10% (w / w), mix them evenly to make a soft material, granulate with a 20-mesh sieve, and dry at 60°C;

[0052] (2) After adding talcum powder and mixing evenly, press it into a medicine chip with a diameter of 2mm;

[0053] (3) Weigh Eudragit RS 100 and polysorbate 20, add 5% (w / w) of its total weight in isopropanol to dissolve as coating solution;

[0054] (4) Carry out fluidized bed coating to the aminophylline drug chip obtained in step (2) using the coating solution obtained in step (3), the air inlet temperature is 50°C, the air inlet volume is 2g / min, and the ...

Embodiment 3

[0057] A kind of aminophylline sustained-release capsule comprises the following components by weight percentage:

[0058] Aminophylline 55%,

[0059] Carbopol 15%,

[0060] Micronized silica gel 0.8%,

[0061] Eudragit RL100 21.2%,

[0062] Polysorbate 20 8%.

[0063] The production method is as follows:

[0064] (1) Weigh aminophylline and carbopol, add 10% (w / w) water of its total weight and mix evenly to make a soft material, granulate with a 20-mesh sieve, and dry at 60°C;

[0065] (2) Add micropowder silica gel and mix well, then press it into a 2mm diameter drug chip;

[0066] (3) Weighing Eudragit RL100 and polysorbate 20, adding 5% (w / w) of its total weight in isopropanol to dissolve as a coating solution;

[0067] (4) Carry out fluidized bed coating to the aminophylline drug chip obtained in step (2) using the coating solution obtained in step (3), the air inlet temperature is 45°C, the air inlet volume is 2.5g / min, and the liquid spray speed is 2.0g / min , to pr...

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Abstract

The invention discloses aminophylline slow-release capsules, which comprise the following components in percentage by weight: 45 to 60 percent of aminophylline, 10 to 20 percent of adhesive, 0.3 to 2 percent of flow aid, 18 to 25 percent of coating material and 7 to 13 percent of porogenic agent. The invention also discloses a preparation method for the aminophylline slow-release capsules. The aminophylline slow-release capsules of the invention greatly improve the defects that the oral aminophylline formulation has poor mouthfeel, poor compliance and low bioavailability. In the method, the aminophylline is prepared into tablets; the aminophylline tablets are prepared into slow-release tablets by adopting a fluidized bed coating method; and then the slow-release tablets are filled into capsules so as to prepare the aminophylline slow-release capsules. The preparation method has simple operation and good repeatability, is easy to implement mass production, and achieves the aim of exerting the therapeutic effect better by optimizing the proportion of the coating material and the porogenic agent to control the slow release of the aminophylline in vivo.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an aminophylline sustained-release capsule and a preparation method thereof. Background technique [0002] Aminophylline can relax bronchial smooth muscle, reduce congestion and edema of bronchial mucosa, and is currently the only anti-asthma drug that has dual effects of bronchodilation and reduction of airway inflammation. Aminophylline is widely used in bronchial asthma and chronic obstructive respiratory disease because of its exact curative effect and low price. Ordinary aminophylline preparations need to be taken orally three times a day, night medication affects sleep, and aminophylline treatment blood concentration range is narrow, the blood concentration range is 10-20ug / mL, its bioavailability is related to the elimination rate in the body, Individual differences are large, and they are easily affected by various factors such as physiology, pathology, and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/522A61K47/32A61K47/36A61K47/38A61P11/00
Inventor 葛海涛唐俊杨长明吕建东王党国
Owner YANGZHOU ZHONGBAO PHARMA
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