Albuterol time controlling pulse slow release oral preparation and its preparation method

A time-controlled pulse, albuterol technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, bulk delivery, etc., can solve the problem of easy tolerance, day-night changes, and the best administration time is early morning. 12 o'clock, drug waste, etc.

Inactive Publication Date: 2005-08-10
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that various physiological indicators of people and certain diseases show rhythmic characteristics. For example, the onset of dyspnea in asthmatic patients

Method used

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  • Albuterol time controlling pulse slow release oral preparation and its preparation method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] (1) Slow-release microspheres:

[0055] Salbutamol sulfate 10g, acrylic resin RS 22g, acrylic resin RL 2g, triethyl citrate 2.4g, magnesium stearate 0.5g, absolute ethanol 90ml, liquid paraffin 270ml;

[0056] (2) Quick-release layer:

[0057] Salbutamol sulfate 10g, hypromellose 20g, water 400g;

[0058] (4) Expansion layer:

[0059] 42g of hydroxypropyl cellulose with a substitution degree of 10%, 13g of Tween 80, 7g of hydroxypropyl cellulose, and 400g of water;

[0060] (3) Isolation layer:

[0061] Hypromellose 2g, polyethylene glycol 4000 0.5g, water 100g;

[0062] (5) Retardation layer:

[0063] Ethyl cellulose 11g, acrylic resin L100 1g, tributyl citrate 1g, ethanol 120ml, talcum powder 1g.

[0064] time (h)

Embodiment 2

[0066] (1) Slow-release microspheres:

[0067] L-albuterol hydrochloride 3g, ethyl cellulose 80g, polyethylene glycol 8g, acetone 90ml, liquid paraffin 270ml;

[0068] (2) Quick-release layer:

[0069] L-albuterol hydrochloride 2.5g, polyvinylpyrrolidone 4g, water 80g;

[0070] (3) swelling layer:

[0071] Sodium carboxymethyl starch 12.6g, sodium lauryl sulfate 6g, hypromellose 1.5g, water 150g;

[0072] (4) Isolation layer:

[0073] Hypromellose 2g, dibutyl sebacate 0.4g, water 40g;

[0074] (5) Retardation layer:

[0075] time (h)

[0076] The process is the same as before. The technical parameters for the preparation of slow-release microspheres are stirring speed: 150 rpm, stirring time: 5 hours

Embodiment 3

[0078] (1) Slow-release microspheres:

[0079] Salbutamol sulfate 8g, ethyl cellulose 24g, polyethylene glycol 2.4g, magnesium stearate 0.63g, absolute ethanol 180ml, liquid paraffin 550ml;

[0080] (2) Quick-release layer:

[0081] Salbutamol sulfate 4g, polyvinylpyrrolidone 8g, water 150g;

[0082] (3) swelling layer:

[0083] Crospovidone 8g, hypromellose 1g, water 100g;

[0084] (4) Isolation layer:

[0085] Hypromellose 1g, polyethylene glycol 0.1g, water 30g;

[0086] (5) Retardation layer:

[0087] time (h)

[0088] The process is the same as before. The process parameters for the preparation of slow-release microspheres are stirring speed: 200 rpm, stirring time: 1 hour

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Abstract

An orally taken salbutamol able to release active components in the sequence: predefined time lag, fast pulse release, and slow release is composed of a slow-release microsphere containing salbutamol, a coated quick release layer, and a coated time-lagging layer.

Description

technical field [0001] The invention relates to an oral formulation of albuterol, in particular to an oral formulation of salbutamol time-controlled pulse sustained release and a preparation method thereof. Background technique [0002] The receptor science of the pathogenesis of asthma points out that the β receptor function is low during the onset of asthma, which may be related to the existence of β receptors in the serum of asthmatic patients. 2 receptor autoantibodies, and thus lead to β in the lung 2 associated with a decrease in receptor density. Clinically, second-generation β-receptor agonists are widely used in the treatment of asthma, especially salbutamol (the annual world sales volume exceeds 1 billion U.S. dollars). With the development of chronobiology and chronopharmacology in recent years, it has been found that various physiological indicators of people and some diseases show rhythmic characteristics. The onset of dyspnea in asthmatic patients changes fro...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/137A61P11/06
Inventor 金方奚泉闻聪俞雄
Owner SHANGHAI INST OF PHARMA IND
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