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 day-night change, the best administration time is 12:00 in the morning, easy to produce resistance. Receptivity, drug waste, etc.

Inactive Publication Date: 2006-06-14
SHANGHAI INST OF PHARMA IND CO LTD
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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 changes from day to night, and the best time for administration is at 12 o'clock in the morning. It will cause unnecessary waste of drugs, and it is easy to develop tolerance

Method used

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

Examples

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

The invention discloses a time-controlled pulse sustained-release oral preparation of albuterol and a preparation method thereof. The oral preparation is composed of sustained-release microspheres containing the main drug, an immediate-release coat layer wrapped outside the microspheres, and a time-lag coat layer wrapped outside the immediate-release coat layer. The present invention uses a combination of pulse and sustained release. dual release system. The dosage form is characterized by delayed pulse release over a predetermined period of time, followed by slow release. The oral preparation can provide a rapid pulse release at a specified time lag, and then continue to release the drug slowly for a period of time, so as to achieve the effect of treatment in line with the rhythm of the disease and control symptoms within a period of time. Such treatment will have maximum patient compliance and minimal side effects.

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] Receptorology of the pathogenesis of asthma points out that the function of β-receptors is low during the onset of asthma, which may be related to the presence of autoantibodies to β2-receptors in the serum of asthmatic patients, which leads to a decrease in the density of β2-receptors in the lungs. 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 from day to night, and the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/137A61K9/16A61P11/06
Inventor 金方奚泉闻聪俞雄
Owner SHANGHAI INST OF PHARMA IND CO LTD
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