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Levalbuterol sulfate pulsatile capsule and preparation method thereof

A technology of salbutamol sulfate and capsules, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc.

Inactive Publication Date: 2013-05-08
深圳飞翔世纪生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The above patents at home and abroad have not yet seen reports about levosalbutamol drug resin pulse capsules

Method used

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  • Levalbuterol sulfate pulsatile capsule and preparation method thereof
  • Levalbuterol sulfate pulsatile capsule and preparation method thereof
  • Levalbuterol sulfate pulsatile capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Preparation of styrenesulfonic acid-methacrylic acid copolymer

[0033] All monomers were distilled under reduced pressure to remove the polymerization inhibitor before the reaction. First, 17mL (0.2mol) of MAA and 5.75mL (0.05mol) of styrene were added to a three-necked flask equipped with mechanical stirring and a reflux condenser, and then 133mg of 0.7wt% crosslinking agent divinylbenzene and 0.5wt% supernatant were added. Benzoyl oxide 95 mg was used as an initiator. Then 20 mL of 10% PVA aqueous solution (w / v) was slowly added dropwise to the mixture, and N 2 About 30 minutes or so to remove the O dissolved in the solution that can prevent the polymerization reaction 2. In the polymerization reaction, the temperature was raised slowly for 30 minutes to 70°C for 2 hours under vigorous stirring. Slowly raise the temperature for 1 hour to above 90°C and react for 4 hours. Polymer microspheres were filtered and washed repeatedly with methanol and hot water at ...

Embodiment 2

[0039] (1) Preparation of styrenesulfonic acid-methacrylic acid copolymer

[0040] All monomers were distilled under reduced pressure to remove the polymerization inhibitor before the reaction. First, add 4.25mL (0.05mol) of MAA and 23mL (0.2mol) of styrene into a three-necked bottle equipped with mechanical stirring and reflux condenser, then add 0.7wt% crosslinking agent divinylbenzene 133mg and 0.5wt% Benzoyl peroxide 95 mg was used as an initiator. Then 20 mL of 10% PVA aqueous solution (w / v) was slowly added dropwise to the mixture, and N 2 About 30 minutes or so to remove the O dissolved in the solution that can prevent the polymerization reaction 2 . In the polymerization reaction, the temperature was raised slowly for 30 minutes to 70°C for 2 hours under vigorous stirring. Slowly raise the temperature for 1 hour to above 90°C and react for 4 hours. Polymer microspheres were filtered and washed repeatedly with methanol and hot water at 70°C to remove unreacted co...

Embodiment 3

[0046] (1) Preparation of styrenesulfonic acid-methacrylic acid copolymer

[0047] All monomers were distilled under reduced pressure to remove the polymerization inhibitor before the reaction. First, MAA8.5mL (0.1mol) and styrene 11.5mL (0.1mol) were added to a three-necked bottle equipped with mechanical stirring and reflux condenser, and then 0.7wt% crosslinking agent divinylbenzene 133mg and 0.5wt % Benzoyl peroxide 95mg as initiator. Then 20 mL of 10% PVA aqueous solution (w / v) was slowly added dropwise to the mixture, and N 2 About 30 minutes or so to remove the O dissolved in the solution that can prevent the polymerization reaction 2 . In the polymerization reaction, the temperature was raised slowly for 30 minutes to 70°C for 2 hours under vigorous stirring. Slowly raise the temperature for 1 hour to above 90°C and react for 4 hours. Polymer microspheres were filtered and washed repeatedly with methanol and hot water at 70°C to remove unreacted components. Let d...

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Abstract

The invention discloses a levalbuterol sulfate pulsatile capsule, which undergoes pulsatile release in the gastrointestinal tract environment. A preparation comprises levalbuterol sulfate and a pharmaceutically-acceptable polymer. The preparation comprises the following components in percentage by weight: 2-25 percent of the levalbuterol sulfate, 15-45 percent of styrene sulfonic acid-methacrylicacid copolymer and the balance auxiliary materials. A brand new styrene sulfonic acid-methacrylic acid copolymer plays a role in realizing the pulse action. Compared with an ordinary preparation, a pulsatile preparation has the advantages that: the levalbuterol sulfate is released after the preparation is taken for 3-4 hours, the peak time of the medicament is consistent with the disease time, the aim of performing chrono-chemotherapy can be fulfilled, and side effects such as tolerance, zero time effect, rebound phenomenon and the like are reduced. The pulsatile capsule is taken as a cough-relieving medicament clinically.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to L-salbutamol sulfate pulse capsules for asthma medicine and a preparation method thereof. Background technique [0002] The chiral drug levosalbutamol is a β-2 adrenergic receptor agonist, which can stimulate the β-2 adrenergic receptors of bronchial smooth muscle, selectively relax bronchial smooth muscle, and has bronchodilator effect. It is used for the treatment of asthma and asthmatic bronchitis , Bronchospasm in patients with emphysema. As one of the enantiomers of the racemic albuterol, compared with the racemic form, levosalbutamol has reduced side effects and further improved curative effect after removing the dextro-isomer that produces adverse effects. At present, levosalbutamol sprays have been launched abroad, and there is no levosalbutamol preparations listed in my country, but many companies have researched and produced its raw materials, and have completed cl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/137A61K47/32A61P11/08A61P11/06
Inventor 刘宏飞赵欣于小凤许颖师双双
Owner 深圳飞翔世纪生物科技有限公司