Simvastatin dry powder inhalant and preparation method thereof

A technology of dry powder inhaler and simvastatin, which is applied in the field of simvastatin dry powder inhaler and its preparation, can solve the problems of mucous membrane irritation and inability to completely eliminate the greenhouse effect, and achieve increased deposition, improved powder fluidity and Good drug release ability and atomization effect

Active Publication Date: 2015-11-25
GUANGZHOU GONGHE MEDICINE TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the inhalation aerosol uses a new type of propellant HFA to replace Freon’s damage to the ozone layer, HFA and Freon are both greenhouse gases and have the potential for greenhouse effects. HFA’s replacement of Freon cannot completely eliminate the greenhouse effect, and the inhalation aerosol The agent uses absolute ethanol, polyethylene glycol, etc. as cosolvents, which are irritating to the mucous membrane

Method used

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  • Simvastatin dry powder inhalant and preparation method thereof
  • Simvastatin dry powder inhalant and preparation method thereof
  • Simvastatin dry powder inhalant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Weigh 100 g of simvastatin and 322 g of sulfobutyl ether-β-cyclodextrin, mix them uniformly in a grinder, add 25% ethanol aqueous solution, grind for 1 hour, and dry at 45° C. to obtain simvastatin cyclodextrin inclusion compound.

[0046] Adopt the SD-1000 spray drier of Japanese EYELA company to prepare simvastatin liposome complex fine powder, the above-mentioned prepared simvastatin cyclodextrin inclusion complex 50g, soybean lecithin 60g are miscible in 2L isopropanol, Spray drying is carried out after filtration, the adopted process parameters are: inlet temperature 100°C, spray speed 2.0mL min -1 , pump pressure 160KPa, air flow 0.7m 3 min -1 , the outlet temperature was 80° C., and the fine powder of simvastatin liposome complex was prepared.

Embodiment 2

[0048] Weigh 100 g of simvastatin and 358 g of hydroxypropylmethyl-β-cyclodextrin, mix them in a grinder, add 25% ethanol aqueous solution, grind for 1 hour, and dry at 45°C to obtain simvastatin cyclodextrin inclusion complex.

[0049] Adopt the SD-1000 spray drier of Japanese EYELA company to prepare simvastatin liposome complex fine powder, the above-mentioned prepared simvastatin cyclodextrin inclusion compound 50g, egg yolk phospholipid 70g are mixed and dissolved in 2L ethanol, after filtering For spray drying, the imported process parameters are as follows: temperature is 85°C, spray speed is 2.0mL min -1 , pump pressure 160KPa, air flow 0.7m 3 min -1 , the outlet temperature was 75° C., and the fine powder of simvastatin liposome complex was prepared.

Embodiment 3

[0051] Weigh 100 g of simvastatin and 271 g of β-cyclodextrin, mix them in a grinder, add 25% aqueous ethanol, grind for 1 hour, and dry at 45° C. to obtain simvastatin cyclodextrin inclusion compound.

[0052] Adopt the SD-1000 spray dryer of Japanese EYELA company to prepare simvastatin liposome complex fine powder, the simvastatin cyclodextrin inclusion compound 50g prepared above, phosphatidylcholine 70g are dissolved in 2L ethyl acetate solution In the process, spray drying is carried out after filtration, the adopted process parameters are: the inlet temperature is 90°C, and the spray speed is 2.0mL·min -1 , pump pressure 160KPa, air flow 0.7m 3 min -1 , the outlet temperature was 70° C., and the fine powder of simvastatin liposome complex was prepared.

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Abstract

The invention provides a simvastatin dry powder inhalant. The simvastatin dry powder inhalant comprises a simvastatin liposome compound and pharmaceutically acceptable auxiliary materials. The simvastatin liposome compound is obtained by compounding cyclodextrin-coated simvastatin with phospholipid. The invention further provides a preparation method of the simvastatin dry powder inhalant. According to the simvastatin dry powder inhalant, the cyclodextrin-coated simvastatin and the phospholipid are compounded into the simvastatin liposome compound which is then compounded with the pharmaceutically acceptable auxiliary materials to obtain the dry powder inhalant; after pulmonary administration of the simvastatin dry powder inhalant, effective part deposition amount of simvastatin can be increased remarkably, so that the efficacy of pulmonary simvastatin administration on treatment of pulmonary diseases such as asthma and chronic pulmonary obstruction is improved. Experimental results show that, by the simvastatin dry powder inhalant, the effective part deposition amount is increased remarkably and curative effect on the pulmonary diseases is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a simvastatin dry powder inhaler and a preparation method thereof. Background technique [0002] Pulmonary diseases such as bronchiectasis, asthma, chronic pulmonary obstruction, and cystic pulmonary fibrosis are characterized by excessive and thick mucus production in the airways, accompanied by chronic airway inflammation, which leads to obstruction of mucociliary clearance and causes tracheal Contraction, increased inflammation, and then cough, dyspnea and other symptoms. The current drugs for the treatment of such diseases include β-adrenergic agonists, steroids and non-steroidal anti-inflammatory drugs. The mechanism of action of these drugs is to dilate the bronchi or reduce inflammation, but the existing drugs still cannot meet the clinical needs. [0003] Simvastatin is an HMG-CoA reductase inhibitor developed by Merck & Co. of the United States. It w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/366A61K47/48A61K47/24A61P11/00A61P11/06
Inventor 谢恒杨舒隽黄芳杨伟
Owner GUANGZHOU GONGHE MEDICINE TECH
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