丁立 张钧寿. 沙丁胺醇/异丁烷气雾剂研究:配方筛选和豚鼠呼吸道吸收J. 药学学报, 2009,44(9): 1040-1045.
引用本文: 丁立 张钧寿. 沙丁胺醇/异丁烷气雾剂研究:配方筛选和豚鼠呼吸道吸收J. 药学学报, 2009,44(9): 1040-1045.
DING Li, Zhang-Jun-Shou. Isobutane driven salbutamol sulfate metered dose inhaler: formulation selection and respiratory tract absorption in guinea pigsJ. 药学学报, 2009,44(9): 1040-1045.
Citation: DING Li, Zhang-Jun-Shou. Isobutane driven salbutamol sulfate metered dose inhaler: formulation selection and respiratory tract absorption in guinea pigsJ. 药学学报, 2009,44(9): 1040-1045.

沙丁胺醇/异丁烷气雾剂研究:配方筛选和豚鼠呼吸道吸收

Isobutane driven salbutamol sulfate metered dose inhaler: formulation selection and respiratory tract absorption in guinea pigs

  • 摘要:

    本文研究了以异丁烷 (A-31) 为抛射剂的硫酸沙丁胺醇 (SS) 定量吸入气雾剂 (MDI) 的配方组成和豚鼠吸入后呼吸道的吸收状况。通过溶解度测定和正交实验设计筛选气雾剂配方; 采用豚鼠鼻腔插管吸入法进行吸入气雾剂给药; 以荧光HPLC检测血药浓度, 并对实验数据进行药动学分析。最终筛选出非氟里昂MDI配方, 建立了SS MDI的体内分析法。结果显示: 豚鼠吸入SS/A-31 MDI, 与对照品和氟里昂 (CFC) 配方零阶矩比值分别为143.26%147.01%, 一阶矩亦最高。初步认定A-31可作为CFC MDI的替代抛射剂, 豚鼠吸入吸收效果优于CFC配方, 与国外市售HFA-134a产品相当。

     

    Abstract:

    This paper is to study the iso-butane (A-31)-driven salbutamol sulfate (SS) metered dose inhaler (MDI) formulations and inhaling status in guinea pigs.  Solubility determination and orthogonal design were used to screen non-chlorofluorocarbon (CFC) SS MDI formulations.  Intubation inhalation of MDI in guinea pigs was useded as a main administration method.  Fluorescence HPLC detection method was testified as a  potential method in assaying the concentration of SS in plasma of guinea pigs after inhaling various SS MDI  formulations.  Analysis of the data was executed with statistical moment calculation from which pharmacokinetic parameters were obtained.  The results show that A-31 based on SS MDI formulations were screened and the guinea pigs in vivo determination method after inhaling SS MDI was established.  The zero-moment rations of SS/A-31 MDI formulation to contrast sample and CFC SS MDI was 143.26% and 147.01%, respectively.  The first moment value of SS/A-31 MDI formulation was the highest.  It is a preliminary conclusion that the absorption result of SS/A-31 MDI formulation inhaled by guinea pigs is equivalent to HFA-134a formulation in sale and better than CFC formulation.  A-31 could be used as a potential substitute candidate for CFC MDI propellant.

     

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