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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SSMDI的体内分析法。结果显示:豚鼠吸入SS/A-31MDI后,与对照品和氟里昂(CFC)配方零阶矩比值分别为143.26%和147.01%,一阶矩亦最高。初步认定A-31可作为CFCMDI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。
In this paper, we studied the formulation of salbutamol sulphate-based quantitative inhalation aerosol (MDI) using isobutane (A-31) as a propellant and the respiratory tract absorption after guinea pig inhalation. The aerosol formulation was screened through the solubility determination and the orthogonal experiment design. Inhalation aerosol was given by inhalation of guinea pig nasal intubation. The plasma concentration of the drug was measured by fluorescence HPLC. The experimental data were analyzed by pharmacokinetics. Finally, the non-Freon MDI formula was screened and the SSMDI in vivo assay was established. The results showed that the zeroth-order moment ratios of the formulated guinea pigs to SS / A-31MDI were 143.26% and 147.01%, respectively, and the first-order moments were the highest. Preliminary identification of A-31 can be used as an alternative to CFCMDI propellant, guinea pig inhalation and absorption better than CFC formula, with the foreign market HFA-134a comparable products.