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丙酸倍氯米松及其溶剂化合物在三氯-氟甲烷的结晶生长动力学对定量气雾剂行为的影响(英文)

Kinetics of Crystal Growth of BDP and Its Solvates in Trichlorofluoromethane and Their Influence on the Performance of Metered Dose Inhalers

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【作者】 毛磊王娟卞祖清张军

【Author】 Mao Lei; Wang Juan; Bian Zuqing and Zhang Jun(The National Institure of Pharmaceutical Research and Development,Beijing 102206)

【机构】 中国医药研究开发中心北京集爱制药有限公司!北京102206

【摘要】 本文研究了丙酸倍氯米松及其醋酸乙酯和三氯-氟甲烷溶剂化物微粉在三氯一氟甲烷中的结晶生长行为。给出了结晶生长曲线并计算了结晶生长动力学参数、结晶生长的趋势及速度为丙酸倍氯米松>丙酸倍氯米松醋酸乙酯溶剂化物>丙酸借氯米松三氯.氟溶剂化物。15℃时丙酸信氯米松及40℃丙酸倍氯米松醋酸乙酯溶剂化物的结晶生长动力学参数限值成别为0.1637μm·min(-1)及0.0138μm·min(-1)。同时观察并计算了最终平衡粒径。双冲程实验结果表明用丙酸倍氯米松,丙酸倍氯米松醋酸乙酯溶剂化物及丙酸倍氯米松三氯-氟甲烷溶剂化物微粉制备的定量气雾剂在深肺部的沉积为8%、54%及59%,在40%、75%RH条件下贮存两周后,降至20、400及57%。

【Abstract】 The purpose of this paper is to investigate the morphology change and crystalgrowth of fine particles of beclomethasone diopropionate (BDP), its ethyl acetate solvate (BDP-EtOAc) and trichlorofluoromethane solvate (BDP-P11) after contacting trichlorofluoromethane.Curves of crystal growth versus time were obtained and kinetic parameters of crystal growth werecalcu1ated. The tendency and velocity of crystal growth wcr B DP>BDP-EtOAC>BDP-P 1 1. K-valuesof crystal growth curves for BDP at 15℃ and BDP-EtOAc at 40℃ were 0. 1637 μm·min(-1) and 0.0 138μm·min(-1) respectively. Final paticle sizes of BDP were calculated and compared with measuredvalues. Results of bon liquid impinger tests showed that BDP pressurized metered dose inhaler(pMDIs) prepared wtth BDP, BDP-EtOAc and BDP-P11 had deep lung drug deposition of 8%, 54%,and 59%, dropping to 2%, 40%, and 57% after storage at 40℃, 75% RH for 2 weeks respectively.

  • 【文献出处】 Journal of Chinese Pharmaceutical Sciences ,中国药学(英文版) , 编辑部邮箱 ,1999年03期
  • 【分类号】R96
  • 【被引频次】2
  • 【下载频次】51
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