目的:考察乙醇-油酸聚乙二醇甘油酯(labrafil M 1944 CS)和聚氧乙烯氢化蓖麻油40(cremophor RH40)的鼻黏膜毒性,探讨其在鼻腔给药系统中应用的可行性。方法:以山梨糖醇酐油酸酯(span-80)和聚山梨酯-80(tween-80)为参比,采用在体蟾蜍上...目的:考察乙醇-油酸聚乙二醇甘油酯(labrafil M 1944 CS)和聚氧乙烯氢化蓖麻油40(cremophor RH40)的鼻黏膜毒性,探讨其在鼻腔给药系统中应用的可行性。方法:以山梨糖醇酐油酸酯(span-80)和聚山梨酯-80(tween-80)为参比,采用在体蟾蜍上腭模型,光学显微镜下观察纤毛持续运动时间,考察cremophor RH40和labrafil M 1944 CS的纤毛毒性作用;运用家兔血细胞溶血试验,考察cremophor RH40和labrafil M 1944 CS对细胞膜完整性的影响。结果:体积分数为1%时,4种表面活性剂对纤毛运动的影响顺序为cremophor RH40<labrafil M 1944 CS<tween-80<span-80;cremophor RH40的细胞膜毒性最小,tween-80和span-80次之,而labrafil M 1944 CS的影响最大;cremophor RH40对细胞膜完整性无影响用量为tween-80和span-80的15倍。结论:在一定体积分数下cremophor RH40的鼻黏膜毒性作用较小,可应用于鼻腔给药制剂的研制。展开更多
In the paper, the in vitro dissolution of borneol in 12 hours from 6 batches of optimized inhalant samples were investigated. As a new dosage form, the in vitro release apparatus of nasal inhalant was invented and a p...In the paper, the in vitro dissolution of borneol in 12 hours from 6 batches of optimized inhalant samples were investigated. As a new dosage form, the in vitro release apparatus of nasal inhalant was invented and a pushing bump was used according to the simulation of the nose expiration and inspiration. Based on the data of r2 in the profile and similar factor f2 from 6 linear release tendencies, a good controlled release and a zero order tendency were observed. It can be suggested that there is a good correlation between the in vitro controlled release and the nose steady self-controllable expiration and inspiration, which will contribute to the trend of insoluble volatile drug controlled release and the effect of quick absorption in nasal pulmonary delivery to cure severe or acute cardiovascular or lung diseases at patients' sleeping, such as angina or breathing obstruction. Also, it was concluded that the prescription composed of insoluble volatile drugs can be prepared to be nasal inhalant from which drugs can be absorbed through nose steady self-controllable inspiration to the lung then into the blood and have a great effectiveness improvement of bioavailability at night timing drug delivery system.展开更多
文摘目的:考察乙醇-油酸聚乙二醇甘油酯(labrafil M 1944 CS)和聚氧乙烯氢化蓖麻油40(cremophor RH40)的鼻黏膜毒性,探讨其在鼻腔给药系统中应用的可行性。方法:以山梨糖醇酐油酸酯(span-80)和聚山梨酯-80(tween-80)为参比,采用在体蟾蜍上腭模型,光学显微镜下观察纤毛持续运动时间,考察cremophor RH40和labrafil M 1944 CS的纤毛毒性作用;运用家兔血细胞溶血试验,考察cremophor RH40和labrafil M 1944 CS对细胞膜完整性的影响。结果:体积分数为1%时,4种表面活性剂对纤毛运动的影响顺序为cremophor RH40<labrafil M 1944 CS<tween-80<span-80;cremophor RH40的细胞膜毒性最小,tween-80和span-80次之,而labrafil M 1944 CS的影响最大;cremophor RH40对细胞膜完整性无影响用量为tween-80和span-80的15倍。结论:在一定体积分数下cremophor RH40的鼻黏膜毒性作用较小,可应用于鼻腔给药制剂的研制。
文摘In the paper, the in vitro dissolution of borneol in 12 hours from 6 batches of optimized inhalant samples were investigated. As a new dosage form, the in vitro release apparatus of nasal inhalant was invented and a pushing bump was used according to the simulation of the nose expiration and inspiration. Based on the data of r2 in the profile and similar factor f2 from 6 linear release tendencies, a good controlled release and a zero order tendency were observed. It can be suggested that there is a good correlation between the in vitro controlled release and the nose steady self-controllable expiration and inspiration, which will contribute to the trend of insoluble volatile drug controlled release and the effect of quick absorption in nasal pulmonary delivery to cure severe or acute cardiovascular or lung diseases at patients' sleeping, such as angina or breathing obstruction. Also, it was concluded that the prescription composed of insoluble volatile drugs can be prepared to be nasal inhalant from which drugs can be absorbed through nose steady self-controllable inspiration to the lung then into the blood and have a great effectiveness improvement of bioavailability at night timing drug delivery system.
