Cheng Yan-ke, Guo Yi-wang, Shang Ke-xin, Guo Qing-li, Du Shou-ying, Lu Yang
Zhongguo Zhong Yao Za Zhi. 2014 Nov;39(22):4335-9.
In order to test the equilibrium solubility of puerarin in different solvents and solubilizer,cilia toxicity and irritation of these excipient, the balance method, toad in the ciliary body toxicity and rat nasal mucosa irritation were used respectively. Results showed that puerarin solubility was 56.44 g x L(-1) in combined solvent of 30% PEG200 and 10% Kolliphor HS 15. With normal saline solution as negative control and sodium deoxycholate as positive control, the effects of 30% PEG200, 30% PEG 400, 10% Kolliphor HS 15 and combination of 30% of PEG200 and 10% Kolliphor HS 15 on toad palate cilium were observed and cilia movement duration was recorded. The results indicated that there was no significant difference in cilia movement duration among 30% PEG200, 10% Kolliphor HS 15 and normal saline group. The rats long-term nasal mucous membrane irritation of 30% PEG 400, 10% Kolliphor HS 15, which had no cilia toxicity, was studied, with normal saline solution as negative control. There were no significant difference revealed on rat nasal mucosa epithelial thickness among 30% PEG 400, 10% Kolliphor HS 15 and normal saline. Above researches showed 30% PEG 400, 10% Kolliphor HS 15 was ideal for solubility of puerarin nasal drops and showed a lower cilia toxicity and irritation, and can be used as the solvent and solubilizer of puerarin nasal drops.
为考察葛根素在不同溶剂和增溶剂中的平衡溶解度、这些辅料的纤毛毒性和刺激性,分别采用平衡法、蟾蜍睫状体毒性试验和大鼠鼻黏膜刺激性试验。结果表明,葛根素在30%聚乙二醇200(PEG200)与10%聚氧乙烯氢化蓖麻油15(Kolliphor HS 15)的混合溶剂中的溶解度为56.44 g·L⁻¹。以生理盐水为阴性对照、脱氧胆酸钠为阳性对照,观察30% PEG200、30%聚乙二醇400(PEG 400)、10% Kolliphor HS 15以及30% PEG200与10% Kolliphor HS 15的组合对蟾蜍上腭纤毛的影响,并记录纤毛运动持续时间。结果表明,30% PEG200、10% Kolliphor HS 15组与生理盐水组的纤毛运动持续时间无显著差异。以生理盐水为阴性对照,研究了无纤毛毒性的30% PEG 400、10% Kolliphor HS 15对大鼠鼻黏膜的长期刺激性。30% PEG 400、10% Kolliphor HS 15组与生理盐水组大鼠鼻黏膜上皮厚度无显著差异。上述研究表明,30% PEG 400、10% Kolliphor HS 15对葛根素滴鼻剂的增溶效果理想,且纤毛毒性和刺激性较低,可作为葛根素滴鼻剂的溶剂和增溶剂。