Critical Pharmaceuticals Ltd., BioCity, Nottingham, Pennyfoot Street, Nottingham NG1 1GF, UK.
J Control Release. 2012 Aug 20;162(1):194-200. doi: 10.1016/j.jconrel.2012.06.014. Epub 2012 Jun 16.
The absorption enhancing efficiency of CriticalSorb for human growth hormone (MW 22 kDa) was investigated in the conscious rat model. The principle absorption enhancing component of CriticalSorb, Solutol HS15, comprises polyglycol mono- and di-esters of 12-hydroxystearic acid combined with free polyethylene glycol. When administering hGH nasally in rats with increasing concentrations of Solutol HS15, it was found that for a 10%w/v solution formulation a bioavailability of 49% was obtained in the first 2h after administration. Furthermore it was shown that the most effective ratio of Solutol HS15 to hGH was 4:1 on a mg to mg basis. Histopathology studies in rats after 5 days repeated nasal administration showed that Solutol HS15 had no toxic effect on the nasal mucosa. These results have been confirmed in a 6 month repeat nasal toxicity study in rats. It can be concluded that the principle absorption enhancing component of CriticalSorb - Solutol HS15 - is a potent and non- toxic nasal absorption enhancer that warrants further development.
在清醒大鼠模型中研究了 CriticalSorb 对人生长激素（MW 22 kDa）的吸收增强效率。CriticalSorb 的主要吸收增强成分 Solutol HS15 由 12-羟基硬脂酸的聚乙二醇单酯和二酯与游离聚乙二醇组成。当以递增浓度的 Solutol HS15 经鼻给予 hGH 时，发现 10%w/v 溶液配方在给药后 2 小时内获得了 49%的生物利用度。此外，还表明以毫克对毫克为基础，Solutol HS15 与 hGH 的最有效比例为 4:1。大鼠重复 5 天经鼻给药后的组织病理学研究表明，Solutol HS15 对鼻黏膜没有毒性作用。这些结果在大鼠的 6 个月重复经鼻毒性研究中得到了证实。可以得出结论，CriticalSorb 的主要吸收增强成分 - Solutol HS15 - 是一种有效的、非毒性的鼻吸收增强剂，值得进一步开发。
