升麻素苷和5-O-甲基维斯阿米醇苷大鼠在体鼻循环吸收研究

Nasal resorption of prim-O-glucosylcimifugin and 5-O-methylvisammioside in rats

对升麻素苷和5-O-甲基维斯阿米醇苷大鼠在体鼻黏膜吸收特性,为头痛宁鼻腔喷雾剂的给药方式提供依据。采用大鼠在体鼻腔循环灌流法,以pH为6的缓冲溶液配制的高、中、低浓度的升麻素苷、5-O-甲基维斯阿米醇苷混合溶液作为鼻腔循环液,进行大鼠在体鼻黏膜吸收试验,用HPLC测定各循环液中待测成分的浓度,并考察了不同pH条件下升麻素苷和5-O-甲基维斯阿米醇苷的吸收速率。结果显示,升麻素苷高、中、低浓度的大鼠在体吸收速率常数为(0.588±0.041)×10^(-3),(0.547±0.023)×10^(-3),(0.592±0.063)×10^(-3)min^(-1)。5-O-甲基维斯阿米醇苷高中低浓度的吸收速率常数为(0.438±0.041)×10^(-3),(0.407±0.023)×10^(-3),(0.412±0.063)×10^(-3)min^(-1)。高、中、低组间无显著性差异。两者在pH为6的情况下吸收情况较其他p H条件好。推测头痛宁鼻腔喷雾剂中的主要活性成分可经鼻黏膜吸收,制成鼻腔喷雾剂是可行的,头痛宁鼻腔喷雾剂p H控制在6是科学合理的。

In this experiment,rat nasal mucosa absorption characteristics of prim-O-glucosylcimifugin and 5-O-methylvisammioside were studied to provide a basis for drug delivery of Toutongning nasal spray. The nasal mucosa absorption test in rats was conducted with in situ nasal perfusion method after p H 6 buffer solution was used to prepare high,medium and low concentrations of prim-O-glucosylcimifugin,5-O-methylvisammioside mixed solution as liquid circulation in nasal cavity. Then the concentrations of the circulating liquid compositions to be measured were determined by HPLC,and the absorption rates of prim-O-glucosylcimifugin and 5-O-methylvisammioside under different p H conditions were also investigated. According to the results,the absorption rate constant was（0. 588 ±0. 041） × 10^-3,（0. 547 ± 0. 023） × 10^-3,（0. 592 ± 0. 063） × 10^-3min-1for prim-O-glucosylcimifugin high,middle and low concentrations,and（0. 438 ± 0. 041） × 10-3,（0. 407 ± 0. 023） × 10^-3,and（0. 412 ± 0. 063） × 10^-3min^-1 for 5-O-methylvisammioside high,middle and low concentrations. There was no significant difference among high,middle and low concentration groups,and the absorption under pH 6 was better than that under other p H conditions. Therefore,we can get the conclusion that the main active ingredient of Toutongning nasal sprays can be absorbed through the nasal mucosa,and it is feasible to make nasal spray; in addition,pH6 of nasal spray is scientific and reasonable.