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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。
The nasal mucosal absorption characteristics of cistonin and 5-O-methyl-Wistaroside in rats provide basis for the administration mode of headache Ning-nasal spray. In vivo rat nasal circulation perfusion method, high, medium and low concentrations of cinnamarin and 5-O-methylWestoside mixed solution prepared with a buffer solution of pH 6 were used as nasal circulation solution, The rat nasal mucosa absorption test was carried out. The concentration of the analyte in each circulating solution was determined by HPLC. The absorption rate of cimnil and 5-O-methyl-Vaisalanthin at different pH . The results showed that the absorption rate constants of high, medium and low concentrations of cilengine were (0.588 ± 0.041) × 10 ~ (-3), (0.547 ± 0.023) × 10 ~ (-3) and ± 0.063) × 10 ~ (-3) min ~ (-1). The absorption rate constants of high and low concentrations of 5-O-methyl-Vaisalanthin were (0.438 ± 0.041) × 10 -3, (0.407 ± 0.023) × 10 -3, (0.412 ± 0.063) ) × 10 ~ (-3) min ~ (-1). There was no significant difference between high, middle and low groups. Both had better absorption at pH 6 than the other p H conditions. It is speculated that the main active ingredient in the nasal spray nasal spray can be absorbed through the nasal mucosa, nasal spray is feasible, headache Ning nasal spray p H controlled at 6 is scientific and rational.