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目的研究栀子环烯醚萜苷类成分鼻腔给药的吸收特性,为其鼻腔给药制剂设计提供依据。方法采用Franz扩散池,选用新鲜猪鼻黏膜为渗透屏障,以栀子苷为测定指标,HPLC测定含量,进行渗透试验;采用大鼠鼻腔循环灌流实验,以PBS溶液(pH7.4)作为鼻腔循环液,HPLC测定栀子苷,进行在体鼻黏膜吸收试验。结果栀子苷表观渗透系数Papp为(2.01±0.23)×10 5cm 2.s 1;药物稳态流量Jss为(1.61±0.18)×10 4μg.cm 2.s 1,透黏膜扩散属于以膜两侧浓度差为动力的被动扩散。栀子苷大鼠在体鼻黏膜吸收动力学方程lnC=1.165 7 0.001 6t,r=0.991 4,k=(1.6±0.021)×10 3min 1。结论栀子环烯醚萜苷可经鼻吸收,可制成经鼻给药的新制剂用于脑部疾病的防治。
OBJECTIVE To study the absorption characteristics of iridoid glycosides in nasal cavity by nasal administration, and provide the basis for the design of nasal preparations. Methods Franz diffusion cells were used to select the fresh pig nasal mucosa as the osmotic barrier. The content of geniposide was determined by HPLC, and the osmotic concentration was determined by HPLC. The rat nasal circulation perfusion experiment was performed with PBS (pH7.4) , HPLC determination of geniposide, in vivo nasal absorption test. Results The apparent permeation coefficient (Papp) of geniposide was (2.01 ± 0.23) × 10 5 cm 2 s -1. The steady-state flow Jss of drug was (1.61 ± 0.18) × 10 4 μg cm 2 s -1. The concentration difference on both sides is the passive diffusion of momentum. The absorption kinetics equation of geniposide in rat nasal mucosa was 1.165 7 0.001 6t, r = 0.991 4, k = (1.6 ± 0.021) × 10 3min 1. Conclusion Gardenia iridoid glycosides can be nasally absorbed and can be made into nasal administration of new preparations for the prevention and treatment of brain diseases.