双黄连注射液家兔直肠给药的药代动力学和相对生物利用度研究1

目的 研究双黄连注射液家兔直肠给药的药代动力学和相对生物利用度,对保留灌肠和口服给药进行比较,为直肠给药的科学性提供理论依据。方法 将双黄连注射液中主药金银花的有效成分绿原酸作为血药浓度定量分析的检测指标,根据药物由用药部位进入体循环的速度(即吸收速率Ka)和药物进入体循环的相对量,即吸收程度,通常用血药浓度时间(C T)曲线下面积作指标,观察直肠给药的吸收动力学变化。结果 药代动力学数据说明保留灌肠组与口服组间的AUC 存在显著性差异(P <0.05)。灌肠剂的生物利用度为100%,口服剂的相对生物利用度则为80.78%;保留灌肠剂和口服剂的达峰时间(T_p 值)分别是0.75 和2.48 h,有显著的统计学意义(P <0.05),说明保留灌肠在吸收速度方面优于口服;C_max受吸收量和吸收时间的影响,保留灌肠剂的血清浓度峰值与口服剂的峰值间存在显著性差异(P <0.05),说明保留灌肠剂的血药浓度明显高于口服剂。结论 双黄连注射液有效成分的吸收,直肠比口服给药快,血药浓度高,其吸收总量和生物利用度均高于口服给药。

Pharmacokinetics and relative bioavailability of shuanghuanglian injection in rabbits by rectal medication1

AIM: To investigate the pharmacokinetics and relative bioavailability of shuanghuanglian injection in rabbits by rectal medication in comparison with oral medication.METHODS: Chlorogenic aci from flos loniceraed,a main component in shuanghuanglian injection,was used as a detection marker in blood drug.According to the velocity of drug entering into systemic circulation from medication site(that is,absorption rate K_a)and the relative quantity of drug entering into systemic circulation from medication site(that is,absorption degree),AUC was usually used as a marker to observe absorption dynamic changes of rectal medication.RESULTS: There was significant difference of AUC between clusis groupand oral group(p<0.05).Bioavailability of enema was 100%,and oral dose 80.87%;The values of T_p of enema and oral dose were 0.75 h and 2.48 h,respectively(p<0.05),showing that clusis was superior to oral medication;C_max was affected by absorption quantity and time.There was significant difference of C_max between enema and oral dose(p<0.05),showing that the blood drug concentration of enema was obviously higher than that of oral dose.CONCLUSION: For the chlorogenic acid from shuanghuanglian injection,the absorption in rectal medication is faster than that in oral medication,and the blood concentration,total absorption quantity and bioavailability of rectal medication are higher than ones of oral medication.