| Naoxuening injection is a traditional Chinese medicine prescription, which is composed of the Cornu Saigae Tataricae, the mouton root bark, the Gardenia jasmineoides Ellis and the Acorus tatarinowii. It is used primarily to the treatment of the apoplexy caused by hypertension. It is at present under clinical study. In this study, we studied the serum pharmacochemistry and the pharmacokinetic characteristics of naoxuening injection after intravenous administration to 10 healthy volunteers.The dissertation is summarized as followed:1．Preliminary study on serum pharmacochemistry of naoxuening inj-ectionAt first, we established a HPLC method to study the fingerprint of naoxuening inj-ection.Based on the established HPLC fingerprint of naoxuening injection, analysis and comparison were carried out among the HPLC profiles of human serum samples obtai-ned after intravenous administration of naoxuening injection, naoxuening injection and blank plasma. Three compounds were detected after intravenous administration of naoxuening injection, one of which is metabolish and two are the original form of the compounds contained in naoxuening injection. One of them which is originated from the Gardenia jasmineoides Ellis is geniposide; the other which is originated from the moutan root bark is paeonol.2．Pharmacokinetic study of geniposide after intravenous administrati- on in humanA HPLC method was developed for the determination of geniposide concentration in human plasma and in human urine.Following intravenous administration of naoxuening injection in dose of 100 mL, in which 120 mg geniposide was contained, plasma concentration and urine concentrat-ion were determined. The result showed that the pharmacokinetic model of geniposide was one compartment model, the chief parameters Tmax, Cmax, t1/2 , Ke, CL, Vd, AUC0→t, AUC0→∞ were 1．15±0．24 h, 3．261±0．947μg·mL-1 , 0．56±0．25 h, 1．44±0．51 h-1 , 0．4712±0．1637 L. (h.kg)-1 , 0．3463±0．1125 L.kg-1 , 4．562±1．431 ng.h.L-1 , 4．728±1．476μg.h.L-1 , respectively. After intravenous administration of naoxuening injection, 70% of the dose was recovered in 10 h; the results indicated that the urine was the main route of its excretion.3．Pharmacokinetic study of paeonol after intravenous administrationin humanA HPLC method was developed for the determination of paeonol concentration in human plasma and in human urine.Following intravenous administration of naoxuening injection in dose of 100 mL, in which 120 mg paeonol was contained, plasma concentration and urine concentration were determined. The result showed that the pharmacokinetic model of paeonol was two compartment open model, the chief parameters Tmax, Cmax, t1/2α, t1/2β, k10 , k12 , k21 , CL, V1, AUC0→t, AUC0→∞ were 0．942±0．35 h, 765±195 ng.mL-1 ,0．597±0．25 h, 4．5±3．01 h,0．76±0．43 h-1 , 0．504±0．32 h-1 , 0．298±0．19 L(h.kg)-1 ,1．122±0．42 L.(h.kg)-1 , 1．706±0．41 L.kg-1 , 1537．7±528．7 ng.h.mL-1 , 1739．7±572 ng.h.mL-1 , respectively. After intravenous administration of naoxuening injection, 0．04% of the dose was recovered in 10 h; the results indicated that the paeonol was extensively metabolished in human body. |
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