The in vitro dissolution of total composition of the tablet of rhizomes of Ligusticum chuanxiong components and in vitro-in vivo correlation by the method of area under the absorbance-wavelength curve / 药学学报

To discuss the availability of evaluation on the dissolution studies of the multicomponents in traditional Chinese medicine, the in vitro dissolution of total composition of the tablet of rhizomes of Ligusticum chuanxiong components and its correlation with the in vivo were studied by the method of area under the absorbance-wavelength curve (AUAWC). Taken the tablet of rhizomes of Ligusticum chuanxiong components which is composed of sodium ferulate and ligustrazine hydrochloride as subject model, the dissolution tests were carried out with basket method. The plasma concentrations of tablets in different rats were determined by AUAWC at different interval times. The in vivo absorption percentage was calculated by Wagner-Nelson equation to evaluate the in vitro and in vivo correlation. According to the results, the cumulative dissolution in vitro of total composition of tablets of rhizomes of Ligusticum chuanxiong components at 60 min was 90.65% in water by AUAWC. The in vivo pharmacokinetics is fitted with an one-compartment model. The linear equation based on the cumulative dissolution rate (fr) and absorption percentage (fa) at 5, 10, 20, 30 and 60 min was fa = 0.819 7 fr+0.183 and the correlation coefficient was 0.959 5, which showed a good correlation between the in vitro dissolution and the in vivo absorption percentage. The method of AUAWC can be used accurately, feasibly and conveniently to evaluate the in vitro and in vivo correlation of total composition of tablets of rhizomes of Ligusticum chuanxiong components, which will provide better guidance to study the in vitro and in vivo correlation of sustained release preparation etc under complex system of traditional Chinese medicine in the future.

Simultaneous determination on absolute bioavailability of preparation of Chuanxiong Radix components in rats by method of AUAWC and HPLC / 中草药

Objective: The absolute bioavailability of the preparation of Chuanxiong Radix components in rats was simultaneously studied by two methods of area under absorbance-wavelength curve (AUAWC) and high performance liquid chromatography (HPLC), which would confirm the feasibility that AUAWC could be used to determine the absolute bioavailability of components of Chinese materia medica (CMM). Methods: Based on the random two-way cross-over design, 60 SD rats were given the injection of Chuanxiong Radix components by iv and the same amount of drug suspension of the tablet of Chuanxiong Radix components by ig, respectively. Blood samples were collected at various time points after the administration. Plasma concentration of the total components, sodium ferulate, and ligustrazine hydrochloride of the two preparations of Chuanxiong Radix components in rats was measured by AUAWC combined with HPLC. Pharmacokinetic parameters and absolute bioavailability were calculated by DAS 2.0 program and the data obtained by the two methods were compared. Results: After ig administration, AUC0-∞ of total components was (77.218±13.492) mg·min/L by AUAWC and AUC0-∞ of total component was (169.775±18.252) mg∙min/L for iv injection. The absolute bioavailability of tablet of ligustrazine hydrochloride were (69.134±4.853) and (16.422±2.584) mg∙min/L, respectively by HPLC. As for iv injection, AUC0-∞ of sodium ferulate and ligustrazine hydrochloride were (155.244±28.994) and (36.754±6.645) mg∙min/L, respectively. The absolute bioavailabilities of ig administration were 44.53% and 44.68%, respectively. The data obtained by AUAWC were similar to by HPLC. Conclusion: The method of AUAWC can be used to determine the absolute bioavailability on the mixed drugs in the tablet of Chuanxiong Radix components, which will be helpful to solve the problem that the total and individual drugs of the preparation can be coanalyzed together under the combination method of HPLC. It will provide better enlightenment to study the absolute bioavailability of the mixed drugs from Western compound chemicals or complex components in CMM.