ABSTRACT
This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and pharmaceutical properties. Firstly, pseudo-ternary phase diagrams were drawn by dripping method which took Chuanxiong oil as the oil phase and the area of microemulsion region as the index. On this basis, suitable emulsifier and co-emulsifier were screened for the preparation of Chuanxiong oil submicron emulsion. Then, the formula realizing the largest oil loading was selected. Finally, puerarin substituted part of emulsifier and co-emulsifier to lower their content, so as to form puerarin-Chuanxiong oil submicron emulsion featuring the combination of medicine and adjuvant. Its particle size, zeta potential, centrifugal stability and storage stability were determined, and the in vitro drug release behavior was investigated by dialysis bag method, based on which the quality of the as-prepared submicron emulsion was evaluated comprehensively. The proposed method was proved feasible for the preparation of Chuanxiong oil submicron emulsion, which adopted polyoxyethylene castor oil(EL-40) as the emulsifier and was free from co-emulsifier. The formula of the maximum oil loading was found as Chuanxiong oil∶EL-40∶water 3∶7∶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarin∶Chuanxiong oil∶EL-40∶water 7∶30∶63∶900. The quality evaluation results of the as-prepared submicron emulsion demonstrated that the average emulsion droplet size was 333.9 nm, the PDI 0.26, and the zeta potential-10.12 mV. The submicron emulsion had a good centrifugal stability and did not present any instable phenomena such as delamination and precipitation during its standing still for 50 days. The evaluation of in vitro drug release behavior indicated that the submicron emulsion was capable of releasing the drug completely. The puerarin-chuanxiong oil submicron emulsion prepared in this study possessed a stable quality and to some extent increased the solubility of puerarin along with a sustained-release effect. This study provided ideas for the clinical application of puerarin.
Subject(s)
Emulsions , Isoflavones , Particle Size , SolubilityABSTRACT
Objective:To explore the quality transmitting relationship between decoction pieces and substance benchmarks with the fingerprint， index component content and dry extract rate as evaluation indexes， and investigate the key quality attributes of 15 batches of substance benchmarks of Yihuangtang， and establish the quality standard of this substance benchmarks. Method:Fifteen batches of Yihuangtang substance benchmarks freeze-dried powder samples were prepared， the fingerprint and index component content of 15 batches of decoction pieces and substance benchmarks were determined by high performance liquid chromatography （HPLC）， the mobile phase was acetonitrile （A）-0.1% phosphoric acid aqueous solution （B） for gradient elution （0-6 min， 97%B； 6-12 min， 97%-92%B； 12-25 min， 92%-90%B； 25-35 min， 90%-89%B； 35-50 min， 89%-82%B； 50-75 min， 82%-72%B； 75-85 min， 72%-35%B）， the detection wavelength was set at 230 nm， combined the dry extract rate to clarify the attribution of characteristic peaks and the range of similarity with the control chromatogram， the content range and transfer rate range of geniposidic acid and berberine hydrochloride， the dry extract rate range and the variation range of the substance benchmarks. Result:The established HPLC fingerprint had good precision， repeatability and stability， and could be used for the simultaneous determination of decoction pieces and substance benchmarks of Yihuangtang. The similarities between the control chromatogram and fingerprint of substance benchmarks were >0.99. A total of 15 characteristic peaks were assigned， and 8 characteristic peaks were identified by the reference substances， of which 6 were from Phellodendri Chinensis Cortex processed with salt， 1 was from Plantaginis Semen processed with wine， and 1 was from stir-fried Dioscoreae Rhizoma. The content ranges of geniposidic acid and berberine hydrochloride in 15 batches of substance benchmarks of Yihuangtang were 0.10%-0.16% and 0.63%-1.05%， the transfer rate ranges of them were 20.91%-32.65% and 19.60%-29.59%， respectively. The dry extract rate range of the substance benchmarks was 8.45%-9.92%. Conclusion:The quality standard of Yihuangtang substance benchmarks can be preliminarily formulated by the combination of fingerprint， dry extract rate and determination of index component， which can provide the basis for the quality control of Yihuangtang and the development of related preparations.