Preparation and in vitro dissolution evaluation of tanshinone IIA for oral self-microemulsion / 中草药

ABSTRACT

Objective: To study the prescription and preparation technology of tanshinone IIA for oral self-microemulsifying drug delivery system. The quality, stability, and in vitro dissolution were evaluated. Methods: The prescription and preparation technology were selected and optimized through the solubility experiment, orthogonal design, and pseudo-ternary phase diagram method, using the self-emulsifying time, appearance, particle diameter, and stability as selection indexes. The droplet morphous, particle size, drug content, stability, and in vitro dissolution were evaluated after self-microemulsification. Results: The prescription composition of tanshinone IIA self microemulsion was aethylis oleas (50%), polysorbate 80 (40%), and PEG 400 (10%), with oil phase-aqueous phase of 150, drug-loaded of 3.0 mg/g, and self-emulsifying time of 1 min. The acquired tanshinone IIA self-microemulsion exhibitted uniform and transparent, with the particle diameter of (51.39 ± 1.50) nm, polydispersity index of 0.211 ± 0.022, Zeta potential of (-11.35 ± 1.19) mV. The results of in vitro dissolution indicated that the accumulative dissolution in 0.1 mol/L HCl solution was able to reach 96% after 30 min. The stability result showed that tanshinone IIA self-microemulsion was affected by high temperature and illumination, indicating having to be stored at 4℃ and protected from light. Conclusion: The preparation of tanshinone IIA self-microemulsion is simple, increasing the solubility in water, making it better absorption in the stomach and intestine, corresponding to the main index of oral drug delivery system and offering the basis for further development and research about tanshinone IIA.