Enhancement of solubility and dissolution of Coenzyme Q_10 using solid dispersion formulation

摘要

This study aimed to develop a stable solid dispersion of Coenzyme Q_10 (CoQ_10) with high aqueous solubility and dissolution rate. Among various carriers screened, poloxamer 407 was most effective to form a superior solid dispersion of CoQ_10 having significantly enhanced solubility. Particularly, solid dispersion of CoQ_10 with poloxamer 407 in the weight ratio of 1:5 prepared by melting method enhanced the solubility of CoQ_10 to the greatest extent. However, it exhibited poor stability and hence Aerosil~R 200 (colloidal silicon dioxide) was incorporated into the solid dispersion as an adsorbent to inhibit the recrystallization process. The solid dispersion of CoQ_10, poloxamer 407 and Aerosil~R 200 in the weight ratio of 1:5:6 exhibited improved stability with no significant change in solubility during the 1-month stability test. Moreover, the solid dispersion formulation containing Aerosil~R 200 significantly enhanced the extent of drug release (approx. 75% release) as well as the dissolution rate of CoQ_10. In conclusion, the present study has developed the stable solid dispersion formulation of CoQ_10 with poloxamer 407 and Aerosil~R 200 for the enhanced solubility and dissolution of CoQ_10, which could also offer some additional advantages including ease of preparation, good flowability and cost-effectiveness.