用三角相图法研究药用微乳的形成条件

APPLICATION OF TRIANGULAR PHASE DIAGRAMS TO INVESTIGATE THE FORMULATION CONDITIONS OF PHARMACEUTICAL MICROEMULSIONS

目的 用建立的改良三角相图法制备低毒药用微乳。方法 选磷脂和聚氧乙烯辛基苯基醚 (OP)为乳化剂 ,乙醇和正辛醇为助乳化剂 ,油酸乙酯和橄榄油为油相 ,以改良三角相图法即固定水相和助乳化剂的比值 (W /A)或油相和助乳化剂的比值 (O/A) ,对比经典三角相图法即固定乳化剂和助乳化剂的比值 (Km)制备的微乳所需乳化剂和助乳化剂的量及相体积比的大小。结果 对磷脂为乳化剂形成的微乳系统 ,改良三角相图法所需乳化剂的量为 6 % - 2 8% ,而经典三角相图法所需乳化剂的量为 2 8% - 2 9 6 %。对OP为乳化剂形成的微乳系统 ,改良三角相图法所需乳化剂为 2 3 % - 40 % ;而经典三角相图法所需乳化剂为 2 7 6 % - 49 8% ,以上两种系统 ,前者均较后者用量小。结论 用改良三角相图代替经典三角相图研究形成药用微乳的理论 ,对寻找低毒性的微乳有积极的指导意义。

AIM To establish innovational triangular phase diagrams for preparation of pharmaceutical microemulsion (ME) with low toxicity as a result of reducing the amount of the emulsifiers. METHODS Lecithin and polyoxyethylene octyl phenyl ether (OP) were used as emulsifiers (E), absolute alcohol and n octyl alcohol as assistant emulsifiers (A), ethyl oleate and olive oil as the oil phase (O). For the innovational triangular phase diagrams, lecithin ethyl oleate water and absolute alcohol (optimized ratio W/A=0 6)system, and OP(olive oil and n octyl alcohol (O/A=0 34) water system were used for preparation of the ME. While for the traditional triangular phase diagrams, OP and n octyl alcohol (E/A= K m=1 5) olive oil water system, lecithin and absolute alcohol (E/A= K m=1 12) ethyl oleate water system were used. Then, the corresponding amounts of the emulsifiers used in both methods were compared. RESULTS In the ME of lecithin systems by the innovational and the traditional methods, the amounts of emulsifier are 6%-28% and 28%-29 6%, respectively. In the ME of OP systems by the innovational and the traditional methods, the amounts of emulsifier are 23%-40% and 27 6%-49 8%, respectively. CONCLUSION The method of innovational triangular phase diagram for preparation of ME is superior to the traditional method in finding out the lower amounts of emulsifiers for ME, and is a feasible method with guiding significance for preparing ME.