Bodmeier R, Wang J, Bhagwatwar H
College of Pharmacy, University of Texas, Austin 78712-1074.
J Microencapsul. 1992 Jan-Mar;9(1):89-98. doi: 10.3109/02652049209021226.
Ibuprofen-wax (carnauba, paraffin, beeswax, and the semisynthetic glyceryl esters--Gelucire 64/02 and Precirol ATO5) microparticles were prepared without organic solvents as an alternative to polymeric microparticles. In the melt dispersion technique, the drug-wax melt was emulsified into a heated aqueous phase followed by cooling to form the microparticles. The microparticles were characterized with respect to their drug loading, and morphological and release properties. They were spherical and non-agglomerated and drug loading close to 60 per cent were achieved. The more hydrophilic waxes (Gelucire 64/02 or Precirol ATO5) could be prepared without the use of surfactants. With the other waxes, increasing amounts of sodium lauryl sulphate in the external aqueous phase decreased the drug loading because of drug solubilization when compared to the polymeric stabilizer, poly(vinyl alcohol). The type of wax, the rate of cooling, and the temperature of the aqueous phase had no significant effect on the drug loading because of the low solubility of the drug in the external aqueous phase. The drug release was controlled by the hydrophobicity of the wax. Besides ibuprofen, other water-soluble drugs (ketoprofen, indomethacin, hydrocortisone) were also encapsulated by this method. The wax microparticles could be formulated into an aqueous sustained-release oral suspension dosage form.
布洛芬 - 蜡（巴西棕榈蜡、石蜡、蜂蜡以及半合成甘油酯——Gelucire 64/02和Precirol ATO5）微粒在不使用有机溶剂的情况下制备而成，作为聚合物微粒的替代物。在熔融分散技术中，药物 - 蜡熔体被乳化到加热的水相中，随后冷却以形成微粒。对微粒的载药量、形态和释放特性进行了表征。它们呈球形且无团聚，载药量接近60%。亲水性更强的蜡（Gelucire 64/02或Precirol ATO5）可以在不使用表面活性剂的情况下制备。对于其他蜡，与聚合物稳定剂聚乙烯醇相比，外部水相中月桂醇硫酸酯钠用量的增加会因药物增溶而降低载药量。由于药物在外部水相中的溶解度较低，蜡的类型、冷却速率和水相温度对载药量没有显著影响。药物释放受蜡的疏水性控制。除布洛芬外，其他水溶性药物（酮洛芬、吲哚美辛、氢化可的松）也通过该方法进行了包封。蜡微粒可制成水性缓释口服混悬剂剂型。
