Lerk C F, Lagas M, Lie-a-Huen L, Broersma P, Zuurman K
J Pharm Sci. 1979 May;68(5):634-8. doi: 10.1002/jps.2600680533.
The effect of phenytoin hydrophilization on the liquid penetration rate into prepared plugs, on the disintegration time, on the in vitro release rate, and on in vivo absorption in humans was studied. Hydrophilization was performed by intensive mixing of the hydrophobic drug with a small amount of methylcellulose solution. Liquid penetration into the treated plugs was independent of the liquid wetting potency and extremely high compared to the pure drug plugs. Analogous results were obtained for the disintegration time and in vitro release rates from capsules loaded with pure and treated drug. A bioavailability study in seven healthy volunteers showed immediate absorption of the treated drug but a 1-hr absorption lag time for the pure drug.
研究了苯妥英的亲水化对制备的栓塞中液体渗透速率、崩解时间、体外释放速率以及人体体内吸收的影响。通过将疏水性药物与少量甲基纤维素溶液充分混合来实现亲水化。液体对经处理栓塞的渗透与液体的润湿能力无关，并且与纯药物栓塞相比极高。对于装有纯药物和经处理药物的胶囊的崩解时间和体外释放速率，也获得了类似结果。一项针对7名健康志愿者的生物利用度研究表明，经处理药物能立即被吸收，而纯药物存在1小时的吸收延迟时间。
