Voigt R, Richter M
Pharmazie. 1984 Sep;39(9):618-20.
Interactions of drugs containing macro-molecular agents (cellulose derivatives, polyvinylpyrrolidone) as determined by equilibrium dialyses influence on the in-vitro liberation (hydrophilic membrane) from hydrogels of the same viscosity acc. to the binding intensity. Utilizing a lipophilic membrane, this can be proved, too, the liberation intensity, however, is substantially determined by the lipoidwater distribution behaviour of the drugs. In-vivo liberations revealed in this, that differentiations in the liberation from methylcellulose and polyvinylpyrrolidone gels occur solely in drugs having a more intense affinity. The penetration intensity of the hydrogel into skin is, however, not caused by the binding tendency but by the lipoidwater distribution behaviour of the drugs. Analysing the in-vitro liberation with the use of a lipophilic membrane or knowing the distribution coefficient, informations on the level of the probable drug penetration gel/skin can be given.
通过平衡透析法测定的含有大分子试剂(纤维素衍生物、聚乙烯吡咯烷酮)的药物相互作用,根据结合强度影响相同粘度水凝胶的体外释放(亲水膜)。利用亲脂性膜也能证明这一点,然而,释放强度基本上由药物的脂水分配行为决定。体内释放表明,从甲基纤维素和聚乙烯吡咯烷酮凝胶中释放的差异仅发生在具有更强亲和力的药物中。然而,水凝胶渗透到皮肤中的强度不是由结合倾向引起的,而是由药物的脂水分配行为引起的。通过使用亲脂性膜分析体外释放或了解分配系数,可以给出关于药物渗透凝胶/皮肤水平的信息。