Konar N, Kim C
School of Pharmacy, Temple University, 3307 N. Broad Street, Philadelphia, PA 19140, USA.
J Control Release. 1999 Feb 1;57(2):141-50. doi: 10.1016/s0168-3659(98)00112-6.
A new erodible, anionic carrier for cationic drugs has been synthesized for oral drug delivery systems. The release properties of tablets prepared from this new material, poly(acrylamido-2-methyl-1-propanesulfonate sodium -co- methyl methacrylate) (PAMPSNa/MMA), are discussed. Pseudo-linear release profiles were obtained and the hydrophobicities of both the polymeric carrier and the bound drugs were found to be an important controlling factor in determining the slopes of these release profiles. The effect of the tablet geometry on the shape of the release profiles was also investigated and tablet thickness was demonstrated to be another key parameter controlling both the linearity of the release profiles, as well as the duration of drug release. The release kinetics are strongly dependent on the drug solubility rather than on the type of amine in the drug (i.e. secondary and tertiary amines). The release of drugs from tablets of drug-PAMPSNa/MMA complexes were well described by the dissociation/erosion mechanism.
一种用于口服给药系统的新型可蚀解阴离子型阳离子药物载体已被合成。本文讨论了由这种新材料聚(丙烯酰胺基-2-甲基-1-丙烷磺酸钠-co-甲基丙烯酸甲酯)(PAMPSNa/MMA)制备的片剂的释放特性。获得了拟线性释放曲线,并且发现聚合物载体和结合药物的疏水性是决定这些释放曲线斜率的重要控制因素。还研究了片剂几何形状对释放曲线形状的影响,结果表明片剂厚度是控制释放曲线线性以及药物释放持续时间的另一个关键参数。释放动力学强烈依赖于药物溶解度,而非药物中胺的类型(即仲胺和叔胺)。药物从药物-PAMPSNa/MMA复合物片剂中的释放可用解离/侵蚀机制很好地描述。