Chun Myung Kwan, Cho Chong Su, Choi Hoo Kyun
College of Pharmacy, Chosun University, 375 Seoseok-dong, Dong-gu, Kwangju, South Korea.
J Control Release. 2002 Jun 17;81(3):327-34. doi: 10.1016/s0168-3659(02)00078-0.
To develop a new mucoadhesive drug carrier, poly(vinyl pyrrolidone) (PVP)/poly(acrylic acid) (PAA) interpolymer complexes were prepared by the template polymerization of acrylic acid using PVP as a template polymer. Fourier transform infrared results showed that the interpolymer complexes were formed by hydrogen bonds between the carboxyl groups of PAA and the carbonyl groups of PVP. The adhesive forces of the PVP/PAA interpolymer complexes were higher than that of commercial Carbopol 971. Moreover, the adhesive force and the release rate can be controlled by changing the mole ratios of PVP and PAA. The release rates of ketoprofen from the PVP/PAA interpolymer complexes showed pH-dependency, and were slower at lower pH. The release rate of ketoprofen from the complex seemed to be mainly controlled by the dissolution rate of the complex above a pK(a) of PAA (4.75) and by the diffusion rate below the pK(a). The prepared complex appears to be an adequate carrier for the mucoadhesive drug delivery system.
为开发一种新型黏膜黏附药物载体,以聚乙烯吡咯烷酮(PVP)为模板聚合物,通过丙烯酸的模板聚合制备了聚乙烯吡咯烷酮(PVP)/聚丙烯酸(PAA)互聚物复合物。傅里叶变换红外光谱结果表明,互聚物复合物是由PAA的羧基与PVP的羰基之间的氢键形成的。PVP/PAA互聚物复合物的黏附力高于市售的卡波姆971。此外,通过改变PVP和PAA的摩尔比可以控制黏附力和释放速率。酮洛芬从PVP/PAA互聚物复合物中的释放速率呈现pH依赖性,在较低pH下较慢。在PAA的pK(a)(4.75)以上,酮洛芬从复合物中的释放速率似乎主要受复合物溶解速率的控制;在pK(a)以下,则受扩散速率的控制。所制备的复合物似乎是用于黏膜黏附药物递送系统的合适载体。