Khan G M, Jiabi Z
Zhong Kun Pharmaceutical Research Institute, School of Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.
J Control Release. 1998 Jul 31;54(2):185-90. doi: 10.1016/s0168-3659(97)00225-3.
In order to assess the potential of carbopol 974P-NF as matrix material in hydrophilic matrix tablets containing a slightly water-soluble drug, ibuprofen (IBF), controlled release matrix tablets of ibuprofen and carbopol 974P-NF, at different drug to polymer ratios, were prepared by the direct compression method. The influence of the concentration of the matrix material (carbopol 974P) and several co-excipients (lactose, microcrystalline cellulose, and starch) on the release rate of the drug was investigated. An in vitro dissolution test in pH 7.2 phosphate buffer solution showed that drug release from all the formulations containing carbopol 974P was considerably prolonged in concentration-dependent manners. Increasing the amount of carbopol 974P in tablets resulted in a reduction in the drug release rate and a linearization of the drug release curve. When the influence of the co-excipients on the release of the drug was examined, all of the co-excipients used in this study enhanced the release rate of IBF. However, lactose demonstrated slower and more linear release behavior as compared in microcrystalline cellulose or starch. The dissolution T50 and T90 values for the three co-excipients were in the order of lactose > microcrystalline cellulose > starch.
为了评估卡波姆974P-NF作为含微溶性药物布洛芬（IBF）的亲水性基质片剂的基质材料的潜力，采用直接压片法制备了不同药物与聚合物比例的布洛芬和卡波姆974P-NF控释基质片剂。研究了基质材料（卡波姆974P）和几种辅料（乳糖、微晶纤维素和淀粉）的浓度对药物释放速率的影响。在pH 7.2磷酸盐缓冲溶液中进行的体外溶出试验表明，所有含卡波姆974P的制剂中药物释放均以浓度依赖方式显著延长。片剂中卡波姆974P用量的增加导致药物释放速率降低和药物释放曲线线性化。当考察辅料对药物释放的影响时，本研究中使用的所有辅料均提高了IBF的释放速率。然而，与微晶纤维素或淀粉相比，乳糖表现出更缓慢、更线性的释放行为。三种辅料的溶出T50和T90值顺序为乳糖＞微晶纤维素＞淀粉。
