Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Pharm Dev Technol. 2012 Sep-Oct;17(5):562-73. doi: 10.3109/10837450.2011.557728. Epub 2011 Mar 23.
A series of either hydrophilic or hydrophobic polymers were used to prepare controlled release Ambroxol hydrochloride (AMX) matrix tablets by direct compression. Both the compatibility and flow properties of AMX/polymer mixtures were investigated. The effect of the amount and type of polymer on the physical properties and in vitro drug release was studied and compared to commercially available Ambroxol(®) SR capsules. A kinetic study of the release profile of AMX from the prepared matrix tablets was performed. All excipients used in the study were compatible with the model drug. AMX/drug mixtures containing sodium alginate (NA) and hydroxypropylmethyl cellulose (HPMC) showed better flow properties than other polymers used in the study. The in vitro drug release studies showed that matrix tablets formulae containing 10% HPMC (S7) or a combination of 30% NA and 5% HPMC (Ah) exhibited a higher ability to control the release of AMX. The kinetic study revealed that a diffusion controlled mechanism prevailed except when carbopol was used. Formula Ah followed a non-fickian diffusion mechanism similar to Ambroxol(®) SR capsules. Both formulae S7 and Ah could be considered as potential candidates for formulation of AMX controlled release matrix tablets.
一系列亲水性或疏水性聚合物被用于通过直接压缩制备盐酸氨溴索（AMX）的控制释放基质片剂。研究了 AMX/聚合物混合物的相容性和流动性能。研究了聚合物的用量和类型对物理性质和体外药物释放的影响，并与市售的 Ambroxol(®) SR 胶囊进行了比较。对从制备的基质片剂中释放的 AMX 的释放曲线进行了动力学研究。研究中使用的所有辅料与模型药物相容。含有海藻酸钠（NA）和羟丙基甲基纤维素（HPMC）的 AMX/药物混合物显示出比研究中使用的其他聚合物更好的流动性能。体外药物释放研究表明，含有 10% HPMC（S7）或 30% NA 和 5% HPMC 的组合（Ah）的基质片剂配方具有更高的控制 AMX 释放的能力。动力学研究表明，除了使用卡波姆外，扩散控制机制占主导地位。Ah 配方遵循类似于 Ambroxol(®) SR 胶囊的非菲克扩散机制。配方 S7 和 Ah 都可以被认为是 AMX 控制释放基质片剂制剂的潜在候选者。
