Tamilvanan Shunmugaperumal, Bangale Ganesh Shesrao, Ananthi Jesudoss Jeya, Sivakumar Vellaichamy, Vinothapooshan Ganesan, Palanivelu Madasamy, Viswanathan Mabepalli Byrappagowbu
Department of Pharmaceutics, Arulmigu Kalasalingam College of Pharmacy, Anand Nagar, Krishnankoil, India.
PDA J Pharm Sci Technol. 2009 May-Jun;63(3):196-206.
The major objectives of the current study were (i) to prepare carvedilol-loaded buccal tablets by direct compression technique, and (ii) to study the influence of low and high proportions of sodium carboxy methylcellulose (SCMC) in conjunction with the corresponding high and low proportions of sodium alginate, polyvinyl pyrrolidone (PVP-K-30), carbopol 974P, and hydroxypropyl methylcellulose (HPMC) on the basic properties (hardness, friability, weight variation, thickness uniformity, drug content, mucoadhesive strength, surface pH, swelling property, and drug release behavior) of the tablets. Altering the polymer combinations did not affect the physical properties of the buccal tablets. However, the presence of SCMC and sodium alginate at 1:2 ratio in the tablet showed a sustained drug release. In addition, this polymer combination at 2:1 ratio did release the drug completely during the stipulated dissolution time. Swelling study indicated the tablet structure collapse over time at 2:1 polymer ratio, thus exposing the drug molecules directly to the dissolution medium to attain the complete drug release from the SCMC and sodium alginate-based tablets. On the other hand, whatever the polymer ratios, the SCMC and carbopol 974P combination always retarded the drug release in an almost similar manner. Though the SCMC- and carbopol 974P-based tablets did display an impressive mucoadhesion property, the surface pH value determined for this polymer combination was found to decrease considerably due to the liberation of the free carboxylic acid over the time period.
（i）采用直接压片技术制备载有卡维地洛的口腔贴片；（ii）研究低比例和高比例的羧甲基纤维素钠（SCMC）与相应的高比例和低比例的海藻酸钠、聚乙烯吡咯烷酮（PVP-K-30）、卡波姆974P和羟丙基甲基纤维素（HPMC）对片剂基本性质（硬度、脆碎度、重量差异、厚度均匀性、药物含量、粘膜粘附强度、表面pH值、溶胀性质和药物释放行为）的影响。改变聚合物组合并未影响口腔贴片的物理性质。然而，片剂中SCMC与海藻酸钠以1:2比例存在时显示出药物的持续释放。此外，这种聚合物组合以2:1比例在规定的溶出时间内确实能使药物完全释放。溶胀研究表明，在聚合物比例为2:1时，片剂结构会随时间崩塌，从而使药物分子直接暴露于溶出介质中，以实现基于SCMC和海藻酸钠的片剂中药物的完全释放。另一方面，无论聚合物比例如何，SCMC与卡波姆974P的组合总是以几乎相似的方式延缓药物释放。虽然基于SCMC和卡波姆974P的片剂确实表现出令人印象深刻的粘膜粘附性能，但由于随着时间的推移游离羧酸的释放，发现该聚合物组合所测定的表面pH值会显著降低。
