Pongjanyakul Thaned, Khuathan Natnicha
a Faculty of Pharmaceutical Sciences , Khon Kaen University , Khon Kaen , Thailand.
Pharm Dev Technol. 2016;21(4):487-98. doi: 10.3109/10837450.2015.1022787. Epub 2015 Mar 11.
The objectives in this study were to characterize quaternary polymethacrylate-sodium alginate (QPM-SA) films prepared using high G block or high M block SA (GSA or MSA, respectively), and to investigate the effects of QPM-SA ratios, film-coating levels and SA block structures on propranolol HCl (PPN) released from coated tablets. The results demonstrated that GSA and MSA shared a similar interaction mechanism with QPM. The QPM-GSA films had higher puncture strength than the QPM-MSA films in dry and wet states, whereas the % elongations were not different. The drug permeability of the QPM-GSA films was lower than that of the QPM-MSA films in both acidic and neutral media, but higher water uptake of the QPM-GSA films was found at neutral pH. Moreover, the QPM-MSA-coated tablets had a greater PPN release rate than the QPM-GSA-coated tablets, and drug release was dependent on the film-coating levels. In addition, the QPM-SA films at a ratio of 4:0.5 produced a stronger film and could sustain PPN release. These results indicate that the QPM-GSA films had greater film strength and lower drug permeability than the QPM-MSA films. Additionally, the QPM-SA films have a strong potential for use in sustained-release tablets.
本研究的目的是表征使用高G嵌段或高M嵌段海藻酸钠（分别为GSA或MSA）制备的季铵化聚甲基丙烯酸酯-海藻酸钠（QPM-SA）薄膜，并研究QPM-SA比例、包衣水平和海藻酸钠嵌段结构对包衣片剂中盐酸普萘洛尔（PPN）释放的影响。结果表明，GSA和MSA与QPM具有相似的相互作用机制。QPM-GSA薄膜在干燥和湿润状态下的穿刺强度均高于QPM-MSA薄膜，而伸长率并无差异。在酸性和中性介质中，QPM-GSA薄膜的药物渗透性均低于QPM-MSA薄膜，但在中性pH值下，QPM-GSA薄膜的吸水量更高。此外，QPM-MSA包衣片剂的PPN释放速率高于QPM-GSA包衣片剂，药物释放取决于包衣水平。另外，比例为4:0.5的QPM-SA薄膜形成的薄膜更强，且能够维持PPN的释放。这些结果表明，QPM-GSA薄膜比QPM-MSA薄膜具有更高的薄膜强度和更低的药物渗透性。此外，QPM-SA薄膜在缓释片剂中具有很强的应用潜力。
