Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, The University of Jordan, Amman 11942, Jordan.
Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University Duesseldorf, Germany.
Eur J Pharm Sci. 2019 Mar 1;129:140-147. doi: 10.1016/j.ejps.2019.01.004. Epub 2019 Jan 7.
Disintegration of immediate release tablets originates from the volume expansion of disintegrants within the formulation. Here, we study the impact of ethanol on the disintegrant expansion and on tablets disintegration. The three most commonly used superdisintegrants, namely sodium starch glycolate (SSG), crospovidone (PVPP) and croscarmellose sodium (CCS) were investigated alone and incorporated in dicalcium phosphate and in drug-containing tablets. High (i.e. 40%), but not moderate (i.e. 10%), aqueous ethanol concentrations reduce the size expansion of the three disintegrants compared to water. This "ethanol effect" is the greatest for SSG, followed by CCS and then PVPP. Moreover, the presence of ethanol in the media can significantly influence the disintegration time of drug-containing tablets via affecting both the disintegrant action itself and the drug solubility. For example, the disintegration time of theophylline tablets containing SSG is 8.1-fold greater in 40% aqueous ethanol compared to water. Overall, this study brought to light the existence of a potentially significant interference of alcohol with the disintegration phenomenon, suggesting that the concomitant administration of tablets and intake of alcoholic beverages may affect, in some cases, tablets disintegration. More studies are now needed to verify the importance of the "ethanol effect" on disintegration of commercial dosage forms. Our findings also suggest that PVPP is the disintegrant that is the least affected by alcohol.
速崩片的崩解起源于配方中崩解剂的体积膨胀。在这里，我们研究了乙醇对崩解剂膨胀和片剂崩解的影响。研究了三种最常用的超级崩解剂，即交联羧甲基淀粉钠（交联羧甲基纤维素钠）、交联聚维酮（交联聚维酮）和交联羧甲基纤维素钠（交联羧甲基纤维素钠），分别单独使用和与磷酸氢钙和含药片剂混合使用。高浓度（即 40%），而不是中等浓度（即 10%）的水乙醇浓度会降低三种崩解剂的体积膨胀。与水相比，这种“乙醇效应”对 SSG 的影响最大，其次是 CCS，然后是 PVPP。此外，介质中存在乙醇会通过影响崩解剂本身的作用和药物的溶解度，显著影响含药片剂的崩解时间。例如，含有 SSG 的茶碱片剂在 40%水乙醇中的崩解时间比在水中长 8.1 倍。总的来说，这项研究揭示了酒精与崩解现象之间可能存在显著干扰，表明片剂与酒精饮料同时服用可能会在某些情况下影响片剂的崩解。现在需要更多的研究来验证“乙醇效应”对商业剂型崩解的重要性。我们的研究结果还表明，交联聚维酮是受酒精影响最小的崩解剂。
