Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313, Porto, Portugal.
AAPS PharmSciTech. 2013 Mar;14(1):121-7. doi: 10.1208/s12249-012-9898-9. Epub 2012 Dec 12.
Alternative vectors to deliver viable cells of probiotics, to those conferring limited resistance to gastrointestinal conditions, still need to be sought. Therefore the main goal of the study was to develop tablets able to protect entrapped probiotic bacteria from gastric acidity, thus providing an easily manufacturing scale-up dosage form to deliver probiotics to the vicinity of the human colon. Whey protein concentrate microparticles with Lactobacillus paracasei L26 were produced by spray-drying and incorporated in tablets with cellulose acetate phthalate and sodium croscarmellose. The viability of L. paracasei L.26 throughout tableting as well as its gastric resistance and release from the tablets were evaluated. Storage stability of L. paracasei L26 tablets was also performed by evaluation of viable cells throughout 60 days at 23°C and 33% relative humidity. A decrease of approximately one logarithmic cycle was observed after the acid stage and the release of L. paracasei L26 from the tablets occurred only after 4 h in the conditions tested. Microencapsulated L. paracasei L26 in tablets revealed some susceptibility to the storage conditions tested since the number of viable cells decreased 2 log cycles after 60 days of storage. However, the viability of L. paracasei L26 after 45 days of storage did not reveal significant susceptibility upon exposure to simulated gastrointestinal conditions. The developed probiotic tablets revealed to be potential vectors for delivering viable cells of L. paracasei L26 and probably other probiotics to persons/patients who might benefit from probiotic therapy.
仍需要寻找替代载体,将具有有限胃肠道耐受力的益生菌活菌递送至体内。因此,本研究的主要目标是开发能够保护包埋益生菌免受胃酸侵蚀的片剂,从而提供一种易于制造的规模化剂型,将益生菌递送至人类结肠附近。通过喷雾干燥生产乳清蛋白浓缩微球,包埋副干酪乳杆菌 L26,并将其与醋酸纤维素邻苯二甲酸酯和交联羧甲基纤维素钠一起制成片剂。评估了副干酪乳杆菌 L.26 在片剂制备过程中的存活率及其在胃中的耐受力和从片剂中的释放情况。通过在 23°C 和 33%相对湿度下储存 60 天,评估副干酪乳杆菌 L26 片剂的储存稳定性。在酸性阶段后,观察到约一个对数周期的减少,并且仅在测试条件下 4 小时后才从片剂中释放出副干酪乳杆菌 L26。在片剂中微囊化的副干酪乳杆菌 L26 对所测试的储存条件有一定的敏感性,因为在储存 60 天后,活菌数减少了 2 个对数周期。然而,在暴露于模拟胃肠道条件 45 天后,储存的副干酪乳杆菌 L26 的存活率并未显示出显著的敏感性。开发的益生菌片剂可能成为将副干酪乳杆菌 L26 等其他益生菌活菌递送至可能受益于益生菌治疗的人群/患者的有效载体。