School of Pharmacy, University of Reading, Reading, RG6 6AD, United Kingdom.
Clasado Research Services Ltd, Science and Technology Centre, University of Reading, Earley Gate, Whiteknights Road, Reading, RG6 6BZ, United Kingdom.
Int J Pharm. 2014 May 15;466(1-2):400-8. doi: 10.1016/j.ijpharm.2014.03.034. Epub 2014 Mar 20.
Probiotic bacteria have gained popularity as a defence against disorders of the bowel. However, the acid sensitivity of these cells results in a loss of viability during gastric passage and, consequently, a loss of efficacy. Probiotic treatment can be supplemented using 'prebiotics', which are carbohydrates fermented specifically by probiotic cells in the body. This combination of probiotic and prebiotic is termed a 'synbiotic'. Within this article a multiparticulate dosage form has been developed, consisting of poly(d,l-lactic-co-glycolic acid) (PLGA) microcapsules containing prebiotic Bimuno™ incorporated into an alginate-chitosan matrix containing probiotic Bifidobacterium breve. The aim of this multiparticulate was that, in vivo, the probiotic would be protected against gastric acid and the release of the prebiotic would occur in the distal colon. After microscopic investigation, this synbiotic multiparticulate was shown to control the release of the prebiotic during in vitro gastrointestinal transit, with the release of galacto-oligosaccharides (GOS) initially occurred over 6h, but with a triphasic release pattern giving further release over 288 h. Encapsulation of B. breve in multiparticulates resulted in a survival of 8.0 ± 0.3 logCFU/mL cells in acid, an improvement over alginate-chitosan microencapsulation of 1.4 logCFU/mL. This was attributed to increased hydrophobicity by the incorporation of PLGA particles.
益生菌已作为预防肠道紊乱的一种方法而受到欢迎。然而,这些细胞的酸敏感性导致在胃中通过时活力丧失,因此功效丧失。可以使用“益生元”来补充益生菌治疗,益生元是被体内益生菌细胞专门发酵的碳水化合物。益生菌和益生元的这种组合被称为“合生菌”。在本文中,开发了一种多颗粒剂型,该剂型由含有掺入到含有短双歧杆菌的藻酸盐-壳聚糖基质中的益生元 Bimuno™的聚(D,L-丙交酯-共-乙交酯)(PLGA)微胶囊组成。这种多颗粒的目的是,在体内,益生菌将免受胃酸的侵害,并且在远端结肠中发生益生元的释放。经过微观研究,表明这种合生菌多颗粒在体外胃肠道转运过程中控制了益生元的释放,半乳糖-低聚糖(GOS)的释放最初发生在 6 小时以上,但呈三相释放模式,在 288 小时内进一步释放。在多颗粒中包封短双歧杆菌导致在酸性条件下存活 8.0 ± 0.3 logCFU/mL 细胞,比藻酸盐-壳聚糖微囊化提高了 1.4 logCFU/mL。这归因于通过掺入 PLGA 颗粒增加了疏水性。