Combinatorial Use of Sodium Laurate with Taurine or L‐Glutamine Enhances Colonic Absorption of Rebamipide, Poorly Absorbable Antiulcer Drug, without Any Serious Histopathological Mucosal Damages

Optimization of Suppository Preparation Containing Sodium Laurate and Taurine That Can Safely Improve Rectal Absorption of Rebamipide

“…These results clearly show that C12 improved the absorption of rebamipide more than C10. Although we have already reported that C12 was better than C10 in terms of absorptionimproving ability, 24,25) the same effect was recognized in the present study using rabbits. The suppositories containing 10-mg C12 with 15-, 30-and 60-mg Tau (suppositories g, h, i), and 20-mg C12 with 30-mg Tau (suppository j) enhanced the absorption of rebamipide about 22, 16, 8 and 51 times larger in BA than the control.…”

“…Table 4 evidenced, 26,27) which might be attributed to the opening of tight junction and the enhancement of membrane fluidity. 26) Although we previously reported that the addition of Tau attenuated the enhancing effect of C12, 25,30) Tau hardly decreased the absorption improving effect of C12 in the case of the suppositories containing 20-mg C12, when compared with the suppositories containing 10-mg C12 (Fig. 3).…”

“…[21][22][23] We have found that C12, a mediumchain fatty acid salt, is a promising absorption enhancer and better than C10 in terms of the absorption improving ability, 24) and that Tau has the most effective cytoprotective activity among amino acids examined. 25) Cytoprotective action by Tau has been evidenced by both biochemical [25][26][27] and histopathological 25) approaches and it has been partially related with the suppression of intracellular Ca 2ϩ level elevated by C12 and the inhibition of histamine release induced by C12. L-Glutamine (L-Gln) also has the cytoprotective action, which is partially attributed to the induction of heat-shock protein 70 (HSP70), 27) a factor protecting cells from injuries caused by several kinds of stresses.…”

Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

“…Therefore, it is necessary to investigate the characteristics of the permeability of rebamipide across M-S or S-M direction at much lower concentration in order to elucidate the exact mechanism of its transport across the intestinal membrane in the future, as more sensitive determination of rebamipide will have to be set up. In addition, we found in this study that the Papp of rebamipide across the colonic membranes in the absorptive direction was about (3.06 ± 0.07) × 10 -6 cm/s (n = 15), while Miyake et al [21] reported the Papp across the same membrane was about (2.93 ± 0.35) × 10 -6 cm/s. The slight difference may be result from the different experimental conditions.…”

Transport of Surface Engineered Polyamidoamine (PAMAM) Dendrimers Across IPEC-J2 Cell Monolayers

“…The tight intercellular junctions between the epithelial cells restrict the absorption of drugs and control the access of potential antigens and pathogens from the lumen to submucosa (De Magistris 2006). Efforts to design novel formulations to breach the mucosal barrier for efficient antigen presentation to the M cells or their transport to draining lymph nodes either by lamina propria dendritic cells or by lymphatics (Rescigno et al 2001), and to enhance the absorption of poorly soluble and poorly absorbable drugs have been increasing recently (Messing et al 1999;Aungst 2000;Yata et al 2001;Endo et al 2002;Ohtake et al 2002;Miyake et al 2003Miyake et al , 2004Miyake et al , 2006Li et al 2005;Seki et al 2005).…”