Microparticulate hot melt pallets technology: a review

Kokate, Shekhar; Rachh, Punit R.

doi:10.22270/jddt.v8i6-s.2131

Cited by 2 publications

(2 citation statements)

References 23 publications

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“…PVPP is a widely used disintegrating agent for tablets and was reported to increase the absorptive transport of rhodamine 123 through the inhibition of P-gp . Meglumine, a derivative of glucose, is usually used as a solubilizer and pH-adjusting agent. , …”

Section: Resultsmentioning

confidence: 99%

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Effect of Pharmaceutical Excipients on Intestinal Absorption of Metformin via Organic Cation-Selective Transporters

Ruan

et al. 2021

Mol. Pharmaceutics

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Growing evidence has shown that some pharmaceutical excipients can act on drug transporters. The present study was aimed at investigating the effects of 13 commonly used excipients on the intestinal absorption of metformin (MTF) and the underlying mechanisms using Caco-2 cells and an ex vivo mouse non-everted gut sac model. First, the uptake of MTF in Caco-2 cells was markedly inhibited by nonionic excipients including Solutol HS 15, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and crospovidone. Second, transport profile studies showed that MTF was taken up via multiple cation-selective transporters, among which a novel pyrilaminesensitive proton-coupled organic cation (H + /OC + ) antiporter played a key role. Third, Solutol HS 15, polysorbate 40, and polysorbate 60 showed cis-inhibitory effects on the uptake of either pyrilamine (prototypical substrate of the pyrilamine-sensitive H + /OC + antiporter) or 1-methyl-4phenylpyridinium (substrate of traditional cation-selective transporters including OCTs, MATEs, PMAT, SERT, and THTR-2), indicating that their suppression on MTF uptake is due to the synergistic inhibition toward multiple influx transporters. Finally, the pH-dependent mouse intestinal absorption of MTF was significantly decreased by Solutol HS 15, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, and pyrilamine. In conclusion, this study revealed that a novel transport process mediated by the pyrilamine-sensitive H + /OC + antiporter contributes to the intestinal absorption of MTF in conjunction with the traditional cationselective transporters. Mechanistic understanding of the interaction of excipients with cation-selective transporters can improve the formulation design and clinical application of cationic drugs.

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Section: Resultsmentioning

confidence: 99%

“…51 Meglumine, a derivative of glucose, is usually used as a solubilizer and pH-adjusting agent. 52,53 Transport Profile of MTF Uptake in Caco-2 Cells. To elucidate the underlying mechanisms of the inhibitory effects of the above excipients, it is important to understand the intestinal transport process of MTF.…”

Section: ■ Results and Discussionmentioning

confidence: 99%