Effects of Different Antisecretory Drugs on Gastric Potential Difference in the Rat: Comparison With Sucralfate

Coruzzi, Gabriella; Coppelli, Gabriella; Frati, Paolo; Bertaccini, G.

doi:10.1006/phrs.1998.0392

Cited by 1 publication

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“…In rats, treatments of proton pump inhibitor and histaminergic H 2 antagonist, acidsuppressive agents, have little influence on gastric pH. 25 Because the acid-suppressive actions of PPT are limited compared with that of proton pump inhibitor and H 2 antagonist, the effect of PPT treatment on pH of rat stomach could be insignificant. Herein, PPT treatment could lead to impairment of gastric motility without significant changes in gastric pH of rat, and so decreased gastric motility could be a main cause for the reduction of MEL absorption in PPT-pretreated rats.…”

Section: Pharmacokinetic Behavior Of Mel Formulationsmentioning

confidence: 99%

Amorphous Solid Dispersion of Meloxicam Enhanced Oral Absorption in Rats With Impaired Gastric Motility

Suzuki

Yakushiji

Matsunaga

et al. 2018

Journal of Pharmaceutical Sciences

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Meloxicam (MEL) shows a slow onset of action in severe pain patients on account of delayed gastric motility. This study aimed to develop an amorphous solid dispersion (ASD) of MEL to achieve rapid oral absorption in severe pain patients. ASD formulations of MEL with hydroxypropylmethylcellulose (ASD-MEL/HPMC) and polyacrylates and polymethacrylates (ASD-MEL/EUD) were prepared and physicochemically characterized. Oral absorption behavior of MEL samples was also clarified in both normal and propantheline (PPT)-pretreated rats with impaired gastric motility. MEL in the formulations was amorphous, and ASD formulations of MEL exhibited high dissolution behavior in acidic solution. After oral administration of crystalline MEL (1 mg-MEL/kg), a 69% reduction in AUC was observed between normal and PPT-pretreated rats. For orally dosed ASD-MEL/HPMC (1 mg-MEL/kg), there were approximately 9- and 12-fold increases of AUC in normal and PPT-pretreated rats, respectively, in comparison with crystalline MEL (1 mg-MEL/kg). However, the oral absorption behavior of ASD-MEL/EUD (1 mg-MEL/kg) was low and similar to that of crystalline MEL. The infrared spectroscopic study revealed potent interactions between MEL and EUD, possibly leading to marked attenuation of MEL absorption. This ASD approach might provide rapid oral absorption of MEL in severe pain patients, possibly leading to better clinical outcomes.

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Section: Pharmacokinetic Behavior Of Mel Formulationsmentioning

confidence: 99%