Gastro-Resistant Microparticles Containing Sodium Pantoprazole: Stability Studies and In Vivo Anti-Ulcer Activity

Raffin, R. P.; Colome, L. M.; Schapoval, Elfrides Eva Scherman; Jornada, D. S.; Pohlmann, A. R.; Guterres, S. S.

doi:10.2174/187412660701012806

Cited by 5 publications

(12 citation statements)

References 20 publications

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“…However, gastric erosions and ulcers are caused by various factors such as gastric over-secretion and retention, mucin layer-depleting agents, blood flow disturbances, and inflammation [1,2,3,4]. The ulcer-inducing agents include non-steroidal anti-inflammatory drugs (NSAIDs) that block production of prostaglandins (PGs), leading to mucin depletion and focal ischemia [5,6,7,8,9], alcohols [7,8,10], stresses [4,7,8], gastric retention [7,8], gastric hypermotility and acetic acid accumulation [8,11,12,13,14], and bacterial infection such as Helicobacter pylori [1,2,15,16,17]. …”

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confidence: 99%

In vitroandin vivoanti-Helicobacter pyloriactivities of FEMY-R7 composed of fucoidan and evening primrose extract

Cai

Kim²,

Jang

et al. 2014

Lab Anim Res

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Effects of FEMY-R7, composed of fucoidan and evening primrose extract, on the bacterial growth and intragastric infection of Helicobacter pylori as well as gastric secretion were investigated in comparison with a proton-pump inhibitor pantoprazole. For in vitro anti-bacterial activity test, H. pylori (1×108 CFU/mL) was incubated with a serially-diluted FEMY-R7 for 3 days. As a result, FEMY-R7 fully inhibited the bacterial growth at 100 µg/mL, which was determined to be a minimal inhibitory concentration. In addition, 6-hour incubation with H. pylori, FEMY-R7 inhibited urease activity in a concentration-dependent manner, showing a median inhibitory concentration of 1,500 µg/mL. In vivo elimination study, male C57BL/6 mice were infected with the bacteria by intragastric inoculation (5×109 CFU/mouse) 3 times at 2-day intervals, and simultaneously, orally treated twice a day with 10, 30 or 100 mg/kg FEMY-R7 for 7 days. In Campylobcter-like organism-detection test and bacterial identification, FEMY-R7 exerted a high bacteria-eliminating capacity at 30-100 mg/kg, comparably to 30 mg/kg pantoprazole. In contrast to a strong antacid activity of pantoprazole in a pylorus-ligation study, FEMY-R7 did not significantly affect gastric pH, free HCl, and total acidity, although it significantly decreased fluid volume at a low dose (10 mg/kg). The results indicate that FEMY-R7 eliminate H. pylori from gastric mucosa by directly killing the bacteria and preventing their adhesion and invasion, rather than by inhibiting gastric secretion or mucosal damage.

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mentioning

confidence: 99%

In vitroandin vivoanti-Helicobacter pyloriactivities of FEMY-R7 composed of fucoidan and evening primrose extract

Cai

Kim²,

Jang

et al. 2014

Lab Anim Res

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“…In many studies, water-immersion restraint stress (WIRS)-, alcohol (ethanol)- and pylorus ligation-induced gastric ulcer models have been used to screen antiulcer compounds, since mechanisms of those models are different (Kitagawa et al, 1979; Wallace and Granger, 1996; Shah et al, 2003; Isobe et al, 2004; Cao et al, 2005; Byun et al, 2007; Raffin et al, 2007). WIRS, a generalized model to induce extreme mental and psychological stresses to rodents, stimulates gastric secretion related to central nervous system as well as pituitary-renal hormonal axis (Kitagawa et al, 1979; Wallace and Granger, 1996; Neal, 2003; Isobe et al, 2004; Cao et al, 2005; Byun et al, 2007).…”

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confidence: 99%

Different Antiulcer Activities of Pantoprazole in Stress, Alcohol and Pylorus Ligation-Induced Ulcer Models

et al. 2011

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Antiulcer effects of pantoprazole, a proton-pump inhibitor, on water-immersion restraint stress (WIRS)-, alcohol (ethanol)- and pylorus ligation-induced gastric ulcers were investigated in male rats. Rats were orally administered with pantoprazole 30 min prior to exposure to various types of ulcer inducers. In stress-induced ulcer model, rats were subjected to WIRS at 22℃ for 4 hours, and the degree of ulcer (in mm) was evaluated. In alcohol-induced ulcer model, rats were orally administered with pure (100%) ethanol (1 mL/kg), and the ulcer lesions were measured 1 hour after ethanol challenge. In pylorus ligation-induced ulcer model, rats were subjected to pylorus ligation, and the degree of erosions and ulcers was scored 17 hours after the operation. Pantoprazole attenuated the ulcer lesions induced by WIRS in a dose-dependent manner, exhibiting a median effective dose (ED50) value of 0.78 mg/kg. By comparison, pantoprazole was effective at relatively-high doses for the improvement of ethanol-induced ulcers, showing an ED50 value of 20.5 mg/kg. Notably, pantoprazole was practically ineffective (ED50>50.0) in pylorus ligation model. Taken together, it was confirmed that pantoprazole showed inhibitory activity on gastric ulcers induced by stress and alcohol, but was ineffective on pylorus ligation-induced ulcer. Therefore, the results indicate that proton-pump inhibitors including pantoprazole might reveal highly-different effects according to the type of ulcer inducers, and that the prescription of antiulcer agents should be carefully selected.

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“…한 편 다양한 원인에 의한 설사는 탈수의 원인으로 유아 및 노인 사망의 주요 원인이 되기도 하는데, 심한 설사는 장 점막의 손상에 따른 전해질 및 수분의 소실과 과도한 장 운동에 기인한다 (Osweiler, 1996). 이러한 심한 설사의 원 인이 되는 장염 및 위궤양의 유발에 있어 장점막의 산화 적 손상이 중요한 역할을 한다 (Radema et al, 1991;Rao et al, 2000;Shah et al, 2003;Raffin et al, 2007).…”

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Antioxidative and Antidiarrheal Effects of Persimmon Extracts

et al. 2010

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Since oxidative stresses are involved in gastroenteritis and diarrhea, we investigated antioxidative and antidiarrheal activities of persimmon flesh extract (PFE) and persimmon calyx extract (PCE) in vitro and in vivo, respectively. PCE significantly scavenged 1,1-diphenyl-2-picrylhydrazyl hydrate and 2,2'-azinobis (3-ethylbenzthiazoline-6-sulfonic acid) from 500 µg/mL, although PFE was ineffective. In addition, PFE and PCE exhibited strong nitric oxide-scavenging effects from 1 µg/mL, in which PCE was superior to ascorbic acid (50 µM). Furthermore, PFE and PCE significantly inhibited FeCl 3 -induced lipid peroxidation as well as Cu 2+ /H 2 O 2 -induced protein oxidation from 10 µg/mL. In vivo charcoal-propulsion assay, in contrast to a negligible effect of PFE, treatment with PCE (160-500 mg/kg) markedly inhibited intestinal motility. The results indicate that extracts of persimmon, especially PCE, possess antioxidative, antiinflammatory and antidiarrheal activities. Therefore, it is suggested that persimmon extracts could be used for the relief of gastroenteritis and diarrhea.

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Gastro-Resistant Microparticles Containing Sodium Pantoprazole: Stability Studies and In Vivo Anti-Ulcer Activity

Cited by 5 publications

References 20 publications

In vitroandin vivoanti-Helicobacter pyloriactivities of FEMY-R7 composed of fucoidan and evening primrose extract

In vitroandin vivoanti-Helicobacter pyloriactivities of FEMY-R7 composed of fucoidan and evening primrose extract

Different Antiulcer Activities of Pantoprazole in Stress, Alcohol and Pylorus Ligation-Induced Ulcer Models

Antioxidative and Antidiarrheal Effects of Persimmon Extracts

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