• 약학회지
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• 제39권6호
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• pp.577-584
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• 1995

On the combination of antacid, the pharmacokinetics and gastric adhesion of [$^{14}c$]aceglutamide aluminium complex([$^{14}C$]AGA) were examined in rats. Specially, this study was focused on the drug interaction that the co-administration of antacid may affect the oral absorption and gastric adhesion of aceglutamide aluminium complex(AGA). In the study of the oral co-administration of [$^{14}C$] AGA and antacid(aluminium hydroxide and magnesium hydroxide(AM)), the radioactivity of plasma and urinary recovery was lower than that of [$^{14}C$]AGA alone administered group. However, the cumulative recovery of radioactivity in feces was increased significantly. The comparative bioavailability of [$^{14}C$] AGA from the plasma concentration-time curve and urinary recovery was about 60%. In vitro, the effect of antacid on the gastric adhesion of AGA was not significatly different between AGA and AGA/antacid treatment. And it accorded well with the result of in vivo experiment. In conclusion, on the combination of antacid, the oral absorption of AGA was decreased by the gastric adhesion was not affected in respect of drug interaction.

• 약학회지
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• 제38권6호
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• pp.800-805
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• 1994

Antacid(AM, 600 mg/kg=aluminium hydroxide, magnesium hydroxide, and simethicone with a ratio of 1 : 1 : 0.1) and aceglutamide aluminium(AGA, 263 mg/kg)-Effect of the combined preparation containing on the gastric mucosal hexosamine, sialic acid, and aluminium contents adhered to the gastric wall of the rat was investigated. Severe ulcers were produced in rats by injecting of $30\;{\mu}l$ acetic acid(30%) into the subserosal layer of one position in the corpus. When given orally for 15 consecutive days, AM(1,200 mg/kg), AGA(525, 1,050 mg/kg), and the combined preparation significantly decreased the ulcer area. AGA(525, 1,050 mg/kg) and the combined preparation also increased the amount of hexosamine and sialic acid in the intact and ulcerated areas. On the other hand, the contents of hexosamine and sialic acid were not affected by AM (600, 1,200 mg/kg). The amount of aluminium adhered to the gastric wall of the rat was higher in the combined preparation when compared to the AM(600 mg/kg) and AGA(263 mg/kg). The aluminium contents adhered may play an important role protecting mucosa from aggresive action of gastric juice and potenting defensive factors through the increase of mucosa-forming components by AGA.

• 약학회지
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• 제38권5호
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• pp.496-503
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• 1994

The combined products of antacids(AM) composed of aluminium hydroxide, magnesium hydroxide, and simethicone with a ratio of 1 : 1 : 0.1 and aceglutamide aluminium(AGA) were assayed for the antiulcer activity. The effect of the antacids(AM) in concurrent treatment with AGA was studied in acute gastric lesion induced by Shay's method, stress, ethanol, and indomethacin, in chronic gastric ulcers induced by acetic acid, and in duodenal ulcer induced by mepirizole. In all experimental models, the combined treatment of AM and AGA in the ratio of 2.3:1 showed significant potentiation in inhibition against acute gastric and duodenal ulcer and revealed a significant potentiation of the healing of chronic gastric ulcer.

• Journal of Pharmaceutical Investigation
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• 제23권4호
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• pp.217-223
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• 1993

The combined products of antacid and anti-ulcer agent were prepared with antacid composed of aluminium hydroxide dried gel, magnesium hydroxide and simethicone with a ratio of 1:1:0.1 (M) and anti-ulcer agent, aceglutamide aluminium (AGA). The efficacy of antacid was evaluated in vitro with Fuchs, Johnson-Duncan and Rosset-Rice methods and in vivo using an aspiration method in rat. The addition of anti-ulcer agent did not affect the neutralizing capacity of M significantly. The combined products with the M/AGA ratios of 2.3:1 and 3.4:1 produced the maximum pH of $4.0{\sim}5.8$ and the duration time of $64{\sim}137$ min in vitro test. The in vivo neutralizing test in rats showed the rapid increase of gastric pH up to 3.5 within 30 min and the gastric pH of $4{\sim}6$ was kept for 5 hr.