Objective: To analyze and evaluate the mechanism of drug release for rabeprazole sodium enteric-coated tablets in ethanolic media and conduct the risk assessment for the dose dumping. The similarity of dissolution curves were compared between reference preparation and generic products. Methods: The dissolution conditions were the paddle method, the speed was 100 r · min-1, the dissolution time was 120 min. Release profiles of rabeprazole sodium enteric-coated tablets from 7 manufacturers in different ethanolic media were determined by HPLC. The release mechanism was studied and the similarity between the commercially available generic preparation and the commercially available reference preparation Pariet® was evaluated. The risk of dose dumping was evaluated by the similarity factor ( f2) of the release data. Results: All preparations showed good tolerance to ethanol in the 0.1 mol · L-1 hydrochloric acid with an alcohol concentration of 5%. All preparations showed good tolerance to ethanol in the 0.1 mol · L-1 hydrochloric acid with an alcohol concentration of 20%, except for D and E manufacturers. All preparations carried the risk of dose dumping in the 0.1 mol · L-1 hydrochloric acid with an alcohol concentration of 40% except F manufacturer. The dissolution behavior of each commercially available generic formulation differs from that of the reference formulation in pH 8.0 Tris buffer with 4 different concentrations of ethanol. Conclusion: In the course of clinical application of this drug, it is necessary to suggest that drinking high-concentration alcoholic beverages such as liquor should be prohibited to avoid the unknown security risks.
GUO Bin
,
ZHANG Shan-shan
,
LI Na
,
CHEN Rong
,
ZHANG Hua-feng
. Study and risk assessment of alcohol-induced dose dumping for rabeprazole sodium enteric-coated tablets[J]. Chinese Journal of Pharmaceutical Analysis, 2025
, 45(6)
: 1079
-1091
.
DOI: 10.16155/j.0254-1793.2024-1124
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