Omeprazole-based PPIs

Figure 8.11 A proposed mechanism of action by which the omeprazole-based PPIs may work.

One of the key potential liabilities associated with omeprazole is its acid labile property, resulting in relatively larger interindividual variability. Thus, increasing its solution stability had been the focus of the omeprazole-based PPI optimization. Approaches to improve the solution stability are as follows ... 

As a result, another omeprazole-based PPI lansoprazole has been developed successfully and marketed in 1991. Both pantoprazole and lansoprazole have showed lower oral clearance and longer plasma half-life in clinic compared to omeprazole or esomeprazole due to improved enzymatic stability and solution stability [71]. 

These approaches have improved omeprazole-based PPIs solution stability and enzymatic stability, thus prolonging the plasma half-life and reducing the... 

Fig. 2. Median gastric pH is elevated about 2 log by 20 mg of omeprazole in H. pylori-negative healthy subjects, and by 4 log in H. pylo-n -positive ones [based on data from 42], Hp = H. pylori, PPI = proton pump inhibitor. 

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