Stabilization Mechanism of Clarithromycin Tablets under Gastric pH Conditions

Evaluation of food effect on the oral absorption of clarithromycin from immediate release tablet using physiological modelling

“…These findings are in agreement with previous reports that investigated the effect of media acidity on the stability of clarithromycin from immediate release tablets. Clarithromycin was shown to be stable at a pH range of 3–8 in aqueous solution, but it rapidly degrades at gastric pH (1–2) with a decomposition half‐life of 10.4 minutes (Fujiki et al, ; Manani, ). Similarly, Manani (2014) reported a degradation rate of 64% of clarithromycin active ingredient within 1 hour at pH = 1.2 (Nakagawa, Itai, Yoshida, & Nagai, ).…”

“…Additional simulations were conducted to account for the loss of clarithromycin due to acid‐induced degradation, using an input table of the observed degradation rates vs. pH. The decomposition rate constants under various pH were obtained from the report of Fujiki et al (Fujiki, Iwao, Kobayashi, Miyagishima, & Itai, ).…”

Increasing gastric juice pH level prior to anti-Helicobacter pylori therapy may be beneficial to the healing of duodenal ulcers

“…Such studies have demonstrated that the decomposition of clarithromycin in solutions and gastric juice proceeded in a pseudo-first order manner and the respective half-lives of clarithromycin were 0.1 and 1.3 h when the pH levels of the solutions were 1.0 and 2.0. Clarithromycin scarcely decomposed when the pH was above 5.0 (19). It has been suggested that the prolonged elevation of intragastric pH may increase the concentration of acid-labile antibiotics in gastric juice, prolong their effectiveness and improve the environment to allow the defense mechanisms of the host to exert their optimal effect.…”

Pharmaceutical Equivalence of Clarithromycin Oral Dosage Forms Marketed in Nairobi County, Kenya

“…Previous studies have reported that clarithromycin undergoes rapid degradation under conditions of low pH that exist in gastric fluid [6,9]. One such study reports 25% drug degradation at pH 2.0 within 30 min of incubation, while incubation at pH 1.5 yields 70% drug degradation within the same period [9].…”

“…One such study reports 25% drug degradation at pH 2.0 within 30 min of incubation, while incubation at pH 1.5 yields 70% drug degradation within the same period [9]. Given that the gastric and intestinal residence times of clarithromycin are 0.5–2 h and 3–6 h, respectively, and since its systemic bioavailability is dependent on gastric stability and intestinal absorption [10], protection from acid degradation may play a key role in enhancing its bioavailability.…”