Comparison of the pharmacokinetics of lansoprazole 15- and 30-mg sachets for suspension versus intact capsules

• Published in: Clinical therapeutics 2004-12, Vol.26 (12), p.2076-2083
• Main Authors: Amer, Fouad, Karol, Michael D., Pan, Wei-Jian, Griffin, Janice S., Lukasik, Nancy L., Locke, Charles S., Chiu, Yi-Lin
• Format: Article
• Language: English
• Subjects: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; alternative dosage formulations; Anti-Ulcer Agents - blood; Anti-Ulcer Agents - pharmacokinetics; Area Under Curve; Biological and medical sciences; Capsules; Cross-Over Studies; Dosage Forms; Drug dosages; Female; Gastroesophageal reflux; Half-Life; Humans; Lansoprazole; lansoprazole capsule; lansoprazole sachet for suspension; Male; Medical sciences; Omeprazole - analogs & derivatives; Omeprazole - blood; Omeprazole - pharmacokinetics; Ostomy; Pharmaceuticals; Pharmacodynamics; Pharmacokinetics; Pharmacology. Drug treatments; proton pump inhibitor; Protons; Solutions; Therapeutic Equivalency; Ulcers
• ISSN: 0149-2918; 1879-114X
• DOI: 10.1016/j.clinthera.2004.12.008

The pharmacokinetic profiles of single doses of lansoprazole 15- and 30-mg sachets for suspension were compared with those of corresponding doses of lansoprazole oral capsules. Healthy adult male and female subjects were randomized (1:1 ratio) into 2 Phase 1, open-label, single-dose, 2-sequence, 2-period complete crossover studies. In the first study, each subject received 1 lansoprazole 15-mg sachet mixed with water and 1 lansoprazole 15-mg oral capsule; in the second study, each subject received 1 lansoprazole 30-mg sachet mixed with water and 1 lansoprazole 30-mg oral capsule. Administration of the 2 formulations was separated by a washout period of ≥7 days. Blood samples were collected before and after each administration to assess the pharmacokinetic parameters of lansoprazole and bioequivalence between suspension and capsule. Thirty-six subjects (19 males, 17 females) with a mean (SD) age of 32.0 (9.6) years and mean (SD) body weight of 68.6 (10.5) kg received lansoprazole 15 mg. Thirty-six subjects (22 males, 14 females) with a mean (SD) age of 38.0 (8.3) years and mean (SD) body weight of 75.1 (9.7) kg received lansoprazole 30 mg. The pharmacokinetic parameters of the 15- and 30-mg lansoprazole sachets for suspension were similar to those of the corresponding doses of the oral capsules. The mean (SD) values for C max and AUC from time 0 to infinity (AUC 0—∞ for the lansoprazole 15-mg sachet (591.9 [242.3] ng/mL and 1614 [2065] ng·h/mL, respectively) did not differ significantly from those for the lansoprazole 15-mg capsules (578.6 [275.2] ng/mL and 1620 [2290] ng·h/mL, respectively). These parameters also did not differ significantly between the lansoprazole 30-mg sachet and 30-mg capsule: mean (SD) C max, 1103 (428.3) and 1077 (465.6) ng/mL, respectively; mean (SD) AUC 0—∞, 2655 (1338) and 2669 (1311) ng·h/mL, respectively. The 90% Cls for C max and AUC 0—∞ ratios were contained within the 0.80 to 1.25 equivalence range, supporting bioequivalence. These findings suggest that the 15- and 30-mg lansoprazole sachets for suspension are bioequivalent to the corresponding doses of oral capsules. The sachet for suspension may provide an alternative route of administration to patients who have difficulty swallowing solid oral formulations.