Formulation and in vivo evaluation of omeprazole buccal adhesive tablet

• Published in: Journal of controlled release 2000-09, Vol.68 (3), p.405-412
• Main Authors: Choi, Han-Gon, Jung, Jac-Hee, Yong, Chul Soon, Rhee, Chong-Dal, Lee, Mi-Kyung, Han, Jeong-Hee, Park, Kyung-Mi, Kim, Chong-Kook
• Format: Article
• Language: English
• Subjects: Adhesiveness; Administration, Oral; Alginates; Animals; Anti-Ulcer Agents - administration & dosage; Anti-Ulcer Agents - chemistry; Anti-Ulcer Agents - pharmacokinetics; Biological and medical sciences; Biological Availability; Buccal adhesive tablet; Chemical Phenomena; Chemistry, Physical; Cricetinae; Croscarmellose sodium; Digestive system; Dissolution; Evaluation Studies as Topic; General pharmacology; Humans; Lactose - analogs & derivatives; Magnesium Oxide; Male; Medical sciences; Mesocricetus; Methylcellulose - analogs & derivatives; Mouth Mucosa - metabolism; Omeprazole; Omeprazole - administration & dosage; Omeprazole - chemistry; Omeprazole - pharmacokinetics; Oxazines; Pharmaceutical technology. Pharmaceutical industry; Pharmacokinetics; Pharmacology. Drug treatments; Tablets
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/S0168-3659(00)00275-3

For the development of omeprazole buccal adhesive tablets, we studied the release and bioavailability of omeprazole delivered by buccal adhesive tablets composed of sodium alginate, hydroxypropylmethylcellulose (HPMC), magnesium oxide and croscarmellose sodium. Croscarmellose sodium enhanced the release of omeprazole from the tablets. The analysis of the release mechanism showed that croscarmellose sodium changed the release profile of omeprazole from first- to zero-order release kinetics by forming porous channels in the tablet matrix. However, it decreased the bioadhesive forces and stability of omeprazole tablets in human saliva. The tablet is composed of omeprazole–sodium alginate–HPMC–magnesium oxide–croscarmellose sodium (20:24:6:50:10 mg). It may be attached to the human cheek without collapse and it enhanced the stability of omeprazole in human saliva for at least 4 h, giving a fast release of omeprazole. The plasma concentration of omeprazole in hamsters increased to reach a maximum of 370 ng/ml at 45 min after buccal administration and remained at the high level of 146–366 ng/ml for 6 h. The buccal bioavailability of omeprazole in hamsters was 13.7±3.2%. These results demonstrate that the omeprazole buccal adhesive tablet would be useful to deliver omeprazole which degrades very rapidly in acidic aqueous medium and undergoes hepatic first-pass metabolism after oral administration.