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Formulation study for lansoprazole fast-disintegrating tablet. I. Effect of compression on dissolution behavior. 2003

Toshihiro Shimizu, and Yoshinori Nakano, and Shuji Morimoto, and Tetsuro Tabata, and Naoru Hamaguchi, and Yasutaka Igari
Pharmaceutical Development Laboratories, Pharmaceutical Production Division, Takeda Chemical Industries, Ltd. Shimizu_Toshihiro@takeda.co.jp

Lansoprazole fast-disintegrating tablet (LFDT) is a new patient-friendly formulation of lansoprazole. Since lansoprazole is an antiulcer agent and is unstable under acidic conditions, we have developed LFDT as an orally disintegrating tablet containing enteric-coated microgranules. The effect of compression on dissolution behavior was investigated, as compression affected cleavage and crushing of the enteric layer. To decrease cleavage and crushing of the enteric layer, the effects of the combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and the concentration of triethyl citrate on the dissolution in the acid stage and the dissolution in the buffer stage were evaluated. By adjusting the ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion to 9 : 1 and adding a 20% triethyl citrate concentration, sufficient flexibility of the enteric layer and sufficient stability against compression forces were achieved. Agglomeration of enteric-coated microgranules during the coating process was decreased at the optimized concentration of triethyl citrate and glyceryl monostearate. We compared the absorption properties of LFDT and lansoprazole capsules in dogs. The absorption profiles of LFDT were similar to those of lansoprazole capsules.

UI MeSH Term Description Entries
D007408 Intestinal Absorption Uptake of substances through the lining of the INTESTINES. Absorption, Intestinal
D008297 Male Males
D009853 Omeprazole A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. H 168-68,Omeprazole Magnesium,Omeprazole Sodium,Prilosec,H 168 68,H 16868,Magnesium, Omeprazole,Sodium, Omeprazole
D002626 Chemistry, Pharmaceutical Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use. Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D013608 Tablets, Enteric-Coated Tablets coated with material that delays release of the medication until after they leave the stomach. (Dorland, 28th ed) Enteric-Coated Tablets,Tablets, Enteric Coated
D053799 2-Pyridinylmethylsulfinylbenzimidazoles Compounds that contain benzimidazole joined to a 2-methylpyridine via a sulfoxide linkage. Several of the compounds in this class are ANTI-ULCER AGENTS that act by inhibiting the POTASSIUM HYDROGEN ATPASE found in the PROTON PUMP of GASTRIC PARIETAL CELLS. 2-Methylpyridine 2-Benzimidazole Sulfoxides,2-Pyridinylmethylsulfinyl-2-Benzimidazoles,Benzimidazole Methylpyridine Sulfoxides,Timoprazole Derivatives,Timoprazoles,2 Methylpyridine 2 Benzimidazole Sulfoxides,2 Pyridinylmethylsulfinyl 2 Benzimidazoles,2 Pyridinylmethylsulfinylbenzimidazoles,2-Benzimidazole Sulfoxides, 2-Methylpyridine,Methylpyridine Sulfoxides, Benzimidazole,Sulfoxides, 2-Methylpyridine 2-Benzimidazole,Sulfoxides, Benzimidazole Methylpyridine
D019245 Compressive Strength The maximum compression a material can withstand without failure. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed, p427) Compressive Strengths,Strength, Compressive,Strengths, Compressive

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