Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Patent
1998-10-20
2000-12-12
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
424452, 424457, 424461, 424462, 424468, 424470, 424474, 424480, 424482, 424458, 514770, 514784, 514951, 514960, 514962, 514970, A61K 922, A61K 928, A61K 952, A61K 954, A61K 956
Patent
active
061594997
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
This present invention relates to a novel composition containing an acid-labile benzimidazole, and to its preparation. This novel composition is perfectly suitable for oral administration. The invention also relates to a process for preparing this composition.
Many substances, of pharmaceutical value, that are labile in an acid medium have been described in the literature. The substances disclosed in the following patents can be given by way of example: EP 244 380, U.S. Pat. No. 4,045,563, EP-0 005 129, BE-898 880, GB-2 141 429, EP-0 146 370, GB-2 082 580, EP-A-0 173 664, EP-A-0 080 602, EP-0127 763, EP-0 134 400, EP-0 130 729, EP-0 150 586, DE-34 15971, GB-2 082 580, SE-A-8504048-3 and U.S. Pat. No. 4,182,766. On the other hand, omeprazole, which is of the family of benzimidazoles, corresponding to an anti-ulcer substance, used conventionally for decreasing gastrointestinal acid secretion, is well known and has been notably discussed in Swedish patent application 78.04231 filed on April 14, 1978, as well as in numerous other patents. Pantoprazole and lansoprazole which both correspond to anti-ulcer substances of the omeprazole family, are notably discussed in U.S. Pat. No. 4,758,579 and in U.S. Pat. No. 4,628,098 respectively.
Chemical substances that are easily destroyed in an acid medium (which is expressed herein by the term "acid-labile, and meaning chemical substances that are labile in an acid medium), such as benzimidazoles and, in particular, omeprazole, lansoprazole and pantoprazole, create a special problem for formulators when it is required to provide a pharmaceutical form designed for oral administration. The product does indeed come into contact with the stomach content, which is a highly acid medium, leading to breakdown of these chemical substances.
In order to avoid contact between the substances and the acid gastric juice following oral administration of the substance, a pharmaceutical formulation is conventionally used, such as a capsule or tablet which contains a core (tablet, microgranule, pellet, etc . . . ) containing the acid-labile active substance and an outer layer that surrounds this core and which consists of a gastro-resistant composition that is entero-soluble. Generally, the coating agent is a compound that is particularly insoluble in an acid medium, but which is soluble in a neutral or alkaline medium.
For substances that are highly labile in an acid medium but which are more stable in a neutral or alkaline medium, such as omeprazole, pantoprazole and lansoprazole, it is necessary to add an inert substance to the composition, which leads to an alkaline reaction aimed at improving stability of the active substance during manufacture thereof, and during storage of the pharmaceutical form.
Several prior art documents describe such compositions that are suitable for oral administration of acid-labile substances.
EP-0,244,380 discloses pharmaceutical formulations that are suitable for oral administration of acid-labile substances. It is stated that these acid-labile substances intended for oral administration must be protected by an enteric coating, but conventional enteric coatings of an acid nature are not suitable for this purpose. If one were indeed to cover acid-labile substances which such coatings, the substance would be rapidly decomposed due to direct or indirect contact with the coating, which manifests itself by a change of color and a decrease in the active substance content with the passage of time. The solution proposed in that patent corresponds to formulations consisting of: (a) a core in the form of small particles, i.e. pellets or compressed powder, containing the active substance along with an alkaline reacting compound, (b) one or several inert intermediate layers containing excipients for tablets which are soluble, and which rapidly disintegrate in water, water-soluble film-forming polymer compounds optionally containing alkaline compounds acting as a pH buffer between the core having an alkaline reaction and the outer layer, a
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Pharma Pass LLC
Spear James M.
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