Method of increasing drug oral bioavailability and...

A - Human Necessities – 61 – K

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A61K 47/22 (2006.01) A61K 31/4192 (2006.01)

Patent

CA 2602379

The present invention relates generally to the method of increasing the oral bioavailability, reducing chemotherapy induced toxicity and side effects, and improving the effectiveness of pharmaceutical agents that are poorly absorbed from the gastrointestinal tract. Specifically, the invention relates to poorly absorbed pharmaceutical drugs and converting them to orotate salts. The orotate salts of the drugs can be dosed at lower doses to provide the efficacy benefits of a higher dose, while reducing the drugs toxic effects at lower doses. Additionally, the orotate salts of pharmaceutical agents have better clearance and reduce the potential for drug-induced hepatic toxicity. Therefore, an especially useful formulation of the orotate salt of the pharmaceutical agent can provide rapid and consistent action using a lower dose while reducing drug interactions and side-effects.

En règle générale, procédé d'augmentation de biodisponibilité orale, de réduction de toxicité et d'effets secondaires induits par la chimiothérapie, et d'amélioration de l'efficacité des agents pharmaceutiques médiocrement absorbés par le tractus gastro-intestinal, et spécifiquement, médicaments à absorption médiocre et leur conversion en sels d'orotate, sachant que les sels d'orotate des médicaments peuvent être dosés à des doses inférieures, assurant l'efficacité de doses supérieures mais réduisant les effets toxiques grâce aux doses inférieures. Enfin, les sels des agents pharmaceutiques ont un meilleur coefficient d'épuration et réduisent le risque de toxicité hépatique induit par un médicament. Ainsi, une formulation particulièrement utile du sel considéré de l'agent pharmaceutique peut assurer une action cohérente et rapide en dose inférieure et réduire aussi les interactions médicamenteuses et les effets secondaires PO dose.

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