Enhancement of Oral Bioavailability of Ester Prodrug

Technology Description

The bioavailability of orally administered therapeutics can be affected by digestion, solubilization rates, absorption, organ uptake, and the action of various enzymes. Bioavailability can be significantly influenced by the chemical form in which a drug is delivered and by the presence of factors in food that may enhance or depress absorption. As the number and chemical diversity of orally active therapeutics increase, strategies are rapidly being developed to increase bioavailability.

Medium-chain triglycerides (MCTs) are fats with an unusual chemical structure that allows the body to digest them easily. Most fats are broken down in the intestine and remade into a special form that can be transported in the blood, but MCTs are absorbed intact.

The technology constitutes a pharmaceutical composition and the process for creating a non-aqueous formulation of the cefuroxime axetil ester prodrug with medium chain triglycerides (MCTs) derived from coconut oil and/or palm seed oil. In particular, the prodrug used is a, cefuroxime axetil, in a non-aqueous suspension in an effective amount of 1 to 10 % (w/v).

The medium chain triglycerides used in the composition are in an amount between 1 and 50% (v/v). The composition is in the form of oral non-aqueous suspension with one or more pharmaceutical excipient or carrier. The resultant ratio of cefuroxime axetil to medium chain triglycerides from palm or coconut oils ranges from 1:1 up to 1:5.

The innovator claims the technology can be used in solids, tablets, capsules, lozenges, suspensions, elixirs, and solutions to solve 50-75% of variable drug absorption issues. This means that using the formulation can help avoid the "Food Effect" and improve intended dosage accuracy. He reports that the composition also masks the unpleasant taste of the drug.

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