| 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.
Contact details:
Information Manager
Email: timeis@ficci.com

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