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Does anyone has looked into the sustained delivery of a drug for 3-4
days administered orally? Is there any proven/approved
gastroretentive mechanism (bioadhesive, floating etc.) to sustain the
blood level of drugs for 3-4 days after oral administration of a
single dose?
(Assume the drug is a lipophilic small molecule with oral
bioavailability of 50% and half-life 4 hours. Inhibition of
elimination to prolong half-life is not desirable).
Thanks for your help.
Delwar
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Delwar,
unfortunately I think that there is no miracle to wait for. As far as I know
no proven oral formulation can enhance drug delivery at this extent.
The concern with floating is that the delivery device is very sensitive to
body position. It's supposed to stay in the stomach due to flotation on the
gastric juice but when you are sleeping the device (always floating) can go
through the pylore into the intestine.
Regardind bioadhesion the kind of polymers used for this property is also
sensitive to degradation (acidic, enzymatic ?). That's why their use is also
limited in time.
Another concern is the amount of drug you consider your formulation should
be loaded with. In the case of sustained release formulations it's commonly
admitted that 500 mg is a quite large amount of drug to be incorporated into
a modified delivery system.
Why don't you consider to come back to a daily dosing ? I guess sustained
release would then make sense.
Regards,
Frederic
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