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Dear Pharmacokinetists,
i am research scholar, pursuing Ph.D. on Controlled release.
i am formulating Tablet with in tablet to accomodate loading dose and
maintanance dose in coat and core respectively.i want to know how much
dose should i kept in outer coat layer to provide a loading dose for
once a daily Tab in Tab formulation. is there any specification that
within 1 hr or 2hrs some fixed % of drug should release for once daily
formulation.
Sincerely yours,
Punit Parejiya
(punit_pharma.aaa.yahoo.co.in)
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Dear Punit,
Generally about 30-35% of the dose is required as loading dose and
then rest of the drug will be kept as loading dose.
Dr Zafar
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Hi Punit,
I am not sure that the concept of a loading dose (to quickly take you
into the therapeutic window) is relevant anymore. Consistent blood
levels within the window happen only at steady state - 5 days of
dosing or so. So long as you approximately match input to output, the
levels will be maintained.
In first 2 hours 10-30% drug seems to be released for many 24-hour
commercial SR products. This is probably because they cannot control
the initial "burst" based on current matrix technologies, rather than
from any ideas of a "loading dose".
To get a uniform API content in the coating will not be easy: The RSD
needs to be below 6%, and pan coating is not geared for that: typical
variations in film coats (film deposited on each tablet) are 25%.
Hope this helps.
Milind
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