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Dear All,
For my research thesis I have been working on Itraconazole
formulation. for establishing the equivalence of the formulation, I
have to do a DPDM study or a dissolution study in biorelavent medias.
I am using Sporanox capsules as my innovator for comparison
purposes.In simulated gatric fluid without enzymes as prescribed by
FDA I get a decet F2 but when I do the dissolution in Ph 4.5 both the
innovator and my formulation release very less amount of drug (less
then 10%). In this case how will it be possible to do a profiling for
90 min as prescribed in FDA. As in such low dissolution it is not easy
to get a decent F2. Kindly revert back with suggestions for performing
DPDM of such pH sensitive molecules. Can I use some surfactants to
increase the dissoultion rate. Is there any reulatory guidelines for
the same. Anyone working on Itraconazole formulations and others in
the field please help. regards
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Hi Shankar,
I would draw your attention to " In vitro evaluation of the
dissolution behaviour of itraconazole in bio-relevant media Heba S.
Ghazal et al, International Journal of Pharmaceutics 366 (2009)
117-123.". They have data at pH 3. They have used SDS and Triton X-100
to get good dissolution profiles.
Hope this helps,
Milind
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Dear Shankar,
Itraconazole dissolution at pH 1.2 resulting in highly supersaturated
solution, maintaining the supersaturation state in neutral aqueous
solutions is also essential. Different polymeric stabilizers can
promote supersaturation in neutral media. I offer the papers of :
Miller DA, et al: Enhanced in vivo absorption of itraconazole via
stabilization of supersaturation following acidic a013to a013neutral
pH transition, Drug Dev Ind Pharm. 2008 Aug;34(8):890-902, and
Matteucci, ME et al: Highly Supersaturated Solutions from Dissolution
of Amorphous Itraconazole Microparticles at pH 6.8, Mol Pharm. 2009
Feb 23. [Epub ahead of print].
Best regards:
Maria Vikmon
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