Itraconazole is a broad spectrum antifungal agent that could be the substitute for the lipid formulation of
Amphotericin B, Ambisome - the gold standard of systemic antifungal agent. And as it is insoluble in water
it needs some solubilizing agent to be solubilized in water. Janssen, the original player, uses
hydroxypropyl-beta-cyclodextrin(HP-beta-CD) for the solubilization and hold the right of formulation patent
for Itraconazole injection and solution.
But HP-beta-CD system has some drawbacks. First, the solubilizing activity of HP-beta-CD is not so reliable.
It requires many precondition; the solution pH should be in the range of 4.5 ~ 4.8. Sporanox injection
(10mg Itraconazole/ml) should not be diluted more than three folds for infusion with saline or WFI.
Even in properly diluted cases, you should use infusion filter against the possible precipitation during one
hour inoculation.
Second, HP-beta-CD is not metabolized in the human body, so it is accumulated in the kidney and it must
be washed out with urine. For that reason, Sporanox injection is not applicable to the patients with
severe renal impairment.
Third, HP-beta-CD can cause hemolysis which limits the infusion time. You should inoculate Sporanox
injection with more than one hour.
SYC has developed the Itraconazole injection and solution using polymer technology which enables us to
avoid Janssen patent and allow the authentic solubility to Itraconazole formulation. In our system
Itraconazole is solubilized with polymers to form polymeric nano-particle. Our polymers are biocompatible
and biodegradable. We can solubilize Itraconazole with our polymers at a wide concentration range of
1mg/ml ~ 10mg/ml under physiological pH condition. Our Itraconazole injection does not cause any
hemolysis and we might be able to inoculate it shortly to the patients. In our experiment scheme the
product showed much better stability and safety in solution state.
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