Intravenous formulations Amphotericin B




1 intravenous formulations

1.1 deoxycholate
1.2 liposomal formulations
1.3 lipid complex formulations





intravenous formulations

amphotericin b alone insoluble in normal saline @ ph of 7. therefore, several formulations have been devised improve intravenous bioavailability.


deoxycholate

the original formulation uses sodium deoxycholate improve solubility. amphotericin b deoxycholate (abd) administered intravenously, though frequent adverse effects detailed in side effects section. original formulation of amphotericin, referred conventional amphotericin.


liposomal formulations

in order improve tolerability of amphotericin , reduce toxicity, several lipid formulations have been developed. liposomal formulations have been found have less renal toxicity deoxycholate, , fewer infusion-related reactions. more expensive amphotericin b deoxycholate.


ambisome (lamb) liposomal formulation of amphotericin b injection , consists of mixture of phosphatidylcholine, cholesterol , distearoyl phosphatidylglycerol in aqueous media spontaneously arrange unilamellar vesicles contain amphotericin b.


guidelines recommend use of lamb cns fungal infections due better pharmacokinetics , cns penetration note based on animal models.


it developed nexstar pharmaceuticals (acquired gilead sciences in 1999). approved fda in 1997. marketed gilead in europe , licensed astellas pharma (formerly fujisawa pharmaceuticals) marketing in usa, , sumitomo pharmaceuticals in japan. fungisome generic liposomal complex of amphotericin b marketed lifecare innovations of india.


lipid complex formulations

a number of lipid complex preparations available. abelcet approved fda in 1995. consists of amphotericin b , 2 lipids in 1:1 ratio form large ribbon-like structures. amphotec complex of amphotericin , sodium cholesteryl sulfate in 1:1 ratio. 2 molecules of each form tetramer aggregate spiral arms on disk-like complex. approved fda in 1996. neither of these true unilamellar liposomes ambisome.








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