evaluation of carbamazepine (cbz) supersaturatable self-microemulsifying (s-smedds) formulation in-vitro and in-vivo

نویسندگان

zhang nan institute of pharmacology and toxicology, academy of military medical sciences, beijing,100850, china

gao lijun institute of pharmacology and toxicology, academy of military medical sciences, beijing,100850, china.

wang tao institute of pharmacology and toxicology, academy of military medical sciences, beijing,100850, china

quan dongqin institute of pharmacology and toxicology, academy of military medical sciences, beijing,100850, china

چکیده

the supersaturatable self-microemulsifying drug delivery system (s-smedds) represents a new thermodynamically stable formulation approach wherein it is designed to contain a reduced amount of surfactant and a water-soluble polymer (precipitation inhibitor or supersaturated promoter) to prevent precipitation of the drug by generating and maintaining a supersaturated state in-vivo. the supersaturatable self-microemulsifying drug delivery system (s-smedds) of cbz was evaluated in-vitro and in-vivo. three different formulations of cbz were prepared and drug precipitation behavior, dissolution rate in-vitro and particle size distribution were evaluated. studies on caco-2 permeability of three formulations were also carried out. pharmacokinetic studies were conducted in beagle dogs with administration dose of 200mg to assess bioavailability in-vivo compared with commercial tablet. the results showed that the presence of a small amount of polymeric precipitation inhibitor (pvp) effectively sustained supersaturated state by retarding precipitation kinetics. the mean particle size after dispersion was about 33.7 nm and the release rate from s-smedds was significantly higher than the commercial tablet in-vitro. s-smedds formulation with precipitation inhibitor decreased impairment to cells due to a lower surfactant level compared to smedds. the absorption of s-smedds in-vivo resulted in about 5-fold increase in bioavailability compared with the commercial tablet and the reproducibility of plasma concentration profiles intra-individual was improved remarkably. this study demonstrates that s-smedds technology provide an effective approach for improving the extent of absorption of poorly-soluble drugs with low level of surfactant.

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Evaluation of Carbamazepine (CBZ) Supersaturatable Self-Microemulsifying (S-SMEDDS) Formulation In-vitro and In-vivo

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عنوان ژورنال:
iranian journal of pharmaceutical research

جلد ۱۱، شماره ۱، صفحات ۲۵۷-۲۶۴

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