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Information Journal Paper

Title

EVALUATION OF CARBAMAZEPINE (CBZ) SUPERSATURATABLE SELF-MICROEMULSIFYING (S-SMEDDS) FORMULATION IN-VITRO AND IN-VIVO

Pages

  257-264

Abstract

 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 STATEin-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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    • Cite

    APA: Copy

    NAN, ZHANG, LIJUN, GAO, TAO, WANG, & DONGQIN, QUAN. (2012). EVALUATION OF CARBAMAZEPINE (CBZ) SUPERSATURATABLE SELF-MICROEMULSIFYING (S-SMEDDS) FORMULATION IN-VITRO AND IN-VIVO. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 11(1), 257-264. SID. https://sid.ir/paper/287915/en

    Vancouver: Copy

    NAN ZHANG, LIJUN GAO, TAO WANG, DONGQIN QUAN. EVALUATION OF CARBAMAZEPINE (CBZ) SUPERSATURATABLE SELF-MICROEMULSIFYING (S-SMEDDS) FORMULATION IN-VITRO AND IN-VIVO. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2012;11(1):257-264. Available from: https://sid.ir/paper/287915/en

    IEEE: Copy

    ZHANG NAN, GAO LIJUN, WANG TAO, and QUAN DONGQIN, “EVALUATION OF CARBAMAZEPINE (CBZ) SUPERSATURATABLE SELF-MICROEMULSIFYING (S-SMEDDS) FORMULATION IN-VITRO AND IN-VIVO,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 11, no. 1, pp. 257–264, 2012, [Online]. Available: https://sid.ir/paper/287915/en

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