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In vitro-in vivo evaluation of carba...

Sethia, Sundeep.

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In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method.

Record Type:	Electronic resources : Monograph/item
Title/Author:	In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method./
Author:	Sethia, Sundeep.
Description:	127 p.
Notes:	Source: Dissertation Abstracts International, Volume: 67-01, Section: B, page: 0283.
Contained By:	Dissertation Abstracts International67-01B.
Subject:	Chemistry, Pharmaceutical. -
Online resource:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3202728
ISBN:	9780542509353

In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method.
Sethia, Sundeep.

In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method. - 127 p.

Source: Dissertation Abstracts International, Volume: 67-01, Section: B, page: 0283.

Thesis (Ph.D.)--St. John's University (New York), School of Pharmacy, 2004.

The problem of incomplete and variable bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development. It has generally been observed that the slow dissolution rate of carbamazepine (CBZ), a poorly water-soluble drug, leads to its relatively low bioavailability.

ISBN: 9780542509353Subjects--Topical Terms:

550957
Chemistry, Pharmaceutical.

In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method.
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100 1 $a Sethia, Sundeep. $3 1916153
245 1 0 $a In vitro-in vivo evaluation of carbamazepine solid dispersions formulated by supercritical and conventional solvent evaporation method.
300 $a 127 p.
500 $a Source: Dissertation Abstracts International, Volume: 67-01, Section: B, page: 0283.
500 $a Adviser: Emilio Squillante.
502 $a Thesis (Ph.D.)--St. John's University (New York), School of Pharmacy, 2004.
520 $a The problem of incomplete and variable bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development. It has generally been observed that the slow dissolution rate of carbamazepine (CBZ), a poorly water-soluble drug, leads to its relatively low bioavailability.
520 $a Solid dispersions of CBZ were formulated by novel supercritical fluid processing (SCP) and conventional solvent evaporation in polyethylene glycol (PEG) 8000 or polyvinylpyrrolidone (PVP) K30 with either Gelucire 44/14 or vitamin E TPGS (d-alpha-tocopheryl polyethylene glycol 1000 succinate). Formulations were evaluated by particulate and/or intrinsic dissolution, scanning electron microscopy (SEM), powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) spectroscopy. Directional transport of CBZ through Caco-2 cell monolayers was determined in the presence and absence of TPGS. Cell viability in presence of various concentrations of amphiphilic carriers was seen by MTS assay. In vivo oral bioavailability of CBZ from various formulations was determined in rats.
520 $a CBZ release was enhanced from SC-treated CBZ. The radically altered morphologies of SCP-samples seen by SEM suggested polymorphic change that was confirmed by the XRD and DSC. Disappearance of the characteristic CBZ melting peak in case of PEG solid dispersions indicated that CBZ was dissolved inside the carrier system while in the case of PVP solid dispersions, CBZ was in an amorphous form inside the carrier system that was confirmed by XRD studies. FTIR spectroscopic studies showed interaction between CBZ and PVP K30 in solid dispersions. Polymorphic change of CBZ in PEG solid dispersions led to faster dissolution. The apparent intrinsic dissolution rates (IDR) of both conventional- and SCF-CBZ/PEG 8000/TPGS solid dispersions were increased by 13 and 10.6 fold, respectively relative to pure CBZ. The best IDR for PVP formulations was obtained for CBZ/PVP K30-SCP that was about 4 fold higher than pure CBZ. PEG formulations showed better IDR compared to PVP formulations and were thus chosen for in vivo studies. Higher CBZ permeability was seen in presence of 0.1% TPGS. Cell viability studies showed significant cytotoxicity only at or above 0.1% amphiphilic carrier. SC-treated formulation (without amphiphilic carrier) displayed oral bioavailability on par with those conventional solid dispersions augmented with amphiphilic carriers. An in vitro-in vivo correlation was seen between IDR and the AUC of the various CBZ solid dispersions.
520 $a Bioavailability of CBZ is more a function of dissolution as opposed to membrane effects. Although bioavailability from SCF processed dispersions was better than conventionally processed counterparts (except for one formulation containing Gelucire 44/14), an interaction of processing method and inclusion of an amphiphilic carrier, rather by one factor alone contributed to optimal absorption. Because the SC-based process produced solid dispersions that rendered inclusion of amphiphilic carrier redundant, stability issues associated with lipid carriers do not apply, which, in turn, implies easier scale up under current Good Manufacturing Practice for this technique.
590 $a School code: 1377.
650 4 $a Chemistry, Pharmaceutical. $3 550957
690 $a 0491
710 2 0 $a St. John's University (New York), School of Pharmacy. $3 1029322
773 0 $t Dissertation Abstracts International $g 67-01B.
790 1 0 $a Squillante, Emilio, $e advisor
790 $a 1377
791 $a Ph.D.
792 $a 2004
856 4 0 $u http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3202728