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Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability

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2015
2403.pdf (1.278Mb)
Authors
Krstić, Marko
Popović, Miljana
Dobričić, Vladimir
Ibrić, Svetlana
Article (Published version)
Metadata
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Abstract
The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formulation strategies to increase the dissolution rate of carbamazepine. Influence of increased dissolution rate on permeability of carbamazepine was evaluated using PAMPA test. In S-SMEDDS and S-SNEDDS formulations, the ratio of liquid SMEDDS/SNEDDS and solid carrier (Neusilin((R)) UFL2) was varied, and carbamazepine content was constant. In SD formulations, the ratio of carbamazepine and Neusilin((R)) UFL2, was varied. Formulations that showed the best dissolution rate of carbamazepine (SD_1:6, SMEDDS_1:1, SNEDDS_1:6) were mutually compared, characterization of these formulations was performed by DSC, PXRD and FT-IR analyses, and a PAMPA test was done. All formulations have shown a significant... increase in dissolution rate compared to pure carbamazepine and immediate-release carbamazepine tablets. Formulation S-SMEDDS_1:1 showed the fastest release rate and permeability of carbamazepine. DSC, PXRD and FT-IR analyses confirmed that in S-SMEDDS and S-SNEDDS carbamazepine remained in polymorph form III, and that it was converted to an amorphous state in SD formulations. All formulations showed increased permeability of carbamazepine, compared to pure carbamazepine.

Keywords:
carbamazepine / dissolution rate / PAMPA test / solid dispersions / S-SMEDDS / S-SNEDDS / characterization
Source:
Molecules, 2015, 20, 8, 14684-14698
Publisher:
  • MDPI, Basel
Projects:
  • Advanced technologies for controlled release from solid drug delivery systems (RS-34007)

DOI: 10.3390/molecules200814684

ISSN: 1420-3049

PubMed: 26287134

WoS: 000361375400071

Scopus: 2-s2.0-84941249098
[ Google Scholar ]
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URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/2405
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  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy

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