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AAPS PharmSciTech. 2018 Feb;19(2):951-960. doi: 10.1208/s12249-017-0912-0. Epub 2017 Nov 2.

Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form.

Author information

1
Faculty of Pharmacy, Department of Drug Form Technology, Wroclaw Medical University, Borowska 211A, 50-556, Wroclaw, Poland. dorota.haznar-garbacz@umed.wroc.pl.
2
Department of Pharmacognosy and Phytochemistry, Medical University of Silesia in Katowice, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, ul. Jagiellonska 4, 41-200, Sosnowiec, Poland.
3
Physiolution GmbH, Walther-Rathenau-Str. 49a, 17489, Greifswald, Germany.
4
Institute of Physics&SMCEiBI, University of Silesia, ul 75 Pulku Piechoty 1, 41-500, Chorzow, Poland.
5
Department of Pharmaceutical Technology and Biopharmaceutics, Pharmaceutical Faculty, Jagiellonian University, ul. Medyczna 9, 30-688, Kraków, Poland.
6
Institute of Technology, Faculty of Mathematics, Physics and Technical Science, Pedagogical University of Cracow, ul. Podchorążych 2, 30-084, Kraków, Poland.

Abstract

The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS). The results indicate that the dissolution profiles of the GSDFs with nifedipine are neither affected by the pH of the dissolution media, type and concentration of surfactants, nor by simulated mechanical stress of biorelevant intensity. Furthermore, it was found that the dissolution profiles of the novel dosage forms were similar to the profiles obtained from the nifedipine OROS. The formulation of GSDFs is relatively simple, and the dosage forms were found to have favorable dissolution characteristics.

KEYWORDS:

acetylated saccharides; amorphous drugs; biorelevant dissolution stress test; modified release; oral osmotic system; sustained release

PMID:
29098644
DOI:
10.1208/s12249-017-0912-0
[Indexed for MEDLINE]

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