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Dissolution and pre...
Dissolution and precipitation behavior of ternary solid dispersions of ezetimibe in biorelevant media
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- Al-Hayali, Amani Ibraheem Younis (författare)
- Luleå tekniska universitet,Medicinsk vetenskap
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- Tavelin, Staffan (författare)
- Umeå universitet,Farmakologi,Departments of Pharmacology and Clinical Neuroscience, Umeå university
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- Velaga, Sitaram (författare)
- Luleå tekniska universitet,Medicinsk vetenskap
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(creator_code:org_t)
- 2016-08-28
- 2017
- Engelska.
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Ingår i: Drug Development and Industrial Pharmacy. - : Informa UK Limited. - 0363-9045 .- 1520-5762. ; 43:1, s. 79-88
- Relaterad länk:
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https://figshare.com...
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visa fler...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
Ämnesord
Stäng
- The effects of different formulations and processes on inducing and maintaining the supersaturation of ternary solid dispersions of ezetimibe (EZ) in two biorelevant media fasted-state simulated intestinal fluid (FaSSIF) and fasted-state simulated gastric fluid (FaSSGF) at different temperatures (25 °C and 37 °C) were investigated in this work.Ternary solid dispersions of EZ were prepared by adding polymer PVP-K30 and surfactant poloxamer 188 using melt-quenching and spray-drying methods. The resulting solid dispersions were characterized using scanning electron microscopy, differential scanning calorimetry (DSC), modulated DSC, powder X-ray diffraction and Fourier transformation infrared spectroscopy. The dissolution of all the ternary solid dispersions was tested in vitro under non-sink conditions.All the prepared solid dispersions were amorphous in nature. In FaSSIF at 25 °C, the melt-quenched (MQ) solid dispersions of EZ were more soluble than the spray-dried (SD) solid dispersions and supersaturation was maintained. However, at 37 °C, rapid and variable precipitation behavior was observed for all the MQ and SD formulations. In FaSSGF, the melting method resulted in better solubility than the spray-drying method at both temperatures.Ternary solid dispersions show potential for improving solubility and supersaturation. However, powder dissolution experiments of these solid dispersions of EZ at 25 °C may not predict the supersaturation behavior at physiologically relevant temperatures.
Ämnesord
- NATURVETENSKAP -- Kemi -- Materialkemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Materials Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Hälsovetenskap -- Annan hälsovetenskap (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Health Sciences -- Other Health Sciences (hsv//eng)
Nyckelord
- Poorly soluble drugs
- ternary solid dispersions
- supersaturation
- biorelevant media
- dissolution
- Health Science
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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