Inulin solid dispersion technology to improve the absorption of the BCS Class IV drug TMC240

TMC240 is a very poorly soluble and poorly permeating HIV protease inhibitor. In order to enhance its oral bioavailability, a fast dissolving inulin-based solid dispersion tablet was developed. During the dissolution test in water (0.5% or 1.0% SLS), this tablet released at least 80% of TMC240 withi...

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Veröffentlicht in:	European journal of pharmaceutics and biopharmaceutics 2010-02, Vol.74 (2), p.233-238
Hauptverfasser:	Visser, Marinella R., Baert, Lieven, Klooster, Gerben van ’t, Schueller, Laurent, Geldof, Marian, Vanwelkenhuysen, Iris, de Kock, Herman, De Meyer, Sandra, Frijlink, Henderik W., Rosier, Jan, Hinrichs, Wouter L.J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Absorption Animals BCS Class IV Benzothiazoles - chemistry Benzothiazoles - pharmacokinetics Biological and medical sciences Dogs Drug Carriers - chemical synthesis Drug Carriers - pharmacokinetics Drug Compounding - methods Drug Interactions General pharmacology HIV Protease Inhibitors - chemistry HIV Protease Inhibitors - pharmacokinetics Intestinal Absorption - drug effects Inulin - chemistry Inulin - pharmacokinetics Inulin solid dispersion Male Medical sciences Pharmaceutical technology. Pharmaceutical industry Pharmacokinetics Pharmacology. Drug treatments Polyethylene Glycols - chemistry Polyethylene Glycols - pharmacokinetics Ritonavir Ritonavir - pharmacology Solubility Sulfones - chemistry Sulfones - pharmacokinetics Suspensions - chemistry Suspensions - pharmacokinetics Tablets - chemistry Tablets - pharmacokinetics TMC240
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Beschreibung
Zusammenfassung:	TMC240 is a very poorly soluble and poorly permeating HIV protease inhibitor. In order to enhance its oral bioavailability, a fast dissolving inulin-based solid dispersion tablet was developed. During the dissolution test in water (0.5% or 1.0% SLS), this tablet released at least 80% of TMC240 within 30 min, while a tablet with the same composition, but manufactured as physical mixture, released only 6% after 2 h. In a subsequent single-dose study in dogs (200 mg of TMC240), plasma concentrations of TMC240 remained below the lower limit of quantification (
ISSN:	0939-6411 1873-3441
DOI:	10.1016/j.ejpb.2009.10.004