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Bioavailability of indomethacin-saccharin cocrystals
Chungnam National University.
Chungnam National University.
Chungnam National University.
Luleå tekniska universitet, Institutionen för hälsovetenskap, Medicinsk vetenskap.ORCID-id: 0000-0002-6050-0432
Vise andre og tillknytning
2010 (engelsk)Inngår i: Journal of Pharmacy and Pharmacology (JPP), ISSN 0022-3573, E-ISSN 2042-7158, Vol. 62, nr 11, s. 1560-1568Artikkel i tidsskrift (Fagfellevurdert) Published
Abstract [en]

Pharmaceutical cocrystals are new solid forms with physicochemical properties that appear promising for drug product development. However, the in-vivo bioavailability of cocrystals has rarely been addressed. The cocrystal of indomethacin (IND), a Biopharmaceutical Classification System class II drug, with saccharin (SAC) has been shown to have higher solubility than IND at all pH. In this study, we aimed to evaluate the in-vitro dissolution and in-vivo bioavailability of IND-SAC cocrystals in comparison with IND in a physical mixture and the marketed product Indomee (R).MethodsScale-up of the cocrystals was undertaken using cooling batch crystallisation without seeding. The chemical and physical purity of the up-scaled material was verified using high-performance liquid chromatography, differential scanning calorimetry and powder X-ray diffraction. The IND-SAC cocrystals and IND plus SAC were mixed with lactose and the formulations were placed into gelatin capsules. In-vitro dissolution studies were then performed using the rotating basket dissolution method. The intrinsic dissolution rate of IND and IND-SAC cocrystals was also determined. Finally, a bioavailability study for the formulations was conducted in beagle dogs. The plasma samples were analysed using high-performance liquid chromatography and the pharmacokinetic data were analysed using standard methodologies.Key findingsThe bulk cocrystals (i.e. scaled-up material) were chemically and physically pure. The in-vitro dissolution rate of the cocrystals was higher than that of IND and similar to that of Indomee (R) at pH 7.4 and pH 1.2. The in-vivo bioavailability of the IND-SAC cocrystals in dogs was significantly higher (ANOVA, P < 0.05) than that of IND but not significantly different from Indomee (R) (ANOVA, P > 0.05).ConclusionsThe study indicates that the improved aqueous solubility of the cocrystals leads to improved bioavailability of IND. Thus, the cocrystals are a viable alternative solid form that can improve the dissolution rate and bioavailability of poorly soluble drugs.

sted, utgiver, år, opplag, sider
2010. Vol. 62, nr 11, s. 1560-1568
Emneord [en]
Pharmacy
Emneord [sv]
Farmaci
HSV kategori
Forskningsprogram
Hälsovetenskap
Identifikatorer
URN: urn:nbn:se:ltu:diva-13905DOI: 10.1111/j.2042-7158.2010.01189.xISI: 000282815300006PubMedID: 21039541Scopus ID: 2-s2.0-78649678462Lokal ID: d37fc300-e33d-11df-8b36-000ea68e967bOAI: oai:DiVA.org:ltu-13905DiVA, id: diva2:986858
Merknad
Validerad; 2010; 20101029 (ysko)Tilgjengelig fra: 2016-09-29 Laget: 2016-09-29 Sist oppdatert: 2018-07-10bibliografisk kontrollert

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