Effect of Gelucire® 44/14 on the Oral Bioavailability of Cyclosporin A
| dc.contributor.author | Lim, Sin Yee | |
| dc.date.accessioned | 2019-03-05T06:35:53Z | |
| dc.date.available | 2019-03-05T06:35:53Z | |
| dc.date.issued | 2007-06 | |
| dc.description.abstract | The present study was conducted to investigate the effect of Gelucire® 44/14 on the oral bioavailability of a model lipophilic polypeptide drug, cyclosporin A. Gelucire® 44/14 formulations of cyclosporin A at drug to Gelucire® 44114 ratios of 1:4, 1:10, 1:14 and 1:20 (w/w) were successfully prepared using a heatfusion method. In vitro studies showed that the aqueous solubility and dissolution of cyclosporin A were proportionally increased with the amount of Gelucire® used in the formulations. All formulations prepared could form stable emulsion products when introduced into an aqueous medium. Moreover, upon introduction into an aqueous medium, formulations with 1:10, 1:14 and 1:20 ratios of cyclosporin A to Gelucire® 44/14 formed emulsion products with comparable droplet sizes to that using Gelucire® alone. Additionally, incorporation of cyclosporin A into Gelucire® 44/14 did not alter the melting point of the base. A liquid chromatography tandem mass spectrometry method was successfully developed for the determination of plasma concentrations of cyclosporin A. The method was simple, sensitive, reproducible and specific and was applied to evaluate the bioavailability of the 1 :10 formulation of cyclosporin A in Gelucire® 44/14. The in vivo study conducted using Sprague-Dawley rats revealed that at a drug to Gelucire® ratio of 1:10, the formulation was capable of increasing the oral bioavailabiJity of cycJosporin A by approximately 2.8-fold compared to an aqueous suspension of the drug and comparable to that of a commercially available self-emulsifying formulation, Sandimmun Neoral®. In conclusion, Gelucire® 44114 enhanced the solubility of a lipophilic polypeptide drug, cyclosporin A, and subsequently increased the oral bioavailability of the drug. Thus Gelucire® 44/14 could be a useful excipient in self-emulsifying formulations for enhancing the oral bioavailability of lipophilic drugs. | en_US |
| dc.identifier.uri | http://hdl.handle.net/123456789/7822 | |
| dc.subject | Gelucire | en_US |
| dc.subject | Cyclosporin A | en_US |
| dc.title | Effect of Gelucire® 44/14 on the Oral Bioavailability of Cyclosporin A | en_US |
| dc.type | Thesis | en_US |
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