Title: Pharmacokinetic study of three different formulations of <scp>l</scp>‐tetrahydropalmatine in brain tissues of rats
Abstract: Abstract l ‐Tetrahydropalmatine ( l‐ THP), an active alkaloid compound isolated from Rhizoma Corydalis‐yanhusuo, has been reported to possess biological activity for treating cocaine use. To enhance both oral bioavailability and brain penetration, three formulations of l ‐THP suspension, mixture of l ‐THP–puerarin and self‐microemulsifying drug delivery systems (SMEDDS) were prepared. A sensitive and reliable ultra‐high‐performance liquid chromatography with tandem mass spectrometry method was developed and validated for the simultaneous determination of l ‐THP and its active metabolite l ‐isocorypalmine ( l ‐ICP) in rat brain. Diazepam was used as the internal standard. The chromatographic separation was achieved on a Bonshell ASB C 18 column at 30°C using acetonitrile–aqueous formic acid as mobile phase in gradient mode. The linearity was validated over the concentration ranges of 4.00–2,500 ng/ml for l ‐THP and 0.400–500 ng/ml for l ‐ICP. Full method validation was within the acceptance limits. The method was successfully used to determine the pharmacokinetics of two analytes following oral administration of these three formulations to rats. A significant difference was observed in the main pharmacokinetic parameters between SMEDDS and the suspension, and a 3.25‐ and 2.97‐fold increase in the relative bioavailability of l ‐THP and l ‐ICP, respectively, was observed with the SMEDDS compared with the suspension formulation. It was concluded that SMEDDS enhanced the absorption of l ‐THP and l ‐ICP and delayed their release in brain.
Publication Year: 2021
Publication Date: 2021-01-15
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 7
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