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KMID : 0614020080230010059
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Journal of Pharmaceutical Sciences (C.N.U.)
2008 Volume.23 No. 1 p.59 ~ p.63
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LC/MS/MS Analyasis and Pharmacokinetic Study of Afloqualone in Human Volunteers
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Lee Seo-Pan
Lee Byung-Yo
Yun Hwi-Yeol
Lee Eun-Joo
Kwon Kwang-Il
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Abstract
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Afloqualone is a centrally acting muscle relaxant that inhibits mono- and polysynaptic reflexes. The purpose of this study was to estimate the pharmacokinetic parameters of afloqualone in healthy volunteers. The pharmacokinetics of afloqualone tablet was examined on 24 healthy volunteers who received a single oral dose(20 Bg) of each preparation in the fasting state. Blood samples were ten at 0, 0.5, 1, 1.5 2 3 4 6 8 10, 12 and 24 hr after drug administration. Blood concentrations of afloqualone were determined using a liquid chromatography tandem mass spectrometry(LC/MS/MS) systems. A two compartment model was used to explain the pharmacokinetic properties of afloqualone. The pharmacokinetic parameters were calculated with model independent(AUC, C_max, T_max, CL_t, V/F) and model dependent(K_ei, K_a, K_cp, K_pc, t_1/2) Pharmacokinetic analysis using WinNonlin program. The estimated means of AUC_0-24hours, C_max, T_max CL_t and V/F were 148.99 ± 127.39 ng·hi/ml 35.11 ± 56.62 ng/ml, 1.81 士 1.34 hr, 189.01 士 79.67 L/hr and 848.61 ± 567.06 L, respectively. The model dependent parameters(K_ei, K_a, K_cp, K_pc, t_1/2) were 0.14 ± 0.18 hr^(-1), 11.64 ± 30.03 hr^(-1), 0.34 ± 0.39 hr^(-1), 0.1 ± 0.16 hr^(-1) and 10.56 ± 4.30 hr, respectively. In conclusion a two compartment model was best described the pharmacokinetic behavior of afloqualone in healthy human.
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KEYWORD
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afloqualone, pharmacokinetic, LC/MS/MS, modeling
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