Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats

<table class="table-group" id="tab4"><tr><td><table class="table"><tr><td class="thead-hr" colspan="5"><hr/></td></tr><tr class="thead"><td align="left"> </td><td align="center">Group</td><td align="center"><svg height="15.4" id="M172" style="vertical-align:-3.3907pt" version="1.1" viewbox="0 0 35.924999 15.4" width="35.924999" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink">
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<g transform="matrix(.012,-0,0,-.012,12.675,15.187)"><path d="M797 0h-214v26q46 5 58 17.5t12 63.5v167q0 116 -88 116q-48 0 -112 -52q3 -18 3 -42v-195q0 -46 11 -58t53 -17v-26h-214v26q48 5 59.5 17t11.5 60v172q0 115 -88 115q-47 0 -109 -52v-235q0 -47 10 -59.5t48 -17.5v-26h-211v26q50 5 62.5 17t12.5 60v207q0 48 -9 59.5
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t-45 -39.5q-24 -29 -78 -110l97 -148q28 -43 46.5 -55.5t63.5 -18.5v-26z" id="x78"></path></g>
</svg> (nmol/min/mgprotein)</td><td align="center"><svg height="15.4" id="M173" style="vertical-align:-3.3907pt" version="1.1" viewbox="0 0 23.325001 15.4" width="23.325001" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink">
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<g transform="matrix(.012,-0,0,-.012,13.25,15.187)"><path d="M766 88q-40 -45 -83.5 -72.5t-63.5 -27.5q-39 0 -16 103l49 224q15 68 -10 68q-36 0 -112.5 -78.5t-105.5 -133.5q-27 -101 -38 -165q-35 -4 -77 -18l-6 6q42 153 70 288q12 55 10 78t-19 23q-38 0 -114 -80.5t-101 -131.5q-24 -68 -41 -165q-36 -3 -76 -18l-8 6
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</svg> (<i><i>μ</i></i>M)</td><td align="center"><svg height="15.65" id="M174" style="vertical-align:-3.3907pt" version="1.1" viewbox="0 0 36.512501 15.65" width="36.512501" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink">
<g transform="matrix(.017,-0,0,-.017,.062,11.362)"><path d="M614 175l29 -10q-33 -109 -57 -154q-121 -26 -184 -26q-90 0 -160.5 29t-112.5 77t-63.5 105.5t-21.5 119.5q0 157 108 253t277 96q36 0 71.5 -5t69 -13.5t36.5 -8.5q15 -102 20 -150l-29 -8q-20 79 -66.5 114t-128.5 35q-119 0 -187.5 -86t-68.5 -207
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</svg> (<i>μ</i>L/min/mg protein)</td></tr><tr><td class="thead-hr" colspan="5"><hr/></td></tr><tr><td align="left"><svg height="17.7125" id="M175" style="vertical-align:-0.0pt" version="1.1" viewbox="0 0 12.4375 17.7125" width="12.4375" xmlns="http://www.w3.org/2000/svg" xmlns:xlink="http://www.w3.org/1999/xlink">
<g transform="matrix(.017,-0,0,-.017,.062,17.65)"><path d="M384 0h-275v27q67 5 81.5 18.5t14.5 68.5v385q0 38 -7.5 47.5t-40.5 10.5l-48 2v24q85 15 178 52v-521q0 -55 14.5 -68.5t82.5 -18.5v-27z" id="x31"></path></g>
<g transform="matrix(.012,-0,0,-.012,8.225,9.488)"><path d="M227 744l-123 -338l-31 15l73 368q12 3 41.5 -8t36.5 -20z" id="x2032"></path></g>
</svg>-Hydroxymidazolam</td><td align="center">Control</td><td align="center">0.528 ± 0.061</td><td align="center">18.6 ± 2.4</td><td align="center">28.4 ± 1.5</td></tr><tr><td align="left"> </td><td align="center">Baicalin</td><td align="center">0.388 ± 0.075**</td><td align="center">18.2 ± 5.0</td><td align="center">21.8 ± 3.1***</td></tr><tr><td align="left">4-Hydroxymidazolam</td><td align="center">Control</td><td align="center">1.188 ± 0.227</td><td align="center">15.4 ± 3.6</td><td align="center">77.9 ± 9.3</td></tr><tr><td align="left"> </td><td align="center">Baicalin</td><td align="center">0.849 ± 0.143**</td><td align="center">14.2 ± 4.0</td><td align="center">61.7 ± 11.1**</td></tr><tr class="table-tr"><td colspan="5"><hr class="tbody-hr"/></td></tr></table></td></tr><tr class="table-fn"><td>Rats received intravenous administration of baicalin at a dose of 0.90 g/kg once daily for 7 days. The results are means ± SD of 8 rats. Significance is indicated as **<i>P </i>&lt; 0.01, ***<i>P </i>&lt; 0.001 compared to the control. <br/></td></tr></table>

Effects of multiple doses of baicalin on MDZ hydroxylation activity in the rat liver.

Evidence-Based Complementary and Alternative Medicine

tab4

Table 4

Table 4: Inhibitory Effects of Baicalin on the Expression and Activity of CYP3A Induce the Pharmacokinetic Changes of Midazolam in Rats 