头孢氨苄缓释片犬体内药动学研究

Pharmacokinetics of cefalexin sustained-release tablet in beagle dogs

目的以上市头孢氨苄普通胶囊为参比制剂,考察24h给药一次的头孢氨苄缓释片beagle犬体内药动学。方法 Beagle犬单剂量口服受试制剂和参比制剂,采用HPLC法进行生物等效性评价。结果方法学研究结果显示线性范围0.5～50μg/mL,高中低相对回收率均大于80%,日内日间精密度均小于15%,最低定量限0.5μg/mL。参比制剂与受试制剂药动学参数分别为:Cmax为(35.02±8.67)和(22.8±74.11)μg/mL,AUC0-∞为(164.59±17.79)和(201.15±89.87)μg/(h·mL),Tmax为(2.1±1.0)和(4.2±0.4)h。受试制剂相对生物利用度为(104.4±21.4)%。结论两种制剂生物等效。

Objective The pharmacokinetic of cefalexin sustained-release tablet in beagle dogs were performed with cefalexin capsule as the control. Methods Pharmacokinetic parameters were evaluated by HPLC method after a single oral dose of the referenced formulation and the tested formulation. Results The linearity was obtained over the concentration range of 0.5-50μg/mL for cefalexin. The relative recovery of cefalexin at high, medium and low concentrations were ≥ 80%. Both inter-and intra-day RSD were ≤ 15% for cefalexin. The limit of detection for cefalexin was 0.5μg/mL. The pharmacokinetic parameters of cefalexin capsules referenced formulation and the tested formulation were shown as follows： Cmax were （35.02±8.67） and （22.8±74.11）μg/mL, AUC0-∞ were （164.59±17.79） and （201.15±89.87） μg/（h·mL）, Tin,x were （2.1±1.0） and （4.2±0.4）h. The relative bioavailability of tested formulation was （104.4±21.4）%. Conclusion The tested formulation is bioequivalent with the referenced formulation.