舒更葡糖钠注射液与罗库溴铵的体外结合与释放

The Binding and Release of Sugenose Sodium Injection and Rocuronium Bromide in Vitro

目的 评价不同厂家舒更葡糖钠注射液与罗库溴铵体外的结合与释放。方法 采用等温滴定量热法(ITC)研究不同厂家舒更葡糖钠与罗库溴铵的相互作用,测定其热力学常数及结合常数。采用高效液相色谱法(HPLC)评价不同厂家舒更葡糖钠与罗库溴铵结合后的释放。结果 舒更葡糖钠与罗库溴铵结合KD值:A制剂(原研药):(8.26×10^(-7)±6.81×10^(-8))mol/L,B制剂(仿制药):(1.42×10^(-6)±3.29×10^(-7))mol/L。罗库溴铵与舒更葡糖的结合物稳定性较强,几乎无释放。结论 不同厂家舒更葡糖钠制剂与罗库溴铵均具有较强的体外结合力,单-羟基舒更葡糖的含量可能影响其结合力和释放速度。

Objective To evaluate the combination and release of Sugammadex Sodium injection and rocuronium bromide from different manufacturers in vitro.Methods isothermal titration calorimetry(ITC)was used to study the interaction between Sugammadex Sodium and rocuronium bromide from different manufacturers,and its thermodynamic constants and binding constants were determined.HPLC method was used to evaluate the release of Sugammadex Sodium from different manufacturers combined with rocuronium bromide.Results The binding KD of Sugammadex Sodium and rocuronium bromide was as follows:preparation A(original drug):(8.26×10^(-7)±6.81×10^(-8))mol/L,and preparation B(imitation):(1.42×10^(-6)±3.29×10^(-7))mol/L.The combination of rocuronium bromide and Sugammadex Sodium has strong stability and almost no release.Conclusion Sugammadex Sodium preparations from different manufacturers have strong binding force with rocuronium bromide in vitro,and the content of mono-hydroxy Sugammadex Sodium may affect its binding force and release rate.