高效液相色谱法测定CsA的房水药物浓度

Determination of CsA in aqueous humor by HPLC

目的 本研究用溶剂挥发法制作了环孢霉素A(cyclosporineA ,CsA)微粒体缓释剂。测定兔眼应用CsA微粒体及注射液后房水药物浓度。方法 结膜下注射CsA微粒体作为实验组 (8只 ) ,结膜下注射CsA溶液作为对照组 (8只 ) ,在注射后 6、12、2 4、4 8、72、14 4h于前房采集房水。采用HPLC(高效液相色谱法 )测定了房水的药物浓度 ,并对CsA的药代动力学进行对比研究。结果 在结膜下注射 2种制剂后 6、12、2 4、4 8、72、14 4h房水药物浓度显示 :环孢霉素A微粒体分别为 (112 0 0± 2 5 8)、(98 0 0± 2 5 7)、(90 0 0±3 90 )、(83 0 0± 4 2 4 )、(80 75± 3 5 0 )、(6 4 0 0± 3 91) μg·L-1;CsA溶液组房水药物始终小于 4 0 μg·L-1。微粒体较CsA溶液在房水中释药浓度较为平稳持久 ,药物浓度较高。结论 CsA微粒体是一种可持久保持药效的眼用缓释剂。

Objective Microspheres containing cyclosporine A(CsA) were prepared using a solvent evaporation process.A simple high performance liquid chromatographic method was established for determination of concentration of CsA in aqueous humor after injecting microspheres containing cyclosporine A and cyclosporine A solution respectively.Methods Microspheres containing cyclosporine A and cyclosporine A solution were injected subconjunctivally in 16 rabbit eyes respectively.The concentration of CsA in the aqueous humor was measured at 6,12,24,48,72 and 144 hours.Results Microspheres containing cyclosporine A had(112.00±2.58)、(98.00±2.57)、(90.00±3.90)、(83.00±4.24)、(80.75±3.50)、(64.00±3.91)μg·L -1 in the aqueous humor at six times respectively,but closporine A solution can not be measured at all times,it is lower than 40μg·L -1 .Comparing to closporine A solution,Microspheres containing cyclosporine A had a higher medicine concerntion and could last for a longer time.Conclusion The data indicate that a microsphere drug delivery system is an effective means of delivering CsA to the anterior chamber.