Sikarwar Mukesh S, Sharma Shalini, Jain Amit K, Parial S D
Department of Pharmacognosy and Phytochemistry, B. R. Nahata College of Pharmacy, Mhow-Neemuch Road, Mandsaur 458001, India.
AAPS PharmSciTech. 2008;9(1):129-37. doi: 10.1208/s12249-007-9020-x. Epub 2008 Jan 18.
The aim of this research was to formulate Marsupsin-phospholipid complex (M-P Complex) in attempt to increase the bioavailability of marsupsin and to characterize this new formulation along with its evaluation. Marsupsin-phospholipid complex was formulated by mechanical dispersion method. In this new formulation, complex formation was confirmed by carrying out transmission electron microscopy (TEM), IR, (1)H-NMR and RP-HPLC analysis. TEM showed M-P Complex diameter range of 0.05-0.5 microm. The entrapment efficiency of M-P Complex was found to be 44%. In vitro release study revealed its first order release profile. Mean blood serum concentration vs time curve of marsupsin was of first order after oral administration of M-P Complex in albino rabbits which clearly showed remarkably increased bioavailability of M-P Complex than standardized marsupsin. The average value of C(max) and T(max) of M-P Complex were found to be 3.02 mg/ml and 10.2 h, respectively. Hence the findings demonstrate that complexing marsupsin with phospholipids results in better oral bioavailability and improved biological response than free form of standardized marsupsin.
本研究的目的是制备紫铆素 - 磷脂复合物（M - P复合物），以提高紫铆素的生物利用度，并对这种新制剂进行表征和评估。采用机械分散法制备紫铆素 - 磷脂复合物。在这种新制剂中，通过透射电子显微镜（TEM）、红外光谱（IR）、氢核磁共振（¹H - NMR）和反相高效液相色谱（RP - HPLC）分析确认了复合物的形成。TEM显示M - P复合物的直径范围为0.05 - 0.5微米。发现M - P复合物的包封率为44%。体外释放研究显示其符合一级释放曲线。在白化兔口服M - P复合物后，紫铆素的平均血清浓度与时间曲线呈一级，这清楚地表明M - P复合物的生物利用度比标准紫铆素显著提高。M - P复合物的C(max)和T(max)平均值分别为3.02毫克/毫升和10.2小时。因此，研究结果表明，与游离形式的标准紫铆素相比，紫铆素与磷脂形成复合物可导致更好的口服生物利用度和改善的生物学反应。
