Regnault C, Soursac M, Roch-Arveiller M, Postaire E, Hazebroucq G
Faculte de Pharmacie Paris XI, Service de Pharmacie Clinique, Chatenay-Malabry, France.
Biopharm Drug Dispos. 1996 Mar;17(2):165-74. doi: 10.1002/(SICI)1099-081X(199603)17:2<165::AID-BDD945>3.0.CO;2-N.
The kinetic behaviour of bovine erythrocyte Cu-Zn SOD was investigated in Sprague Dawley male rats after subcutaneous and oral administrations of doses ranging from 0 center dot 5 to 20 mg kg-1. Studies have been carried out with SOD and SOD encapsulated into liposomes containing or not containing ceramides. The maximum concentration (Cmax) in blood cell pellets ranged from 8 center dot 65 to 11 center dot 03 U/mg haemoglobin (Hb) after subcutaneous injection, and from 4 center dot 48 to 8 center dot 23 U/mg Hb after oral administration. The maximum concentrations were reached in 5 h (t max) for the two routes. Comparison between the areas under the curves (AUCs) obtained after subcutaneous and oral administration allowed the calculation of relative bioavailability (F'). The maximum bioavailability after oral administration was 14% for free SOD, 22% for SOD encapsulated into liposomes, and 57% when ceramides were added to liposomes. Poor SOD bioavailability was enhanced by liposome encapsulation, and ceramide addition seemed to be beneficial for oral encapsulated SOD administration.
在给予Sprague Dawley雄性大鼠皮下和口服剂量范围为0.5至20 mg kg-1的牛红细胞铜锌超氧化物歧化酶(Cu-Zn SOD)后,对其动力学行为进行了研究。已对超氧化物歧化酶以及封装于含或不含神经酰胺脂质体中的超氧化物歧化酶进行了研究。皮下注射后,血细胞沉淀中的最大浓度(Cmax)范围为8.65至11.03 U/mg血红蛋白(Hb),口服给药后为4.48至8.23 U/mg Hb。两种给药途径均在5小时(tmax)达到最大浓度。通过比较皮下和口服给药后获得的曲线下面积(AUC),计算相对生物利用度(F')。口服给药后,游离超氧化物歧化酶的最大生物利用度为14%,封装于脂质体中的超氧化物歧化酶为22%,当向脂质体中添加神经酰胺时为57%。脂质体封装提高了超氧化物歧化酶较差的生物利用度,添加神经酰胺似乎有利于口服封装的超氧化物歧化酶给药。