抗生物質の生体内動態に関する基礎的研究

第1編血清蛋白との結合について

抄録

The binding of penicillin G and other 29 antibiotics to the bovine plasma proteins, a part of the pharmacokinetics of antibiotics, was investigated by the ultrafiltrating technique at 4°C.
As the rates of the binding, inactivation, recovery and binding activity, following values were obtained in order : 64. 9 to 82. 7%, 11. 96 to 56. 85%, 7. 77 to 25. 75% and 8. 9 to 34. 11% in penicillin antibiotics; 0 to 61. 4%, 0 to 10. 66%, 0. 49 to 12. 8% and 14. 91 to 41. 72% in glycoside antibiotics; 91. 0 to 99. 9%, 16. 0 to 46. 19%, 44. 98 to 71. 01% and 4. 33 to 21. 06% in tetracycline antibiotics; 55. 22 to 94. 1%, 5. 37 to 57. 36%, 1. 32 to 31. 5% and 9. 66 to 40. 65% in macrolide antibiotics; and 72. 6 to 95. 68%, 14. 34 to 51. 85%, 8. 19 to 30. 12%, and 17. 28 to 41. 54% in chloramphenicol antibiotics, respectively.
Optimum pH of the binding of antibiotics to the plasma proteins was in the range 5. 0 to 8. 0, i. e. 8. 0 in penicillin antibiotics, 5. 0 in glycoside antibiotics, 7. 0 to 8. 0 in tetracycline antibiotics, 6. 0 to 7. 0 in macrolide antibiotics, and 7. 0 to 8. 0 in chloramphenicol antibiotics, respectively.