Matsumoto S, Iwamoto A, Yoneyama C, Hagiwara A, Takahashi T, Yoshikawa H, Muranishi S
Dept. of Biopharmaceutics, Kyoto College of Pharmacy.
Gan To Kagaku Ryoho. 1991 Feb;18(2):227-31.
A new dosage form (ACR-CH), aclarubicin(ACR) adsorbed on activated carbon particles (CH), was studied for adsorption and desorption onto and from CH. The adsorption isotherm at 37 degrees C in saline and phosphate buffer (pH 7.4-7.5) were shown as M = 175 Co.15 and M = 207 Co.24, respectively (M = ACR amount adsorbed on CH, microgram/mg; C = ACR concentration in a free state, microgram/ml). In both fluids, CH adsorbed more than 100-1,000 times more amount of ACR than ACR in a free state. ACR-CH was lavaged 7 times and the released ACR in a free state was measured. The results showed that ACR-CH desorbed constantly a small amount of ACR, namely, 1.5-8 percent of initial concentration of ACR in a free state in saline, 0.1-10% in phosphate buffer, and 0.5-4.0% in Ringer's solution. Under the same conditions, desorption of ACR-CH was measured in dog's blood plasma. The first lavage made ACR-CH desorb at 25.7 +/- 0.85 percent of ACR initial concentration in a free state, and two times' to 7 times' lavage made 1-3%. Overall, 43.3 +/- 0.99% of ACR were desorbed from the activated carbon. It was concluded that ACR-CH slowly released a constant amount of ACR for a long period.
研究了一种新剂型（ACR-CH），即吸附在活性炭颗粒（CH）上的阿克拉霉素（ACR），考察其在CH上的吸附和解吸情况。在37℃的生理盐水和磷酸盐缓冲液（pH 7.4 - 7.5）中的吸附等温线分别为M = 175C⁰.¹⁵和M = 207C⁰.²⁴（M = CH上吸附的ACR量，微克/毫克；C = 游离状态下ACR的浓度，微克/毫升）。在这两种液体中，CH吸附的ACR量比游离状态下的ACR多100 - 1000倍以上。对ACR-CH进行7次灌洗，并测定释放出的游离状态的ACR。结果表明，ACR-CH持续释放少量ACR，即在生理盐水中为游离状态下ACR初始浓度的1.5 - 8%，在磷酸盐缓冲液中为0.1 - 10%，在林格氏液中为0.5 - 4.0%。在相同条件下，在犬血浆中测定ACR-CH的解吸情况。第一次灌洗使ACR-CH解吸出游离状态下ACR初始浓度的25.7±0.85%，两次至七次灌洗使解吸率为1 - 3%。总体而言，43.3±0.99%的ACR从活性炭上解吸下来。得出的结论是，ACR-CH能在较长时间内缓慢释放恒定剂量的ACR。
