Flasch H, Asmussen B, Heinz N
Arzneimittelforschung. 1978;28(2):326-30.
The bioavailability of digoxin from 3 silica matrix formulations was assessed in single-dose crossover studies in 12 healthy human volunteers: digoxin/silica matrix tablets (I, Digacin), digoxin/silica matrix in capsule form (II) and digoxin/silica matrix dragées, protected against gastrict juice by film coating (III). Urinary glycoside excretion for 6 days after 0.5 mg doses were measured by radioimmunoasay. Referring to an intravenous injection the bioavailability of digoxin from Digacin tablets is 82%, from the encapsulated matrix 69%, and from the dragées 54%. In comparison with corresponding results from other investigators Digacin tablets havet the same high bioavailability as digoxin solutions. In vitro liberations of digoxin from the silica matrix formulations (94% in 90 s) is significantly better than from conventional tablets produces from a digoxin-lactose trituration (61% in 90 s).
在12名健康人体志愿者中进行的单剂量交叉研究,评估了地高辛从3种二氧化硅基质制剂中的生物利用度:地高辛/二氧化硅基质片(I,狄戈辛)、胶囊形式的地高辛/二氧化硅基质(II)和经薄膜包衣保护免受胃液影响的地高辛/二氧化硅基质糖衣丸(III)。通过放射免疫分析测定0.5毫克剂量后6天的尿苷排泄量。与静脉注射相比,狄戈辛片的地高辛生物利用度为82%,胶囊基质为69%,糖衣丸为54%。与其他研究者的相应结果相比,狄戈辛片与地高辛溶液具有相同的高生物利用度。二氧化硅基质制剂中地高辛的体外释放率(90秒内为94%)明显优于由地高辛-乳糖研磨制成的传统片剂(90秒内为61%)。