Cheng H, Sutton S C, Pipkin J D, Zentner G M, Rogers J D, Schwartz J I, Mitchel Y B, Grasing K, Schwartz M S, Amin R D
Merck Research Laboratories, West Point, Pennsylvania 19468.
Pharm Res. 1993 Nov;10(11):1683-7. doi: 10.1023/a:1018997308946.
Seven sustained/controlled-release dosage forms were designed for gastrointestinal delivery of lovastatin or simvastatin, two potent HMG-CoA reductase inhibitors for the treatment of hypercholesterolemia. The in vivo performance of these formulations was evaluated in dogs and healthy volunteers in terms of the cholesterol lowering efficacy and/or systemic concentrations of HMG-CoA reductase inhibitors. Results from the present and previous studies suggest that, through the controlled release of HMG-CoA reductase inhibitors, sustained lower plasma concentrations of HMG-CoA reductase inhibitors may result in an equal or better therapeutic efficacy.
设计了七种用于洛伐他汀或辛伐他汀胃肠道给药的缓释/控释剂型，洛伐他汀和辛伐他汀是两种用于治疗高胆固醇血症的强效HMG-CoA还原酶抑制剂。根据HMG-CoA还原酶抑制剂的降胆固醇疗效和/或全身浓度，在犬和健康志愿者中评估了这些制剂的体内性能。当前研究和既往研究的结果表明，通过HMG-CoA还原酶抑制剂的控释，持续较低的HMG-CoA还原酶抑制剂血浆浓度可能产生同等或更好的治疗效果。
