Frishman W H
Department of Medicine, Albert Einstein College of Medicine/Montefiore Medical Center, Bronx, New York.
J Clin Pharmacol. 1993 Jul;33(7):612-22. doi: 10.1002/j.1552-4604.1993.tb04713.x.
Calcium-channel blockers are a safe and effective treatment modality and have been used extensively in the treatment of angina and hypertension. Dilacor XR capsules, a new extended-release formulation of diltiazem, has been developed for the treatment of hypertension. Dilacor XR (Rhône-Poulenc Rorer Pharmaceuticals Inc., Collegeville, PA) uses a novel drug delivery system, the Geomatrix (JAGO Research AG, Zollikon, Switzerland) controlled-release system, to deliver diltiazem at a constant rate for 24 hours. The rate of absorption is also slower. As doses of Dilacor XR were increased from 120 mg to 540 mg/day, there were disproportionate increases observed in area under the curve, maximum peak plasma concentration, minimum peak plasma concentration, and average peak plasma concentration. The efficacy data from two clinical trials have confirmed the established efficacy of diltiazem and the 24-hour efficacy of Dilacor XR in the control of mild-to-moderate hypertension. The incidence of adverse effects with Dilacor XR in doses as high as 540 mg/day was generally comparable to that of placebo. This new extended-release formulation of diltiazem should significantly facilitate blood pressure control because of better patient compliance with a once daily regimen.
钙通道阻滞剂是一种安全有效的治疗方式，已广泛用于治疗心绞痛和高血压。地尔硫䓬缓释胶囊（Dilacor XR）是一种新型的地尔硫䓬缓释制剂，已被开发用于治疗高血压。Dilacor XR（罗纳普朗克罗瑞尔制药公司，宾夕法尼亚州科利奇维尔）采用了一种新型药物递送系统——Geomatrix（瑞士苏黎世JAGO研究公司）控释系统，以恒定速率持续24小时递送地尔硫䓬。其吸收速率也较慢。随着Dilacor XR的剂量从120毫克/天增加到540毫克/天，曲线下面积、最大血浆峰浓度、最小血浆峰浓度和平均血浆峰浓度均出现不成比例的增加。两项临床试验的疗效数据证实了地尔硫䓬已确立的疗效以及Dilacor XR在控制轻度至中度高血压方面的24小时疗效。高达540毫克/天剂量的Dilacor XR的不良反应发生率通常与安慰剂相当。由于患者对每日一次给药方案的依从性更好，这种新型的地尔硫䓬缓释制剂应能显著促进血压控制。
