Perkins A C, Wilson C G, Frier M, Vincent R M, Blackshaw P E, Dansereau R J, Juhlin K D, Bekker P J, Spiller R C
Departments of Medical Physics and Therapeutics, Queen's Medical Centre, University Hospital, Nottingham, UK.
Int J Pharm. 1999 Sep 20;186(2):169-75. doi: 10.1016/s0378-5173(99)00172-6.
Risedronate sodium is an orally active antiresorptive agent and a member of the pyridinyl class of bisphosphonates. It has been approved for the treatment of Paget's disease of the bone and is under development as a chronic therapy for the treatment and prevention of osteoporosis. A novel cellulose film-coated tablet formulation was developed to optimize esophageal transit of this bisphosphonate. The aim of the present study was to compare the esophageal transit of the film-coated tablet formulation of risedronate with its original gelatin capsule dose form. A total of 25 elderly, healthy volunteers (mean 66 years), who were dysphagia-free, participated in this randomized cross-over study. On separate occasions, volunteers swallowed radiolabeled placebo formulations with 50 ml water. Dynamic images with participants in a sitting position were recorded for 10 min using a gamma camera. Scintigraphic imaging showed a delay in esophageal transit (greater than 15 s) in 28% of patients in the capsule group but in none of the tablet group (P<0.05). The mean transit times of the capsules and tablets were 23.8 and 3.3 s, respectively. Esophageal transit of film-coated tablets was faster than gelatin capsules, suggesting that film-coated tablets would be the appropriate formulation for all pivotal trials with risedronate and for subsequent commercialization.
利塞膦酸钠是一种口服活性抗吸收剂，属于吡啶基双膦酸盐类。它已被批准用于治疗骨佩吉特病，并且正在开发作为治疗和预防骨质疏松症的慢性疗法。开发了一种新型的纤维素薄膜包衣片剂剂型，以优化这种双膦酸盐在食管中的转运。本研究的目的是比较利塞膦酸薄膜包衣片剂剂型与其原有的明胶胶囊剂型在食管中的转运情况。共有25名无吞咽困难的老年健康志愿者（平均66岁）参与了这项随机交叉研究。在不同的时间，志愿者用50毫升水吞服放射性标记的安慰剂制剂。使用γ相机记录参与者坐姿下的动态图像10分钟。闪烁显像显示，胶囊组28%的患者食管转运延迟（大于15秒），而片剂组无一例出现这种情况（P<0.05）。胶囊和片剂的平均转运时间分别为23.8秒和3.3秒。薄膜包衣片剂在食管中的转运比明胶胶囊快，这表明薄膜包衣片剂将是所有利塞膦酸关键试验及后续商业化的合适剂型。
