Filler Guido, Lathia Anita, LeBlanc Claire, Christians Uwe
Division of Nephrology, Children's Hospital of Eastern Ontario, University of Ottawa, 401 Smyth Road, Ottawa, ON, K1H 8L1, Canada.
Pediatr Nephrol. 2006 Aug;21(8):1206-8. doi: 10.1007/s00467-006-0139-x. Epub 2006 May 24.
Enteric-coated mycophenolate sodium (EC-MPS) has a mean half-life of 11.7 hours, which encouraged hope of using this drug once daily in a nonadherent adolescent SLE patient. This is a case report on a 17-year-old adolescent with a history of noncompliance who was switched from twice-daily mycophenolate mofetil (MMF) to once-daily EC-MPS. The EC-MPS dose was equimolar to the daily MMF dose (1 g MMF BID and 1.44 g of EC-MPS OD). The active compound of both drugs, mycophenolic acid, was measured using a commercially available EMIT assay. Both drugs were well-tolerated and maintained remission of the SLE. The average of three 12-hour areas under the time-concentration curves (AUC) on 1 g of MMF BID was 59.0 mgxh/L. In contrast, the 24-hour AUC after 1.44 g EC-MPS OD was 283.2 mgxh/L, more than double the expected 118.0 mgxh/L of two MMF dosing intervals. A repeat 24-hour AUC after 1.08 g of EC-MPS was 218.2 mgxh/L. EC-MPS once daily may be a well-tolerated therapeutic option for nonadherent adolescent lupus patients, but may be associated with a significantly higher exposure than the equivalent MMF BID dose.
肠溶包衣的吗替麦考酚酯钠（EC-MPS）的平均半衰期为11.7小时，这使得人们有望在不依从的青少年系统性红斑狼疮（SLE）患者中每日使用一次该药物。本文报告了一名17岁有不依从病史的青少年患者，其从每日两次的吗替麦考酚酯（MMF）转换为每日一次的EC-MPS。EC-MPS的剂量与每日MMF剂量等摩尔（1g MMF每日两次和1.44g EC-MPS每日一次）。使用市售的发射免疫分析（EMIT）法测量两种药物的活性成分麦考酚酸。两种药物耐受性良好，维持了SLE的缓解。1g MMF每日两次时，三个12小时时间-浓度曲线下面积（AUC）的平均值为59.0mgxh/L。相比之下，1.44g EC-MPS每日一次后的24小时AUC为283.2mgxh/L，超过了两个MMF给药间隔预期的118.0mgxh/L的两倍多。1.08g EC-MPS后的重复24小时AUC为218.2mgxh/L。对于不依从的青少年狼疮患者，每日一次的EC-MPS可能是一种耐受性良好的治疗选择，但可能与比等效的MMF每日两次剂量显著更高的暴露量相关。
