Grass P, Marbach P, Bruns C, Lancranjan I
Sandoz Pharma Ltd, Basel, Switzerland.
Metabolism. 1996 Aug;45(8 Suppl 1):27-30. doi: 10.1016/s0026-0495(96)90075-x.
Double-blind, single-dose studies of 120 acromegalic patients given 10, 20, and 30 mg Sandostatin LAR (Sandoz Pharma Ltd, Basel, Switzerland) established the drug's pharmacokinetic profile. Patients then entered open-labeled extension phases, with Sandostatin LAR intramuscular (IM) injections every 4 weeks. These produced broadly constant octreotide concentrations with dose proportionality. Area fluctuations were minimal. Steady-state conditions were generally reached after the second to third injection. There was no evidence of downregulation with Sandostatin LAR over 1 year of study. Based on the pharmacokinetic/pharmacodynamic relationship of octreotide, a starting dose of 20 mg Sandostatin LAR and administrations every 4 weeks provide growth hormone (GH) control comparable to the thrice-daily subcutaneous (SC) injection regimen, which is commonly 0.3 to 0.6 mg/d. The reduction from the burden of two to three SC injections per day is a particular advantage of Sandostatin LAR, which is an attractive alternative to the approved Sandostatin injection.
对120例肢端肥大症患者进行的双盲、单剂量研究，给予10毫克、20毫克和30毫克善龙（瑞士巴塞尔山德士制药有限公司），确定了该药的药代动力学特征。然后患者进入开放标签的延长期，每4周进行一次善龙肌肉注射。这些注射产生了大致恒定的奥曲肽浓度，且与剂量成比例。血药浓度波动极小。一般在第二次至第三次注射后达到稳态。在长达1年的研究中，没有证据表明善龙会导致药物下调。基于奥曲肽的药代动力学/药效学关系，20毫克善龙的起始剂量及每4周给药一次可实现与每日三次皮下注射方案相当的生长激素控制效果，后者通常为每日0.3至0.6毫克。减少每日两至三次皮下注射的负担是善龙的一个特别优势，它是已获批的善宁注射剂的一个有吸引力的替代方案。
