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CNS Drugs. 2018 Sep;32(9):875-882. doi: 10.1007/s40263-018-0560-2.
A new sublingual buprenorphine/naloxone tablet (hereafter referred to as buprenorphine/naloxone; Zubsolv), combining a long-acting partial µ receptor agonist and an opioid antagonist, is approved for the treatment of opioid dependence in adults and adolescents aged > 15 years. This formulation has a higher bioavailability, better taste and faster sublingual dissolve time than a reference sublingual buprenorphine/naloxone tablet (Suboxone), advantages that provide greater patient preference (potentially improving adherence) and importantly may reduce the risk of buprenorphine parenteral abuse by providing similar buprenorphine exposure at an ≈ 30% lower dosage than reference buprenorphine/naloxone. In large phase III trials of up to 28 days, buprenorphine/naloxone was associated with high treatment retention rates during the induction and stabilization phases, and also reduced opioid craving and opioid withdrawal symptoms. Although noninferiority of buprenorphine/naloxone to sublingual buprenorphine tablet during the 2-day induction phase was only shown in one of the two similarly designed trials, pooled analyses confirmed that treatment retention rates were similar in the buprenorphine/naloxone and buprenorphine groups. Where evaluated, noninferiority of buprenorphine/naloxone to sublingual buprenorphine/naloxone film (only approved in the USA) was also demonstrated at 15 days in the stabilization phase. During the 24-week extension study, buprenorphine/naloxone maintenance therapy sustained improvements in opioid craving and addiction severity scores. Buprenorphine/naloxone was generally well tolerated, displaying a tolerability profile that was generally consistent with that seen with reference buprenorphine/naloxone. In conclusion, with potentially greater patient preference and a lower potential for parenteral buprenorphine abuse than reference buprenorphine/naloxone, buprenorphine/naloxone expands the treatment options available for adults and adolescent (aged > 15 years) patients with opioid dependence.
一种新的舌下含服丁丙诺啡/纳洛酮片（以下简称丁丙诺啡/纳洛酮；Zubsolv），结合了一种长效部分μ受体激动剂和一种阿片类拮抗剂，已被批准用于治疗成人和 15 岁以上青少年的阿片类药物依赖。与参比舌下含服丁丙诺啡/纳洛酮片（Suboxone）相比，该制剂具有更高的生物利用度、更好的口感和更快的舌下溶解时间，这为患者提供了更大的偏好（可能提高了依从性），并且重要的是，通过提供与参比丁丙诺啡/纳洛酮相似的丁丙诺啡暴露量，但剂量约低 30%，从而降低了丁丙诺啡的注射滥用风险。在长达 28 天的大型 III 期试验中，丁丙诺啡/纳洛酮在诱导和稳定阶段的治疗保留率较高，并且还减少了阿片类药物渴求感和阿片类药物戒断症状。尽管在为期 2 天的诱导阶段，只有两项设计相似的试验之一显示丁丙诺啡/纳洛酮与舌下含服丁丙诺啡片非劣效，但汇总分析证实，丁丙诺啡/纳洛酮组和丁丙诺啡组的治疗保留率相似。在评估的情况下，在稳定阶段的第 15 天，丁丙诺啡/纳洛酮也显示出与舌下含服丁丙诺啡/纳洛酮膜（仅在美国获准使用）非劣效。在 24 周的扩展研究中，丁丙诺啡/纳洛酮维持治疗维持了阿片类药物渴求感和成瘾严重程度评分的改善。丁丙诺啡/纳洛酮通常具有良好的耐受性，其耐受性与参比丁丙诺啡/纳洛酮的耐受性一致。总之，与参比丁丙诺啡/纳洛酮相比，丁丙诺啡/纳洛酮具有潜在更大的患者偏好和较低的丁丙诺啡注射滥用潜力，为阿片类药物依赖的成人和青少年（15 岁以上）患者提供了更多的治疗选择。
