J Drugs Dermatol. 2021 May 1;20(5):s5-s11. doi: 10.36849/JDD.s072A.
Since its approval in 1982, oral isotretinoin has revolutionized acne therapy. However, oral isotretinoin use has long been associated with challenges of variable bioavailability and food dependence. It is recommended to ingest oral isotretinoin with a high-fat meal in order to maximize absorption, but many patients fail to adhere to this recommendation. This may lead to inadequate isotretinoin absorption levels. Patients who fail to achieve isotretinoin target cumulative dose are more likely to experience symptom relapse. To address the challenge of traditional isotretinoin variable bioavailability, subsequent isotretinoin formulations have attempted to improve its absorption abilities. In 2014, an isotretinoin formulation utilizing Lidose technology, known as Absorica, showed significant improvements in absorption levels compared to traditional oral isotretinoin in the fasted state. In 2019, isotretinoin absorption levels were further advanced in a new formulation approved by the FDA known as Absorica LD. Utilizing advanced micronization technology that physically reduces the size of the drug molecule, Absorica LD exhibits twice the absorption levels of Absorica under fasting conditions. In the fed state, Absorica LD achieves similar plasma levels to Absorica with a 20 percent lower dose. Absorica LD also produces consistent serum isotretinoin levels irrespective of gastrointestinal contents. By eliminating the “food effect” seen in traditional oral isotretinoin, Absorica LD has the potential to improve patient adherence and long-term patient outcomes. J Drugs Dermatol. 20:5(Suppl):s5-11.
自 1982 年获得批准以来,口服异维 A 酸彻底改变了痤疮的治疗方法。然而,口服异维 A 酸的使用长期以来一直存在生物利用度变化和食物依赖性的挑战。建议随高脂肪餐服用口服异维 A 酸,以最大限度地吸收,但许多患者未能遵守这一建议。这可能导致异维 A 酸吸收水平不足。未能达到异维 A 酸目标累积剂量的患者更有可能出现症状复发。为了解决传统异维 A 酸生物利用度变化的挑战,随后的异维 A 酸制剂试图提高其吸收能力。2014 年,一种利用 Lidose 技术的异维 A 酸制剂,名为 Absorica,与空腹状态下的传统口服异维 A 酸相比,吸收水平显著提高。2019 年,一种新的 FDA 批准的异维 A 酸制剂 Absorica LD 在吸收水平上进一步得到了提高。该制剂利用先进的微粉化技术,使药物分子的大小物理减小,在空腹状态下,Absorica LD 的吸收水平是 Absorica 的两倍。在进食状态下,Absorica LD 以低 20%的剂量达到与 Absorica 相似的血浆水平。Absorica LD 还能产生一致的血清异维 A 酸水平,与胃肠道内容物无关。通过消除传统口服异维 A 酸中出现的“食物效应”,Absorica LD 有可能提高患者的依从性和长期患者结局。J 皮肤病药物杂志。20:5(增刊):s5-11。