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New Formulations of Isotretinoin for Acne Treatment: Expanded Options and Clinical Implications.用于痤疮治疗的异维A酸新制剂:拓展的选择及临床意义
J Clin Aesthet Dermatol. 2021 Dec;14(12 Suppl 1):S18-S23.
2
Rationale for Use of Micronized Isotretinoin for Treatment of Acne Vulgaris: Practical Considerations and Therapeutic Advantages.使用微粉化异维A酸治疗寻常痤疮的理论依据:实际考量与治疗优势
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Enhancing Bioavailability: Advances in Oral Isotretinoin Formulations.提高生物利用度:口服异维 A 酸制剂的进展。
Skin Therapy Lett. 2024 Sep;29(5):10-12.
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Comparative pharmacokinetic profiles of a novel isotretinoin formulation (isotretinoin-Lidose) and the innovator isotretinoin formulation: a randomized, 4-treatment, crossover study.一种新型异维 A 酸制剂(异维 A 酸-利朵司)与原研异维 A 酸制剂的比较药代动力学特征:一项随机、4 治疗、交叉研究。
J Am Acad Dermatol. 2013 Nov;69(5):762-767. doi: 10.1016/j.jaad.2013.05.036. Epub 2013 Aug 13.
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Consensus Statements on the Use of Novel Formulations of Isotretinoin: A Modified Delphi Process.共识声明:新型异维 A 酸制剂的使用:改良 Delphi 法。
J Drugs Dermatol. 2024 Jun 1;23(6):429-432. doi: 10.36849/JDD.7971.
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Results of a Phase III, double-blind, randomized, parallel-group, non-inferiority study evaluating the safety and efficacy of isotretinoin-Lidose in patients with severe recalcitrant nodular acne.一项评估异维A酸-利多塞对重度顽固性结节性痤疮患者安全性和有效性的III期双盲随机平行组非劣效性研究结果。
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An Open-label, Phase IV Study Evaluating Lidose-isotretinoin Administered without Food in Patients with Severe Recalcitrant Nodular Acne: Low Relapse Rates Observed Over the 104-week Post-treatment Period.一项开放标签的IV期研究,评估重度顽固性结节性痤疮患者空腹服用异维A酸胶丸的疗效:治疗后104周观察到低复发率
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Comparative Pharmacokinetic Profiles of a Novel Low-dose Micronized-isotretinoin 32 mg Formulation and Lidose-isotretinoin 40 mg in Fed and Fasted Conditions: Two Open-label, Randomized, Crossover Studies in Healthy Adult Participants.新型低剂量微粉化异维 A 酸 32 毫克制剂和利朵斯异维 A 酸 40 毫克在进食和禁食条件下的药代动力学比较:两项在健康成年参与者中进行的开放标签、随机、交叉研究。
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A randomized trial of the efficacy of a new micronized formulation versus a standard formulation of isotretinoin in patients with severe recalcitrant nodular acne.一项关于新的微粉化制剂与异维甲酸标准制剂治疗重度顽固性结节性痤疮疗效的随机试验。
J Am Acad Dermatol. 2001 Aug;45(2):187-95. doi: 10.1067/mjd.2001.115965.
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Safety of a new micronized formulation of isotretinoin in patients with severe recalcitrant nodular acne: A randomized trial comparing micronized isotretinoin with standard isotretinoin.异维A酸新微粉化制剂用于重度顽固性结节性痤疮患者的安全性:一项比较微粉化异维A酸与标准异维A酸的随机试验
J Am Acad Dermatol. 2001 Aug;45(2):196-207. doi: 10.1067/mjd.2001.115966.

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Virtual and in Vitro Screening Employing a Repurposing Approach Reveal 13-cis-Retinoic Acid is a PTP1B Inhibitor.采用重新利用方法的虚拟和体外筛选表明13-顺式维甲酸是一种蛋白酪氨酸磷酸酶1B(PTP1B)抑制剂。
ChemMedChem. 2024 Dec 2;19(23):e202400452. doi: 10.1002/cmdc.202400452. Epub 2024 Oct 8.
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Acne among Patients Visiting Outpatient Department of Dermatology Centres.皮肤科中心门诊患者的痤疮问题。
JNMA J Nepal Med Assoc. 2023 Oct 1;61(266):811-813. doi: 10.31729/jnma.8312.
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Oral Isotretinoin and Its Uses in Dermatology: A Review.口服异维 A 酸及其在皮肤科的应用:综述。
Drug Des Devel Ther. 2023 Aug 25;17:2573-2591. doi: 10.2147/DDDT.S427530. eCollection 2023.

本文引用的文献

1
Lidose-Isotretinoin Administered Without Food Improves Quality of Life in Patients With Severe Recalcitrant Nodular Acne: An Open-Label, Single-Arm, Phase IV Study.空腹服用利度胺-异维A酸可改善重度顽固性结节性痤疮患者的生活质量:一项开放标签、单臂、IV期研究。
J Clin Aesthet Dermatol. 2020 Sep;13(9):15-20. Epub 2020 Sep 1.
2
Association Between Adult Acne and Dietary Behaviors: Findings From the NutriNet-Santé Prospective Cohort Study.成人痤疮与饮食行为的关联:NutriNet-Santé 前瞻性队列研究的结果。
JAMA Dermatol. 2020 Aug 1;156(8):854-862. doi: 10.1001/jamadermatol.2020.1602.
3
An Open-label, Phase IV Study Evaluating Lidose-isotretinoin Administered without Food in Patients with Severe Recalcitrant Nodular Acne: Low Relapse Rates Observed Over the 104-week Post-treatment Period.一项开放标签的IV期研究,评估重度顽固性结节性痤疮患者空腹服用异维A酸胶丸的疗效:治疗后104周观察到低复发率
J Clin Aesthet Dermatol. 2019 Nov;12(11):13-18. Epub 2019 Nov 1.
4
Challenges and Solutions in Oral Isotretinoin in Acne: Reflections on 35 Years of Experience.口服异维A酸治疗痤疮的挑战与解决方案:35年经验反思
Clin Cosmet Investig Dermatol. 2019 Dec 30;12:943-951. doi: 10.2147/CCID.S234231. eCollection 2019.
5
Comparative Pharmacokinetic Profiles of a Novel Low-dose Micronized-isotretinoin 32 mg Formulation and Lidose-isotretinoin 40 mg in Fed and Fasted Conditions: Two Open-label, Randomized, Crossover Studies in Healthy Adult Participants.新型低剂量微粉化异维 A 酸 32 毫克制剂和利朵斯异维 A 酸 40 毫克在进食和禁食条件下的药代动力学比较:两项在健康成年参与者中进行的开放标签、随机、交叉研究。
Acta Derm Venereol. 2020 Feb 5;100(4):adv00049. doi: 10.2340/00015555-3381.
6
Acne relapses: impact on quality of life and productivity.痤疮复发:对生活质量和生产力的影响。
J Eur Acad Dermatol Venereol. 2019 May;33(5):937-943. doi: 10.1111/jdv.15419. Epub 2019 Feb 22.
7
Cutibacterium acnes (Propionibacterium acnes) and acne vulgaris: a brief look at the latest updates.痤疮丙酸杆菌(痤疮丙酸杆菌)与寻常痤疮:最新研究进展简述。
J Eur Acad Dermatol Venereol. 2018 Jun;32 Suppl 2:5-14. doi: 10.1111/jdv.15043.
8
Comparing the Efficacy of Low Dose and Conventional Dose of Oral Isotretinoin in Treatment of Moderate and Severe Acne Vulgaris.比较低剂量与常规剂量口服异维A酸治疗中度和重度寻常痤疮的疗效
J Res Pharm Pract. 2017 Oct-Dec;6(4):233-238. doi: 10.4103/jrpp.JRPP_17_30.
9
Adult Acne Versus Adolescent Acne: A Retrospective Study of 1,167 Patients.成人痤疮与青少年痤疮:1167例患者的回顾性研究
J Clin Aesthet Dermatol. 2018 Jan;11(1):21-25. Epub 2018 Jan 1.
10
Psychosocial Impact of Postinflammatory Hyperpigmentation in Patients with Acne Vulgaris.寻常痤疮患者炎症后色素沉着的心理社会影响
J Clin Aesthet Dermatol. 2017 May;10(5):18-23. Epub 2017 May 1.

用于痤疮治疗的异维A酸新制剂:拓展的选择及临床意义

New Formulations of Isotretinoin for Acne Treatment: Expanded Options and Clinical Implications.

作者信息

Bellomo Risha, Brunner Matthew, Tadjally Ella

机构信息

Dr. Bellomo is with Allele Medical, in Orlando, Florida. Dr Brunner is with the Dermatology & Skin Surgery Center P.C., in Stockbridge, Georgia.

出版信息

J Clin Aesthet Dermatol. 2021 Dec;14(12 Suppl 1):S18-S23.

PMID:35291260
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8903225/
Abstract

BACKGROUND

Isotretinoin is a widely used and effective drug in the treatment of severe, recalcitrant, nodular acne. However, its poor aqueous solubility limits oral bioavailability and requires administration with a high-fat, high-calorie meal (HF/HC) for optimal absorption; poor patient adherence may decrease effective dosing and treatment efficacy.

OBJECTIVE

This review covers the properties of the lidose isotretinoin and micronized isotretinoin formulations and their use in acne therapy.

METHOD OF LITERATURE SEARCH

PubMed was searched using the terms , , , , and Additional articles were searched using reference lists from the obtained results.

RESULTS

Our review discusses pathology and approved treatment options for acne; provides mechanism of action of isotretinoin; presents clinical challenges associated with isotretinoin safety; and summarizes implications in clinical practice. Newer formulations show enhanced bioavailability in both fed and fasting states.

LIMITATIONS

Few published studies of real-world use of the identified formulations were available.

CONCLUSION

Newer drug delivery technologies can simplify isotretinoin use while maximizing bioavailability and efficacy. Based on our analysis, lidose isotretinoin and micronized isotretinoin improve oral bioavailability, pharmacological bioactivity, and increase therapeutic efficacy in patients who are unwilling or unable to consistently take the medication with an HF/HC meal. Healthcare providers should consider these formulations as tools to optimize treatment based on each patient's individual needs.

摘要

背景

异维A酸是治疗重度、顽固性结节性痤疮广泛使用且有效的药物。然而,其水溶性差限制了口服生物利用度,需要与高脂、高热量餐食(HF/HC)一起服用以实现最佳吸收;患者依从性差可能会降低有效剂量和治疗效果。

目的

本综述涵盖了利度异维A酸和微粉化异维A酸制剂的特性及其在痤疮治疗中的应用。

文献检索方法

使用术语、、、和在PubMed上进行检索。使用从所得结果的参考文献列表中检索其他文章。

结果

我们的综述讨论了痤疮的病理和已批准的治疗选择;提供了异维A酸的作用机制;介绍了与异维A酸安全性相关的临床挑战;并总结了在临床实践中的意义。新型制剂在进食和禁食状态下均显示出提高的生物利用度。

局限性

关于所鉴定制剂实际应用的已发表研究很少。

结论

更新的药物递送技术可以简化异维A酸的使用,同时最大限度地提高生物利用度和疗效。根据我们的分析,利度异维A酸和微粉化异维A酸可提高口服生物利用度、药理生物活性,并提高不愿或无法始终与HF/HC餐一起服药的患者的治疗效果。医疗保健提供者应将这些制剂视为根据每个患者的个体需求优化治疗的工具。