A new, specific, rapid and stability indicating reversed phase liquid chro-matographic (RP-LC) method for the determination of process related and degradation related impurities of Apremilast has been developed and va...A new, specific, rapid and stability indicating reversed phase liquid chro-matographic (RP-LC) method for the determination of process related and degradation related impurities of Apremilast has been developed and validated. The degradation study performed in acid, base, oxidative, photolytic, and thermal stressed conditions. Eight process related impurities (Imp-1 to Imp-8) in test sample of Apremilast have been detected by developed RP-LC method. The good chromatographic resolution between the peaks of process related impurities, degradation impurities and Apremilast has been achieved on a Synergi Max-RP 80 A (150 × 4.6 mm ID), 4 μ column. The process and degradation related impurities were characterized by mass spectrometry, 1H NMR and FT-IR spectral data. The method was validated as per ICH guideline and found to be specific, rapid, and stability indicating. The proposed RP-PLC method was successfully applied to the analysis of drug substance samples of Apremilast.展开更多
Two selective phosphodiesterase-4 (PDE4) inhibitors—viz., crisaborole (Eucrisa®, Pfizer) and apremilast (Otezla®, Celgene)—have recently received approval by the United States Food and Drug Administr...Two selective phosphodiesterase-4 (PDE4) inhibitors—viz., crisaborole (Eucrisa®, Pfizer) and apremilast (Otezla®, Celgene)—have recently received approval by the United States Food and Drug Administration for the treatment of related but different dermatologic skin conditions (viz., atopic dermatitis and plaque psoriasis, respectively). The purpose of this review is to summarize the underlying biochemistry and pathophysiology associated with these dermatologic conditions, review the chemistry, pharmacology and safety of each of these products, and present preclinical and clinical evidence that may help explain why these two PDE4 inhibitors offer new treatment options for these skin conditions.展开更多
目的:探讨阿普米司特的临床研究现状、热点以及发展趋势。方法:以Web of Science核心合集为检索源进行文献提取,运用CiteSpace软件对发文作者、发文机构、国家/地区、关键词等进行可视化分析。结果:本研究共纳入文献537篇。发文量最多...目的:探讨阿普米司特的临床研究现状、热点以及发展趋势。方法:以Web of Science核心合集为检索源进行文献提取,运用CiteSpace软件对发文作者、发文机构、国家/地区、关键词等进行可视化分析。结果:本研究共纳入文献537篇。发文量最多的作者、机构、国家分别是Paris Maria(18篇)、美国Bristol-Myers Squibb公司(80篇)、美国(253篇);作者、机构以及国家间合作紧密。通过关键词分析发现,适应证内/外用药的疗效和安全性、对比用药、联合用药、药效学和药动学是阿普米司特临床研究的热点。结论:阿普米司特的临床研究引起了国内外学者的广泛关注,特别是针对适应证外用药的探究,涉及的疾病种类已超过15个,阿普米司特未来临床用药方向具有较大的挖掘价值且安全性良好,具有极高的临床研究意义。目前,适应证外用药仍处于探索阶段,亟待国内外研究者开展更多的研究。展开更多
文摘A new, specific, rapid and stability indicating reversed phase liquid chro-matographic (RP-LC) method for the determination of process related and degradation related impurities of Apremilast has been developed and validated. The degradation study performed in acid, base, oxidative, photolytic, and thermal stressed conditions. Eight process related impurities (Imp-1 to Imp-8) in test sample of Apremilast have been detected by developed RP-LC method. The good chromatographic resolution between the peaks of process related impurities, degradation impurities and Apremilast has been achieved on a Synergi Max-RP 80 A (150 × 4.6 mm ID), 4 μ column. The process and degradation related impurities were characterized by mass spectrometry, 1H NMR and FT-IR spectral data. The method was validated as per ICH guideline and found to be specific, rapid, and stability indicating. The proposed RP-PLC method was successfully applied to the analysis of drug substance samples of Apremilast.
文摘Two selective phosphodiesterase-4 (PDE4) inhibitors—viz., crisaborole (Eucrisa®, Pfizer) and apremilast (Otezla®, Celgene)—have recently received approval by the United States Food and Drug Administration for the treatment of related but different dermatologic skin conditions (viz., atopic dermatitis and plaque psoriasis, respectively). The purpose of this review is to summarize the underlying biochemistry and pathophysiology associated with these dermatologic conditions, review the chemistry, pharmacology and safety of each of these products, and present preclinical and clinical evidence that may help explain why these two PDE4 inhibitors offer new treatment options for these skin conditions.
文摘目的:探讨阿普米司特的临床研究现状、热点以及发展趋势。方法:以Web of Science核心合集为检索源进行文献提取,运用CiteSpace软件对发文作者、发文机构、国家/地区、关键词等进行可视化分析。结果:本研究共纳入文献537篇。发文量最多的作者、机构、国家分别是Paris Maria(18篇)、美国Bristol-Myers Squibb公司(80篇)、美国(253篇);作者、机构以及国家间合作紧密。通过关键词分析发现,适应证内/外用药的疗效和安全性、对比用药、联合用药、药效学和药动学是阿普米司特临床研究的热点。结论:阿普米司特的临床研究引起了国内外学者的广泛关注,特别是针对适应证外用药的探究,涉及的疾病种类已超过15个,阿普米司特未来临床用药方向具有较大的挖掘价值且安全性良好,具有极高的临床研究意义。目前,适应证外用药仍处于探索阶段,亟待国内外研究者开展更多的研究。
