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更新于：2025-02-01
Antipyrine
安替比林
更新于：2025-02-01
概要
基本信息
结构/序列
分子式C11H12N2O |
InChIKeyVEQOALNAAJBPNY-UHFFFAOYSA-N |
CAS号60-80-0 |
关联
1
项与 安替比林 相关的临床试验NCT02037893
A Four-arm, Randomized, Double-blind, Active and Placebo Controlled Study to Determine the Safety and Efficacy of a Combination Antipyrine and Benzocaine Otic Solution Compared With Antipyrine Otic Solution Alone, Benzocaine Otic Solution Alone and to Placebo Otic Solution to Relieve Pain Symptoms in Children With Acute Otitis Media.
100 项与 安替比林 相关的临床结果
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100 项与 安替比林 相关的转化医学
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100 项与 安替比林 相关的专利（医药）
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7,811
项与 安替比林 相关的文献（医药）2025-02-01EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
In vivo systemic evaluation of nasal drug absorption from powder formulations in rats
Article
作者: Ogawara, Ken-Ichi ; Higaki, Kazutaka ; Tatsuta, Ryosuke ; Sakane, Toshiyasu ; Tanaka, Akiko ; Furubayashi, Tomoyuki
Despite the potential benefits of nasal drug delivery, there is a need for a systematic evaluation of the efficacy of powder formulations adhering to the nasal mucosa. This study aims to establish a systematic evaluation method for nasal drug absorption from powder formulations. We selected three model compounds-antipyrine, griseofulvin, and acyclovir-and analyzed their pharmacokinetics following nasal administration of powder formulations under physiological conditions. Our experimental design incorporated assessments of the drug absorption patterns. Antipyrine demonstrated rapid absorption exclusively from the nasal cavity. In contrast, griseofulvin exhibited absorption from the nasal cavity and the gastrointestinal tract. This phenomenon could be attributed to the rapid nasal clearance of the drug with an initial half-life of 5 min. To further establish the physiological validity of our method, we conducted an experiment to investigate the impact of changing the mucociliary clearance (MC) on nasal absorption that resulted in a 1.2-fold increase in the bioavailability of acyclovir upon prolonged MC. Our findings support the utility of established methods in evaluating nasal absorption and their behavior in the nasal cavity. This study holds a promising advancement toward effective drug delivery via nasal administration, potentially leading to targeted delivery and improved therapeutic outcomes.
2025-01-06MOLECULAR PHARMACEUTICS
FormulationBCS: A Machine Learning Platform Based on Diverse Molecular Representations for Biopharmaceutical Classification System (BCS) Class Prediction
Article
作者: Ouyang, Defang ; Ye, Zhuyifan ; Chan, Ging ; Wang, Nannan ; Wu, Zheng ; Xu, Huanle
The Biopharmaceutics Classification System (BCS) has facilitated biowaivers and played a significant role in enhancing drug regulation and development efficiency. However, the productivity of measuring the key discriminative properties of BCS, solubility and permeability, still requires improvement, limiting high-throughput applications of BCS, which is essential for evaluating drug candidate developability and guiding formulation decisions in the early stages of drug development. In recent years, advancements in machine learning (ML) and molecular characterization have revealed the potential of quantitative structure-performance relationships (QSPR) for rapid and accurate in silico BCS classification. The present study aims to develop a web platform for high-throughput BCS classification based on high-performance ML models. Initially, four data sets of BCS-related molecular properties: log S, log P, log D, and log Papp were curated. Subsequently, 6 ML algorithms or deep learning frameworks were employed to construct models, with diverse molecular representations ranging from one-dimensional molecular fingerprints, descriptors, and molecular graphs to three-dimensional molecular spatial coordinates. By comparing different combinations of molecular representations and learning algorithms, LightGBM exhibited excellent performance in solubility prediction, with an R2 of 0.84; AttentiveFP outperformed others in permeability prediction, with R2 values of 0.96 and 0.76 for log P and log D, respectively; and XGBoost was the most accurate for log Papp prediction, with an R2 of 0.71. When externally validated on a marketed drug BCS category data set, the best-performing models achieved classification accuracies of over 77 and 73% for solubility and permeability, respectively. Finally, the well-trained models were embedded into the first ML-based BCS class prediction web platform (x f), enabling pharmaceutical scientists to quickly determine the BCS category of candidate drugs, which will aid in the high-throughput BCS assessment for candidate drugs during the preformulation stage, thereby promoting reduced risk and enhanced efficiency in drug development and regulation.
2025-01-01WATER RESEARCH
Assessment of trace organic chemicals in anaerobically digested sludge and their partitioning behaviour: Simultaneous Soxhlet chemical extraction and quantification via LC-MS/MS analysis
Article
作者: Cesaro, Alessandra ; Koch, Konrad ; Esposito, Giovanni ; Ciotola, Enrica ; Sottorff, Ignacio
The increasing number of trace organic contaminants (TrOCs) detected in anaerobically digested sludge (ADS) is triggering increasing concern on its circular-economy reuse practices. A large scientific effort has been performed to define their concentration limits, partition behaviour, and innovative technologies for their removal, which require the definition of versatile and economically sustainable analytical methodologies. In this study, a Soxhlet extraction method coupled with LC-MS/MS analysis was developed to simultaneously determine 32 TrOCs in ADS, 11 of them being quantified in this matrix for the first time. The targeted TrOCs were selected based on the European Urban Wastewater Treatment Directive, and on their frequency of detection in municipal wastewater and/or sludge and chemical diversity. The use of methanol as solvent allowed good recovery efficiencies from ADS solid phase, with an extraction time of 3.5 h and without the need for subsequent clean-up procedures. The targeted LC-MS/MS method enabled high-sensitivity quantification of TrOCs in the liquid phase. At least 25 out of the 32 target compounds were detected in ADS samples from two wastewater treatment plants in Germany, providing their concentration data and highlighting the influence of TrOCs characteristics and sludge properties on contaminant partition coefficients (KD). The experimental outcomes highlight the versatility of the Soxhlet method, which is effective in extracting compounds characterized by diverse properties and structures, and opens new perspectives for the analysis of various substrates. This could support the European Sewage Sludge Directive, expanding its application to soils and cultivated foods and offering insights into TrOCs transfer among different substrates and their influence when used as fertilizer, aiding in the efficient definition of risk assessment methodologies and regulatory concentration limits.
2
项与 安替比林 相关的新闻（医药）2023-03-20
并购带量采购抗体药物偶联物
100 项与 安替比林 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 中耳炎 | - | - | - |
| 疼痛 | - | - | - |
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临床结果
临床结果
适应症
分期
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临床2期 | 112 | (Antipyrine and Benzocaine Otic Solution) | 膚廠鹽窪淵觸鑰獵願築(齋艱齋糧夢襯醖獵窪選) = 壓鏇願糧廠鬱築鏇膚鹹 範繭簾衊廠積鹹憲壓艱 (餘壓簾遞夢網繭鬱壓餘, 襯選鑰選廠遞簾窪糧鑰 ~ 製構簾蓋觸艱鹹淵遞膚) 更多 | - | 2018-08-31 | ||
Placebo Otic solution+Antipyrine Otic Solution (Antipyrine Otic Solution) | 膚廠鹽窪淵觸鑰獵願築(齋艱齋糧夢襯醖獵窪選) = 簾觸顧繭積淵夢醖觸觸 範繭簾衊廠積鹹憲壓艱 (餘壓簾遞夢網繭鬱壓餘, 願願夢鹹築衊廠膚夢築 ~ 願顧夢餘糧襯壓簾鹹壓) 更多 |
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