AAPS Open最新文献_第2页

Utility of in vitro release testing (IVRT) to assess ‘sameness’ of 1% clotrimazole creams for use as a biowaiver 利用体外释放试验(IVRT)评估1%克霉唑乳膏作为生物缓释剂的“一致性”

AAPS Open Pub Date : 2023-11-01 DOI: 10.1186/s41120-023-00087-4

Hannah Wellington, Seeprarani Rath, Sagaran Abboo, Isadore Kanfer

{"title":"Utility of in vitro release testing (IVRT) to assess ‘sameness’ of 1% clotrimazole creams for use as a biowaiver","authors":"Hannah Wellington, Seeprarani Rath, Sagaran Abboo, Isadore Kanfer","doi":"10.1186/s41120-023-00087-4","DOIUrl":"https://doi.org/10.1186/s41120-023-00087-4","url":null,"abstract":"Abstract The October 2022 draft United States Food and Drug Administration (FDA) guidance presents an option of in vitro release test (IVRT) studies as a biowaiver for topical drug products submitted in abbreviated new drug applications (ANDAs). However, the product-specific guidance (PSG) for 1% clotrimazole (CLZ) topical cream does not provide an in vitro option for biowaiver and requires a clinical endpoint study to demonstrate bioequivalence (BE). Therefore, the main objective was to use IVRT to investigate pharmaceutical equivalence of several 1% CLZ topical creams from two countries — South Africa (SA) and Canada. This investigation aims at demonstrating the utility of IVRT to determine ‘sameness’ and/or differences between topical creams containing 1% CLZ and the potential of IVRT for supporting biowaivers, thereby obviating the necessity to conduct clinical endpoint studies in patients. A validated IVRT method was applied to conduct comparative IVRT runs on five generic products marketed in SA and one Canadian generic, which were compared against a relevant comparator product from their country of origin in accordance with the FDA’s acceptance criteria of 75–133.33%. All five SA-marketed generic creams showed pharmaceutical inequivalence to the SA comparator product indicating Q1/Q2/Q3 differences. Despite containing the same excipients as both comparator products, the Canadian generic showed substantially lower release rate compared to the comparator products which could be attributed to Q2/Q3 differences. The IVRT method displayed the requisite ability to assess the various 1% CLZ creams and confirmed the potential of the IVRT method to support a biowaiver for 1% CLZ topical creams. Graphical Abstract","PeriodicalId":453,"journal":{"name":"AAPS Open","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135215857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Self-microemulsifying system of an ethanolic extract of Heliopsis longipes root for enhanced solubility and release of affinin 向日葵根乙醇提取物的自微乳化体系，以提高其溶解度和释放亲和蛋白

AAPS Open Pub Date : 2023-10-16 DOI: 10.1186/s41120-023-00086-5

Dailenys Marrero-Morfa, César Ibarra-Alvarado, Francisco J. Luna-Vázquez, Miriam Estévez, Eremy Miranda Ledesma, Alejandra Rojas-Molina, Carlos T. Quirino-Barreda

{"title":"Self-microemulsifying system of an ethanolic extract of Heliopsis longipes root for enhanced solubility and release of affinin","authors":"Dailenys Marrero-Morfa, César Ibarra-Alvarado, Francisco J. Luna-Vázquez, Miriam Estévez, Eremy Miranda Ledesma, Alejandra Rojas-Molina, Carlos T. Quirino-Barreda","doi":"10.1186/s41120-023-00086-5","DOIUrl":"https://doi.org/10.1186/s41120-023-00086-5","url":null,"abstract":"Abstract Self-microemulsifying or self-nanoemulsifying drug delivery systems (SMEDDS/SNEDDS) are well known to improve the dissolution and increase the oral bioavailability of hydrophobic drugs, including herbal extracts. Organic extracts of Heliopsis longipes root and affinin, its main component, induce a vasodilator effect; however, they are poorly water soluble and therefore are difficult to administer and dose by the oral route. This research aimed to develop, through pseudo-ternary phase diagrams, a self-microemulsifying system prepared from an ethanolic extract of H. longipes root (HL-SMDS). In addition, the optimized lipid-based formulation was characterized and its in vitro gastrointestinal simulated dissolution was determined. The formulation composed of Transcutol, 55% (solubilizer); Tween80/PG, 10% (surfactant/co-solvent); Labrasol, 35% (surfactant); and the herbal extract was selected as optimal and identified as a SMEDDS, since when coming into contact with water, it forms a micro-emulsion with droplet sizes less than 100 nm. The stability tests showed that HL-SMDS remained stable over time under extreme conditions. Furthermore, the amount of affinin released from HL-SMDS at pH 1 and 6.8 was higher than that of the ethanolic extract from H. longipes root. These results indicate that HL-SMDS is a novel alternative to improve the aqueous solubility and therefore the oral bioavailability of the ethanolic extract of H. longipes root.","PeriodicalId":453,"journal":{"name":"AAPS Open","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136077599","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Preparation, characterization, and biological activity of the inclusion complex of dihydroquercetin and β-Cyclodextrin 二氢槲皮素- β-环糊精包合物的制备、表征及生物活性研究

AAPS Open Pub Date : 2023-10-03 DOI: 10.1186/s41120-023-00083-8

Yaping Xu, Yue Wang, Chujie Li, Tao Han, Haiming Chen, Wenxue Chen, Qiuping Zhong, Jianfei Pei, Guido R. M. M. Haenen, Zhengwen Li, Mohamed Moalin, Ming Zhang, Weijun Chen

{"title":"Preparation, characterization, and biological activity of the inclusion complex of dihydroquercetin and β-Cyclodextrin","authors":"Yaping Xu, Yue Wang, Chujie Li, Tao Han, Haiming Chen, Wenxue Chen, Qiuping Zhong, Jianfei Pei, Guido R. M. M. Haenen, Zhengwen Li, Mohamed Moalin, Ming Zhang, Weijun Chen","doi":"10.1186/s41120-023-00083-8","DOIUrl":"https://doi.org/10.1186/s41120-023-00083-8","url":null,"abstract":"Abstract Dihydroquercetin (DHQ) is a natural occurring dihydroflavonol that has strong antioxidant and antibacterial activities. However, its application is limited due to its poor solubility. This study aims to improve the aqueous solubility of DHQ by complexing DHQ with β-cyclodextrin (β-CD) to boost its biological activity. DHQ was encapsulated with β-CD by freeze drying at a 1:1-M ratio. The structure of DHQ/β-CD complex prepared was elucidated by using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, and 1 H nuclear magnetic resonance ( 1 H NMR). In addition, molecular docking further revealed two energetically favorable conformations of the DHQ/β-CD complex, in which DHQ interacted with β-CD via hydrogen bonds. Experimental results showed that the solubility of the DHQ increased 22.63-fold by encapsulating with β-CD. Also the dissolution rate, antioxidant activity and antibacterial activity of the DHQ were significantly improved by encapsulating. The encapsulating with β-CD solves the problem of the poor aqueous solubility of DHQ, and broadens the path for a more optimal use of the health promoting effect of DHQ in pharmaceutical and food products.","PeriodicalId":453,"journal":{"name":"AAPS Open","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135688721","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Bioequivalence clinical trial simulation: a case study of apalutamide administered in applesauce versus whole tablets 生物等效性临床试验模拟:阿帕鲁胺应用于苹果酱和整片的案例研究

AAPS Open Pub Date : 2023-08-07 DOI: 10.1186/s41120-023-00082-9

A. Yu, O. Ackaert

引用次数: 0

Compatibility study of patiromer with juices/liquids and soft foods 与果汁/液体及软质食物的相容性研究

AAPS Open Pub Date : 2023-08-01 DOI: 10.1186/s41120-023-00081-w

Martin Khoeiklang, Maria Wilhelm, Lingyun Li, Carol P. Moreno Quinn

引用次数: 0

A review on lipid-based nanocarriers mimicking chylomicron and their potential in drug delivery and targeting infectious and cancerous diseases 基于脂质的乳糜微粒纳米载体及其在药物传递和靶向感染性和癌变疾病中的潜力综述

AAPS Open Pub Date : 2023-07-03 DOI: 10.1186/s41120-023-00080-x

Rana E. Elnady, M. Amin, Mohamed Y. Zakaria