Pharmaceutical Development and Technology最新文献_第7页

Formulation development, characterization, and evaluation of bedaquiline fumarate - Soluplus^® - solid dispersion. 富马酸贝达喹啉 -Soluplus® - 固体分散剂的配方开发、表征和评估。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-10 DOI: 10.1080/10837450.2024.2348585

Vishwas P Pardhi, Manisha Patel, Keerti Jain

{"title":"Formulation development, characterization, and evaluation of bedaquiline fumarate - Soluplus® - solid dispersion.","authors":"Vishwas P Pardhi, Manisha Patel, Keerti Jain","doi":"10.1080/10837450.2024.2348585","DOIUrl":"10.1080/10837450.2024.2348585","url":null,"abstract":"Bedaquiline fumarate (BQF) is classified as a BCS class II drug and has poor water solubility and dissolution rate, which ultimately compromises bioavailability. The objective of this study is to improve the biopharmaceutical properties of BQF through a solid dispersion system by using Soluplus®. Two solid dispersion systems were prepared i.e. binary solid dispersion (BSD) and ternary solid dispersion (TSD) where 14.31-fold and 20.43-fold increase in solubility of BQF was observed with BSD and TSD in comparison to BQF. In our previous research work, we explored the BSD and TSD of BQF with a crystalline polymer, poloxamer 188, which showed an increment in the solubility of BQF. In the current research, amorphous Soluplus® polymer was selected to formulate BSD and TSD with BQF and showed higher solubility than poloxamer 188. The various solid and liquid state characterization results confirmed the presence of an amorphous form of BQF inside solid dispersion. The Fourier transform infrared spectroscopy showed no chemical interactions between BQF and polymer. The cellular uptake results demonstrated higher uptake in Caco-2 cell lines. Pharmacokinetic studies showed enhanced solubility and bioavailability of TSDs. Hence, the present research shows a promising formulation strategy for enhancing the biopharmaceutical performance of BQF by increasing its solubility.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"492-503"},"PeriodicalIF":3.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140852735","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of posaconazole nanocrystalline solid dispersion: preparation, characterization and in vivo evaluation. 泊沙康唑纳米晶体固体分散体的开发：制备、表征和体内评价。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-28 DOI: 10.1080/10837450.2024.2353314

Ranga Goud Rayapolu, Balvant Yadav, Shashank S Apte, Venkata Vamsi Krishna Venuganti

{"title":"Development of posaconazole nanocrystalline solid dispersion: preparation, characterization and in vivo evaluation.","authors":"Ranga Goud Rayapolu, Balvant Yadav, Shashank S Apte, Venkata Vamsi Krishna Venuganti","doi":"10.1080/10837450.2024.2353314","DOIUrl":"10.1080/10837450.2024.2353314","url":null,"abstract":"Objective: Posaconazole (PCZ) is an antifungal drug, which acts by inhibiting the lanosterol-14α-demethylase enzyme. It is a biopharmaceutical classification system class II drug with its bioavailability being limited by poor aqueous solubility. The aim of this study was to improve the oral bioavailability of PCZ by preparing nanocrystalline solid dispersion (NCS).Methods: PCZ-NCS was prepared by a combination of precipitation and high-pressure homogenization followed by freeze-drying. Several different surfactants and polymers were screened to produce NCS with smaller particle size and higher stability.Results: The optimized NCS formulation containing 0.2% Eudragit S100 and 0.2% SLS was found to provide the average particle size of 73.31 ± 4.7 nm with a polydispersity index of 0.23 ± 0.03. Scanning electron microscopy revealed the preparation of homogeneous and rounded particles. Differential scanning calorimetry and X-ray diffraction confirmed crystalline nature of NCS. Nanonization increased the saturation solubility of PCZ by about 18-fold in comparison with the neat drug. Intrinsic dissolution study showed 93% dissolution of PCZ within the first 10 min. In vivo pharmacokinetic study in Wistar rats showed that Cmax and AUCtotal of PCZ-NCS increased by 2.58- and 2.64-fold compared to the marketed formulation.Conclusion: PCZ-NCS formulation presents a viable approach for enhancing the oral bioavailability of PCZ.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"530-540"},"PeriodicalIF":3.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140876958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Manufacturing classification system (MCS): enabling better understanding of oral solid dosage formulation design. 制造分类系统（MCS）：让人们更好地了解口服固体制剂配方设计。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-21 DOI: 10.1080/10837450.2024.2354416

Michael Leane

引用次数: 0

Modern trends in the formulation of microparticles for lung delivery using porogens: methods, principles and examples. 使用致孔剂配制肺部给药微粒的现代趋势：方法、原理和实例。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-23 DOI: 10.1080/10837450.2024.2350530

Andrea Peštálová, Jan Gajdziok

{"title":"Modern trends in the formulation of microparticles for lung delivery using porogens: methods, principles and examples.","authors":"Andrea Peštálová, Jan Gajdziok","doi":"10.1080/10837450.2024.2350530","DOIUrl":"10.1080/10837450.2024.2350530","url":null,"abstract":"Inhalation drug administration is increasingly used for local pharmacotherapy of lung disorders and as an alternative route for systemic drug delivery. Modern inhalation powder systems aim to target drug deposition in the required site of action. Large porous particles (LPP), characterized by an aerodynamic diameter over 5 μm, density below 0.4 g/cm3, and the ability to avoid protective lung mechanisms, come to the forefront of the research. They are mostly prepared by spray techniques such as spray drying or lyophilization using pore-forming substances (porogens). These substances could be gaseous, solid, or liquid, and their selection depends on their polarity, solubility, and mutual compatibility with the carrier material and the drug. According to the pores-forming mechanism, porogens can be divided into groups, such as osmogens, extractable porogens, and porogens developing gases during decomposition. This review characterizes modern trends in the formulation of solid microparticles for lung delivery; describes the mechanisms of action of the most often used porogens, discusses their applicability in various formulation methods, emphasizes spray techniques; and documents discussed topics by examples from experimental studies.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"504-516"},"PeriodicalIF":3.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140855461","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Injectable testosterone PLGA microsphere with different characteristics: effect of preparation method (paddle mixing versus microfluidic device). 具有不同特性的可注射睾酮 PLGA 微球：制备方法（桨式混合与微流控装置）的影响

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-15 DOI: 10.1080/10837450.2024.2348580

Yusuke Oe, Masanori Kobayashi, Takayuki Yoshida, Hiroyuki Kojima, Takayuki Terukina, Hiromu Kondo

{"title":"Injectable testosterone PLGA microsphere with different characteristics: effect of preparation method (paddle mixing versus microfluidic device).","authors":"Yusuke Oe, Masanori Kobayashi, Takayuki Yoshida, Hiroyuki Kojima, Takayuki Terukina, Hiromu Kondo","doi":"10.1080/10837450.2024.2348580","DOIUrl":"10.1080/10837450.2024.2348580","url":null,"abstract":"The purpose of this study was to compare the characteristics of testosterone polylactic-co-glycolic (PLGA) microspheres prepared by a paddle mixer or microfluidics device. The comparison was conducted by not only in vitro evaluation but also in vivo evaluation which has not been reported up to date. We discovered that, among the steps in microsphere preparation, the solvent removal process strongly impacted drug content, particle size and surface morphology. Spectroscopic measurements suggested that molecular interactions and crystallinity of the drug incorporated in the microspheres differed. For the drug release profile, although both mixer- and microfluidics-prepared samples showed similar sustained release of the incorporated drug for approximately one month in vitro, they exhibited different plasma concentration profiles in vivo. Together, our findings show that the preparation process, especially the solvent removal process, may affect the physicochemical characteristics of testosterone PLGA microspheres, leading to different in vivo performance.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"482-491"},"PeriodicalIF":3.4,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140865100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmaceutical applications and requirements of resins for printing by digital light processing (DLP) 数字光处理（DLP）印刷用树脂的制药应用和要求

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-04-20 DOI: 10.1080/10837450.2024.2345144

Denise Tiemi Uchida, Marcos Luciano Bruschi

引用次数: 0

Cytisine eye drops for benzalkonium chloride-induced dry eye: safety and efficacy evaluation 治疗苯扎氯铵引起的干眼症的胞二辛滴眼液：安全性和有效性评估

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-04-17 DOI: 10.1080/10837450.2024.2345148

Zijian Wang, Xixi Song, Yanjun Wei, Xianggen Wu, Ying Jie

引用次数: 0

Dissolving microneedles loaded with nimodipine for prevention of sleep disorders at a high altitude 装载尼莫地平的溶解微针用于预防高海拔地区的睡眠障碍

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-04-16 DOI: 10.1080/10837450.2024.2342965

Chunqing Wang, Xin Huang, Ziyan Tang, Yizhi Zhang, Meng Wei, Shumin Du, Xingshuang Song, Yanping Wu, Qiang Chi, Xiaomei Zhuang, Du Lina, Yiguan Jin

引用次数: 0

Ten Years of the Manufacturing Classification System: A review of literature applications and an extension of the framework to continuous manufacture 制造分类系统十年：文献应用回顾及将框架扩展至连续制造

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-04-15 DOI: 10.1080/10837450.2024.2342953

Michael Leane, Kendal Pitt, Gavin Reynolds, Sune Andersen, Brian Carlin, Abina Crean, John Gamble, Michael Gamlen, Bindhu Gururajan, Yaroslav Z. Khimyak, Peter Kleinebudde, Martin Kuentz, Zdravka Misic, Chris Moreton, Stefanie Peter, Stephen Sheehan, Elaine Stone, Anthony Tantuccio, Bernd Van Snick

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Development and characterization of magnetic hydrogels loaded with greenly synthesized iron-oxide nanoparticles conjugated with cisplatin 开发并表征负载有绿色合成的顺铂共轭氧化铁纳米粒子的磁性水凝胶

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-04-15 DOI: 10.1080/10837450.2024.2341244

Ali Shammeri, Rana Abu-Huwaij, Rania Hamed

引用次数: 0