Journal of pharmaceutical sciences最新文献_第4页

Physical Compatibility and Chemical Stability of Bupivacaine, Epinephrine, and Nalbuphine in 0.45% Sodium Chloride, 0.9% Sodium Chloride, or Plasma-Lyte A. 布比卡因、肾上腺素和纳布啡在 0.45%氯化钠、0.9%氯化钠或血浆-Lyte A 中的物理兼容性和化学稳定性。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-17 DOI: 10.1016/j.xphs.2024.10.003

Zachary SengerGladys Uwera Mihigo, Mitchell S Howard, Gabriella Baki, Mariann D Churchwell, Virender Kumar, Justin P Reinert

{"title":"Physical Compatibility and Chemical Stability of Bupivacaine, Epinephrine, and Nalbuphine in 0.45% Sodium Chloride, 0.9% Sodium Chloride, or Plasma-Lyte A.","authors":"Zachary SengerGladys Uwera Mihigo, Mitchell S Howard, Gabriella Baki, Mariann D Churchwell, Virender Kumar, Justin P Reinert","doi":"10.1016/j.xphs.2024.10.003","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.10.003","url":null,"abstract":"Purpose: To evaluate the physical compatibility and chemical stability of the combination of bupivacaine, epinephrine, and nalbuphine when in mixed in 0.45% sodium chloride, 0.9% sodium chloride, or Plasma-Lyte A.Methods: Bupivacaine 0.5% (15 mL), epinephrine 1 mg/mL (0.15 mL), and nalbuphine 10 mg/mL (0.5 mL) were combined to prepare three distinct admixtures with 0.45% sodium chloride, 0.9% sodium chloride, or Plasma-Lyte A. Visual inspection, spectrophotometric analysis, pH evaluation, and high-performance liquid chromatography tests were conducted at hours 0, 1, 5, 8, and 24. Samples were stored in ambient room light at room temperature.Results: There were no demonstrable changes identified in any of the samples with regards to visual changes, spectrophotometric absorbance, or pH. In each studied fluid, the remaining drug concentrations were an average of 100.92% bupivacaine, 95.8% epinephrine, and 100.02% nalbuphine.Conclusions: The combination of bupivacaine, epinephrine, and nalbuphine was found to be physically compatibility and chemically stable for a period of 24 hours at room temperature.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468296","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Impact of drug incorporation into micelle on reduced griseofulvin and meloxicam permeation across a hollow fiber membrane. 药物加入胶束对降低格列齐芬和美洛昔康在中空纤维膜上的渗透率的影响

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-17 DOI: 10.1016/j.xphs.2024.10.017

Roshni P Patel, Lynne S Taylor, James E Polli

{"title":"Impact of drug incorporation into micelle on reduced griseofulvin and meloxicam permeation across a hollow fiber membrane.","authors":"Roshni P Patel, Lynne S Taylor, James E Polli","doi":"10.1016/j.xphs.2024.10.017","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.10.017","url":null,"abstract":"A hollow fiber membrane (HFM) was previously characterized as a potential permeation component of a dissolution/permeation system. Two objectives were to assess the impact of micellization on drug permeation across HFM and identify a preferred permeation model from three models: permeation from only free drug, permeation from both free drug and micelle-bound drug, and permeation with enhancement from micelle shuttling. HFM studies were conducted under unsaturated drug conditions, using griseofulvin and the more hydrophilic drug meloxicam, with and without surfactant [sodium lauryl sulfate, polysorbate 80, and polyoxyethylene (10) lauryl ether]. Griseofulvin was micelle incorporated to a greater extent than meloxicam, such that griseofulvin flux decreased to a greater extent than for meloxicam. The griseofulvin permeation model from only free drug was rejected, since griseofulvin flux required free drug to be about 5-20 fold higher in HFM flux studies than supported by solubility studies, depending on surfactant. Permeation from both free griseofulvin and micelle-bound griseofulvin successfully accommodated observed flux, where micelle permeability was about 5-fold lower than free drug permeability for HFM with 10KDa MWCO. Permeation with enhancement from micelle shuttling was not the preferred explanation, although the model accommodated flux data and provided aqueous boundary layer thicknesses similar to other setups.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468291","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Evaluation of the impact of the polymer end groups and molecular weight on in vitro and in vivo performances of PLGA based in situ forming implants for ketoprofen. 评估聚合物端基和分子量对基于 PLGA 的酮洛芬原位成型植入物的体外和体内性能的影响。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-17 DOI: 10.1016/j.xphs.2024.10.019

Sanjib Saha, Xinhao Lin, Liping Zhou, Aixiang Xue, Eric Gosselin, Paresh P Chothe, Mittal Darji, Xiuling Lu, Wenzhan Yang

{"title":"Evaluation of the impact of the polymer end groups and molecular weight on in vitro and in vivo performances of PLGA based in situ forming implants for ketoprofen.","authors":"Sanjib Saha, Xinhao Lin, Liping Zhou, Aixiang Xue, Eric Gosselin, Paresh P Chothe, Mittal Darji, Xiuling Lu, Wenzhan Yang","doi":"10.1016/j.xphs.2024.10.019","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.10.019","url":null,"abstract":"In situ forming implants are appealing long-acting dosage forms for both preclinical and clinical applications due to their simple manufacturing process and easy delivery. This study aims to develop extended-release in situ forming solid implants for subcutaneous administration using two types of commercially available triblock poly (lactic-co-glycolic acid)-poly (ethylene glycol)-poly (lactic-co-glycolic acid) (PLGA-PEG-PLGA) polymers, with either an acid or ester end group. Both types of polymers instantly form in situ implants when injected directly into an aqueous medium. The performance of these implants, containing a model compound ketoprofen, was evaluated by comparing the in vitro drug release profiles with the in vivo performance following subcutaneous administration in rats. Analytical characterizations of two representative in situ implants were conducted to understand their structural impact on polymer degradation and drug release. All tested in situ forming implants demonstrated prolonged drug release profiles both in vitro and in vivo. This study illustrates the successful preparation of sustained-release in situ forming implant formulations for ketoprofen using commercially available polymers, with the molecular weight and the end group of the polymers affecting their degradation and the drug release from the in situ formed implants.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468290","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Mechanisms of drug release from a melt-milled, poorly soluble drug substance. 熔融研磨的难溶性药物释放机制

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-17 DOI: 10.1016/j.xphs.2024.10.016

Dominik Sleziona, David R Ely, Markus Thommes

引用次数: 0

Differentiation of puerarin chelate from salt by phase solubility test. 通过相溶性测试区分葛根素螯合物和盐类

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-16 DOI: 10.1016/j.xphs.2024.10.007

Yuanfeng Wei, Xin Chen, Runxue Ding, Jingwen Zhang, Hui Chen, Junxiao Zhu, Jianjun Zhang, Peiya Shen

{"title":"Differentiation of puerarin chelate from salt by phase solubility test.","authors":"Yuanfeng Wei, Xin Chen, Runxue Ding, Jingwen Zhang, Hui Chen, Junxiao Zhu, Jianjun Zhang, Peiya Shen","doi":"10.1016/j.xphs.2024.10.007","DOIUrl":"10.1016/j.xphs.2024.10.007","url":null,"abstract":"Different from salt, metal chelate is a novel state of drug constructed by more separate coordinate bonds to form a chelating circle. Due to their composition similarity, it is hard to distinguish them except identifying ionic bond (i.e., salt) or coordinate bond (i.e., chelate) in the single crystal structure. In this study, sodium chelate (CDCC No: 1865670) and lithium salt (CDCC No: 2161617) of puerarin (PUE) was prepared. In addition to difference in single crystal structure, it was found that they showed totally different phase solubility behaviors: lithium salt demonstrated a typical inverse proportion curve as other common salts, while sodium chelate exhibited disordered scatters. However, when incorporating the unit PUE-Na complex in solution state and complexation constant K11 in chemical equation, the scatters in phase solubility diagram of chelate could be well fitted and the value of K11 was dramatically higher with orders of magnitude than the dissociation constant Kc; while processing phase solubility curve of lithium salt by incorporating complex item, it could not well match the curve at all. PUE sodium chelate is more likely to be a weak electrolyte with partial dissociation, while PUE lithium salt acted as a strong electrolyte with complete dissociation. The phase solubility test would be served as a surrogate tool for differentiation of chelates from salts when single crystal was not available.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468271","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

An integrated approach combining experimental, informatics and energetic methods for solid form derisking of PF-06282999. 结合实验、信息学和能量学方法的综合方法用于 PF-06282999 的固态脱脂。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-16 DOI: 10.1016/j.xphs.2024.10.013

Ghazala Sadiq, Shubham Sharma, Joanna S Stevens, Pablo Martinez-Bulit, Lily M Hunnisett, Christopher Cameron, Brian Samas, Emma Hawking, Nicholas Francia, Jeff Lengyel, Elna Pidcock, Sadia Rahman, Matthew Nisbet, Kevin Back, Cheryl Doherty, Patricia Basford, Timothy G Cooper, Garry O'Connor, Rajni M Bhardwaj

引用次数: 0

Dissolution, phase behavior and mass transport of amorphous solid dispersions in aspirated human intestinal fluids. 无定形固体分散体在吸入人体肠液中的溶解、相态行为和质量传输。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-16 DOI: 10.1016/j.xphs.2024.10.005

Ahmed Elkhabaz, Dana E Moseson, Joachim Brouwers, Patrick Augustijns, Lynne S Taylor

{"title":"Dissolution, phase behavior and mass transport of amorphous solid dispersions in aspirated human intestinal fluids.","authors":"Ahmed Elkhabaz, Dana E Moseson, Joachim Brouwers, Patrick Augustijns, Lynne S Taylor","doi":"10.1016/j.xphs.2024.10.005","DOIUrl":"10.1016/j.xphs.2024.10.005","url":null,"abstract":"Amorphous solid dispersions (ASDs) typically show improved dissolution and generate supersaturated solutions, enhancing the oral bioavailability of poorly soluble drugs. To gain insights into intraluminal ASD behavior, we utilized two poorly soluble drugs with different crystallization tendencies, atazanavir and posaconazole, prepared as ASDs at a 10% drug loading with hydroxypropyl methylcellulose acetyl succinate (HPMCAS). We evaluated their release in aspirated fasted-state human intestinal fluid (FaHIF), and multi-component fasted-state simulated intestinal fluid (composite-FaSSIF), characterizing the supersaturation profiles and drug-rich nanodroplets that formed. Complete release was observed for atazanavir ASDs over a 90 min period. Flux for dissolved atazanavir ASDs remained high over the experimental time period of 3 h. In contrast, posaconazole solution concentrations were initially high and then decreased. Likewise, flux was initially high and then decreased where these changes are attributed to crystallization of the drug. Generation of spherical nano-sized amorphous droplets of ∼100-150 nm was found to occur in ex vivo FaHIF media for both ASDs, maximizing the diffusive flux during the supersaturation window. Moreover, buffer capacity differences were postulated to influence release rates of ASDs in simulated vs aspirated fluids. Importantly, the solution phase phenomena observed during ASD release in simulated fluids, namely amorphous nanodroplet formation and drug crystallization, were also found to occur in aspirated luminal fluids.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Impact of Surface Tension, Viscosity, Pump Settings, and Nozzle Size on Filling Process Capability and Accuracy in High-Concentration Biopharmaceuticals. 表面张力、粘度、泵设置和喷嘴尺寸对高浓度生物制药灌装工艺能力和精度的影响

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-16 DOI: 10.1016/j.xphs.2024.10.020

Qizhou Chen, Chenxi Wang, Tingting Wang, Bin Lei, Jing Wang, Jeremy Guo

{"title":"Impact of Surface Tension, Viscosity, Pump Settings, and Nozzle Size on Filling Process Capability and Accuracy in High-Concentration Biopharmaceuticals.","authors":"Qizhou Chen, Chenxi Wang, Tingting Wang, Bin Lei, Jing Wang, Jeremy Guo","doi":"10.1016/j.xphs.2024.10.020","DOIUrl":"https://doi.org/10.1016/j.xphs.2024.10.020","url":null,"abstract":"Filling is the final critical unit operation in the manufacturing process of liquid biological drug products. This paper thoroughly investigates the influence and mechanisms of peristaltic pump settings, nozzle size, product surface tension and viscosity on the biopharmaceutical filling processes based on the established filling process model of surrogates. Our study highlights the significant role of pump settings in influencing filling process capability indexes, in addition to their primary function of regulating flow rate. Surface tension minimally impacts flow behavior but significantly regulates the final drop's behavior, with lower surface tension increasing dripping tendencies. Viscosity proves crucial; higher viscosity intensifies friction and head loss of filling flow in tube/nozzle, causing pressure and flow rate losses, more pronounced dripping, and worse filling accuracy. Furthermore, nozzle size moderates the impact of pump settings, surface tension, and viscosity on filling performance. Larger nozzles help mitigate these effects, contributing to enhanced stability in filling performance under challenging conditions. For high-concentration biopharmaceuticals with elevated viscosity during filling, utilizing larger nozzles and reducing pump speed could achieve enhanced Cpk values and improved filling accuracy. Understanding the complex interactions among these factors is vital for optimizing the biopharmaceutical industry, promoting cost-effective practices, and enhancing production efficiency.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468292","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Letter to Editor: Comments about "Structural studies of a non-stoichiometric channel hydrate using high resolution X-ray powder diffraction, solid-state nuclear magnetic resonance, and moisture sorption methods". 致编辑的信：关于 "利用高分辨率 X 射线粉末衍射、固态核磁共振和吸湿方法对非均匀通道水合物进行结构研究 "的评论。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-16 DOI: 10.1016/j.xphs.2024.10.006

Jean René Authelin

引用次数: 0

Changes in drug crystallinity in a commercial tacrolimus amorphous formulation result in variable pharmacokinetics. 商用他克莫司无定形制剂中药物结晶度的变化导致不同的药代动力学。

IF 3.7 3区医学

Journal of pharmaceutical sciences Pub Date : 2024-10-15 DOI: 10.1016/j.xphs.2024.09.025

Lynne S Taylor, Niraj E Trasi, Hitesh S Purohit, Dajun Sun, Minori Kinjo, Zhanglin Ni, Sanjida Mahjabeen, Kairui Kevin Feng, Wei-Jhe Sun, Murali K Matta, Brian Decker, Raymond E Galinsky

{"title":"Changes in drug crystallinity in a commercial tacrolimus amorphous formulation result in variable pharmacokinetics.","authors":"Lynne S Taylor, Niraj E Trasi, Hitesh S Purohit, Dajun Sun, Minori Kinjo, Zhanglin Ni, Sanjida Mahjabeen, Kairui Kevin Feng, Wei-Jhe Sun, Murali K Matta, Brian Decker, Raymond E Galinsky","doi":"10.1016/j.xphs.2024.09.025","DOIUrl":"10.1016/j.xphs.2024.09.025","url":null,"abstract":"Tacrolimus capsules contain the drug as the amorphous form. It is well known that drug crystallinity is a risk factor for the performance of amorphous formulations. This study investigated the impact of varying levels of crystalline drug on the pharmacokinetics of tacrolimus following oral dosing of a 5 mg capsule under fasting conditions. Two treatments with percent crystallinity of 20% and 50% were achieved by exposing a marketed generic tacrolimus product to open dish storage conditions of 35 °C and 75% relative humidity (RH) for up to 20 days. Crystallinity was monitored with X-ray powder diffraction. Prograf®, the reference listed drug (RLD), an amorphous generic drug product, and generic drug products containing 20% and 50% crystalline tacrolimus were evaluated. All four treatments were administered to healthy participants in a randomized, single-dose, four-treatment, four-period, four-way crossover study. Blood sampling occurred over 24 h. The amorphous generic tacrolimus product was determined not to be bioequivalent to the RLD. The capsules containing both 20% and 50% crystalline tacrolimus also failed the bioequivalence recommendations when compared to the amorphous generic or to the RLD. Both levels of crystalline tacrolimus resulted in BE failure for both Cmax and AUC parameters. The impact of tacrolimus crystallization was greater for maximum blood concentration (Cmax) values relative to the area-under-the-curve (AUC) values. This study demonstrates that crystalline tacrolimus formed in a marketed generic product and these changes resulted in variable pharmacokinetics which could be of significant clinical concern.","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":3.7,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142468269","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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