abstract：:Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform in...

journal_title：Journal of pharmaceutical sciences

authors： Ferreira NN,Caetano BL,Boni FI,Sousa F,Magnani M,Sarmento B,Ferreira Cury BS,Daflon Gremião MP

更新日期：2019-04-01 00:00:00

abstract：:The aim of this study was to synthetize cocrystals of nateglinide, an antidiabetic agent of biopharmaceutics classification system Class IIa, as a strategy to improve both the solubility and the dissolution rate of the drug. Benzamide was selected by a screening procedure as a suitable coformer, and binary mixtures wi...

journal_title：Journal of pharmaceutical sciences

authors： Bruni G,Maggi L,Mustarelli P,Sakaj M,Friuli V,Ferrara C,Berbenni V,Girella A,Milanese C,Marini A

更新日期：2019-04-01 00:00:00

abstract：:The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

journal_title：Journal of pharmaceutical sciences

authors： Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

更新日期：2019-04-01 00:00:00

abstract：:High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...

journal_title：Journal of pharmaceutical sciences

authors： Pansare SK,Patel SM

更新日期：2019-04-01 00:00:00

abstract：:Solution preparation is the first unit operation of the manufacturing process for spray-dried solid dispersions. Visual inspection and offline high-performance liquid chromatography analysis are routinely used to assess the solution preparation end point as well as the final solution composition. However, the accuracy...

journal_title：Journal of pharmaceutical sciences

authors： Lee YC,Zhou G,Ikeda C,Chouzouri G,Howell L

更新日期：2019-03-01 00:00:00

abstract：:Die filling is a critical process step during tablet production as it defines the tablet weight. Achieving die fill consistency during production of mini-tablets, tablets with diameters ≤6 mm, is considerably more challenging. Although die filling in rotary presses had been studied in relation to the feed paddle desig...

journal_title：Journal of pharmaceutical sciences

authors： Goh HP,Sia Heng PW,Liew CV

更新日期：2019-03-01 00:00:00

abstract：:Levetiracetam therapy is often associated with high levels of individual variation in the recommended dose required to achieve preferential treatment. Thus, a reliable and dynamic regulation system to accurately tailor dose is necessary. The main objective of this study is to explore and prepare a dose-flexible contro...

journal_title：Journal of pharmaceutical sciences

authors： Cui M,Li Y,Wang S,Chai Y,Lou J,Chen F,Li Q,Pan W,Ding P

更新日期：2019-02-01 00:00:00

abstract：:In this article, we show that crystalline lactulose can be amorphized directly in the solid state by mechanical milling. Moreover, compared to similar materials, the amorphization kinetics of lactulose is found to be very rapid and the amorphous state thus obtained appears to be very stable against recrystallization o...

journal_title：Journal of pharmaceutical sciences

authors： Ngono F,Willart JF,Cuello G,Jimenez-Ruiz M,Affouard F

更新日期：2019-02-01 00:00:00

abstract：:In liver microsomes, selexipag (NS-304; ACT-293987) mainly undergoes hydrolytic removal of the sulfonamide moiety by carboxylesterase 1 (CES1) to yield the pharmacologically active metabolite MRE-269 (ACT-333679). However, it is not known how much CES in the liver and intestine contributes to the hydrolysis of selexip...

journal_title：Journal of pharmaceutical sciences

authors： Imai S,Ichikawa T,Sugiyama C,Nonaka K,Yamada T

更新日期：2019-02-01 00:00:00

abstract：:The purpose of the present study was to develop a physiologically based pharmacokinetic model for dextromethorphan (DEX) and its metabolites in extensive and poor metabolizers. The model was used to study the influence of dissolution rates on the sensitivity of maximum plasma concentration and area under the concentra...

journal_title：Journal of pharmaceutical sciences

authors： Bolger MB,Macwan JS,Sarfraz M,Almukainzi M,Löbenberg R

更新日期：2019-01-01 00:00:00

abstract：:SPRYCEL® (Dasatinib) is a Biopharmaceutical Classification System II weakly basic drug that exhibits strong pH-dependent solubility. Dasatinib is currently presented in 2 drug product formulations as an adult immediate release tablet and a pediatric powder for oral suspension. A bioequivalence study comparing the form...

journal_title：Journal of pharmaceutical sciences

authors： Vaidhyanathan S,Wang X,Crison J,Varia S,Gao JZH,Saxena A,Good D

更新日期：2019-01-01 00:00:00

abstract：:In the present study, the interaction between phenobarbital and activated carbons which is driven by hydrophobic bonding was evaluated. The Two-Mechanism Langmuir-Like Equation was proposed to describe the isotherms for phenobarbital adsorbing to activated carbons. The parameters in the Two-Mechanism Langmuir-Like Equ...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2019-01-01 00:00:00

abstract：:The insidious nature of Zika virus (ZIKV) infections can have a devastating consequence for fetal development. Recent reports have highlighted that chloroquine (CQ) is capable of inhibiting ZIKV endocytosis in brain cells. We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an...

journal_title：Journal of pharmaceutical sciences

authors： Olafuyi O,Badhan RKS

更新日期：2019-01-01 00:00:00

abstract：:Spray-dried dispersions (SDDs) are an important technology for enhancing the oral bioavailability of poorly water-soluble drugs. To design an effective oral SDD formulation, the key rate-determining step(s) for oral drug absorption must be understood. This work combined in vivo and in vitro tests with in silico modeli...

journal_title：Journal of pharmaceutical sciences

authors： Stewart A,Yates I,Mudie D,Pivette P,Goodwin A,Sarmiento A,Winter M,Morgen M,Vodak D

更新日期：2019-01-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:To reduce the risk of immunogenicity that may be caused by therapeutic protein products, it is important to properly characterize subvisible particles and to develop strategies to reduce the levels of particles delivered to patients. In the present study, by using state-of-the-art methods to quantify particle levels, ...

journal_title：Journal of pharmaceutical sciences

authors： Ueda T,Nakamura K,Abe Y,Carpenter JF

更新日期：2019-01-01 00:00:00

abstract：:There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

journal_title：Journal of pharmaceutical sciences

authors： Li T,Balthasar JP

更新日期：2019-01-01 00:00:00

abstract：:Hard gelatin capsule (HGC) shells are widely used to encapsulate drugs for oral delivery but are vulnerable to gelatin cross-linking, which can lead to slower and more variable in vitro dissolution rates. Adding proteolytic enzymes to the dissolution medium can attenuate these problems, but this complicates dissolutio...

journal_title：Journal of pharmaceutical sciences

authors： Likar MD,Carroll SC,Colgan ST,Yeoh T,MacDonald BC,Johnson GM,Space JS

更新日期：2018-12-01 00:00:00

abstract：:Protein immunogenicity is intensively researched by academics, biopharmaceutical companies, and authorities as it can compromise the safety and efficacy of a biopharmaceutical drug. So far, the exact protein aggregate properties inducing immune responses are not known. Possible protein-related factors could be size, c...

journal_title：Journal of pharmaceutical sciences

authors： Werner BP,Winter G

更新日期：2018-11-01 00:00:00

abstract：:Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility...

journal_title：Journal of pharmaceutical sciences

authors： Zha J,Zhang Q,Li M,Wang JR,Mei X

更新日期：2018-11-01 00:00:00

abstract：:The health effects of green tea are associated with catechins: (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin, (-)-epicatechin-3-O-gallate, and (-)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biol...

journal_title：Journal of pharmaceutical sciences

authors： Matić S,Jadrijević-Mladar Takač M,Barbarić M,Lučić B,Gall Trošelj K,Stepanić V

更新日期：2018-11-01 00:00:00

abstract：:Protein higher order structure (HOS) is an essential quality attribute to ensure protein stability and proper biological function. Protein HOS characterization is performed during comparability assessments for product consistency as well as during forced degradation studies for structural alteration upon stress. Circu...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Meengs B,Meyer J,Bongers J,Ludwig R,Tao L,Das TK,Leone A,Kar SR

更新日期：2018-10-01 00:00:00

abstract：:A hollow cylinder intravitreal implant was developed to achieve sustained release of protein to the retina for the treatment of retinal diseases. Hollow cylinders were fabricated by molding and cross-linking hyaluronic acid, the major component of the vitreous humor. Hollow cylinders were filled with a concentrated pr...

journal_title：Journal of pharmaceutical sciences

authors： Van Kampen E,Vandervelden C,Fakhari A,Qian J,Berkland C,Gehrke SH

更新日期：2018-09-01 00:00:00

abstract：:The concept of cosolvent exclusion was developed by a group of Timasheff's laboratory in 1970-1990 and is currently used widely to explain the effects of a variety of cosolvents on the stability and solubility of macromolecules. Not surprisingly, these concepts have had substantial influence in the fields of formulati...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Gagnon P

更新日期：2018-09-01 00:00:00

abstract：:During the freeze-drying process, vials located at the border of the shelf usually present higher heat flow rates that result in higher product temperatures than vials in the center. This phenomenon, referred to as edge vial effect, can lead to product quality variability within the same batch of vials and between bat...

journal_title：Journal of pharmaceutical sciences

authors： Scutellà B,Bourlès E,Plana-Fattori A,Fonseca F,Flick D,Trelea IC,Passot S

更新日期：2018-08-01 00:00:00

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

journal_title：Journal of pharmaceutical sciences

authors： Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

更新日期：2018-07-01 00:00:00

abstract：:Increasing costs of research and development in the pharmaceutical industry has necessitated a growing interest in the early prediction of human pharmacokinetics of drug candidates. Of growing interest is the need to understand oral absorption, the most common route of small molecule drug administration. The fraction ...

journal_title：Journal of pharmaceutical sciences

authors： Chiang PC,Liu J,Fan P,Wong H

更新日期：2018-07-01 00:00:00

abstract：:Literature data relevant to the decision to waive in vivo bioequivalence testing for the approval of generic immediate release solid oral dosage forms of proguanil hydrochloride are reviewed. To elucidate the Biopharmaceutics Classification System (BCS) classification, experimental solubility and dissolution studies w...

journal_title：Journal of pharmaceutical sciences

authors： Plöger GF,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Mehta MU,Parr A,Polli JE,Shah VP,Tajiri T,Dressman JB

更新日期：2018-07-01 00:00:00

abstract：:In this study, we investigated the potential roles of nanoparticles (<100 nm) and submicron (100-1000 nm) particles in the formation of microparticles (>1000 nm) in protein formulations under some pharmaceutically relevant stress conditions. Exposure of intravenous immunoglobulin solutions to the interface-associated ...

journal_title：Journal of pharmaceutical sciences

authors： Pardeshi NN,Zhou C,Randolph TW,Carpenter JF

更新日期：2018-07-01 00:00:00

abstract：:Comparability studies used to assess a proposed manufacturing change for a biological product include sensitive analytical studies to confirm there are no significant differences in structural or functional attributes that may contribute to clinically meaningful changes in efficacy or safety. When a proposed change is...

journal_title：Journal of pharmaceutical sciences

authors： Grampp G,McElroy PL,Camblin G,Pollock A

更新日期：2018-06-01 00:00:00

abstract：:This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...

journal_title：Journal of pharmaceutical sciences

authors： Bommana R,Chai Q,Schöneich C,Weiss WF 4th,Majumdar R

更新日期：2018-06-01 00:00:00

abstract：:We report the preparation and structural characterization of a family of primary alcohol solvates of a small-molecule hydrochloride salt. The structures of the solvates are probed by powder and single crystal X-ray diffraction, and the compounds were additionally characterized by polarized light microscopy, thermograv...

journal_title：Journal of pharmaceutical sciences

authors： Vasudevan KV,Peterson ML

更新日期：2018-06-01 00:00:00

abstract：:Chagas disease due to chronic infection with Trypanosoma cruzi is a neglected cause of heart disease, affecting approximately 6-10 million individuals in Latin America and elsewhere. T. cruzi Tc24, a calcium-binding protein in the flagellar pocket of the parasite, is a candidate antigen for an injectable therapeutic v...

journal_title：Journal of pharmaceutical sciences

authors： Biter AB,Weltje S,Hudspeth EM,Seid CA,McAtee CP,Chen WH,Pollet JB,Strych U,Hotez PJ,Bottazzi ME

更新日期：2018-05-01 00:00:00

abstract：:Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

journal_title：Journal of pharmaceutical sciences

authors： Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

更新日期：2018-05-01 00:00:00

abstract：:There is a growing clinical interest in developing and commercializing pharmaceutical-grade cannabinoid products, containing primarily tetrahydrocannabinol (THC) and cannabidiol (CBD). The oral bioavailability of THC and CBD is very low due to extensive "first-pass" metabolism. A novel oral THC and CBD formulation, PT...

journal_title：Journal of pharmaceutical sciences

authors： Atsmon J,Cherniakov I,Izgelov D,Hoffman A,Domb AJ,Deutsch L,Deutsch F,Heffetz D,Sacks H

更新日期：2018-05-01 00:00:00

abstract：:The presence of subvisible particles in formulations of therapeutic proteins is a risk factor for adverse immune responses. Although the immunogenic potential of particulate contaminants likely depends on particle structural characteristics (e.g., composition, size, and shape), exact structure-immunogenicity relations...

journal_title：Journal of pharmaceutical sciences

authors： Daniels AL,Randolph TW

更新日期：2018-05-01 00:00:00

abstract：:Econazole is a feasible alternative treatment in the management of fungal keratitis. Nevertheless, its low water solubility is considered the main limitation to the incorporation into ophthalmic formulations. In this work, econazole nitrate is solubilized by using cyclodextrins to achieve an optimum therapeutic concen...

journal_title：Journal of pharmaceutical sciences

authors： Díaz-Tomé V,Luaces-Rodríguez A,Silva-Rodríguez J,Blanco-Dorado S,García-Quintanilla L,Llovo-Taboada J,Blanco-Méndez J,García-Otero X,Varela-Fernández R,Herranz M,Gil-Martínez M,Lamas MJ,González-Barcia M,Otero-Espinar FJ,Fern

更新日期：2018-05-01 00:00:00

abstract：:Nanoparticle tracking analysis (NTA) obtains particle size by analysis of particle diffusion through a time series of micrographs and particle count by a count of imaged particles. The number of observed particles imaged is controlled by the scattering cross-section of the particles and by camera settings such as sens...

journal_title：Journal of pharmaceutical sciences

authors： Defante AP,Vreeland WN,Benkstein KD,Ripple DC

更新日期：2018-05-01 00:00:00

abstract：:Various neutral, cationic, and anionic chemicals contained in hair care products can be absorbed into hair fiber to modulate physicochemical properties such as color, strength, style, and volume. For environmental safety, there is also an interest in understanding hair absorption to wide chemical pollutants. There hav...

journal_title：Journal of pharmaceutical sciences

authors： Li L,Yang S,Chen T,Han L,Lian G

更新日期：2018-04-01 00:00:00