abstract：:Many active pharmaceutical ingredients exhibit a needle-like (acicular) crystal habit, which can significantly complicate their downstream processing. In this study, the acicular crystal habit of a model active pharmaceutical ingredient, 5-aminosalicylic acid (5-ASA), was modified by addition of selected organic solve...

journal_title：Journal of pharmaceutical sciences

authors： Pudasaini N,Parker CR,Hagen SU,Bond AD,Rantanen J

更新日期：2018-04-01 00:00:00

abstract：:A dual pH/redox responsive copper-glyglycine-prednisolone succinate-loaded nanoliposomal (NL) sludge was successfully synthesized and optimized using a Box-Behnken design of experiments. Preformulation design variables indicated that relative ratios of phospholipids, considerably influences NL size, thus altering the ...

journal_title：Journal of pharmaceutical sciences

authors： Mavuso S,Marimuthu T,Kumar P,Kondiah PPD,du Toit LC,Choonara YE,Pillay V

更新日期：2018-04-01 00:00:00

abstract：:A Modified Crisp Equation, describing the differential Gibbs free energy of the adsorption process, is being proposed, which considers multiple sites available on the surface for adsorption and their relative fractions. The differential Gibbs free energy can be calculated by the van't Hoff Equation, which depends on t...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2018-04-01 00:00:00

abstract：:Flexible manufacturing technologies for solid oral dosage forms with a continuous adjustability of the manufactured dose strength are of interest for applications in personalized medicine. This study explored the feasibility of using microvalve technology for the manufacturing of different solid oral dosage form conce...

journal_title：Journal of pharmaceutical sciences

authors： Bonhoeffer B,Kwade A,Juhnke M

更新日期：2018-03-01 00:00:00

abstract：:Pharmaceutical aerosols are used to treat many pulmonary diseases. The use of low-density powders has proven useful to support efficient drug delivery. Measurements must account for the low-density, spherical particle features contributing to aerodynamic behavior. Ideally, the aerodynamic particle size distribution (A...

journal_title：Journal of pharmaceutical sciences

authors： Hickey AJ,Edwards DA

更新日期：2018-03-01 00:00:00

abstract：:CAM2038, FluidCrystal injection depot, is an extended release formulation of buprenorphine given subcutaneously every 1 week (Q1W) or every 4 weeks (Q4W). The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physio...

journal_title：Journal of pharmaceutical sciences

authors： Liu T,Gobburu JVS

更新日期：2018-03-01 00:00:00

abstract：:Several controlled ice nucleation techniques have been developed to increase the efficiency of the freeze-drying process as well as to improve the quality of pharmaceutical products. Owing to the reduction in ice surface area, these techniques have the potential to reduce the degradation of proteins labile during free...

journal_title：Journal of pharmaceutical sciences

authors： Fang R,Tanaka K,Mudhivarthi V,Bogner RH,Pikal MJ

更新日期：2018-03-01 00:00:00

abstract：:Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evalua...

journal_title：Journal of pharmaceutical sciences

authors： Aitipamula S,Wong ABH,Kanaujia P

更新日期：2018-02-01 00:00:00

abstract：:The transdermal delivery of 2 fluorescent probes with similar molecular weight but different lipophilicity, into and through the skin from 2 commercially available transdermal bases, pluronic lecithin organogel, and Lipoderm® has been evaluated. First, in vitro penetration of fluorescein sodium and fluorescein (free a...

journal_title：Journal of pharmaceutical sciences

authors： Zhang Q,Song Y,Page SW,Garg S

更新日期：2018-02-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely col...

journal_title：Journal of pharmaceutical sciences

authors： Barmpalexis P,Grypioti A,Vardaka E,Karagianni A,Kachrimanis K

更新日期：2018-01-01 00:00:00

abstract：:The aim of this study is to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions using mesoporous silica (PSi). Ibuprofen and carvedilol were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of an API:PS...

journal_title：Journal of pharmaceutical sciences

authors： Genina N,Hadi B,Löbmann K

更新日期：2018-01-01 00:00:00

abstract：:A roadmap for the selection of a pharmaceutical salt form for a development candidate is presented. The free base of the candidate did not have sufficient chemical stability for development. The initially selected salt form turned out to be undevelopable because it was unstable during scale-up synthesis and storage. T...

journal_title：Journal of pharmaceutical sciences

authors： He Y,Orton E,Yang D

更新日期：2018-01-01 00:00:00

abstract：:The purpose of this study was to investigate the feasibility of delivering sinomenine hydrochloride (SH) transdermally using composite dissolving microneedles (DM) which integrated with liquid crystals (H2). The fabricated SH-loaded composite DM was evaluated for their appearance, mechanical strength, irritation, and ...

journal_title：Journal of pharmaceutical sciences

authors： Gui Z,Wu X,Wang S,Cao Y,Wan J,Shan Q,Yang Z,Zhang J,Gui S

更新日期：2017-12-01 00:00:00

abstract：:Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Schlich M,Cryan JF,O'Driscoll CM

更新日期：2017-12-01 00:00:00

abstract：:The progress in continuous downstream manufacturing of oral solid doses demands effective real-time process management, with monitoring at its core. This study evaluates the feasibility of using a commercial sensor to measure the mass flow rate of the particulates, a critical process variable in continuous manufacturi...

journal_title：Journal of pharmaceutical sciences

authors： Ganesh S,Troscinski R,Schmall N,Lim J,Nagy Z,Reklaitis G

更新日期：2017-12-01 00:00:00

abstract：:High protein concentration formulations are required for low-volume administration of therapeutic antibodies targeted for subcutaneous, self-administration by patients. Ultra-high concentrations (≥150 mg/mL) can lead to dramatically increased solution viscosities, which in turn can lead to stability, manufacturing, an...

journal_title：Journal of pharmaceutical sciences

authors： Whitaker N,Xiong J,Pace SE,Kumar V,Middaugh CR,Joshi SB,Volkin DB

更新日期：2017-11-01 00:00:00

abstract：:The purpose of this study was to develop a nanocarrier system for codelivery of paclitaxel (PTX) and piperlongumine (PL) and investigate the therapeutic potential of improving efficacy and reducing toxicity. PTX and PL were formulated into poly lactic-co-glycolic acid and D-α-tocopheryl polyethylene glycol succinate v...

journal_title：Journal of pharmaceutical sciences

authors： Liu Q,Zhao D,Zhu X,Chen H,Yang Y,Xu J,Zhang Q,Fan A,Li N,Guo C,Kong Y,Lu Y,Chen X

更新日期：2017-10-01 00:00:00

abstract：:The pneumococcal histidine triad protein D (PhtD) is believed to play a central role in pneumococcal metal ion homeostasis and has been proposed as a promising vaccine candidate against pneumococcal disease. To investigate for potential stabilizers, a panel of physiologically relevant metals was screened using the the...

journal_title：Journal of pharmaceutical sciences

authors： Ausar SF,Jayasundara K,Akawi L,Roque C,Sheung A,Hu J,Kirkitadze M,Rahman N

更新日期：2017-10-01 00:00:00

abstract：:Solvent-induced 3 frameworks (the monohydrate, methanol solvate, and dimethyl formamide [DMF] solvate) of an anticancer drug, 7-ethyl-10-hydroxycamptothecin (SN38), were constructed. The crystal structures of the 3 pseudopolymorphs were characterized by single-crystal X-ray diffraction technique for the first time. Cr...

journal_title：Journal of pharmaceutical sciences

authors： Fang L,Wang L,Yao C,Song S,Wu Z,Tao X

更新日期：2017-10-01 00:00:00

abstract：:Personalized medicine aims to determine the most adequate treatment and dose regimen to obtain the maximum efficacy and minimum side effect by taking into account patients' characteristics. For numerous reasons, one being ethical and methodological hurdles in including specific populations in clinical trials, innovati...

journal_title：Journal of pharmaceutical sciences

authors： Marsousi N,Desmeules JA,Rudaz S,Daali Y

更新日期：2017-09-01 00:00:00

abstract：:Although insulin receptor is expressed at the human blood-brain barrier (BBB), the physiological and pathologic roles of insulin signaling in biologic responses at the BBB remain unclear. Here, we investigate insulin signaling at the human BBB using human cerebral microvascular endothelial cell line (hCMEC/D3) as a we...

journal_title：Journal of pharmaceutical sciences

authors： Ito S,Yanai M,Yamaguchi S,Couraud PO,Ohtsuki S

更新日期：2017-09-01 00:00:00

abstract：:The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen HQ,Lin J,Kimoto E,Callegari E,Tse S,Obach RS

更新日期：2017-09-01 00:00:00

abstract：:Accurate prediction of target occupancy facilitates central nervous system drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma), as well as the impa...

journal_title：Journal of pharmaceutical sciences

authors： Yahata M,Chiba K,Watanabe T,Sugiyama Y

更新日期：2017-09-01 00:00:00

abstract：:A α-helical GALA peptide (WEAALAEALAEALAEHLAEALAEALEALAA) has been found to possess dual functions: a pH-dependent inducer of endosomal escape, and a ligand that targets lung endothelium. In the present study, the flexibility of GALA was improved by modifying the edge with polyethylene glycol linker, to increase lung-...

journal_title：Journal of pharmaceutical sciences

authors： Santiwarangkool S,Akita H,Nakatani T,Kusumoto K,Kimura H,Suzuki M,Nishimura M,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. Although the expression and function of this solute carrier transporter is well characterized in the human liver and other tissues, little i...

journal_title：Journal of pharmaceutical sciences

authors： Keiser M,Kaltheuner L,Wildberg C,Müller J,Grube M,Partecke LI,Heidecke CD,Oswald S

更新日期：2017-09-01 00:00:00

abstract：:Conjunctiva occupies most of the ocular surface area, and conjunctival permeability affects ocular and systemic drug absorption of topical ocular medications. Therefore, the aim of this study was to obtain a computational in silico model for structure-based prediction of conjunctival drug permeability. This was done b...

journal_title：Journal of pharmaceutical sciences

authors： Ramsay E,Ruponen M,Picardat T,Tengvall U,Tuomainen M,Auriola S,Toropainen E,Urtti A,Del Amo EM

更新日期：2017-09-01 00:00:00

abstract：:This article discusses the evaluation of drug candidates as hepatic transporter substrates. Recently, research on the applications of hepatic transporters in the pharmaceutical industry has improved to meet the requirements of the regulatory guidelines for the evaluation of drug interactions. To identify the risk of t...

journal_title：Journal of pharmaceutical sciences

authors： Okudaira N

更新日期：2017-09-01 00:00:00

abstract：:Most anticancer drugs are intended to function in the nuclei of cancer cells. If an anticancer drug could be delivered to mitochondria, the source of cellular energy, this organelle would be destroyed, resulting in the arrest of the energy supply and the killing of the cancer cells. To achieve such an innovative strat...

journal_title：Journal of pharmaceutical sciences

authors： Yamada Y,Munechika R,Kawamura E,Sakurai Y,Sato Y,Harashima H

更新日期：2017-09-01 00:00:00

abstract：:Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...

journal_title：Journal of pharmaceutical sciences

authors： Yamamoto S,Karashima M,Arai Y,Tohyama K,Amano N

更新日期：2017-09-01 00:00:00

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 00:00:00

abstract：:This study aims to investigate the drug-drug interactions (DDIs) between orally administered atorvastatin (ATV) and rifampicin (RIF) in rats. The isotope-IV method was used for the analysis of the increased systemic exposure (AUCpo) of ATV, in which a small amount of deuterium-labeled ATV (ATV-d5) was intravenously in...

journal_title：Journal of pharmaceutical sciences

authors： Yamashita S,Hasegawa T,Tachihara M,Minami K,Higashino H,Togashi K,Mutaguchi K,Kataoka M

更新日期：2017-09-01 00:00:00

abstract：:The storage of drug substance at subzero temperatures mitigates potential risks associated with liquid storage, such as degradation and shipping stress, making it the best solution for long-term storage. However, slower (generally uncontrolled) rates of freezing and thawing of drug substance in conventional large stor...

journal_title：Journal of pharmaceutical sciences

authors： Rayfield WJ,Kandula S,Khan H,Tugcu N

更新日期：2017-08-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 00:00:00

abstract：:Maintaining good content uniformity (CU) is a significant challenge for low-dose oral tablets in particular when using direct compression (DC). Using 6 model active pharmaceutical ingredients, we show that a platform DC tablet formulation suitable for developing low-dose API with excellent CU can be developed. This pl...

journal_title：Journal of pharmaceutical sciences

authors： Sun WJ,Aburub A,Sun CC

更新日期：2017-07-01 00:00:00

abstract：:Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...

journal_title：Journal of pharmaceutical sciences

authors： Haidari H,Zhang Q,Melville E,Kopecki Z,Song Y,Cowin AJ,Garg S

更新日期：2017-07-01 00:00:00

abstract：:Stirred media milling is the main technology for producing colloidal nanocrystalline suspensions. A number of studies have been reported on the effect of different operating parameters for lab, pilot, and industrial scales. However, typical milling tool box that can be used to support candidate from selection up to ph...

journal_title：Journal of pharmaceutical sciences

authors： Nakach M,Authelin JR,Agut C

更新日期：2017-07-01 00:00:00

abstract：:This study examined the safety, pharmacodynamic and pharmacokinetic similarity of the human recombinant filgrastim products ior®LeukoCIM and Neupogen® following a 28-day repeated subcutaneous dose administration in male and female Sprague-Dawley rats with a 14-day recovery period. Safety profiling was based on clinica...

journal_title：Journal of pharmaceutical sciences

authors： Licollari A,Riddle K,Taylor SR,Ledon N,Bolger GT

更新日期：2017-06-01 00:00:00

abstract：:This study reports, for the first time, development of tyrosine kinase inhibitor-loaded, thermosensitive liposomes (TKI/TSLs) and their efficacy for treatment of renal cell carcinoma when triggered by focused ultrasound (FUS). Uptake of these nanoparticles into renal cancer cells was visualized with confocal and fluor...

journal_title：Journal of pharmaceutical sciences

authors： Abshire C,Murad HY,Arora JS,Liu J,Mandava SH,John VT,Khismatullin DB,Lee BR

更新日期：2017-05-01 00:00:00

abstract：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

journal_title：Journal of pharmaceutical sciences

authors： Hamada Y,Ono M,Ohara M,Yonemochi E

更新日期：2017-04-01 00:00:00