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Journal of Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/28549909/poor-quality-and-counterfeit-drugs-a-systematic-assessment-of-prevalence-and-risks-based-on-data-published-from-2007-2016
#1
Andreas Koczwara, Jennifer Dressman
Counterfeit drugs can hurt patients and harm the pharmaceutical industry. In 2006, the International Medical Products Anti-Counterfeiting Taskforce expressed a need to generate more and better data to calculate a worldwide prevalence of counterfeiting. This review analyzes field test data that were published in the time-frame January 2007 to December 2016, were accessible via Pubmed, and which addressed the prevalence of counterfeit drugs. Based on the 41 studies identified, it is still not possible to make a reliable statement about the prevalence of counterfeit drugs due to the heterogeneity of the results...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549908/elucidation-of-the-intestinal-absorption-of-para-aminobenzoic-acid-a-marker-for-dietary-intake
#2
Teruko Imai, Keiichiro Tanaka, Takahiro Yonemitsu, Yuta Yakushiji, Kayoko Ohura
para-Aminobenzoic acid (PABA) has long been used as an indicator of the completeness of 24-hour urine collection by determination of total urinary excretion of PABA and its metabolite, N-acetyl-PABA. N-Acetyl-PABA is formed by human arylamine N-acetyltransferase 1 (NAT1) in liver and intestine. This intestinal metabolism may reduce the urinary recovery of PABA due to secretion of N-acetyl-PABA into the intestinal lumen. In the present study, the effect of intestinal metabolism of PABA on its absorption was quantitatively evaluated by the in situ single-pass perfusion method using rat intestine expressing rat arylamine N-acetyltransferase 2 (Nat2), which is similar to human NAT1...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549907/transformation-of-bcs-class-i-and-iii-drugs-into-ionic-liquids-and-lipophilic-salts-for-enhanced-developability-using-lipid-formulations
#3
Hywel D Williams, Leigh Ford, Shea Lim, Sifei Han, John Baumann, Hannah Sullivan, David Vodak, Annabel Igonin, Hassan Benameur, Colin W Pouton, Peter J Scammells, Christopher J H Porter
Higher lipid solubility of lipophilic salt forms creates new product development opportunities for high-dose liquid-filled capsules. The purpose of this study was to determine if lipophilic salts of BCS Class I amlodipine and BCS Class III fexofenadine, ranitidine and metformin were better lipid formulation candidates than existing commercial salts. Lipophilic salts were prepared from lipophilic anions and commercial HCl or besylate salt forms, as verified by (1)H NMR. Thermal properties were assessed by DSC and hot-stage microscopy...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549906/using-potentiometric-free-drug-sensors-to-determine-the-free-concentration-of-ionisable-drugs-in-colloidal-systems
#4
Thuy Tran, Anjan Chakraborty, Xi Xi, Hugo Bohets, Claus Cornett, Konstantin Tsinman, Thomas Rades, Anette Müllertz
The current study investigates the use of free drug sensors (FDS) to measure free ionized drug concentrations in colloidal systems, including micellar solutions and emulsions and lipid formulations during in vitro lipolysis. Diphenhydramine hydrochloride (DPH) and loperamide hydrochloride (LOP) were selected as model drugs. Self-diffusion nuclear magnetic resonance (NMR) studies were performed and confirmed the entrapment of drugs in micelles in Brij 35 and sodium taurodeoxycholate (TDC)/phosphatidylcholine (PC) micellar solutions...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549905/on-the-use-of-group-sequential-study-designs-for-the-test-of-bioequivalence-for-complicated-products
#5
Rajesh Krishna, Wen-Lin Luo, Patrick J Larson, Paul H Fackler
A novel modeling approach together with a use of group sequential study design for a complicated triple fixed-dose combination was attempted. Probability of success (POS) was used for determining a weighted average power, where weight was based on available information such as data from previous pilot studies or literature. A simulation study was conducted that resulted in the development of the necessary sample size for the studies in addition to identifying a decision algorithm that was prospectively defined in the protocols...
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549904/editorial
#6
EDITORIAL
Ronald T Borchardt
No abstract text is available yet for this article.
May 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28535977/identification-and-evaluation-of-the-minimum-unit-of-a-kala-peptide-required-for-gene-delivery-and-immune-activation
#7
Naoya Miura, Kota Tange, Yuta Nakai, Hideyoshi Harashima, Hidetaka Akita
The KALA peptide (WEAKLAKALAKALAKHLAKALAKALKA) is an amphiphilic peptide that forms an α-helical structure at physiological pH. We previously reported that, when a pDNA-encapsulating liposomal membrane is modified with the KALA peptide, transgene expression and immune activation are facilitated in bone marrow-derived dendritic cells (BMDCs). However, the minimum unit of the KALA peptide and the importance of its secondary structure for these activities are not completely known at this time. We herein report on the identification of the minimum unit of the KALA peptide (short-KALA) required for activity, as determined by the stepwise removal of "K-A-L-A" units...
May 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28535976/oatp-and-efflux-transporter-mediated-hepatic-uptake-and-biliary-excretion-of-cilostazol-and-its-metabolites-in-rats-and-humans
#8
Chong Wang, Xiaokui Huo, Changyuan Wang, Qiang Meng, Zhihao Liu, Pengyuan Sun, Jian Cang, Huijun Sun, Kexin Liu
Cilostazol undergoes extensive liver metabolism. However, the transporter-mediated hepatic disposition of cilostazol remains unknown. The present study was performed to investigate the hepatic uptake and biliary excretion of cilostazol and its metabolites (OPC-13015 and OPC-13213) using rat liver and human transporter-transfected cells in vitro. Cilostazol uptake by rat liver slices and isolated rat hepatocytes exhibited time-, concentration-, and temperature-dependency and was decreased by Oatp inhibitors, which suggested that Oatp was involved in the hepatic uptake of cilostazol...
May 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28535975/novel-poly-diol-sebacate-s-as-additives-to-modify-paclitaxel-release-from-poly-lactic-co-glycolic-acid-thin-films
#9
Lucila Navarro, Diana-Elena Mogosanu, Natalia Ceaglio, Julio Luna, Peter Dubruel, Ignacio Rintoul
Paclitaxel (PTX) incorporation in poly (lactic acid-co-glycolic acid) (PLGA) matrices produce films with high tensile rigidity and slow release that fail to deliver the required release rate for most biomedical applications such as in drug eluting stents and cancer treatments. To modify and improve this behavior, a set of poly (diol sebacate)s were synthesized and fully characterized as possible additives. The tensile properties of PLGA blends were evaluated as these materials could be used as coatings in drug eluting stent applications...
May 20, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28533121/recent-progress-in-hepatocyte-culture-models-and-their-application-to-the-assessment-of-drug-metabolism-transport-and-toxicity-in-drug-discovery-the-value-of-tissue-engineering-for-the-successful-development-of-a-microphysiological-system
#10
REVIEW
Kazuhiro Tetsuka, Masato Ohbuchi, Kenji Tabata
Tissue engineering technology has provided many useful culture models. This article reviews the merits of this technology in a hepatocyte culture system, and describes the applications of the sandwich-cultured hepatocyte model in drug discovery. In addition, we also review recent investigations of the utility of the three-dimensional bioprinted human liver tissue model and spheroid model. Finally, we present the future direction and developmental challenges of a hepatocyte culture model for the successful establishment of a microphysiological system, represented as an organ-on-a-chip and even as a human-on-a-chip...
May 19, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28533120/evaluation-of-new-chemical-entities-as-substrates-of-liver-transporters-in-the-pharmaceutical-industry-response-to-regulatory-requirements-and-future-steps
#11
Noriko Okudaira
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 transporter-mediated drug-drug interactions (DDIs) at an early stage of drug development, we employed a strategy of reviewing the in vivo animal pharmacokinetics and tissue distribution data obtained in the discovery stage together with the in vitro data obtained for regulatory submission...
May 19, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28502797/understanding-the-potential-interethnic-difference-in-rosuvastatin-pharmacokinetics
#12
Leslie Z Benet, Hsin-Fang Wu
No abstract text is available yet for this article.
May 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28501470/possibility-of-predicting-sert-occupancy-from-the-in-vitro-inhibition-constant-for-sert-the-clinically-relevant-plasma-concentration-of-unbound-drugs-and-their-profiles-for-substrates-of-transporters
#13
REVIEW
Masahiro Yahata, Koji Chiba, Takao Watanabe, Yuichi Sugiyama
Accurate prediction of target occupancy facilitates CNS 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 impact of drug transporters in the blood-brain barrier. First, the geometric means of in vitro Ki values were compared with the means of in vivo Ki values (Ki,u,plasma) which were calculated as Cu,plasma values at 50% occupancy of SERT obtained from previous clinical PET/SPECT imaging studies for 6 selective serotonin transporter reuptake inhibitors (SSRIs) and 3 serotonin norepinephrine reuptake inhibitors (SNRIs)...
May 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28501469/routes-for-drug-translocation-across-the-blood-brain-barrier-exploiting-peptides-as-delivery-vectors
#14
REVIEW
Mie Kristensen, Birger Brodin
A number of potent drugs for the treatment of brain diseases are available. However, in order for them to reach their target site of action, they must pass the blood-brain barrier (BBB). The capillary endothelium comprises the major barrier of the BBB and allows only passive permeation of some small lipophilic molecules. Brain delivery of the larger biopharmaceuticals, which today includes an increasing number of novel drug entities, is therefore restricted; both due to their molecular size and their hydrophilic nature...
May 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28499879/developing-a-flexible-pediatric-dosage-form-for-antiretroviral-therapy-a-fast-dissolving-tablet
#15
Manjari Lal, Manshun Lai, Marcus Estrada, Changcheng Zhu
Current presentations of the anti-HIV drugs lopinavir and ritonavir make appropriate dosing for children difficult. We conducted a feasibility study to develop a formulation for these drugs with child-safe excipients in a flexible dosage form for children across the pediatric age spectrum. The freeze-drying-in-blister approach was used to produce fast-dissolving tablets (FDTs), as these can be dispersed in fluids for easy administration, even to infants, and appropriate portions of the dispersion can be given for different ages/weights...
May 9, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28499878/possible-role-of-organic-cation-transporters-in-the-distribution-of-11-c-sulpiride-a-dopamine-d2-receptor-antagonist
#16
Harumasa Takano, Sumito Ito, Xuan Zhang, Hiroshi Ito, Ming-Rong Zhang, Hiroshi Suzuki, Kazuya Maeda, Hiroyuki Kusuhara, Tetsuya Suhara, Yuichi Sugiyama
We synthesized [(11)C]sulpiride as a positron emission tomography (PET) probe for investigating the drug distribution in the human body. [(11)C]Sulpiride was injected to healthy male subjects in either tracer dose of [(11)C]sulpiride (ca 222 MBq) or with therapeutic dose of sulpiride (500 mg, po) 3 hours prior to the injection in a crossover fashion. Whole body PET imaging demonstrated that [(11)C]sulpiride accumulated exceedingly in the bladder, followed by liver, gall bladder and kidney respectively; at 30 minutes after the injection, whereas scarcely in the brain...
May 9, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28499877/novel-superparamagnetic-micro-devices-based-on-magnetised-plga-pla-microparticles-obtained-by-supercritical-fluid-emulsion-and-coating-by-carboxybetaine-functionalised-chitosan-allowing-the-tuneable-release-of-therapeutics
#17
Cricchio Vincenzo, Mark Best, Ernesto Reverchon, Nicola Maffulli, Gary Phillips, Matteo Santin, Della Porta Giovanna
When superparamagnetic nanoparticles are loaded within micro-carriers of thermosensitive and injectable biopolymers, "smart" microdevices are obtained: they respond to an external magnetic field (EMF) through the release of any co-encapsulated molecules with a remote on-off control. Creating reliable and effective fabrication technologies for the production of these smart nano/micro-devices remains a challenge. In this work Supercritical Emulsion Extraction technology (SEE) is proposed for the fabrication of microcapsules with a core of poly-lactic-co-glycolic acid (PLGA) or poly-lactic acid (PLA) covered by carboxybetaine-functionalized chitosan (f-chi) and loaded with paramagnetic nanoparticles (MAG, mean size of 6...
May 9, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28495569/journal-of-pharmaceutical-sciences-notes-plasma-lipidomics-of-healthy-japanese-adults-reveals-gender-and-age-related-differences
#18
Keiko Maekawa, Kazuo Okemoto, Masaki Ishikawa, Rieko Tanaka, Yuji Kumagai, Yoshiro Saito
Lipid metabolites in the blood are expected to be biomarker candidates to reflect disease states and responses to therapeutic drugs. However, their profiles are influenced by subject background, which may lead to confounding results. This study aimed to evaluate whether age and gender affect lipid metabolite levels in the plasma of healthy Japanese adults. Comprehensive lipidomic analysis was performed using liquid chromatography-mass spectrometry for overnight-fasted volunteers consisting of four groups of 15 subjects each: young males (25-35 years old), elderly males (55-64 years old), young females (25-35 years old), and elderly females (55-65 years old)...
May 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28495568/quantitative-analyses-of-the-influence-of-parameters-governing-rate-determining-process-of-hepatic-elimination-of-drugs-on-the-magnitudes-of-drug-drug-interactions-via-hepatic-oatps-and-cyp3a-using-physiologically-based-pharmacokinetic-models
#19
Takashi Yoshikado, Maeda Kazuya, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
Physiologically-based pharmacokinetic (PBPK) models were constructed for hepatic organic anion transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) substrates (bosentan, repaglinide, clarithromycin, and simeprevir), a CYP3A probe substrate (midazolam), and selective inhibitors for OATPs (rifampicin) and CYP3A (itraconazole), though the role of OATPs in the hepatic uptake of clarithromycin is unclear. The pharmacokinetic data were obtained from our previous clinical drug-drug interaction (DDI) study...
May 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28495567/transporters-involved-in-metformin-pharmacokinetics-and-treatment-response
#20
Xiaomin Liang, Kathleen M Giacomini
Metformin, widely used as first-line treatment for type 2 diabetes, exists primarily as a hydrophilic cation at physiological pHs. As such, membrane transporters play a substantial role in its absorption, tissues distribution, and renal elimination. Multiple organic cation transporters are determinants of the pharmacokinetics of metformin, and many of them are important in its pharmacological action, as mediators of metformin entry into target tissues. Further, a recent genomewide association study (GWAS) in a large multi-ethnic population implicated polymorphisms in SLC2A2, encoding the glucose transporter, GLUT2, as important determinants of response to metformin...
May 8, 2017: Journal of Pharmaceutical Sciences
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