21,656 results match your criteria Journal of Pharmaceutical Sciences [Journal]


Prediction of Dissolution Profiles from Process Parameters, Formulation and Spectroscopic Measurements.

J Pharm Sci 2019 Feb 8. Epub 2019 Feb 8.

Graduate School of Pharmaceutical Sciences, Duquesne University. Electronic address:

This study utilized multiple modeling approaches to predict immediate release tablet dissolution profiles of two model drugs: theophylline and carbamazepine. Two sets of designs of experiments were applied based on individual drug characteristics to build in adequate dissolution variability. The tablets were scanned using a near infrared (NIR) spectrometer and then subjected to in vitro dissolution test at critical time points. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.023DOI Listing
February 2019

The effects of clioquinol on P-glycoprotein expression and biometal distribution in the mouse brain microvasculature.

J Pharm Sci 2019 Feb 7. Epub 2019 Feb 7.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia. Electronic address:

Previous studies have demonstrated that the ionophore clioquinol (CQ), in conjunction with the biometals copper and zinc, increases the expression of P-glycoprotein (P-gp) in human cerebral microvascular endothelial (hCMEC/D3) cells. As P-gp expression and function at the blood-brain barrier (BBB) is of great interest regarding CNS drug access and endogenous toxin trafficking (e.g. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.030DOI Listing
February 2019

An Integrated Analysis of Solid Form Change Impact on Solubility and Permeability: Case Study of Oral Exposure in Rats of a RORc Inhibitor.

J Pharm Sci 2019 Feb 7. Epub 2019 Feb 7.

Drug Metabolism and Pharmacokinetics.

It is well acknowledged that the oral absorption of a drug can be influenced by its solubility, which is usually associated with its solid form properties. G1032 is a Retinoic Acid-Related Orphan Receptor inverse agonist. Crystalline solid (Form A) was identified with an aqueous solubility of 130 μg/mL. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.031DOI Listing
February 2019

Conjugation of emtansine onto trastuzumab promotes aggregation of the antibody-drug conjugate by reducing repulsive electrostatic interactions and increasing hydrophobic interactions.

J Pharm Sci 2019 Feb 5. Epub 2019 Feb 5.

Center for Pharmaceutical Biotechnology, Department of Pharmaceutical Sciences, University of Colorado, Aurora, Colorado. Electronic address:

The impact of drug conjugation on intra- and intermolecular interactions of trastuzumab (TmAb) was determined by comparing the conformational and colloidal stabilities of TmAb and trastuzumab emtansine (T-DM1). In low ionic strength formulations, drug conjugation to native lysine residues of TmAb significantly reduced the repulsive electrostatic interactions between T-DM1 molecules. When these electrostatic interactions were screened in solutions with high ionic strength, intermolecular interactions between T-DM1 molecules were found to be more attractive than those between TmAb molecules. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.029DOI Listing
February 2019

Using the transtheoretical model's stages of change to predict medication adherence in patients with type 2 diabetes mellitus in a primary health care setting.

Daru 2019 Feb 7. Epub 2019 Feb 7.

Pharmacy Department, Westbay Healthcare Center, Doha, Qatar.

Background: Qatar is currently experiencing a worrying increase in the prevalence of diabetes mellitus (DM). One of the most common reasons for uncontrolled DM is non-adherence to medications. The socio-behavioral intervention has proven effective in some chronic illnesses. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00246-7DOI Listing
February 2019

Liquid oil marbles: increasing the bio-availability of poorly water-soluble drugs.

J Pharm Sci 2019 Feb 2. Epub 2019 Feb 2.

Chemical Robotics Laboratory, Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 5, 166 28 Prague 6, Czech Republic. Electronic address:

Many new therapeutic candidates - active pharmaceutical ingredients (APIs) are poorly soluble in an aqueous environment resulting in their reduced bioavailability. A promising way of enhancing the release of an API and, thus, its bioavailability seems to be the use of liquid oil marbles (LOMs). A LOM system behaves as a solid form but consists of an oil droplet in which an already dissolved API is encapsulated by a powder. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.026DOI Listing
February 2019

Physiologically based pharmacokinetic modeling to supplement nilotinib pharmacokinetics and confirm dose selection in pediatric patients.

J Pharm Sci 2019 Feb 2. Epub 2019 Feb 2.

Novartis Institutes for BioMedical Research, East Hanover 07936, New Jersey, USA.

In adult patients nilotinib is indicated for chronic myeloid leukemia at an approved oral dose of 300 or 400 mg BID. Physiologically based pharmacokinetic (PBPK) model was developed to describe and supplement limited PK data in the pediatric population ranging from 2 to less than 6 years of age and ultimately inform dosing regimen. An adult Simcyp PBPK model was established and verified with clinical pharmacokinetic data after a single or multiple oral doses of 400 mg nilotinib (230 mg/m). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.028DOI Listing
February 2019

A delivery system for oral administration of proteins/peptides through bile acid transport channels.

J Pharm Sci 2019 Feb 2. Epub 2019 Feb 2.

Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China. Electronic address:

Proteins/peptides are poorly absorbed via oral administration because of the gastrointestinal tract environment and lysosomal digestion after apical endocytosis. A delivery system, consisting of a deoxycholic acid-conjugated nanometer-sized carrier, may enhance the absorption of proteins/peptides in the intestine via the bile acid pathway. Deoxycholic acid is first conjugated to chitosan. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193007
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.027DOI Listing
February 2019
2 Reads
2.590 Impact Factor

Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology.

J Pharm Sci 2019 Feb 2. Epub 2019 Feb 2.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China. Electronic address:

Absorption enhancers are often a major component of solid oral peptide formulations as compared to the active pharmaceutical ingredient and excipients. This commonly results in poor tabletability that is hard to mitigate in direct compaction by addition of small amounts of excipients. To improve the tabletability of bulky absorption enhancers, the model absorption enhancers, sodium cholate and deoxycholic acid, were co-spray dried with hydroxypropyl methylcellulose (HPMC) E5 where the percentage of absorption enhancers was not lower than 90% (w/w). Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193007
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.025DOI Listing
February 2019
1 Read

Whole body Physiologically Based Pharmacokinetic Modeling of Trastuzumab and Prediction of Human Pharmacokinetics.

J Pharm Sci 2019 Feb 1. Epub 2019 Feb 1.

Department of Clinical Pharmacology and Therapeutics, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Republic of Korea. Electronic address:

In the current study, we evaluated the pharmacokinetics (PK) of trastuzumab and sought to predict human PK based on animal studies, through the use of optical imaging and a whole-body physiologically based pharmacokinetic (WB-PBPK) modeling approach. The PK study was conducted in 24 mice, where serial blood samples were withdrawn and major organs were isolated after the last blood withdrawal. The drug concentrations in blood and major organs were measured via optical imaging. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193007
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.024DOI Listing
February 2019
2 Reads
2.590 Impact Factor

Current status of the acquired immune system of Iranian patients with long-term complications of sulfur mustard poisoning.

Daru 2019 Feb 4. Epub 2019 Feb 4.

Medical Toxicology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Background: Sulfur mustard (SM) is a powerful blistering chemical warfare agent that has genotoxic effects. Cells with excessive proliferation such as lymphocytes may inherit this cellular toxicity which can lead to their malfunctions in the long-term. This study was designed to evaluate the status of acquired immunity among SM poisoned veterans around three decades after exposure. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00239-6DOI Listing
February 2019
1 Read

Microwave assisted synthesis of polyacrylamide grafted polymeric blend of fenugreek seed mucilage-Polyvinyl alcohol (FSM-PVA-g-PAM) and its characterizations as tissue engineered scaffold and as a drug delivery device.

Daru 2019 Feb 2. Epub 2019 Feb 2.

Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology Mesra, Ranchi, Jharkhand, 835215, India.

Microwave assisted synthesis of graft copolymer of polymeric blend of Fenugreek seed mucilage (FSM)-Polyvinyl alcohol (PVA) with acrylamide (AM) was done by free radical polymerization using ammonium per sulfate (APS) as initiator. Varying amount of AM and APS was used to optimize the best grade based on highest percentage grafting efficiency and investigated with intrinsic viscosity measurement, Fourier Transformation infrared spectroscopy (FTIR),C NMR spectra, X-ray diffraction, elemental analysis, Thermogravimetric analysis, Scanning electron microscopy. The results of intrinsic viscosity indicate that the optimized sample GF4 has longer chain length than in comparison to the native mucilage and thus exhibits more swelling tendencies and thus can be used as very good controlled release matrix system. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00237-8DOI Listing
February 2019
1 Read

Iron oxide nanoparticulate system as a cornerstone in the effective delivery of Tc-99 m radionuclide: a potential molecular imaging probe for tumor diagnosis.

Daru 2019 Jan 31. Epub 2019 Jan 31.

Radioactive Isotopes and Generator Department, Hot Labs Center, Egyptian Atomic Energy Authority, PO13759, Cairo, Egypt.

Background: The evolution of nanoparticles has gained prominence as platforms for developing diagnostic and/or therapeutic radiotracers. This study aims to develop a novel technique for fabricating a tumor diagnostic probe based on iron oxide nanoparticles excluding the utilization of chelating ligands.

Methods: Tc-99 m radionuclide was loaded into magnetic iron oxide nanoparticles platform (MIONPs) by sonication. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00241-yDOI Listing
January 2019

Physical Characterisation of Halofantrine Encapsulated Fat Nano-Emulsions.

J Pharm Sci 2019 Jan 28. Epub 2019 Jan 28.

Howard Hughes Medical Institute, California Institute of Technology, Pasadena, CA 91125, U.S.A. and University of Queensland, Brisbane, QLD 4072 Australia.

We report the colloidal characterisation of halofantrine (Hf) laden soybean oil (SBO) fat emulsions. Hf increased the zeta potential, at all pH values, of the fat emulsions. Concomitant with this, the isoelectric point (i. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.021DOI Listing
January 2019

Proniosomal gel for transdermal delivery of lornoxicam: optimization using factorial design and in vivo evaluation in rats.

Daru 2019 Jan 30. Epub 2019 Jan 30.

Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.

Objective: Clinical utility of lornoxicam in oral therapy is primarily restricted by the low solubility and gastric adverse effects. This study evaluated the prospective of optimized proniosomal gel to improve the clinical efficacy of lornoxicam and compare with oral therapy.

Methods: Proniosomes were formulated by coacervation phase separation technique using span 60, lecithin and cholesterol. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00242-xDOI Listing
January 2019
1 Read
1.111 Impact Factor

Skin Permeation of Urea Under Finite Dose Condition.

J Pharm Sci 2019 Feb 26;108(2):987-995. Epub 2018 Oct 26.

Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, Ohio 45267. Electronic address:

In a previous study investigating the relationships between solute physicochemical properties and solvent effects on skin permeation of solutes under finite dose conditions, urea was found to have the highest percent dose absorbed among the model solutes studied. The objective of this study is to probe the mechanism of the observed high skin permeation of urea at finite dose, in contrast to its permeability coefficient obtained under infinite dose condition. Skin permeation experiments were performed with Franz diffusion cells and human epidermal membrane. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549183062
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2018.10.026DOI Listing
February 2019
3 Reads

Editorial Invitation to Become a Reviewer for the Journal of Pharmaceutical Sciences.

J Pharm Sci 2018 May 6;107(5):1209-1210. Epub 2018 Feb 6.

Department of Pharmaceutical Chemistry, University of Kansas, Lawrence, Kansas. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.01.028DOI Listing

Development and validation of a discriminatory dissolution method for rifaximin products.

J Pharm Sci 2019 Jan 24. Epub 2019 Jan 24.

Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, College Station, TX 77843. Electronic address:

The commercial product of rifaximin (RFX) contains α form. The α form can change to β form on exposure to high humidity that can occur during manufacturing, stability and/or in-use period. It is critical to maintain α form of the drug in a drug product to avoid variability in clinical response. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.020DOI Listing
January 2019

Influx and efflux transporters contribute to the increased dermal exposure to active metabolite of regorafenib after repeated oral administration in mice.

J Pharm Sci 2019 Jan 24. Epub 2019 Jan 24.

Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kakuma-machi, Kanazawa University, Kanazawa 920-1192. Electronic address:

The multi-kinase inhibitor regorafenib, which is a standard treatment for certain cancer patients after disease progression following other approved therapies, exhibits delayed-onset dermal toxicity. Here, we aimed to clarify the mechanisms that contribute to the increased dermal exposure to active metabolite M-5 of regorafenib after repeated oral administration. The dermal concentration of M-5 at 24 h after the last of five oral administrations of regorafenib in mdr1a/1b/bcrp mice was more than 190 times that in wild-type mice. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.018DOI Listing
January 2019
1 Read

Hyperhydration effect on pharmacokinetic parameters and detection sensitivity of recombinant human erythropoietin in urine and serum doping control analysis of males.

J Pharm Sci 2019 Jan 23. Epub 2019 Jan 23.

Anti-Doping Lab Qatar, Sports City Road, Sports City, P.O. Box 27775, Doha, Qatar. Electronic address:

Excessive fluid intake, i.e., hyperhydration may be adopted by athletes as a masking method during anti-doping sample collection to influence the excretion patterns of doping agents and, therefore, manipulate their detection. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.017DOI Listing
January 2019
1 Read

Impact of Precipitation of Antibody Therapeutics following Subcutaneous Injection on Pharmacokinetics and Immunogenicity.

J Pharm Sci 2019 Jan 23. Epub 2019 Jan 23.

Biosimilars Business Unit, Amgen Inc, Thousand Oaks, CA 91320.

Antibody therapeutics with poor solubility in the subcutaneous matrix may carry unintended risks when administered to patients. The objective of this work was to estimate the risk of antibodies that precipitate in vitro at neutral pH by determining the impact of poor solubility on distribution of the drug from the injection site as well as immunogenicity in vivo. Using fluorescence imaging in a mouse model, we show that one such precipitation-prone antibody is retained at the injection site in the subcutaneous space longer than a control antibody. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193003
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.015DOI Listing
January 2019
4 Reads

The Role of Surface Active Agents in Ophthalmic Drug Delivery: a comprehensive review.

J Pharm Sci 2019 Jan 23. Epub 2019 Jan 23.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt. Electronic address:

With the significant advances made in nanotechnology, research efforts focused on developing novel drug delivery platforms that can overcome the multitude of challenges encountered in ophthalmic drug delivery. Surface active agents (SAA) have been extensively used for the formulation of many of the dosage forms targeting ocular tissues. Novel ophthalmic carriers utilizing SAAs were broadly classified into particulate, vesicular and controlled release drug delivery systems. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.016DOI Listing
January 2019

Rapid Prediction of Deamidation Rates of Proteins to Assess Their Long-Term Stability Using Hydrogen Exchange-Mass Spectrometry (HX-MS).

J Pharm Sci 2019 Jan 23. Epub 2019 Jan 23.

Department of Chemistry and the Ralph N, Adams Institute for Bioanalytical Chemistry; Department of Pharmaceutical Chemistry, The University of Kansas, 1567 Irving Hill Road, Lawrence, KS 66045. Electronic address:

Deamidation is an important degradation pathway for proteins. Estimating deamidation propensities is essential for predicting their long-term stability. However, predicting deamidation rates in folded proteins is challenging because higher-order structure has a significant and unpredictable effect on deamidation. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.019DOI Listing
January 2019
1 Read

Bulk Dynamic Spray Freeze-Drying Part 2: Model-Based Parametric Study for sssssSpray-Freezing Process Characterization.

J Pharm Sci 2019 Jan 22. Epub 2019 Jan 22.

Purdue University, West Lafayette, IN.

Spray freeze-drying (SFD) is an evolving technology that combines the benefits of spray-drying and conventional lyophilization techniques to produce drug substance (DS) and drug product (DP) as free-flowing powders. The high surface-to-volume ratio associated to the sub-millimeter spray-frozen particles contributes to shorter drying and reconstitution times. The formation of frozen particles is the most critical part of this dehydration technique since it defines the properties of final product. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.011DOI Listing
January 2019
1 Read

Experiences of self-medication among people: a qualitative meta-synthesis.

Daru 2019 Jan 24. Epub 2019 Jan 24.

Department of Medical-Surgical Nursing, School of Nursing and Midwifery, Shiraz University of Medical Sciences, Shiraz, Iran.

Background: Self-medication is one of the major health-related problems in the world, which causes many problems for people and health systems. No comprehensive qualitative meta-synthesis has been done to understand the perceptions and experiences of self-medication among people.

Objectives: This study aimed to analyze, re-interpret, and synthesize the existing qualitative studies on perceptions and experiences of self-medication among people around the world. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00244-9DOI Listing
January 2019
1.111 Impact Factor

Folate-targeted polyethylene-glycol-modified photosensitizers for photodynamic therapy.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

State Key Laboratory of Medicinal Chemical Biology, Tianjin Key Laboratory of Protein Sciences, College of Life Sciences, Nankai University, Tianjin 300071, P.R.China. Electronic address:

Pyropheophorbide a (Pyro) is a promising photosensitizer; however, it has no tumor selectivity and enrichment capability. In our former work, the prepared folic acid-Pyro conjugates showed considerably improved tumor accumulation and photodynamic therapy (PDT) activity in cell- and animal-based studies. However, the targeting capability, selectivity and water solubility of the conjugate remain problematic. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.014DOI Listing
January 2019
4 Reads

Mechanism of Drug Release From Temperature-Sensitive Formulations Composed of Low-Melting-Point Microcrystalline Wax.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Department of Pharmaceutical Engineering and Drug Delivery Science, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan. Electronic address:

It was reported that wax matrix (WM) particles composed of low-melting-point microcrystalline wax showed unique release behaviors; the particles released only a small amount of the entrapped drug (non-diffusion-controlled release) at 37°C, whereas it showed comparatively fast drug release in a diffusion-controlled manner at 25°C. However, the mechanism of the drug release is still unclear. The objective of this study was to determine the mechanism of drug release from the WM particles using X-ray computed tomography. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.010DOI Listing
January 2019

Orthogonal redundant monitoring of a new continuous fluid-bed dryer for pharmaceutical processing by means of mass and energy balance calculations and spectroscopic techniques.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Novartis AG, 4002 Basel, Switzerland. Electronic address:

In line with the ongoing shift from batch- to continuous pharmaceutical production of solid oral dosage forms, a novel continuous fluid-bed dryer was developed. The forced-feed nature of the Glatt GPCG2 CM fluid-bed dryer allows continuous, first-in-first-out drying of wet granulate materials based on its compartmentalized, rotating fluidizing chamber. The presented work aims to introduce the dryer's functionalities in detail, and to demonstrate that the rotating fluid-bed chambers facilitates a stable drying behavior, which ensures robust and repeatable residual moisture contents (loss-on-drying; LOD) of the discharged granules. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.028DOI Listing
January 2019
1 Read

How Far Have We Come? Challenges to Orphan Drug Access in China, 2011-2017.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Department of Pharmacy Administration and Clinical Pharmacy, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; International Research Center for Medicinal Administration, Peking University, Beijing 100191, China. Electronic address:

Rare diseases are an important global public health issue. One significant challenge is to ensure the access to orphan drugs for patients with rare disease. This study aims to evaluate the accessibility of orphan drugs in China. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193002
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.012DOI Listing
January 2019
5 Reads

Bulk Dynamic Spray Freeze-Drying Part 1: Modeling of Droplet Cooling and Phase Change.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Purdue University, West Lafayette, IN. Electronic address:

In spray freeze-drying (SFD), the solution is typically dispersed into a gaseous cold environment producing frozen microparticles that are subsequently dried via sublimation. This technology can potentially manufacture bulk lyophilized drugs at higher rates compared to conventional freeze-drying in trays and vials since small frozen particles provide larger surface area available for sublimation. While drying in SFD still has to meet the material collapse temperature requirements, the final characteristics of the respective products are mainly controlled by the spray-freezing dynamics. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.009DOI Listing
January 2019

Physical Stability of an Amorphous Sugar Matrix Dried From Methanol as an Amorphous Solid Dispersion Carrier and the Influence of Heat Treatment.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Division of Chemistry and Biochemistry, Graduate School of Natural Science and Technology, Okayama University, 3-1-1 Tsushima-naka, Kita-ku, Okayama 700-8530, Japan. Electronic address:

An amorphous sugar matrix, after drying from an organic solvent, was investigated for use as a method for dispersing hydrophobic drugs (solid dispersion). However, the amorphous sugar, originally contained in the organic solvent, had a significantly low glass transition temperature (T), thus rendering it physically unstable. In this study, we examined the physicochemical properties of a sugar in a dried matrix and in an organic solvent, using α-maltose and methanol as a representative sugar and organic solvent. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193001
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.008DOI Listing
January 2019
1 Read

Clinical and economic impacts of clinical pharmacists' interventions in Iran: a systematic review.

Daru 2019 Jan 23. Epub 2019 Jan 23.

Department of Clinical Pharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box: 14155/6451, Tehran, 1417614411, Iran.

Objectives: There are many studies about Iranian clinical pharmacists' interventions and their impacts on medication safety and cost. The aim of this study is to collect data and critically evaluate the clinical and economic effects of Iranian clinical pharmacist interventions and activities. To our best of knowledge, this research is the first review of publications about Iranian clinical pharmacists' interventions and activities. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00245-8DOI Listing
January 2019
2 Reads

Pharmacology of dipeptidyl peptidase-4 inhibitors and its use in the management of metabolic syndrome: a comprehensive review on drug repositioning.

Daru 2019 Jan 23. Epub 2019 Jan 23.

Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

Objectives: Despite advances in our understanding of metabolic syndrome (MetS) and the treatment of each of its components separately, currently there is no single therapy approved to manage it as a single condition. Since multi-drug treatment increases drug interactions, decreases patient compliance and increases health costs, it is important to introduce single therapies that improve all of the MetS components.

Evidence Acquisition: We conducted a PubMed, Scopus, Google Scholar, Web of Science, US FDA, utdo. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00238-7DOI Listing
January 2019
1 Read

Modeling of semi-continuous fluid bed drying of pharmaceutical granules with respect to granule size.

J Pharm Sci 2019 Jan 19. Epub 2019 Jan 19.

BIOMATH, Department of Data Analysis and Mathematical Modelling, Ghent University, Belgium. Electronic address:

In the transition of the pharmaceutical industry from batch-wise to continuous drug product manufacturing, the drying process has proven challenging to control and understand. In a semi-continuous fluid bed dryer, part of the ConsiGmaTM wet granulation line, the aforementioned production methods converge. De Leersnyder et al. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.013DOI Listing
January 2019
1 Read

CRISPR/Cas9 for overcoming drug resistance in solid tumors.

Daru 2019 Jan 21. Epub 2019 Jan 21.

Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Groningen, The Netherlands.

Objectives: In this review, we focus on the application of clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR associated nuclease 9 (Cas9), as a powerful genome editing system, in the identification of resistance mechanisms and in overcoming drug resistance in the most frequent solid tumors.

Data Acquisition: Data were collected by conducting systematic searching of scientific English literature using specific keywords such as "cancer", "CRISPR" and related combinations.

Results: The review findings revealed the importance of CRISPR/Cas9 system in understanding drug resistance mechanisms and identification of resistance-related genes such as PBRM1, SLFN11 and ATPE1 in different cancers. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-019-00240-zDOI Listing
January 2019

Formation of nanosuspensions in bottom-up approach: theories and optimization.

Daru 2019 Jan 19. Epub 2019 Jan 19.

Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.

Background: Nanosuspensions, liquid dispersions with nanometer size distribution, are becoming trendy in pharmaceutical practice to formulate poorly water-soluble drugs and to enhance their bioavailability. Generally, nanosuspensions are produced in two main approaches; top-down or bottom-up. The former is based on size-reduction of large particles via milling or high pressure homogenization. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/s40199-018-00235-2DOI Listing
January 2019
1 Read

Solubility and Permeability Improvement of Quercetin by an Interaction Between α-Glucosyl Stevia Nanoaggregates and Hydrophilic Polymer.

J Pharm Sci 2019 Jan 14. Epub 2019 Jan 14.

Laboratory of Formulation Design and Pharmaceutical Technology, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan. Electronic address:

The effect of composite formation between α-glucosyl stevia (Stevia-G) and hydrophilic polymers on solubility and permeability enhancement of quercetin hydrate (QUE) was evaluated. Polyvinylpyrrolidone K-30 (PVP), hydroxypropyl methylcellulose 2910-E (HPMC), and hydroxypropyl cellulose SSL (HPC) were selected as candidate hydrophilic polymers. Fluorescence studies with pyrene and curcumin suggested composite formation occurs between Stevia-G aggregate and polymers. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193001
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.007DOI Listing
January 2019
12 Reads

Incorporation With Dendrimer-Like Biopolymer Leads to Improved Soluble Amount and In Vitro Anticancer Efficacy of Paclitaxel.

Authors:
Ying Xie Yuan Yao

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Department of Food Science, Purdue University, West Lafayette, Indiana 47907. Electronic address:

The aim of this study was to explore the solubilization efficacy of octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer, in improving the soluble amount and efficacy of paclitaxel (PTX), a potent anticancer active pharmaceutical ingredient. PTX was incorporated with OHPP in the form of solid dispersion (PTX-OHPP SD), which was characterized for its PTX crystallinity, interactions between PTX and OHPP, PTX soluble amount and dissolution profile, and in vitro inhibitory efficacy against cancer cell lines. The incorporation with OHPP led to the amorphous state of PTX. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.026DOI Listing
January 2019
1 Read

Quantitative X-Ray Microcomputed Tomography Assessment of Internal Tablet Defects.

J Pharm Sci 2019 Jan 10. Epub 2019 Jan 10.

Small Molecule Pharmaceutics, Genentech, Inc., One DNA Way, South San Francisco, California 94080. Electronic address:

Physical tablet defects are related to internal structural defects that are not easily assessed by the traditional methods, such as dusting, laminating, or fracturing during appearance, friability, or hardness testing. Also, these methods do not allow objective and quantitative investigation of the role of formulation and process variables, which is essential for quality-by-design drug product development. In this study, an X-ray microcomputed tomography (XμCT) method to analyze internal tablet defects is developed using tablets from a quality-by-design design-of-experiment study. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.024DOI Listing
January 2019

A Kinetic Approach to Determining Drug Distribution in Complex Biphasic Systems.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Division of Product Quality Research, Office of Testing and Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, Maryland 20993. Electronic address:

Pharmaceutical emulsions contain multiple components, such as micellar, aqueous, and oil phases, leading to complex drug transfer and equilibrium phenomena. These complex components present challenges for the bioequivalence assessment of the drug products. The objective of the study was to develop a method that can probe the underlying mechanism and process of drug distribution. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193000
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.003DOI Listing
January 2019
4 Reads

Drug Carrier-Oriented Polygeline for Preparing Novel Polygeline-Bound Paclitaxel Nanoparticles.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

School of Life Science, Wuchang University of Technology, Wuhan 430223, PR China. Electronic address:

Polygeline is a highly promising drug carrier-oriented material for important applications in pharmacy field due to its low-cost and unique properties similar to albumin. In this study, polygeline-bound paclitaxel nanoparticles (Npb-PTXS) were fabricated through a combination of low-pressure emulsification and high-pressure homogenization. The effects of a series of production parameters on mean particle size, particle size distribution and drug loading of Npb-PTXS were systematically evaluated. Read More

View Article

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S00223549193001
Publisher Site
http://dx.doi.org/10.1016/j.xphs.2019.01.005DOI Listing
January 2019
6 Reads

Probing the Tryptophan Environment in Therapeutic Proteins: Implications for Higher Order Structure on Tryptophan Oxidation.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Molecular and Analytical Development, Bristol-Myers Squibb, 311 Pennington Rocky Hill Road, Pennington, New Jersey 08534.

Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,2'-azobis(2-amidinopropane) dihydrochloride. Fluorescence spectroscopy, in combination with second derivative analysis, demonstrates that the loss of Trp fluorescence intensity is a sensitive indicator of Trp oxidation in mAbs. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.027DOI Listing
January 2019
1 Read

Modeling the Air Pressure Increase Within a Powder Bed During Compression-A Step Toward Understanding Tablet Defects.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Merck & Co. Inc., Kenilworth, New Jersey 07033.

The cause of tablet defects, such as cracking, bubbling, and capping, during compression is currently not fully understood. Prior experimental work suggests that an increase in internal air pressure on powder compression can directly contribute to the formation of cracks within a tablet. The present study examines the air pressure increase on compression in a fully two-dimensional axisymmetric tablet geometry while being coupled to a plasticity model describing the evolution of tablet relative density on consolidation. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.002DOI Listing
January 2019

Factors influencing polysorbate's sensitivity against enzymatic hydrolysis and oxidative degradation.

J Pharm Sci 2019 Jan 10. Epub 2019 Jan 10.

Coriolis Pharma Research, Fraunhoferstr. 18b, 82152 Martinsried, Germany.

The aim was to compare the sensitivity of different grades of polysorbate 20 and polysorbate 80 against enzymatic hydrolysis and oxidative degradation in pharmaceutically relevant buffer systems. For this purpose, a fast liquid chromatography charged aerosol detection (LC-CAD) method was developed which allows to (i) differentiate between hydrolytic and oxidative polysorbate degradation, and (ii) to monitor the polysorbate decay over time. Systematic enzymatic and oxidative forced degradation studies were conducted with multicompendial polysorbate 20 and 80, as well as all-laurate PS20 and all-oleate PS80 (with >98% oleic acid, as required by the Chinese Pharmacopoiea since 2015). Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.006DOI Listing
January 2019
1 Read

In Vitro Oral Cavity Model for Screening the Disintegration Behavior of Orodispersible Films: A Bespoke Design.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Department of Mechanical Engineering, London, UK.

The availability of biorelevant methods for the disintegration study of pharmaceutical orodispersible dosage forms is required. The disintegration of orodispersibles should be assessed using in vitro methods that can combine biorelevant volumes of disintegration medium and mechanical stresses mimicking in vivo conditions. This study proposes an adaptation of a mechanical oral cavity model for the disintegration study of orodispersible films. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.025DOI Listing
January 2019

Cyclodextrin Reduces Intravenous Toxicity of a Model Compound.

J Pharm Sci 2019 Jan 11. Epub 2019 Jan 11.

Departments of Small Molecule Pharmaceutical Sciences, Genentech, Inc., One DNA Way, South San Francisco, California 94080. Electronic address:

Solubilization of new chemical entities for toxicity assessment must use excipients that do not negatively impact drug pharmacokinetics and toxicology. In this study, we investigated the tolerability of a model freebase compound, GDC-0152, solubilized by pH adjustment with succinic acid and complexation with hydroxypropyl-β-cyclodextrin (HP-β-CD) to enable intravenous use. Solubility, critical micelle concentration, and association constant with HP-β-CD were determined. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2019.01.004DOI Listing
January 2019
1 Read
2.590 Impact Factor

Control of protein adsorption to cyclo olefin polymer by the Hofmeister effect.

J Pharm Sci 2019 Jan 8. Epub 2019 Jan 8.

Institute of Medical Science, The University of Tokyo, Shirokanedai, Minato-ku, Tokyo 108-8639, Japan; Department of Bioengineering, School of Engineering, The University of Tokyo, Hongo, Tokyo 113-8656, Japan. Electronic address:

Cyclo olefin polymer (COP) is an attractive plastic because it has low protein adsorption despite its hydrophobic chemical structure. Here, the adsorption of model proteins to the COP was evaluated in comparison with a representative plastic, polystyrene (PSt), using reflectometry interference spectroscopy (RIfS) technology. The effects of different salts on adsorption were then examined. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.023DOI Listing
January 2019
1 Read

Impact of Surface-Engineered ZnO Nanoparticles on Protein Corona Configuration and Their Interactions With Biological System.

J Pharm Sci 2019 Jan 5. Epub 2019 Jan 5.

Biochemistry Laboratory, Animal Facility, Regulatory Toxicology Group, CSIR-Indian Institute of Toxicology Research (CSIR-IITR), Vishvigyan Bhavan, 31, Mahatma Gandhi Marg, Lucknow 226001, Uttar Pradesh, India. Electronic address:

In biological system, the interaction between nanoparticles (NPs) and serum biomolecules results in the formation of a dynamic corona of different affinities. The formed corona enriched with opsonin protein is recognized by macrophages and immune effector cells, resulting in rapid clearance with induced toxicity. Hence, to reduce corona genesis, surface-engineered ZnO (c-ZnO) NPs were in situ synthesized using a polyacrylamide-grafted guar gum (PAm-g-GG) polymer that provided surface neutrality to the NPs. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.021DOI Listing
January 2019
2 Reads
2.590 Impact Factor

The CSD Drug Subset: The Changing Chemistry and Crystallography of Small Molecule Pharmaceuticals.

J Pharm Sci 2019 Jan 5. Epub 2019 Jan 5.

AstraZeneca, PR&D, Silk Road Business Park, Macclesfield SK10 2NA, Cheshire.

We report the generation and statistical analysis of the CSD drug subset: a subset of the Cambridge Structural Database (CSD) consisting of every published small-molecule crystal structure containing an approved drug molecule. By making use of InChI matching, a CSD Python API workflow to link CSD entries to the online database Drugbank.ca has been produced. Read More

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.xphs.2018.12.011DOI Listing
January 2019
1 Read