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https://www.readbyqxmd.com/read/29326082/pharmaceutical-nanocrystals-production-by-wet-milling-and-applications
#1
REVIEW
Maria Malamatari, Kevin M G Taylor, Stavros Malamataris, Dennis Douroumis, Kyriakos Kachrimanis
Nanocrystals are regarded as an important nanoformulation approach exhibiting advantages of increased dissolution and saturation solubility with chemical stability and low toxicity. Nanocrystals are produced in the form of nanosuspensions using top-down (e.g., wet milling or high pressure homogenization) and bottom-up methods (e.g., antisolvent precipitation). Wet milling is a scalable method applicable to drugs with different physicochemical and mechanical properties. Nanocrystalline-based formulations, either as liquid nanosuspensions or after downstream processing to solid dosage forms, have been developed as drug delivery systems for various routes of administration (i...
January 8, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29306735/identification-of-metabolites-of-mdr-1339-an-inhibitor-of-%C3%AE-amyloid-protein-aggregation-and-kinetic-characterization-of-the-major-metabolites-in-rats
#2
Jun-Hyeng Son, Yoo-Seong Jeong, Jong-Hwa Lee, Min-Soo Kim, Kyeong-Ryoon Lee, Chang-Koo Shim, Young Ho Kim, Suk-Jae Chung
We previously reported that MDR-1339, an inhibitor of β-amyloid protein aggregation, was likely to be eliminated by biotransformation in rats. The objective of this study was to determine the chemical identity of metabolites derived from this aggregate inhibitor and to characterize the kinetics of formation of these metabolites in rats. Using high performance liquid chromatography coupled with mass spectrometry with a hybrid triple quadrupole-linear ion trap, 7 metabolites and 1 potential metabolic intermediate were identified in RLM incubations containing MDR-1339...
January 3, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29301050/field-detection-of-drugs-of-abuse-in-oral-fluid-using-the-alere%C3%A2-dds%C3%A2-2-mobile-test-system-with-confirmation-by-liquid-chromatography-tandem-mass-spectrometry-lc-ms-ms
#3
Alex J Krotulski, Amanda L A Mohr, Melissa Friscia, Barry K Logan
The collection and analysis of drugs in oral fluid (OF) at the roadside has become more feasible with the introduction of portable testing devices such as the Alere™ DDS®2 Mobile Test System (DDS®2). The objective of this study was to compare the on-site results for the DDS®2 to laboratory-based confirmatory assays with respect to detection of drugs of abuse in human subjects. As part of a larger Institutional Review Board approved study, two OF samples were collected from each participant at a music festival in Miami, FL, USA...
December 28, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29296084/development-and-characterization-of-p1025-loaded-bioadhesive-liquid-crystalline-system-for-the-prevention-of-streptococcus-mutans-biofilms
#4
Giovana Maria Fioramonti Calixto, Cristiane Duque, Kelly Limi Aida, Vanessa Rodrigues Dos Santos, Loiane Massunari, Marlus Chorilli
Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025-1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29291414/5-fu-induced-gastrointestinal-damage-impairs-the-absorption-and-anticoagulant-effects-of-dabigatran-etexilate
#5
Kazunari Tsujii, Tomoki Hattori, Ayuko Imaoka, Takeshi Akiyoshi, Hisakazu Ohtani
PURPOSE: Fluoropyrimidines, including 5-fluororacil (5-FU), cause gastrointestinal damage in the clinical setting and might affect the gastrointestinal absorption of concomitantly administered drugs. We aimed to evaluate the effects of fluoropyrimidine-induced gastrointestinal damage on the pharmacokinetics and pharmacodynamics of dabigatran etexilate (DABE), an anticoagulant, in rats with gastrointestinal damage induced by the repeated oral administration of 5-FU. METHODS: Rats were administered DABE orally or dabigatran (DAB), an active moiety of DABE, intravenously...
December 29, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29290355/in%C3%A2-vitro-and-in%C3%A2-vivo-effects-of-selected-fibers-on-the-pharmacokinetics-of-orally-administered-carbamazepine-possible-interaction-between-therapeutic-drugs-and-semisolid-enteral-nutrients
#6
Katsuhito Nagai, Sachiko Omotani, Miki Otani, Moe Sasatani, Takahiro Takashima, Yasutoshi Hatsuda, Junji Mukai, Michiaki Myotoku
OBJECTIVE: The management of nutrition using semisolid enteral nutrients is considered useful for avoiding the adverse effects associated with liquid enteral nutrients. In the present study, we used an in vitro analysis to investigate whether carbamazepine (CBZ) is adsorbed by the fibers included in semisolid enteral nutrients. The effects of these fibers on the pharmacokinetic profile of CBZ following its oral administration were also examined in rats. METHODS: The adsorption of CBZ onto fibers was examined by absorbance monitoring of the filtrate after centrifugation using an ultrafiltration device...
February 2018: Nutrition
https://www.readbyqxmd.com/read/29286316/development-and-validation-of-an-uplc-ms-ms-method-for-pharmacokinetic-comparison-of-five-alkaloids-from-jinqi-jiangtang-tablets-and-its-monarch-drug-coptidis-rhizoma
#7
Lili Sun, Feifei Ding, Guangjiao You, Han Liu, Meng Wang, Xiaoliang Ren, Yanru Deng
JinQi Jiangtang (JQJT) tablets, a Chinese patent medicine approved by the State Food and Drug Administration, are composed of Coptidis Rhizoma, Astragali Radix, and Lonicerae Japonicae Flos, and have a significant effect on diabetes. Coptidis Rhizoma is monarch drug in the prescription. The aim of the present study was to investigate and compare the pharmacokinetics of multiple ingredients from JQJT tablets and Coptidis Rhizoma extract (CRE) following oral administration in rats. Five alkaloids: coptisine chloride, epiberberine chloride, berberine chloride, jatrorrhizine chloride, and palmatine chloride, were simultaneously determined in rat plasma using established and validated ultra-high performance liquid chromatography mass spectrometry (UPLC-MS/MS)...
December 29, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29284110/efficacy-of-lenvatinib-a-multitargeted-tyrosine-kinase-inhibitor-on-laser-induced-cnv-mouse-model-of-neovascular-amd
#8
Xian Wei, Ting Zhang, Yuqin Yao, Shaoxue Zeng, Min Li, Haotian Xiang, Chengjian Zhao, Guiqun Cao, Minhui Li, Ran Wan, Ping Yang, Jinliang Yang
Neovascular age-related macular degeneration (AMD) is a leading cause of vision loss worldwide. Although intravitreal injection of anti-VEGF antibodies and VEGF Trap have significant clinical benefits, the complications of intravitreal injection, drug resistance and patient compliance still need to be concerned. In this study, the effects of an orally administered multi-targeted tyrosine kinase inhibitor (Lenvatinib, E7080) were evaluated in vitro and in vivo on neovascular AMD mouse model. The results showed that E7080 effectively inhibited the proliferation, migration and tubule formation of human choroidal microvascular endothelial cells (HCMECs), and suppressed the angiogenesis of zebrafish subintestinal vessels without causing malformation...
December 25, 2017: Experimental Eye Research
https://www.readbyqxmd.com/read/29283445/simultaneous-analysis-of-oral-anticancer-drugs-for-renal-cell-carcinoma-in-human-plasma-using-liquid-chromatography-electrospray-ionization-tandem-mass-spectrometry
#9
Shinya Takasaki, Masaki Tanaka, Masafumi Kikuchi, Masamitsu Maekawa, Yoshihide Kawasaki, Akihiro Ito, Yoichi Arai, Hiroaki Yamaguchi, Nariyasu Mano
An analytical method using high performance liquid chromatography/electrospray ionization tandem mass spectrometry has been developed and validated for simultaneous measurement of four tyrosine kinase inhibitors used for renal cell carcinoma and their metabolites in human plasma. Despite their similar structures, it is difficult to measure plasma levels of these compounds simultaneously using optimal MS parameters for each compound because a quantitative range exceeding 50,000-fold is required. To overcome this problem, we used a linear range shift technique using in-source collision-induced dissociation...
December 28, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29259982/pharmacokinetics-tissue-distribution-and-metabolism-study-of-icariin-in-rat
#10
Shunjun Xu, Jiejing Yu, Jingjing Zhan, Liu Yang, Longgang Guo, Yijuan Xu
Icariin is one of the predominant flavonoids contained in Herba Epimedii (Yin-yang-huo in Chinese), a well-known Chinese medicine for the treatment of cancers and immune system diseases. Although Herba Epimedii has been widely used in China and there are so many and various research reports on the herbal drug and its main flavones, very limited data is available on the tissue distribution and biotransformation of icariin. In the present study, a liquid chromatographic method combined with electrospray ionization tandem mass spectrometry was developed to quantify the concentration of icariin in rat plasma and various tissues collected at different time points after oral administration of the total flavonoid extract of Herba Epimedii at a dose of 0...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29248606/comparison-of-a-revaprazan-loaded-solid-dispersion-solid-snedds-and-inclusion-compound-physicochemical-characterisation-and-pharmacokinetics
#11
Jong Hyuck Park, Dong Shik Kim, Omer Mustapha, Abid Mehmood Yousaf, Jung Suk Kim, Dong Wuk Kim, Chul Soon Yong, Yu Seok Youn, Kyung Taek Oh, Soo-Jeong Lim, Jong Oh Kim, Han-Gon Choi
The aim of this research was to compare three strategies for enhancing the solubility of poorly water-soluble revaprazan hydrochloride: solid dispersion, solid SNEDDS and inclusion compound. The influence of polymers, surfactants and oils on the drug solubility was assessed, and via the chosen carriers, the three types of formulations were prepared utilising spray drying technique. Their physicochemical properties, solubility, dissolution and pharmacokinetics in rats were performed compared with revaprazan powder...
December 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29247960/application-of-miniaturized-near-infrared-spectroscopy-for-quality-control-of-extemporaneous-orodispersible-films
#12
Wen Chin Foo, Effendi Widjaja, Yuet Mei Khong, Rajeev Gokhale, Sui Yung Chan
Extemporaneous oral preparations are routinely compounded in the pharmacy due to a lack of suitable formulations for special populations. Such small-scale pharmacy preparations also present an avenue for individualized pharmacotherapy. Orodispersible films (ODF) have increasingly been evaluated as a suitable dosage form for extemporaneous oral preparations. Nevertheless, as with all other extemporaneous preparations, safety and quality remain a concern. Although the United States Pharmacopeia (USP) recommends analytical testing of compounded preparations for quality assurance, pharmaceutical assays are typically not routinely performed for such non-sterile pharmacy preparations, due to the complexity and high cost of conventional assay methods such as high performance liquid chromatography (HPLC)...
December 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29246439/development-of-solidified-self-microemulsifying-drug-delivery-systems-containing-l-tetrahydropalmatine-design-of-experiment-approach-and-bioavailability-comparison
#13
Nguyen-Thach Tung, Cao-Son Tran, Thi-Minh-Hue Pham, Hoang-Anh Nguyen, Tran-Linh Nguyen, Sang-Cheol Chi, Dinh-Duc Nguyen, Thi-Bich-Huong Bui
The study first aimed to apply a design of experiment (DoE) approach to investigate the influences of excipients on the properties of liquid self-microemulsifying drug delivery system (SMEDDS) and SMEDDS loaded in the pellet (pellet-SMEDDS) containing l-tetrahydropalmatine (l-THP). Another aim of the study was to compare the bioavailability of l-THP suspension, liquid SMEDDS and pellet-SMEDDS in the rabbit model. By using Central Composite Face design (CCF), the optimum ratio of Capryol 90, and Smix `(Cremophor RH 40: Transcutol HP) in the formulation of SMEDDS was determined...
December 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29246256/effect-of-oral-glycine-on-the-clinical-spirometric-and-inflammatory-status-in-subjects-with-cystic-fibrosis-a-pilot-randomized-trial
#14
Mario H Vargas, Rosangela Del-Razo-Rodríguez, Amando López-García, José Luis Lezana-Fernández, Jaime Chávez, María E Y Furuya, Juan Carlos Marín-Santana
BACKGROUND: Patients with cystic fibrosis (CF) have airway inflammation that contributes to symptoms and to pulmonary function derangement. Current drugs used to diminish airway inflammation improve the clinical and spirometric status of patients with CF, but their use is limited due to their undesired side effects, for example, glucose intolerance, growth retardation, and cataracts with corticosteroids, gastrointestinal toxicity with ibuprofen, and macrolide resistance with azythromycin...
December 15, 2017: BMC Pulmonary Medicine
https://www.readbyqxmd.com/read/29220339/to-flavor-or-not-to-flavor-extemporaneous-omeprazole-liquid
#15
Monica C Chuong, Catherine A Taglieri, Stephen G Kerr
Omeprazole is a proton pump inhibitor used to treat the symptoms of gastro esophageal reflux disease, ulcers, excess stomach acid, infection with Helicobacter pylori, and to control the gastric side effects of various drugs. The approved dosage forms in the U.S. are powder in compounding kits, delayed-release granules for oral suspension, oral delayed-release tablets, and oral delayed-release capsules. An extemporaneously compounded unsweetened oral liquid method, published in the International Journal of Pharmaceutical Compounding, was found to be commonly used by pharmacists...
November 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/29217494/regulation-of-the-kynurenine-metabolism-pathway-by-xiaoyao-san-and-the-underlying-effect-in-the-hippocampus-of-the-depressed-rat
#16
Jiajia Wang, Xiaofang Li, Shugui He, Lijun Hu, Jiewen Guo, Xiangning Huang, Jinqing Hu, Yaoqun Qi, Bin Chen, Dewei Shang, Yuguan Wen
ETHNOPHARMACOLOGICAL RELEVANCE: Xiaoyao San (XYS) is a classic Chinese herbal formula for treatment of depression. The present study aimed to investigate the antidepressant effects of XYS in a rat model of chronic unpredictable mild stress (CUMS) and the underlying mechanisms. MATERIALS AND METHODS: A CUMS rat model of depression was established via 4 weeks of unpredictable stimulation. Then the rats were orally administered paroxetine and XYS for 2 weeks with continued stress...
December 4, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29216620/physicochemical-stability-of-an-oral-suspension-of-trimethoprim-20-mg-ml-in-combination-with-sulfadiazine-200-mg-ml-in-pcca-base-suspendit
#17
Richard A Graves, Kelly V Phan, Levon A Bostanian, Tarun K Mandal, Yashoda V Pramar
Trimethoprim is a diaminopyrimidine antibacterial agent that, like sulfonamides, inhibits bacterial folic acid synthesis, but at a different stage in the metabolic pathway. It has a similar spectrum of activity to the sulfonamides and is given by mouth or by injection, either alone or in conjunction with a sulfonamide, such as sulfadiazine. Sulfadiazine is a bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. The combination of the two drugs produces a synergistic effect against both Gram-positive and Gram-negative aerobic bacteria, by inhibiting enzymes in the folic acid pathways, which in turn inhibits bacterial thymidine synthesis...
September 2017: International Journal of Pharmaceutical Compounding
https://www.readbyqxmd.com/read/29208749/development-of-anti-virulence-approaches-for-candidiasis-via-a-novel-series-of-small-molecule-inhibitors-of-candida-albicans-filamentation
#18
Jesus A Romo, Christopher G Pierce, Ashok K Chaturvedi, Anna L Lazzell, Stanton F McHardy, Stephen P Saville, Jose L Lopez-Ribot
Candida albicans remains the main etiologic agent of candidiasis, the most common fungal infection and now the third most frequent infection in U.S. hospitals. The scarcity of antifungal agents and their limited efficacy contribute to the unacceptably high morbidity and mortality rates associated with these infections. The yeast-to-hypha transition represents the main virulence factor associated with the pathogenesis of C. albicans infections. In addition, filamentation is pivotal for robust biofilm development, which represents another major virulence factor for candidiasis and further complicates treatment...
December 5, 2017: MBio
https://www.readbyqxmd.com/read/29205111/a-review-on-oral-liquid-as-an-emerging-technology-in-controlled-drug-delivery-system
#19
Sangmesh Raosaheb Torne, Angappan Sheela, N C Sarada
BACKGROUND: The oral liquid drug delivery system (OLDDS) remains as the primary choice of dosage form, though challenging, for the pharmaceutical scientists. In the last two decades, Oral Liquid Controlled Release (OLCR) formulation has gained a lot of attention because of its advantages over the conventional dosage forms. METHOD: The world of nanotechnology has paved multiple ways to administer the drug through oral cavity in liquid dosage form with an additional advantage of control over the release...
December 3, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29201457/the-effect-of-cm082-an-oral-tyrosine-kinase-inhibitor-on-experimental-choroidal-neovascularization-in-rats
#20
Chengda Ren, Hui Shi, Juanjuan Jiang, Qingyu Liu, Yaru Du, Mengmei He, Wenting Cai, Qingquan Wei, Jing Yu
The aims of this study were to evaluate the effects of CM082 on the development of choroidal neovascularization (CNV) in a laser-induced CNV rat model and to determine the drug concentration in the ocular tissues. After the laser-induced CNV model was established in rats, CM082 was orally administered. The effects of CM082 on the CNV lesions were assessed using fundus fluorescein angiography (FFA), CNV histology, and retinal pigment epithelium- (RPE-) choroid-sclera eyecup analysis. The concentrations of CM082 in the plasma and eye tissues were determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS)...
2017: Journal of Ophthalmology
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