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https://www.readbyqxmd.com/read/28533680/preparation-characterization-and-in-vitro-vivo-studies-of-oleanolic-acid-loaded-lactoferrin-nanoparticles
#1
Xiaojing Xia, Haowei Liu, Huixia Lv, Jing Zhang, Jianping Zhou, Zhiying Zhao
Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailability owing to low solubility (<1 μg/mL) and biomembrane permeability. We developed a novel OA nanoparticle (OA-NP)-loaded lactoferrin (Lf) nanodelivery system with enhanced in vitro OA dissolution and improved oral absorption and bioavailability. The OA-NPs were prepared using NP albumin-bound technology and characterized using dynamic light scattering, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro dissolution test...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28530056/-cutaneous-leishmaniasis-in-israel-2016-an-update
#2
REVIEW
Michal Solomon, Eli Schwartz
Leishmaniasis is endemic in Israel and is increasing in its frequency. The pathogens that cause cutaneous leishmaniasis (CL) in Israel are Leishmania major (L. major) and Leishmania tropica (L. tropica). In recent years, there have been significant changes in the distribution of these species. L. major is endemic mainly in the Negev, Arava and the Beit She'an Valley. L. tropica is endemic in Tiberias, northern Sea of Galilee, Samaria and in the vicinity of Jerusalem such as at Kfar Adumim, Ma'ale Adumim and Anathoth (north-east of Jerusalem)...
October 2016: Harefuah
https://www.readbyqxmd.com/read/28528850/overview-of-solidification-techniques-for-self-emulsifying-drug-delivery-systems-from-industrial-perspective
#3
J Mandić, A Zvonar Pobirk, F Vrečer, M Gašperlin
Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different solidification techniques selfemulsifying powders, granules, pellets and tablets can be produced...
May 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28512133/quality-of-compounded-hydrocortisone-capsules-used-in-the-treatment-of-children
#4
Uta Neumann, Daniela Burau, Sarah Spielmann, Martin Whitaker, Richard J Ross, Charlotte Kloft, Oliver Blankenstein
Objectives: Due to the lack of paediatric licensed formulations, children are often treated with individualized pharmacy-compounded adult medication. An international web-based survey about the types of medication in children with adrenal insufficiency (AI) revealed that the majority of paediatric physicians are using pharmacy-compounded medication to treat children with AI. Observations of loss of therapy control in children with congenital adrenal hyperplasia with compounded hydrocortisone capsules and regained control after prescribing a new hydrocortisone batch led to this "real world" evaluation of pharmacy-compounded paediatric hydrocortisone capsules...
May 16, 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/28495196/pharmacokinetics-of-a-novel-spot-on-formulation-of-praziquantel-for-dogs
#5
María Laura Gutiérrez, Guillermo Di Federico, Jorge A Dale, Juan M Minoia, Carlos D Corrales, Paula Schaiquevich, Silvia Wikinski
Praziquantel (PZQ) is an anthelmintic drug used both in humans and animals that can be administered through various routes. There are transdermal formulations for cats, but only oral or subcutaneous dosage forms for dogs. Given the fact that the cat's skin and the dog's skin have different characteristics, which in turn affect bioavailability, we developed a PZQ spot-on formulation for dogs. This study was aimed at determining the plasmatic behavior of topically administered PZQ (Labyes(®)) in adult dogs. Dogs were administered PZQ (14...
May 30, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28494732/pharmacokinetics-of-botanical-drugs-and-plant-extracts
#6
Gina Paola Domínguez Moré, Paola Andrea Cárdenas, Geison M Costa, Cláudia M O Simões, Diana Marcela Aragón
Botanical drugs contain plant extracts, which are complex mixtures of compounds. As with conventional drugs, it is necessary to validate their efficacy and safety through preclinical and clinical studies. However, pharmacokinetic studies for active constituents or characteristic markers in botanical drugs are rare. The objective of this review was to investigate the global state of the art in pharmacokinetic studies of active ingredients present in plant extracts and botanical drugs. A review of pharmacokinetics studies of chemical constituents of plant extracts and botanical drugs was performed, with a total of 135 studies published between January 2004 and February 2015 available in recognized scientific databases...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28485775/determination-of-phloroglucinol-by-hplc-ms-ms-and-its-application-to-a-bioequivalence-study-in-healthy-volunteers
#7
X-Q Li, R-T Wang, Q-H Wang, X-L Tang, C-T Lu, H-G Gong, A-D Wen
OBJECTIVE: The aim of this study was to compare the pharmacokinetic characteristics of phloroglucinol between an orally disintegrating tablet and an orally lyophilized tablet of phloroglucinol in healthy volunteers under fasting condition. PATIENTS AND METHODS: A rapid and simple method based on high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method has been developed and validated for the determination of phloroglucinol in human plasma...
April 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28482575/risedronate-transdermal-delivery-system-based-on-a-fumaric-copolymer-for-therapy-of-osteoporosis
#8
Magalí Pasqualone, Héctor A Andreetta, M Susana Cortizo
Transdermal drug delivery system (TDDS) could be seen as alternative to the oral administration which avoids several adverse effects. In this study a novel TDDS for risedronate (RI), a bisphosphonate used for osteoporosis treatment, based on a vinyl acetate-dioctylfumarate copolymer, poly(VA-co-DOF), previously synthetized, was developed. Two membranes including 6 and 12% (w/w) of drug were obtained, which exhibited good transparence and homogeneous drug distribution, as evaluated by optical microscopy. FTIR spectroscopy and differential scanning calorimetry (DSC) analysis showed no significant drug/polymer interactions, only a plasticizer effect...
July 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28479357/hexagonal-liquid-crystalline-nanodispersions-proven-superiority-for-enhanced-oral-delivery-of-rosuvastatin-in-vitro-characterization-and-in-vivo-pharmacokinetic-study
#9
Mai Mahmoud Gabr, Sana Mohamed Mortada, Marwa Ahmed Sallam
This study aimed to explore the potential of tailoring the liquid crystalline structure for augmenting the oral absorption and biopharmaceutical performance of Rosuvastatin. Rosuvastatin-loaded liquid crystalline nanodispersions (LCNDs) were prepared via emulsification technique. The effect of incorporating oleic acid (OA) in various proportions in the lipid domain of the LCNDs was studied. The formulations were characterized for particle size, zeta potential, in-vitro release, ex-vivo intestinal permeation, in-vivo oral bioavailability and stability...
May 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28478689/micropellets-coated-with-kollicoat%C3%A2-smartseal-30d-for-taste-masking-in-liquid-oral-dosage-forms
#10
Andriy Dashevskiy, Valentyn Mohylyuk, Abid Riaz Ahmed, Karl Kolter, Felicitas Guth, Roland Bodmeier
The objective of this study was to develop delivery systems for taste masking based on multiparticulates coated with Kollicoat(®) Smartseal 30 D formulated as liquid oral suspensions. Coating of particles containing bitter drugs with Kollicoat(®) Smartseal reduced drug leaching into aqueous medium, especially when increasing pH, therefore can be used for the formulation of liquid dosage forms. Application of an intermediate layer of ion exchange resins between drug layer and coating can further decrease drug leaching into aqueous vehicle that is beneficial in terms of taste masking...
May 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28476132/efficacy-and-safety-of-rebamipide-liquid-for-chemoradiotherapy-induced-oral-mucositis-in-patients-with-head-and-neck-cancer-a-multicenter-randomized-double-blind-placebo-controlled-parallel-group-phase-ii-study
#11
T Yokota, T Ogawa, S Takahashi, K Okami, T Fujii, K Tanaka, S Iwae, I Ota, T Ueda, N Monden, K Matsuura, H Kojima, S Ueda, K Sasaki, Y Fujimoto, Y Hasegawa, T Beppu, H Nishimori, S Hirano, Y Naka, Y Matsushima, M Fujii, M Tahara
BACKGROUND: Recent preclinical and phase I studies have reported that rebamipide decreased the severity of chemoradiotherapy-induced oral mucositis in patients with oral cancer. This placebo-controlled randomized phase II study assessed the clinical benefit of rebamipide in reducing the incidence of severe chemoradiotherapy-induced oral mucositis in patients with head and neck cancer (HNC). METHODS: Patients aged 20-75 years with HNC who were scheduled to receive chemoradiotherapy were enrolled...
May 5, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28473245/the-development-and-use-of-a-drug-induced-immunosuppressed-rat-model-to-screen-phela-for-mechanism-of-immune-stimulation
#12
Makhotso Rose Lekhooa, Andrew Walubo, Jan B du Plessis, Motlalepula Gilbert Matsabisa
ETHNOPHARMACOLOGY RELEVANCY: Phela, is code name for a medicinal product made from four South African traditional medicinal plants (Clerodendrum glabrum E. Mey, Polianthes tuberosa (Linn.), Rotheca myricoides (Hochst.) Steane & Mabb. and Senna occidentalis (L.) Link). All these plants have established traditional use in a wide spectrum of diseases. It is under development for use as an immune booster in immunocompromised patients, which includes patients with the human immunodeficiency virus (HIV)...
May 1, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28461264/development-of-nanostructured-lipid-carriers-for-intraoral-delivery-of-domperidone
#13
Carolin Tetyczka, Martin Griesbacher, Markus Absenger-Novak, Eleonore Fröhlich, Eva Roblegg
The oral cavity displays one potentially attractive route that is not associated with gastric transit and hepatic first pass metabolism. However, poorly soluble active candidates require a drug delivery system to facilitate their transport through oral biological membranes. To this end, nanostructured lipid carriers (NLC) were loaded with Domperidone and produced with high pressure homogenization. NLC were characterized regarding particle size, particle size distribution, zeta potential, entrapment efficiency and crystallinity...
April 29, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28460889/safety-and-efficacy-of-olesoxime-in-patients-with-type-2-or-non-ambulatory-type-3-spinal-muscular-atrophy-a-randomised-double-blind-placebo-controlled-phase-2-trial
#14
Enrico Bertini, Eric Dessaud, Eugenio Mercuri, Francesco Muntoni, Janbernd Kirschner, Carol Reid, Anna Lusakowska, Giacomo P Comi, Jean-Marie Cuisset, Jean-Louis Abitbol, Bruno Scherrer, Patricia Sanwald Ducray, Jeppe Buchbjerg, Eduardo Vianna, W Ludo van der Pol, Carole Vuillerot, Thomas Blaettler, Paulo Fontoura
BACKGROUND: Spinal muscular atrophy (SMA) is a progressive motor neuron disease causing loss of motor function and reduced life expectancy, for which limited treatment is available. We investigated the safety and efficacy of olesoxime in patients with type 2 or non-ambulatory type 3 SMA. METHODS: This randomised, double-blind, placebo-controlled, phase 2 study was done in 22 neuromuscular care centres in Belgium, France, Germany, Italy, Netherlands, Poland, and the UK...
April 28, 2017: Lancet Neurology
https://www.readbyqxmd.com/read/28460165/development-of-a-rapidly-dissolvable-oral-pediatric-formulation-for-mefloquine-using-liposomes
#15
Wei-Lun Tang, Wei-Hsin Sophia Tang, Weihsu Claire Chen, Charles Diako, Carolyn F Ross, Shyh-Dar Li
Mefloquine (Mef), a poorly soluble and highly bitter drug, has been used for malaria prophylaxis and treatment. The dosage form for Mef is mostly available as adult tablets, and thus children under the age of 5 suffer from poor medication adherence. We have developed a stable, rapidly dissolvable, and palatable pediatric formulation for Mef using liposomes composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol with a mean diameter of ~110 nm. Mef was actively loaded into the liposomes via an ammonium sulfate gradient using the solvent-assisted loading technology (SALT) developed in our lab...
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28452061/evaluation-of-real-life-dosing-of-oral-medicines-with-respect-to-fluid-and-food-intake-in-a-dutch-speaking-population
#16
B Hens, J Van Den Abeele, J Rubbens, M Keirsebilck, J Roelens, C Schreurs, K Verheyen, M Casteels, G Laekeman, P Augustijns
WHAT IS KNOWN AND OBJECTIVE: Oral drug administration is the most preferred route of drug administration. For some specific classes of drugs, recommendations regarding the intake of the drug product are provided by and approved in the summary of product characteristics (SmPC) after testing the oral drug product in clinical trials under strict and predefined conditions. The aim of this study was to investigate how certain classes of medicines are taken in a "real-life" setting in terms of concomitant fluid and food intake by a Dutch-speaking population in Flanders (Belgium)...
April 27, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28447882/development-of-novel-amisulpride-loaded-solid-self-nanoemulsifying-tablets-preparation-and-pharmacokinetic-evaluation-in-rabbits
#17
Wael Gamal, Rania H Fahmy, Magdy I Mohamed
OBJECTIVE: the current investigation is focused on the formulation and in-vivo evaluation of optimized solid-self-nanoemulsifying drug delivery systems (S-SNEDDS) of amisulpride (AMS) for improving its oral dissolution and bioavailability. METHODS: liquid SNEDDS (L-SNEDDS) composed of Capryol™ 90 (oil), Cremophor® RH40 (surfactant) and Transcutol(®) HP (co-surfactant) were transformed to solid systems via physical adsorption onto magnesium aluminometasilicate (Neusilin US2)...
April 27, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28447878/development-of-novel-amisulpride-loaded-liquid-self-nanoemulsifying-drug-delivery-systems-via-dual-tackling-of-its-solubility-and-intestinal-permeability
#18
Wael Gamal, Rania H Fahmy, Magdy I Mohamed
OBJECTIVE: the aim of the current investigation was to enhance the oral biopharmaceutical behavior; solubility and intestinal permeability of amisulpride (AMS) via development of liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) containing bioenhancing excipients. METHODS: the components of L-SNEDDS were identified via solubility studies and emulsification efficiency tests, and ternary phase diagrams were constructed to identify the efficient self-emulsification regions...
April 27, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28442499/absorption-distribution-metabolism-and-excretion-of-the-oral-prostaglandin-d2-receptor-2-dp2-antagonist-fevipiprant-qaw039-in-healthy-volunteers-and-in-vitro
#19
David Pearson, H Markus Weiss, Yi Jin, Jan Jaap van Lier, Veit J Erpenbeck, Ulrike Glaenzel, Peter End, Ralph Woessner, Fabian Eggimann, Gian Camenisch
Fevipiprant is a novel oral prostaglandin D2 receptor 2 (DP2; also known as CRTh2) antagonist, which is currently in development for the treatment of severe asthma and atopic dermatitis. We investigated the absorption, distribution, metabolism, and excretion properties of fevipiprant in healthy subjects after a single 200 mg oral dose of [(14)C]-radiolabeled fevipiprant. Fevipiprant and metabolites were analyzed by liquid chromatography coupled to tandem mass spectrometry and radioactivity measurements, and mechanistic in vitro studies were performed to investigate clearance pathways and covalent plasma protein binding...
April 25, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28437488/the-novel-carboxylesterase-1-variant-c-662a-g-may-decrease-the-bioactivation-of-oseltamivir-in-humans
#20
Jaeseong Oh, SeungHwan Lee, Howard Lee, Joo-Youn Cho, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu, Kyoung Soo Lim
BACKGROUND: Human carboxylesterase 1 (CES1) is a serine esterase that hydrolyses various exogenous and endogenous compounds including oseltamivir, a prodrug used to treat influenza. A novel CES1 c.662A>G single nucleotide polymorphism (SNP) was predicted to decrease CES1 enzymatic activity in an in silico analysis. This study evaluated the effect of the c.662A>G SNP on the pharmacokinetics (PK) of oseltamivir in humans. METHODS: A single oral dose of oseltamivir at 75 mg was administered to 20 healthy subjects, 8 heterozygous c...
2017: PloS One
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