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Drug Development and Industrial Pharmacy

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https://www.readbyqxmd.com/read/28447882/development-of-novel-amisulpride-loaded-solid-self-nanoemulsifying-tablets-preparation-and-pharmacokinetic-evaluation-in-rabbits
#1
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
#2
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/28443689/recent-achievements-in-tc-99m-radiopharmaceutical-direct-production-by-medical-cyclotrons
#3
Alessandra Boschi, Petra Martini, Micol Pasquali, Licia Uccelli
(99m)Tc is the most commonly used radionuclide in the field of diagnostic imaging, a noninvasive method intended to diagnose a disease, assess the disease state and monitor the effects of treatments. Annually, the use of (99m)Tc, covers about 85% of nuclear medicine applications. This isotope releases gamma rays at about the same wavelength as conventional X-ray diagnostic equipment, and owing to its short half-life (t½ = 6 hours) is ideal for diagnostic nuclear imaging. A patient can be injected with a small amount of (99m)Tc and within 24 hours almost 94% of the injected radionuclide would have decayed and left the body, limiting the patient's radiation exposure...
April 26, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28436310/synthesis-and-characterization-of-poly-n-vinylcaprolactam-based-spray-dried-microparticles-exhibiting-temperature-and-ph-sensitive-properties-for-controlled-release-of-ketoprofen
#4
Simone F Medeiros, Milene V Lopes, Bartira Rossi-Bergmann, Maria Inês Ré, Amilton M Santos
Poly(N-vinylcaprolactam) (PNVCL) and poly(N-vinylcaprolactam-co-acrylic acid) (poly(NVCL-co-AA)) were synthesized by solution free radical polymerization and displayed thermo-responsive behavior, with lower critical solution temperatures (LCSTs) of 35°C and 39°C, respectively. The incorporation of AA unities made the poly(NVCL-co-AA) sensitive to both pH- and temperature. They were exploited in this work in preparing microparticles loaded with ketoprofen via spray-drying to modulate the drug release rate by changing pH or temperature...
April 22, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28426341/mydriatics-release-from-solid-and-semi-solid-ophthalmic-formulations-using-different-in-vitro-methods
#5
Silvia Pescina, Claudio Macaluso, Gloria Antonia Gioia, Cristina Padula, Patrizia Santi, Sara Nicoli
The aim of the present paper was the development of semisolid (hydrogels) and solid (film) ophthalmic formulations for the controlled release of two mydriatics: phenylephrine and tropicamide. The formulations - based on polyvinylalchol and hyaluronic acid - were characterized, and release studies were performed with three different in vitro set-ups, i.e. Franz-type diffusion cell, vial method and inclined plane; for comparison, a solution and a commercial insert, both clinically used to induce mydriasis, were evaluated...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28425323/enhanced-solubility-of-piperine-using-hydrophilic-carrier-based-potent-solid-dispersion-systems
#6
Thenmozhi Kathavarayan, Young Je Yoo
CONTEXT: Piperine alkaloid, an important constituent of black pepper exhibits numerous therapeutic properties whereas its usage as a drug is limited due to its poor solubility in aqueous medium, which leads to poor bioavailability. OBJECTIVE: Herein a new method has been developed to improve the solubility of this drug based on the development of solid dispersions with improved dissolution rate using hydrophilic carriers such as sorbitol (Sor), polyethylene glycol (PEG) and polyvinyl pyrrolidone K30 (PVP) by solvent method...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28425305/development-of-a-soluplus%C3%A2-budesonide-freeze-dried-powder-for-nasal-drug-delivery
#7
Michele Pozzoli, Daniela Traini, Paul M Young, Maria B Sukkar, Fabio Sonvico
OBJECTIVE: The aim of this work was to develop an amorphous solid dispersions/solutions (ASD) of a poorly soluble drug, Budesonide (BUD) with a novel polymer Soluplus(®) (BASF, Germany) using a freeze-drying technique, in order to improve dissolution and absorption through the nasal route. SIGNIFICANCE: The small volume of fluid present in the nasal cavity limits the absorption of a poorly soluble drug. Budesonide is a corticosteroid, practically insoluble, and normally administered as a suspension-based nasal spray...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28423953/evaluation-of-polyvinyl-alcohols-as-mucoadhesive-polymers-for-mucoadhesive-buccal-tablets-prepared-by-direct-compression
#8
Yuri Ikeuchi-Takahashi, Chizuko Ishihara, Hiraku Onishi
The purpose of the present work was to evaluate polyvinyl alcohols (PVAs) as a mucoadhesive polymer for mucoadhesive buccal tablets prepared by direct compression. Various polymerization degree and particle diameter PVAs were investigated for their usability. The tensile strength, in vitro adhesive force and water absorption properties of the tablets were determined to compare the various PVAs. The highest values of the tensile strength and the in vitro adhesive force were observed for PVAs with a medium viscosity and small particle size...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28422529/implant-compositions-for-the-unidirectional-delivery-of-drugs-to-the-brain
#9
Michael McGinity, John Floyd, James McGinity, Feng Zhang
The overall objective of this study was to design and characterize the properties of a bioadhesive trilayer sustained-release implant device for the unidirectional local delivery of anticancer compounds to the brain following the removal of glioblastoma multiforme tumors. Using acetaminophen as a model drug compound, we compressed trilayer wafers that contained (a) a bioadhesive layer, (b) a drug layer that contained a lipid and a pore-forming hydrophilic polymer, and (c) a third layer comprising a lipid substance...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28420295/optimization-of-methotrexate-loaded-niosomes-by-box-behnken-design-an-understanding-of-solvent-effect-and-formulation-variability
#10
Ahmed S Zidan, Mahmoud Mokhtar Ibrahim, Nagia A El Megrab
Dermal drug delivery system which localizes methotrexate (MTX) in the skin is advantageous in topical treatment of psoriasis. The aim of the current study was to understand dilution effects and formulation variability for the potential formation of niosomes from proniosome gels of MTX. Box-Behenken design was employed to prepare a series of MTX proniosome gels of Span 40, cholesterol (Chol-X1) and Tween 20 (T20-X2). Short chain alcohols (X3), namely ethanol (Et), propylene glycol (Pg) and glycerol (G) were evaluated for their dilution effects on proniosomes...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28420288/microemulsion-loaded-hydrogel-as-a-promising-vehicle-for-dermal-delivery-of-the-antifungal-sertaconazole-design-optimization-and-ex-vivo-evaluation
#11
Shaimaa Ali Ali Radwan, Aliaa Nabil ElMeshad, Raguia Aly Shoukri
The purpose of the present study was to develop and optimize sertaconazole microemulsion-loaded hydrogel (STZ ME G) to enhance the dermal delivery and skin retention of the drug. Following screening of various oils for maximum drug solubility, twelve pseudoternary phase diagrams were constructed using oils (Peceol®, Capryol(®) 90), surfactants (Tween(®) 80, Cremophor(®) EL), a cosurfactant (Transcutol(®) P) and water. A 2(1)x 3(1)x 2(1)x 3(1) full factorial design was employed to optimize a ME of desirable characteristics...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28420285/dry-powders-for-the-inhalation-of-ciprofloxacin-or-levofloxacin-combined-with-a-mucolytic-agent-for-cystic-fibrosis-patients
#12
Yagmur Akdag Cayli, Selma Sahin, Francesca Buttini, Anna Giulia Balducci, Serena Montanari, Imran Vural, Levent Oner
OBJECTIVE: This study aimed to design and characterize an inhalable dry powder of ciprofloxacin or levofloxacin combined with the mucolytics acetylcysteine and dornase alfa for the management of pulmonary infections in patients with cystic fibrosis. METHODS: Ball milling, homogenization in isopropyl alcohol, and spray drying processes were used to prepare dry powders for inhalation. Physico-chemical characteristics of the dry powders were assessed via thermogravimetric analysis, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffractometry, and scanning electron microscopy...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28420283/design-and-characteristics-of-gellan-gum-beads-for-modified-release-of-meloxicam
#13
Tomasz Osmałek, Bartłomiej Milanowski, Anna Froelich, Mirosław Szybowicz, Wojciech Białowąs, Marcin Kapela, Piotr Gadziński, Katarzyna Ancukiewicz
The aim of the presented work was to design, formulate and evaluate the properties of low-acyl gellan macro beads with the potential application as carriers for oral delivery of meloxicam (MLX) in the prophylaxis of colorectal cancer. The beads were obtained by means of ionotropic gelation technique. Calcium chloride (1.0%, 9.0 × 10(-2) M) was used as the cross-linking agent. Nine different polymer, drug and surfactant (Tween®80) mixtures were used for production of the beads. The quantitative compositions of the mixtures were generated with the application of the Design of Experiments (DoE) modulus from the STATISTICA Software...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28398095/influence-of-drug-load-on-dissolution-behavior-of-tablets-containing-a-poorly-water-soluble-drug-estimation-of-the-percolation-threshold
#14
Tim Wenzel, Cordula Stillhart, Peter Kleinebudde, Anikó Szepes
Drug load plays an important role in the development of solid dosage forms, since it can significantly influence both processability and final product properties. The percolation threshold of the active pharmaceutical ingredient (API) corresponds to a critical concentration, above which an abrupt change in drug product characteristics can occur. The objective of this study was to identify the percolation threshold of a poorly water-soluble drug with regard to the dissolution behavior from immediate release tablets...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28367654/a-review-of-co-milling-techniques-for-the-production-of-high-dose-dry-powder-inhaler-formulation
#15
Michael Lau, Paul M Young, Daniela Traini
Drug delivery by inhalation offers several advantages compared to other dosage forms, including rapid clinical onset, high bioavailability, and minimal systemic side effects. Drug delivery to the lung can be achieved as liquid suspensions or solutions in nebulizers and pressurized metered-dose inhalers (pMDI), or as dry powders in dry powder inhalers (DPIs). Compared to other delivery systems, DPIs are, in many cases, considered the most convenient as they are breath actuated and do not require the use of propellants...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28406045/a-methacrylic-hyaluronic-acid-derivative-for-potential-application-in-oral-treatment-of-celiac-disease
#16
Giovanna Pitarresi, Fabio Salvatore Palumbo, Daniela Triolo, Calogero Fiorica, Gaetano Giammona
OBJECTIVE: Aim of this work was the synthesis of a methacrylic hyaluronic acid derivative and the production, via photocrosslinking, of related hydrogels loaded with an endopeptidase intended for a potential oral treatment of celiac disease. METHODS: The methacrylic derivative of hyaluronic acid (HA) was prepared through a one-pot procedure involving the reaction with ethylenediamine (EDA) and methacrylic anhydride (MA). The obtained derivative, named HA-EDA-MA, was used to prepare photocrosslinked hydrogels loaded with a prolyl endopeptidase derived from Flavobacterium meningosepticum (PEP FM) able to detoxify gliadin...
April 13, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28402205/non-ionic-surfactant-based-thymoquinone-loaded-nanoproniosomal-formulation-in-vitro-physicochemical-evaluation-and-in-vivohepatoprotective-efficacy
#17
Sanowar Sayeed, Syed Sarim Imam, Abul Kalam Najmi, Mohd Aqil, Mohd Akhtar
CONTEXT: The present study was carried out to formulate thymoquinone proniosomal formulation (TQP) and evaluate their efficacy in methotrexate (Mtx) induced hepatotoxicity in rats. OBJECTIVE: Theobjective of the study was to explore a new therapeutic approach focusing on hepatoprotectiveactivity using thymoquinone proniosomal formulation. MATERIAL AND METHODS: TQP was formulated using span60, cholesterol and phospholipid by film hydration technique...
April 12, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28402193/controlled-precipitation-for-enhanced-dissolution-rate-of-flurbiprofen-development-of-rapidly-disintegrating-tablets
#18
Ebtessam A Essa, Amira O Elmarakby, Ahmed M A Donia, Gamal M El Maghraby
OBJECTIVE: The aim of this work was to investigate the potential of controlled precipitation of flurbiprofen on solid surface, in presence or absence of hydrophilic polymers, as a tool for enhnaced dissolution rate of the drug. The work was extended to develop rapidly disintegrated tablets. SIGNIFICANCE: This strategy provide simple technique for dissolution enhancement of slowly dissolving drugs with high scaling up potential. METHOD: Aerosil was dispersed in ethanolic solution of flurbiprofen in presence and absence of hydrophilic polymers...
April 12, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28402175/development-of-drug-loaded-chitosan-hollow-nanoparticles-for-delivery-of-paclitaxel-to-human-lung-cancer-a549-cells
#19
Jie Jiang, Ying Liu, Chao Wu, Yang Qiu, Xiaoyan Xu, Huiling Lv, Andi Bai, Xuan Liu
In this study, biodegradable chitosan hollow nanospheres (CHN) were fabricated using polystyrene nanospheres (PS) as templates. CHN were applied to increase the solubility of poorly water-soluble drugs. The lung cancer drug paclitaxel (PTX), which is used as a model drug, was loaded into CHN by the adsorption equilibrium method. The drug-loaded sample (PTX-CHN) offered sustained PTX release and good bioavailability. The state characterization of PTX by DSC, XRD and FTIR showed that the PTX absorbed into CHN existed in an amorphous state...
April 12, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28402147/solubility-and-dissolution-rate-improvement-of-the-inclusion-complex-of-apigenin-with-2-hydroxypropyl-%C3%AE-cyclodextrin-prepared-using-the-liquid-antisolvent-precipitation-and-solvent-removal-combination-methods
#20
Weiwei Wu, Yuangang Zu, Xiuhua Zhao, Xinxin Zhang, Lingling Wang, Yuanyuan Li, Li Wang, Yin Zhang, Bolin Lian
Apigenin (AP) has many pharmacological activities. AP has poor solubility in some solvents. AP is insoluble in water and slightly soluble in ethanol (1.93 mg/mL). It has limited application and exploitation. Therefore, the liquid antisolvent precipitation (LAP) method was applied to improve the solubility of AP in ethanol by changing its crystal form or producing ultra-fine particles. Then, the inclusion complex of AP with 2-Hydroxypropyl-β-cyclodextrin (HP-β-CD) is prepared using the solvent removal method...
April 12, 2017: Drug Development and Industrial Pharmacy
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