journal
MENU ▼
Read by QxMD icon Read
search

Drug Development and Industrial Pharmacy

journal
https://www.readbyqxmd.com/read/28541760/inhibition-of-proteases-activity-in-intestine-needs-a-sustainable-acidic-environment-rather-than-a-transient
#1
Chang Xing, Jin-Feng Xing, Zhi-Qiang Ge
α-Chymotrypsin (α-CT) and trypsin are important components of the enzymatic barrier. They could degrade the therapeutic proteins and peptides, inhibit their activity consequently, and thereby reduce their oral bioavailability. Acidic agents, as one type of indirect protease inhibitors, have shown proof of concept in clinical trials. We report here the inactivated proteases due to acid influence can be reactivated immediately by environmental pH recovery regardless of how long the inactivation last. To keep the inactivation time of proteases for 4 to 5 h, we designed and prepared a sustained-release tablet containing citric acid (CA) which can effectively reduce the pH below 5...
May 25, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28523942/combinatorial-therapeutic-approaches-with-rnai-and-anticancer-drugs-using-nanodrug-delivery-systems
#2
Anish Babu, Anupama Munshi, Rajagopal Ramesh
RNA interference (RNAi) is emerging as a powerful approach in cancer treatment. siRNA is an important RNAi tool that can be designed to specifically silence the expression of genes involved in drug resistance and chemotherapeutic inactivity. Combining siRNA and other therapeutic agents can overcome the multidrug resistance (MDR) phenomenon by simultaneously silencing genes and enhancing chemotherapeutic activity. Moreover, the therapeutic efficiency of anticancer drugs can be significantly improved by additive or synergistic effects induced by siRNA and combined therapies...
May 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28489426/preparation-characterization-and-in-vitro-evaluation-of-microemulsion-of-raloxifene-hydrochloride
#3
Shiva Golmohammadzadeh, Nafiseh Farhadian, Amir Biriaee, Faranak Dehghani, Bahman Khameneh
Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator which is orally used for treatment of osteoporosis and prevention of breast cancer. The drug has low aqueous solubility and bioavailability. The aim of the present study is to formulate and characterize oil-in-water microemulsion systems for oral delivery of RLX. To enhance the drug aqueous solubility, microemulsion based on sesame oil was prepared. Sesame oil and Tween 80 were selected as the drug solvent oil and surfactant, respectively...
May 10, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28489424/a-novel-ph-responsive-hydrogel-based-on-calcium-alginate-engineered-by-the-previous-formation-of-polyelectrolyte-complexes-pecs-intended-to-vaginal-administration
#4
Natália Noronha Ferreira, Taciane Alvarenga Perez, Liliane Neves Pedreiro, Fabíola Garavello Prezotti, Fernanda Isadora Boni, Valéria Maria de Oliveira Cardoso, Tiago Venâncio, Maria Palmira Daflon Gremião
This work aimed to develop a calcium alginate hydrogel as a pH responsive delivery system for polymyxin B (PMX) sustained-release through the vaginal route. Two samples of sodium alginate from different suppliers were characterized. The molecular weight and M/G ratio determined were, approximately, 107 KDa and 1.93 for alginate_S and 32 KDa and 1.36 for alginate_V. Polymer rheological investigations were further performed through the preparation of hydrogels. Alginate_V was selected for subsequent incorporation of PMX due to the acquisition of pseudoplastic viscous system able to acquiring a differential structure in simulated vaginal microenvironment (pH 4...
May 10, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28481735/characterization-of-new-functionalized-calcium-carbonate-polycaprolactone-composite-material-for-application-in-geometry-constrained-drug-release-formulation-development
#5
Leonie Wagner-Hattler, Joachim Schoelkopf, Jörg Huwyler, Maxim Puchkov
A new mineral-polymer composite (FCC-PCL) performance is assessed to produce complex geometries to aid in development of controlled release tablet formulations. The mechanical characteristics of a developed material such as compactibility, compressibility and elastoplastic deformation were measured. The results and comparative analysis versus other common excipients suggest efficient formation of a complex, stable and impermeable geometries for constrained drug release modifications under compression. The performance of the proposed composite material has been tested by compacting it into a geometrically altered tablet (Tablet-In-Cup, TIC) and the drug release was compared to commercially available product...
May 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28481717/implementation-of-quality-by-design-approach-in-manufacturing-process-optimization-of-dry-granulated-immediate-release-coated-tablets-a-case-study
#6
Michał Teżyk, Emilia Jakubowska, Bartłomiej Milanowski, Janina Lulek
The aim of this study was to optimize the process of tablets compression and identification of film-coating critical process parameters (CPPs) affecting critical quality attributes (CQAs) using Quality by Design approach. Design of experiment (DOE) and regression methods were employed to investigate hardness, disintegration time and thickness of uncoated tablets depending on slugging and tableting compression force (CPPs). Plackett-Burman experimental design was applied to identify critical coating process parameters among selected ones, that is: drying and preheating time, atomization air pressure, spray rate, air volume, inlet air temperature and drum pressure, that may influence the hardness and disintegration time of coated tablets...
May 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28481661/in-vitro-and-in-vivo-evaluation-of-folate-mediated-pegylated-nanostructured-lipid-carriers-for-the-efficient-delivery-of-furanodiene
#7
Jianmei Zhang, Yunpeng He, Jianqi Jiang, Meng Li, Chenhao Jin, Lin Wang, Dongkai Wang
Furanodiene (FN) loaded FA-PEG2000-DSPE modified nanostructured lipid carriers (FA-FN-NLCs) were developed to increase the solubility and bioavailability of FN, prolong the circulation time in blood and improve the targeting ability. FA-FN-NLCs were prepared using emulsification-ultrasonic and low temperature-solidification method and optimized by central composition design (CCD). In vitro and in vivo characteristics of FA-FN-NLCs were investigated in detail. The optimized formulations exhibited a spherical shape with particle size of 127...
May 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28481657/enhanced-oral-bioavailability-of-10-hydroxycamptothecin-through-the-use-of-poly-n-butyl-cyanoacrylate-nanospheres
#8
Xin Jin, Sajid Asghar, Xieting Zhu, Zhipeng Chen, Junhong Liu, Yibo Li, Hongying Li, Qineng Ping, Yanyu Xiao
The article describes the preparation, physicochemical characterization, drug release, and in vivo behavior of 10-hydroxycamptothecin-loaded poly (n-butyl cyanoacrylate) nanospheres (HCPT-PBCA-NSs). HCPT-PBCA-NSs were successfully prepared via emulsion polymerization of n-butyl cyanoacrylate (BCA) monomer in acidic medium with the aid of two colloidal stabilizers (Poloxamer 188 and Dextran 70). The influence of pH, the time of polymerization, and the dosage of the drug on particle size and encapsulation efficiency (EE) were studied...
May 8, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28480773/new-gentle-wing-high-shear-granulator-impact-of-processing-variables-on-granules-and-tablets-characteristics-of-high-drug-loading-formulation-using-design-of-experiment-approach
#9
Mohamed H Fayed, Sayed I Abdel-Rahman, Fars K Alanazi, Mahrous O Ahmed, Hesham M Tawfeek, Ramadan I Al-Shdefat
The aim of this work was to study the application of design of experiment (DoE) approach in defining design space for granulation and tableting processes using a novel gentle-wing high shear granulator. According to quality-by-design (QbD) prospective, critical attributes of granules and tablets should be ensured by manufacturing process design. A face centered central composite design has been employed in order to investigate the effect of water amount (X1), impeller speed (X2), wet massing time (X3) and water addition rate (X4) as independent process variables on granules and tablets characteristics...
May 8, 2017: Drug Development and Industrial Pharmacy
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/28425323/enhanced-solubility-of-piperine-using-hydrophilic-carrier-based-potent-solid-dispersion-systems
#11
Kathavarayan Thenmozhi, 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...
May 5, 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
#12
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...
May 5, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28471266/preparation-and-characterization-of-safe-microparticles-based-on-xylan
#13
Silvana Cartaxo da Costa Urtiga, Camilla Aquino Azevedo de Lucena Gabi, Giovanna Rodrigues de Araújo Eleamen, Bartolomeu Santos Souza, Hilzeth de Luna Freire Pessôa, Henrique Rodrigues Marcelino, Elisângela Afonso de Moura Mendonça, Eryvaldo Sócrates Tabosa do Egito, Elquio Eleamen Oliveira
This work describes the preparation and evaluation of safe xylan-based microparticles prepared by cross-linking polymerization using sodium trimetaphosphate. The resulting microparticles were evaluated for morphology, particle size, polymer-cross-link agent interaction and in vitro toxicity. The microparticles showed narrow monodisperse size distributions with their mean sizes being between 3.5 µm and 12.5 µm in dried state. FT-IR analyses confirmed the interaction between sodium trimetaphosphate and xylan during the cross-linking process with formation of phosphate ester bonds...
May 4, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28447882/development-of-novel-amisulpride-loaded-solid-self-nanoemulsifying-tablets-preparation-and-pharmacokinetic-evaluation-in-rabbits
#14
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
#15
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/28420295/optimization-of-methotrexate-loaded-niosomes-by-box-behnken-design-an-understanding-of-solvent-effect-and-formulation-variability
#16
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-Behnken's 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 27, 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
#17
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, 12 pseudoternary phase diagrams were constructed using oils (Peceol(®), Capryol(®) 90), surfactants (Tween(®) 80, Cremophor(®) EL), a cosurfactant (Transcutol(®) P) and water. A 2(1) × 3(1) × 2(1) × 3(1) full factorial design was employed to optimize a ME of desirable characteristics...
April 27, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28420283/design-and-characteristics-of-gellan-gum-beads-for-modified-release-of-meloxicam
#18
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 27, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28443689/recent-achievements-in-tc-99m-radiopharmaceutical-direct-production-by-medical-cyclotrons
#19
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
#20
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
journal
journal
27292
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"