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Drug Development and Industrial Pharmacy

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https://read.qxmd.com/read/31418598/combined-site-specific-release-retardant-mini-matrix-tablets-c-ssrrmt-for-extended-oral-delivery-of-dexketoprofen-trometamol-in-vitro-evaluation-and-single-versus-multiple-doses-pharmacokinetic-study-in-human-volunteers
#1
Nabila M Sweed, Emad B Basalious, Samia A Nour
Development of extended release oral formulations of dexketoprofen trometamol (DT), a rapidly eliminated drug with high solubility, poses a great challenge especially when a portion of the dose is to be absorbed from the colon. In this study, site-specific release retardant mini-matrix tablets (SSRRMT) were developed and functionally coated with pH-responsive materials to achieve a site-specific delivery of DT at the duodenojejunal (DSRRMT) and ileocecal (ISRRMT) regions. Stomach-specific coated mini-tablets (SSCMT) were manufactured for immediate release of about 16% of the daily dose of DT in the stomach...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31418595/halogenated-boroxine-dipotassium-trioxohydroxytetrafluorotriborate-k-2-b-3-o-3-f-4-oh-inhibits-emerging-multidrug-resistant-and-%C3%AE-lactamase-producing-opportunistic-pathogens
#2
Ana Maravić, Tomislav Rončević, Lucija Krce, Nada Ilić, Borivoj Galić, Vedrana Čikeš Čulić, Ivana Carev
Halogenated boroxine dipotassium trioxohydroxytetrafluorotriborate, K2 [B3 O3 F4 OH] (boroxine) was previously shown to be very effective in inhibition of several carcinoma cell lines, including the skin cancer. Here, we investigated its antimicrobial potential by targeting the multidrug-resistant opportunistic pathogens associated with skin and wound infections. The antimicrobial testing against eleven bacterial and four fungal species revealed good activity of boroxine against pathogenic filamentous fungi Penicillium funiculosum and Aspergillus niger (MIC50 64 and 128 µg/ml), and a moderate bioactivity against the yeast Candida albicans (MIC50 512 µg/ml)...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31418592/development-and-evaluation-of-rapidly-dissolving-buccal-films-of-naftopidil-in-vitro-and-in-vivo-evaluation
#3
Heba I Elagamy, Ebtessam A Essa, Ahmed Nouh, Gamal M El Maghraby
OBJECTIVES: Development and evaluation of rapidly dissolving film for intra-oral administration of naftopidil. SIGNIFICANCE: Formulation of naftopidil in the form of rapidly dissolving buccal film can eliminate the dissolution problem of naftopidil and provide greater chance for direct absorption into the systemic circulation bypassing the presystemic metabolism. This can improve the oral bioavailability. In addition, this film guarantees patient compliance and is suitable for geriatric patients...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31418582/development-of-stable-emulsified-formulations-of-terminalia-arjuna-for-topical-application-evaluation-of-antioxidant-activity-of-final-product-and-molecular-docking-study
#4
Dinanath Gaikwad, Namdeo Jadhav
Objective: The aim of this work was to develop stable emulsified formulations containing Terminalia arjuna ( T. arjuna ) extract and to assess antioxidant potential of the final product with in silico molecular screening. Methods: T. arjuna emulsified formulations were prepared by application of ternary phase diagram design and were evaluated for phytochemical screening, solubility studies, ex vivo permeation study, DPPH free radical scavenging assay, anti-tyrosinase activity, skin irritation, stability studies, molecular docking study and pharmacophore modeling...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31418304/identification-of-somatostatin-receptors-using-labelled-pegylated-octreotide-as-an-active-internalization
#5
Ahmed A H Abdellatif
Numerous normal and tumors cells are well-known to express the somatostatin receptors (SSTRs) on their surface which make the receptor be useful for tumor scintigraphy. Thus, identification of SSTRs is beneficial, especially SSTR2. The somatostatin analogue, Octreotide (OCT) was chosen as a ligand, as it is known to selectively bind to SSTR2. Moreover, polyethylene glycol (PEG), 8armPEG was used as a branched PEG to provide a low non-specific cell binding and easily chemical modification. OCT, and fluorescein (Flu) were conjugated to branched PEG using a water-soluble carbodiimide (EDC) and N-hydroxy succinimide (NHS) so as to activate its carboxylic acid group...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31416366/effect-of-casting-solvent-film-forming-agent-and-solubilizer-on-orodispersible-films-of-a-polymorphic-poorly-soluble-drug-an-in-vitro-in-silico-study
#6
Ahmed Abd El-Bary, Ibrahim Al Sharabi, Balqees Saeed Haza'a
In the current work, a full factorial experimental design was utilized to formulate piroxicam into orodispersible films while investigating the effects of some formulation factors on the properties of the resulting films. These factors were (A) the casting solvent: water and acetone/water mixture; (B) the film forming agent: HPMC K4M and Na-alginate; (C) the solubilization system: no solubilizer, L-arginine, poloxamer and L-arginine/poloxamer mixture. Sixteen formulation runs were prepared by solvent casting method to obtain 10 mg piroxicam dosage units...
August 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31407925/eco-friendly-green-synthesis-of-silver-nanoparticles-and-their-potential-applications-as-antioxidant-and-anticancer-agents
#7
Muhammad Jamil Ahmed, Ghulam Murtaza, Faisal Rashid, Jamshed Iqbal
Eco-friendly green synthesis of nanoparticles using medicinal plants gained immense importance due to its potential therapeutic uses. In the current study, silver nanoparticles (AgNPs) were synthesized using water extract of Jurinea dolomiaea leaf and root at room temperature. MTT assay was used to study anticancer potential of AgNPs against cervical cancer cell line (HeLa), breast cancer cell lines (MCF-7) and mouse embryonic fibroblast (NIH-3 T3) cell line for toxicity evaluation. The antioxidant potential was evaluated using stable DPPH radicals...
August 13, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31389270/dry-powder-inhaler-of-colistimethate-sodium-for-lung-infections-in-cystic-fibrosis-optimization-of-powder-construction
#8
Jana Kozáková, Ayça Altay, Vladimír Ždímal, Ludmila Mašková, Fabio Sonvico, Eride Quarta, Alessandra Rossi, Francesca Buttini, Gaia Colombo
Colistimethate sodium (CMS) for treatment of lung infections in cystic fibrosis patient was transformed into a dry powder for inhalation by spray drying. Design of Experiment was applied for understanding the role of the spray drying process parameters on the critical quality attributes of the CMS spray-dried powders (SD) and agglomerates thereof. Eleven experimental SD microparticle powders were constructed under different process conditions according to a Central Composite Design. The SD microparticles were then agglomerated in soft pellets...
August 7, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31382790/phospholipid-polymer-hybrid-nanoparticles-mediated-transfollicular-delivery-of-quercetin-prospective-implement-for-the-treatment-of-androgenic-alopecia
#9
Lenin Das, Monika Kaurav, Ravi Shankar Pandey
Objectives : The aim of the study was to deliver effective doses of Quercetin (Que) to the lower region of hair follicles (HFs) using the transfollicular route through dipalmotylphosphatidylcholine (DPPC) reinforced poly lactide- co- glycolide nanoparticles (DPPC-PLGA hybrid NPs) for the treatment of alopecia. Method: PLGA and DPPC-PLGA hybrid NPs were prepared by double emulsification solvent evaporation method. NPs were characterized for size, shape, zeta potential entrapment and drug release. Drug-polymer interactions were determined by infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC)...
August 6, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31378098/development-of-immediate-release-rupatadine-fumarate-10-mg-tablets-a-quality-by-design-qbd-approach
#10
Luis Castillo Henríquez, Rolando Vargas Zúñiga, Gustavo Carazo Berrocal, German Madrigal Redondo, Briner Calvo Guzmán, Eleaneth Baltodano Viales
The main objective of this research is to develop an immediate release Rupatadine fumarate 10 mg tablets formulation by direct compression, through a Quality by Design approach in Costa Rica. Methods: According to a Quality by Design approach; Target Product Profile, Quality Target Product Profile and the Critical Quality Attributes were defined. In the preformulation study, compatibility tests were carried out between the raw materials. The Critical Material Attributes were established using Quality Risk Management...
August 3, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31353967/nanosized-nasal-emulgel-of-resveratrol-preparation-optimization-in-vitro-evaluation-and-in-vivo-pharmacokinetic-study
#11
Heba F Salem, Rasha M Kharshoum, Heba A Abou-Taleb, Demiana M Naguib
Nano-emulgel has become one of the most significant controlled release systems which has the advantages of both gels and nano-emulsions. This work aims at the formulation of nasal nano-emulgel for resveratrol, employing carbopol 934 and poloxamer 407 as the gelling agent. The optimum nano-emulsion was determined through further characterization of the selected system. The nasal nano-emulgel was prepared and tested for the in vitro release, the release kinetics, FTIR, ex vivo permeation, nasal mucosa toxicity and in vivo pharmacokinetic study...
July 29, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31353966/effect-of-the-filler-grade-on-the-characteristics-and-the-sublingual-permeability-of-atropine-sulfate-fast-disintegrating-sublingual-tablets
#12
Rawan Bafail, Mohamad Rawas-Qalaji, Alhussain Aodah, Mutasem Rawas-Qalaji
OBJECTIVE: the effects of changing the filler grade on the characteristics of atropine sulfate (AS) fast disintegrating sublingual tablets (FDSTs) and AS sublingual permeability were investigated in order to optimize the formulation of AS FDSTs and, therefore, AS sublingual permeability. SIGNIFICANCE: AS FDSTs will provide an accessible alternative for AS autoinjector (ATROPEN®), and a non-invasive first-aid antidote for the treatment of organophosphate (OP) poisoning and reduce the number of fatalities due to nerve gas attacks or OP pesticide poisoning...
July 29, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31342807/evaluating-the-bioequivalence-of-metronidazole-tablets-and-analyzing-the-effect-of-in-vitro-dissolution-on-in-vivo-absorption-based-on-pbpk-modeling
#13
Shuqi Zhang, Mengna Fang, Qi Zhang, Xiaoting Li, Tianhong Zhang
Metronidazole, a BCS class I drug, could be waived based on the BCS principles, thus enabling in vitro dissolution data as a surrogate of BE study. However, the impact of dissolution profiles of metronidazole tablets on the in vivo performance has never been studied systematically. So the aim of the present study was to conduct a multipronged approach of in vitro dissolution, in silico simulation and in vivo study to evaluate the effect of dissolution performance on oral absorption of metronidazole tablets, as well as the accuracy of PBPK model to predict the oral bioavailability for BCS I drug...
July 25, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31342792/preparation-characterization-and-pharmacokinetic-evaluation-of-rosuvastatin-calcium-incorporated-cyclodextrin-polyanhydride-nanoparticles
#14
Fawaz N S Al-Heibshy, Ebru Başaran, Rana Arslan, Naile Öztürk, İmran Vural, Müzeyyen Demirel
Objective: The aim of the study was to formulate, cyclodextrin (CD)-polyanhydride (PA) nanoparticles (CPNs) with rosuvastatin calcium (RCa) in order to enhance the poor oral bioavailability. Methods: CPNs containing RCa/CD complexes were prepared by a modified solvent displacement method and morphological analyses, particle size (PS), polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (EE), DSC, FT-IR, XRD, 1 H-NMR analyses were performed. In vitro release properties, release kinetics, cytotoxicity, in vitro permeability and pharmacokinetic studies were also studied...
July 25, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31311329/rat-palatability-pharmacodynamics-effect-and-bioavailability-of-mefenamic-acid-formulations-utilizing-hot-melt-extrusion-technology
#15
Sultan Alshehri, Faiyaz Shakeel, Ehab Elzayat, Osaid Almeanazel, Mohammad Altamimi, Gamal Shazly, Kazi Mohsin, Bjad Almutairy, Bader Alsulays, Abdullah Alshetaili, Ahmed Alalaiwe, Michael Repka
Mefenamic acid (MA) has been reported as a weakly soluble drug which presents weak in vivo absorption upon oral administration using conventional formulations. Solid dispersions (SDs) have been investigated extensively in literature for enhancing the solubility and bioavailability of weakly-soluble molecules. Hence, the aim of proposed study was to prepare MA novel formulations in the form of SDs using hot-melt extrusion technology in order to enhance its palatability, bioavailability and pharmacodynamics effects/anti-inflammatory efficacy...
July 16, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31306048/synthesis-and-in-vivo-taste-assessment-of-meloxicam-pivalate
#16
Bandoo C Chatale, Mariam S Degani
Meloxicam (MX), a nonsteroidal anti-inflammatory drug, widely used to treat arthritis, has a very bitter taste. Chemical modification of the bitter functionality was achieved by synthesis of a prodrug, meloxicam pivalate (MXP). Taste improvement was evaluated using single bottle-test rat model. It was found that palatability of MXP solution improved significantly as compared to MX.
July 15, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31305162/correction
#17
(no author information available yet)
No abstract text is available yet for this article.
July 15, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31282753/near-infrared-spectroscopic-applications-in-pharmaceutical-particle-technology
#18
M Razuc, A Grafia, L Gallo, M V Ramírez-Rigo, R J Romañach
Near infrared spectroscopy (NIRS) is nowadays an established analytical technique in the pharmaceutical industry. The aim of this review is to present the progress of NIRS in providing useful information for pharmaceutical particle technology. NIR methods are now developed to characterize a wide variety of materials (active pharmaceutical ingredients, excipients, co-processed powders and physical mixtures) and pharmaceutical dosage forms (conventional, modified drug release technologies and phytomedicines)...
July 8, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31241372/potent-activity-of-bioconjugated-peptide-and-selenium-nanoparticles-against-colorectal-adenocarcinoma-cells
#19
V R Ranjitha, Umashankar Muddegowda, V Ravishankar Rai
Nanomaterial based anticancer treatment is promising nowadays because of their small size that can penetrate and interact both inside and outside the cell surface. In this study, a simple protocol was followed for the conjugation of the biologically synthesized selenium nanoparticles (SeNPs) and short chain synthetic peptide. SeNPs was synthesized by using the culture supernatant of Streptomyces griseoruber, actinomycetes isolated from the soil. The short chain peptide Boc-L-F-OMe was synthesized by the conventional solution phase chemistry using a racemization-free fragment condensation strategy...
July 5, 2019: Drug Development and Industrial Pharmacy
https://read.qxmd.com/read/31271324/use-of-sorbitol-as-pharmaceutical-excipient-in-the-present-day-formulations-issues-and-challenges-for-drug-absorption-and-bioavailability
#20
Ranjeet Prasad Dash, Nuggehally R Srinivas, R Jayachandra Babu
Sorbitol is a popular sugar alcohol which has been used as an excipient in formulations of various drugs. Although from a safety perspective the presence of sorbitol in drug formulations does not raise a concern, reports have emerged and these suggest that sorbitol in drug formulations may alter oral absorption and bioavailability of certain drugs. The focus of this paper was to review the published literature of various drugs where pharmacokinetic data has been reported for the drug alone versus drug administered with sorbitol and provide perspectives on the pharmacokinetic findings...
July 4, 2019: Drug Development and Industrial Pharmacy
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