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Pharmaceutical Development and Technology

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https://www.readbyqxmd.com/read/28540754/zero-order-release-and-bioavailability-enhancement-of-poorly-water-soluble-vinpocetine-from-self-nanoemulsifying-osmotic-pump-tablet
#1
Sally A El-Zahaby, Mohamed H H AbouGhaly, Ghada A Abdelbary, Omaima N El-Gazayerly
Solid self-nanoemulsifying (S-SNEDDS) asymmetrically coated osmotic tablets of the poorly water-soluble drug Vinpocetine (VNP) were designed. The aim was to control the release of VNP by the osmotic technology taking advantage of the solubility and bioavailability-enhancing capacity of S-SNEDDS. Liquid SNEDDS loaded with 2.5 mg VNP composed of Maisine™ 35-1, Transcutol® HP and Cremophor(®) EL was adsorbed on the solid carrier Aeroperl(®). S-SNEDDS was mixed with the osmotic tablet excipients (Sodium chloride, Avicel(®), HPMC-K4M, PVP-K30 and Lubripharm(®)), then directly compressed to form the core tablet...
May 25, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28535125/preparation-and-characterization-of-adefovir-dipivoxil-stearic-acid-cocrystal-with-enhanced-physicochemical-properties
#2
Jeong-Woong Seo, Kyu-Min Hwang, Sung-Hoon Lee, Dong-Wook Kim, Eun-Seok Park
The objectives of this study were to prepare cocrystal composed of adefovir dipivoxil (AD) and stearic acid (SA) and to investigate the enhanced properties of the cocrystal. The cocrystal was prepared by antisolvent precipitation and characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC). The enhanced properties were evaluated by dissolution testing, permeability studies, and powder rheology analysis...
May 23, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28535123/topical-otic-drugs-in-a-multi-purpose-manufacturing-facility-a-guide-on-determination-and-application-of-permitted-daily-exposure-pde
#3
Lisa Wiesner, Maarten Prause, Ester Lovsin Barle
Due to newly introduced EU GMP guideline for Medicinal Products for Human and Veterinary use (PIC/S, 2015), product specific PDE for toxicological evaluation in multi-purpose facilities are required within a documented process for risk assessment. EMA (2014) guidance on setting PDE limits so far focused on systemic administration routes such as IV, oral or inhalation. This manuscript wants to give guidance on setting PDE values for risk management purposes in multi-purpose facilities for Active Pharmaceutical Ingredients (APIs) applied as topical otic drugs to the outer ear canal...
May 23, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28535094/rheological-and-physical-parameters-correlations-in-formulations-with-pinh%C3%A3-o-derivatives-stability-study-building-up-an-analytical-route
#4
Renata Moschini Daudt, Nilo Sergio Medeiros Cardozo, Ligia Damasceno Ferreira Marczak, Irene Clemes Külkamp Guerreiro
This study focuses on the correlations investigation between rheological and physical parameters and how it can contribute to optimize the topical formulations development. A gel and an emulgel containing pinhão derivatives, and their respective controls, were analyzed along six months of storage. A flowchart of analyses was proposed to use in topical formulation development when a benchmark is the goal or when it is necessary to change some raw material. All formulations were stable over the storage time and the formulations containing pinhão starch and coat extract presented similar properties to those of the control formulations...
May 23, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28532266/soft-chewable-gelatin-based-pharmaceutical-oral-formulations-a-technical-approach
#5
Morten J Dille, Magnus N Hattrem, Kurt I Draget
OBJECTIVE: Hard tablets and capsules for oral drug delivery cause problems for people experiencing dysphagia. The present work describes the formulation and properties of a gelatin based, self-preserved and soft chewable tablet as an alternative and novel drug delivery format. MATERIALS AND METHODS: Gelatin (8.8-10% in 24.7-29% water) constituted the matrix of the soft, semi-solid tablets. Three different pharmaceuticals (Ibuprofen 10%, Acetaminophen 15%, Meloxicam 1...
May 22, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28524719/polyester-based-microdisc-systems-for-sustained-release-of-neuroprotective-phosphine-borane-complexes
#6
David A Janus, Christopher J Lieven, Megan E Crowe, Leonard A Levin
Phosphine-borane complexes are recently developed redox-active drugs that are neuroprotective in models of optic nerve injury and radioprotective in endothelial cells. However, a single dose of these compounds is short-lived, necessitating development of sustained-release formulations of these novel molecules. We screened a library of biodegradable co- and non-block polyester polymer systems for release of incorporated phosphine-borane complexes to evaluate them as drug delivery systems for use in chronic disease...
May 19, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28521578/improved-photostability-and-cytotoxic-effect-of-coenzyme-q10-by-its-association-with-vitamin-e-acetate-in-polymeric-nanocapsules
#7
Natháli S Pegoraro, Juliane Mattiazzi, Elita F da Silveira, Juliana H Azambuja, Elizandra Braganhol, Letícia Cruz
The present study showed the development of nanocapsules containing the association of the coenzyme Q10 and vitamin E acetate and the evaluation of their effect on in vitro cells culture of malignant glioma and melanoma. In order to investigate if nanocapsules are able to protect coenzyme Q10 from degradation under UVC radiation, a photostability study was carried out. For this, three concentrations of vitamin E acetate were evaluated (1, 2 or 3%). Nanocapsules presented suitable physicochemical characteristics and were able to protect coenzyme Q10 from photodegradation...
May 18, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28504046/formulation-and-characterization-of-phospholipon%C3%A2-90%C3%A2-g-and-tween-%C3%A2-80-based-transfersomes-for-transdermal-delivery-of-eprosartan-mesylate
#8
Abdul Ahad, Abdulmohsen A Al-Saleh, Abdullah M Al-Mohizea, Fahad I Al-Jenoobi, Mohammad Raish, Alaa Eldeen B Yassin, Mohd Aftab Alam
The objective of the current study was to formulate the eprosartan mesylate loaded transfersomes using different proportions of Phospholipon(®) 90 G and Tween(®) 80 (95-75: 5-25% w/w). The prepared transfersomes were characterized for their vesicles size, shape, polydispersity index, zeta potential, entrapment efficiency, in vitro skin permeation, confocal laser scanning microscopy and in vivo skin irritation. Results revealed that the formulated transfersomes were negatively charged, spherical unilamellar structure of 71...
May 15, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28503983/design-and-in-vitro-evaluation-of-tenofovir-loaded-vaginal-gels-for-the-prevention-of-hiv-infections
#9
Selin Seda Timur, Adem Şahin, Eren Aytekin, Naile Öztürk, Kerem Heybet Polat, Nurten Tezel, Reyhan Neslihan Gürsoy, Sema Çalış
Infection with the human immunodeficiency virus (HIV) is affecting women disproportionally with increasing incidence rates over the last decades. Tenofovir is one of the most commonly used antiretroviral agents, which belongs to the nucleoside/nucleotide reverse transcriptase inhibitor family, for the prevention of HIV acquisition. In scope of this study, a thermogelling system containing tenofovir - loaded chitosan nanoparticles for the controlled release of tenofovir was developed and characterized. The in vitro release studies have shown that the burst release effect was decreased to 27% with f-TFV CS NPs-Gel...
May 15, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28489472/enalapril-maleate-orally-disintegrating-tablets-tableting-and-in-vivo-evaluation-in-hypertensive-rats
#10
Hesham M Tawfeek, Waleed Faisal, Ghareb M Soliman
The aim of this study was to develop orally disintegrating tablets (ODTs) for enalapril maleate (EnM) to facilitate its administration to the elderly or other patients having dysphagia. Compatibility between EnM and various excipients was studied using differential scanning calorimetry. ODTs of EnM were prepared by direct compression of EnM mixtures with various superdisintegrants. The tablets were evaluated for physical properties including drug content, hardness, friability, disintegration time, wetting time and drug release...
May 10, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28488447/increasing-efficacy-and-reducing-systemic-absorption-of-brimonidine-tartrate-ophthalmic-gels-in-rabbits
#11
Xiaochen Pang, Jiawei Li, Jiaxin Pi, Dongli Qi, Pan Guo, Nan Li, Yumei Wu, Zhidong Liu
Systemic absorption of ocularly administered Brimonidine Tartrate has been reported to give rise to several side-effects. Hence, it has become crucial to develop a delivery system that could increase efficacy and reduce systemic absorption. Therefore, the present work aims to develop Brimonidine Tartrate gels with different concentrations (0.05%, 0.1% and 0.2% w/v, respectively) using Carbopol 974P and HPMC E4M, and compare the therapeutic efficacy and systemic absorption with that of eye drop (0.2%, w/v) by UPLC-MS/MS...
May 10, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28430010/prolonged-injectable-formulation-of-nafarelin-using-in-situ-gel-combination-delivery-system
#12
Behnoush Alizadeh, Nika Bahari Javan, Hamid Akbari Javar, Mohammad Reza Khoshayand, Farid Dorkoosh
The principal purpose of the present study was to prepare and characterize a complex drug delivery system consisting of Nafarelin-poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) nanoparticles (NPs) in combination with sodium alginate/poloxamer 407 in situ gel. Nafarelin-loaded PHBV NPs were prepared via double emulsion solvent evaporation technique. Box-Behnken Response Surface Methodology was utilized to optimize NPs. Mean particle size, polydispersity index (PDI), entrapment efficiency (EE), and drug loading (DL) of the optimized NPs were measured...
May 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28368746/continuous-production-of-aqueous-suspensions-of-ultra-fine-particles-of-curcumin-using-ultrasonically-driven-mixing-device
#13
Komal Pandey, Amruta Chatte, Sameer Dalvi
Developing drug formulations for poorly water-soluble drugs is a major challenge for pharmaceutical industries as the poor water solubility limits bioavailability of these drugs. Production of nanoparticles/microparticles of these drugs is one of the ways to improve dissolution rates by increasing interfacial area for dissolution. Curcumin, a compound obtained from the rhizome of curcuma longa (turmeric roots), is a pharmaceutically viable molecule. However, poor aqueous solubility limits its therapeutic use...
April 24, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28436282/the-effect-of-chamomile-extract-obtained-in-supercritical-carbon-dioxide-conditions-on-physicochemical-and-usable-properties-of-pharmaceutical-ointments
#14
Emilia Klimaszewska, Artur Seweryn, Anna Małysa, Małgorzata Zięba, Joanna Lipińska
The study investigated the effect of chamomile extract obtained in supercritical carbon dioxide conditions on the basic properties of pharmaceutical ointments. A total of five formulations were designed and prepared, differing in the weight ratio of sunflower oil to chamomile extract (5:0; 3.5:1.5; 2.5:2.5; 1.5:3.5 and 0:5). An increase in the concentration of chamomile extract was found to be accompanied by a decrease in hardness, adhesive power and flow limit. Based on viscosity measurements it was shown that ointments containing the hydrophobic plant extract under study were prone to larger drops in viscosity under the effect of the set shear rate...
April 22, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28425310/comments-on-prediction-of-the-aqueous-solubility-using-the-general-solubility-equation-gse-versus-genetic-algorithm-and-support-vector-machine-model
#15
Doaa Alantary, Samuel Yalkowsky
The General Solubility Equation (GSE) is the state of the art method for estimating the aqueous solubilities of organic compounds. It is an extremely simple equation that expresses aqueous solubility as a function of only two inputs: the octanol-water partition coefficient calculated by readily available softwares like clogp and acdlogp, and the commonly known melting point of the solute. Recently, Bahadori, et al. (2016) proposed that their genetic algorithm support vector machine is a "better" predictor...
April 20, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28425308/the-effect-of-molecular-weights-of-microencapsulating-polymers-on-viability-of-mouse-cloned-pancreatic-%C3%AE-cells-biomaterials-osmotic-forces-and-potential-applications-in-diabetes-treatment
#16
Armin Mooranian, Ryu Tackechi, Emma Jamieson, Grant Morahan, Hani Al-Salami
INTRODUCTION: Ideal cell-containing microcapsules should be capable of maintaining cell viability and exhibit significant structural stability to support cellular functionality. To date, such microcapsules remain unavailable, thus, this study used our well-established microencapsulating methods to examine a total of 32 different microencapsulating formulations and correlate polymers' molecular weights (Mwt) and UDCA addition, with cell viability and microcapsules' stability, postmicroencapsulation...
April 20, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28406344/fabrication-and-evaluation-of-eudragit%C3%A2-polymeric-films-for-transdermal-delivery-of-piroxicam
#17
Doungdaw Chantasart, Preeda Tocanitchart, Amaraporn Wongrakpanich, Veerawat Teeranachaideekul, Varaporn Buraphacheep Junyaprasert
The aims of this work were to develop and characterize the prolonged release piroxicam transdermal patch as a prototype to substitute oral formulations, to reduce side effects and improve patient compliance. The patches were composed of film formers (Eudragit(®)) as a matrix backbone, with PVC as a backing membrane and PEG200 used as a plasticizer. Results from X-ray diffraction patterns and Fourier transform-infrared spectroscopy indicated that loading piroxicam into films changed the drug crystallinity from needle to an amorphous or dissolved form...
April 13, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28379057/metoclopramide-nasal-spray-in-vitro-evaluation-and-in-vivo-pharmacokinetic-studies-in-dogs
#18
Ying Li, Xianpeng Fan, Wanqing Li, Peng Yang, Hui Zhang, Daoquan Tang, Xiaoxin Yin, Jianxu Sun, Aiping Zheng
Metoclopramide (MCP) can effectively alleviate motion sickness-caused nausea and vomiting. Nasal administration offers the greatest patient compliance. It is suitable for self-administration and offers rapid and complete absorption, no first-pass effects, and high bioavailability. In present study, a MCP nasal spray was prepared and evaluated in vitro and in vivo. Nasal cilia toxicity of Bufo toads was used to screen the preservative types and concentrations. Rabbit nasal mucosa was used to evaluate the mucosa permeability of different MCP nasal sprays with different penetration enhancers and preservative...
April 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28378604/pva-peg-physically-cross-linked-hydrogel-film-as-a-wound-dressing-experimental-design-and-optimization
#19
Afnan Sh Ahmed, Uttam Kumar Mandal, Muhammad Taher, Deny Susanti, Juliana Md Jaffri
The development of hydrogel films as wound healing dressings is of a great interest owing to their biological tissue-like nature. Polyvinyl alcohol/polyethylene glycol (PVA/PEG) hydrogels loaded with asiaticoside, a standardized rich fraction of Centella asiatica, were successfully developed using the freeze-thaw method. Response surface methodology with Box-Behnken experimental design was employed to optimize the hydrogels. The hydrogels were characterized and optimized by gel fraction, swelling behavior, water vapor transmission rate and mechanical strength...
April 5, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28378601/can-we-estimate-the-critical-micelle-concentration-of-amphiphilic-drug-bases-from-molecular-connectivity-indices
#20
Wiebke Saal, Nicole Wyttenbach, Jochem Alsenz, Martin Kuentz
Self-aggregation of drugs is since many years an important topic in the pharmaceutical sciences. Drugs can aggregate similar to surfactants and thereby exhibit a critical micelle concentration (CMC). The present work focused on amphiphilic drug bases and it was aimed to predict log(CMC) based on chemical structure alone. A dataset of 35 compounds was gathered mostly form the literature and complemented with own measurements based on ultrasonic resonator technology. The hydrophilic-lipophilic balance (HLB) values of the protonated bases were calculated and provided a range of 22...
April 5, 2017: Pharmaceutical Development and Technology
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