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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28224393/coamorphous-loratadine-citric-acid-system-with-enhanced-physical-stability-and-bioavailability
#1
Jin Wang, Ruimiao Chang, Yanan Zhao, Jiye Zhang, Ting Zhang, Qiang Fu, Chun Chang, Aiguo Zeng
Coamorphous systems using citric acid as a small molecular excipient were studied for improving physical stability and bioavailability of loratadine, a BCS class II drug with low water solubility and high permeability. Coamorphous loratadine-citric acid systems were prepared by solvent evaporation technique and characterized by differential scanning calorimetry, X-ray powder diffraction, and Fourier transform infrared spectroscopy. Solid-state analysis proofed that coamorphous loratadine-citric acid system (1:1) was amorphous and homogeneous, had a higher T g over amorphous loratadine, and the intermolecular hydrogen bond interactions between loratadine and citric acid exist...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#2
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28224391/development-and-evaluation-of-a-nanoemulsion-containing-ursolic-acid-a-promising-trypanocidal-agent-nanoemulsion-with-ursolic-acid-against-t-cruzi
#3
Erika Cristina Vargas de Oliveira, Zumira Aparecida Carneiro, Sérgio de Albuquerque, Juliana Maldonado Marchetti
Over a hundred years after the discovery of Chagas disease, this ailment continues to affect thousands of people. For more than 40 years, only two drugs have been available to treat it. Ursolic acid is a naturally occurring terpene that has shown a good trypanocidal action. However, the hydrophobicity of this compound presents a challenge for the development of proper delivery systems. Nanostructured systems are a prominent in delivering lipophilic drugs. Thus, a nanoemulsion containing ursolic acid was developed and had its trypanocidal activity and cytotoxicity evaluated...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28224390/plga-nanoparticles-as-subconjunctival-injection-for-management-of-glaucoma
#4
Hamed A Salama, Mahmoud Ghorab, Azza A Mahmoud, Mayssa Abdel Hady
Nanoparticles fabricated from the biodegradable and biocompatible polymer, polylactic-co-glycolic acid (PLGA), could be a promising system for targeting ocular drug delivery. The objective of this work was to investigate the possibility of encapsulating brinzolamide in PLGA nanoparticles in order to be applied as a subconjunctival injection that could represent a starting point for developing new therapeutic strategies against increase in ocular pressure. The brinzolamide-loaded PLGA nanoparticles were fabricated using emulsion-diffusion-evaporation method with varying concentrations of Tween 80 or poloxamer 188 (Plx) in aqueous and organic phases...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28224389/development-of-a-discriminative-in-vitro-release-test-for-rivastigmine-transdermal-patches-using-pharmacopeial-apparatuses-usp-5-and-usp-6
#5
Alice Simon, Maria Inês Amaro, Anne Marie Healy, Lucio Mendes Cabral, Valeria Pereira de Sousa
The aim of this study was to develop and validate a discriminating in vitro release test to evaluate rivastigmine transdermal patches. The Exelon® Patch was chosen as a model transdermal product. The studies of in vitro release were designed to determine the impact of the official apparatus chosen (USP apparatus 5 and USP apparatus 6), the rotation speed, and the dissolution medium characteristics on the rivastigmine release profile from transdermal patches. Patches with different drug release profiles were tested in order to evaluate the discriminating power of the in vitro release test developed and validated...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28213845/topical-formulation-containing-beeswax-based-nanoparticles-improved-in-vivo-skin-barrier-function
#6
Carla Souza, Luis Alexandre Pedro de Freitas, Patrícia Maria Berardo Gonçalves Maia Campos
Lipid nanoparticles have shown many advantages for treatment/prevention of skin disorders with damaged skin barrier function. Beeswax is a favorable candidate for the development of nanosystems in the cosmetic and dermatological fields because of its advantages for the development of products for topical application. In the present study, beeswax-based nanoparticles (BNs) were prepared using the hot melt microemulsion technique and incorporated to a gel-cream formulation. The formulation was subsequently evaluated for its rheological stability and effect on stratum corneum water content (SCWC) and transepidermal water loss (TEWL) using in vivo biophysical techniques...
February 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28213844/self-nanoemulsified-drug-delivery-system-of-hydrochlorothiazide-for-increasing-dissolution-rate-and-diuretic-activity
#7
Cassiana Mendes, Aline Buttchevitz, Jéssica Henriques Kruger, Thiago Caon, Patricia de Oliveira Benedet, Elenara Lemos-Senna, Marcos Antônio Segatto Silva
Hydrochlorothiazide (HCTZ) is a class IV drug according to the Biopharmaceutical Classification System. This study aimed the development of self-nanoemulsifying drug delivery system (SNEDDS) for HCTZ as an approach to overcome the biopharmaceutical limitations. Pre-formulation screening and ternary phase diagrams were carried out to select the oil phase, the surfactant, and the co-surfactant as the amount of each constituent. The optimized formulations, with reduced amount of surfactant, and composed of medium chain triglycerides, Cremophor EL and Transcutol P did not affect the pH or show drug incompatibilities...
February 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28205144/recommended-best-practices-for-process-monitoring-instrumentation-in-pharmaceutical-freeze-drying-2017
#8
Steven Nail, Serguei Tchessalov, Evgenyi Shalaev, Arnab Ganguly, Ernesto Renzi, Frank Dimarco, Lindsay Wegiel, Steven Ferris, William Kessler, Michael Pikal, Greg Sacha, Alina Alexeenko, T N Thompson, Cindy Reiter, James Searles, Paul Coiteux
Recommended best practices in monitoring of product status during pharmaceutical freeze drying are presented, focusing on methods that apply to both laboratory and production scale. With respect to product temperature measurement, sources of uncertainty associated with any type of measurement probe are discussed, as well as important differences between the two most common types of temperature-measuring instruments-thermocouples and resistance temperature detectors (RTD). Two types of pressure transducers are discussed-thermal conductivity-type gauges and capacitance manometers, with the Pirani gauge being the thermal conductivity-type gauge of choice...
February 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28205143/development-of-a-gastric-absorptive-immediate-responsive-oral-protein-loaded-versatile-polymeric-delivery-system
#9
Pierre P D Kondiah, Yahya E Choonara, Lomas K Tomar, Charu Tyagi, Pradeep Kumar, Lisa C du Toit, Thashree Marimuthu, Girish Modi, Viness Pillay
A multifunctional platform to deliver three diverse proteins of insulin, interferon beta (INF-β) and erythropoietin (EPO), using a novel copolymeric microparticulate system of TMC-PEGDMA-MAA, was synthesised as an intelligent pH-responsive 2-fold gastric and intestinal absorptive system. Physiochemical and physicomechanical studies proved the degree of crystallinity that supported the controlled protein delivery of the microparticulate system. The copolymer was tableted before undertaking in vitro and in vivo analysis...
February 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28185211/clear-aqueous-topical-drop-of-triamcinolone-acetonide
#10
Hoang M Trinh, Kishore Cholkar, Mary Joseph, Xiaoyan Yang, Ashim K Mitra
The objective of this study was to develop a clear aqueous mixed nanomicellar formulation (NMF) of triamcinolone acetonide (TA) with a combination of nonionic surfactant hydrogenated castor oil 60 (HCO-60) and octoxynol-40 (Oc-40). In order to delineate the effects of drug-polymer interactions on entrapment efficiency (EE), loading efficiency (LE), and critical micellar concentration (CMC), a design of experiment (DOE) was performed to optimize the formulation. In this study, full-factorial design has been used with HCO-60 and OC-40 as independent variables...
February 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28176213/development-of-a-new-dissolution-test-method-for-soft-chewable-dosage-forms
#11
Carmen Stomberg, Venkata-Rangarao Kanikanti, Hans-Jürgen Hamann, Peter Kleinebudde
Soft chewable dosage forms are a new approach to improve the compliance of medication for special patient populations. Based on their texture, they are chewed several times before they get swallowed. A suitable dissolution method based on in vivo chewing data was developed. The method covers parts of dissolution within the oral cavity (simulation of chewing) as well as the dissolution of the swallowed bolus within the gastrointestinal tract. Chewing was simulated by the help of a steel tooth assembled to a texture analyzer and wedge gliding on an inclined plane, imitating the occlusal glide...
February 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28176212/stable-co-crystals-of-glipizide-with-enhanced-dissolution-profiles-preparation-and-characterization
#12
Narendra Kumar Pandey, Hans Raj Sehal, Varun Garg, Tejasvi Gaur, Bimlesh Kumar, Sachin Kumar Singh, Monica Gulati, K Gowthamarajan, Palak Bawa, Sarvi Yadav Rajesh, Parth Sharma, Rakesh Narang
Present study deciphers preparation of co-crystals of lipophilic glipizide by using four different acids, oxalic, malonic, stearic, and benzoic acids, in order to achieve enhanced solubility and dissolution along with stability. All co-crystals were prepared by dissolving drug and individual acids in the ratio of 1:0.5 in acetonitrile at 60-70°C for 15 min, followed by cooling at room temperature for 24 h. FT-IR spectroscopy revealed no molecular interaction between acids and drug as the internal structure and their geometric configurations remain unchanged...
February 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28168626/influence-of-drug-brittleness-nanomilling-time-and-freeze-drying-on-the-crystallinity-of-poorly-water-soluble-drugs-and-its-implications-for-solubility-enhancement
#13
Miriam Colombo, Steven Orthmann, Marco Bellini, Sven Staufenbiel, Roland Bodmeier
The aim of this study was to assess whether wet bead milling of dexamethasone and tacrolimus suspensions leads to a lower degree of crystallinity of nanocrystals, and if the degree of crystallinity affects the drug solubility, in addition to particle size. Powder X-ray diffraction (XRD) was used to determine the degree of crystallinity of the particles, which decreased during milling until reaching a plateau: the particles had ∼79% degree of crystallinity after 5 h milling. Different milling times were required for the two drugs in order to reach their plateaux, 2 h for dexamethasone and 3 h for tacrolimus...
February 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28168625/formulation-of-polyherbal-patches-based-on-polyvinyl-alcohol-and-hydroxypropylmethyl-cellulose-characterization-and-in-vitro-evaluation
#14
Jirapornchai Suksaeree, Noramon Nawathong, Rinrada Anakkawee, Wiwat Pichayakorn
The purpose of this research was to prepare and characterize polyherbal patches made from polyvinyl alcohol (PVA) and hydroxypropylmethyl cellulose (HPMC) with glycerine as a plasticizer. Polyherbal extracts were Luk-Pra-Kob recipes extracted with 95% ethanol. They were prepared by mixing the polymer solutions and glycerine in a beaker; subsequently, the polyherbal extracts were homogeneously mixed. Then, they were transferred into a Petri dish and dried in a hot-air oven at 70 ± 2°C for 5 h. The dry polyherbal patches were evaluated for physicochemical properties by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and a scanning electron microscope...
February 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28160208/enhancement-of-skin-permeation-and-skin-immunization-of-ovalbumin-antigen-via-microneedles
#15
Boonnada Pamornpathomkul, Theerasak Rojanarata, Praneet Opanasopit, Tanasait Ngawhirunpat
The purpose of this study was to evaluate the use of different types of microneedles and doses of ovalbumin antigen for in vitro skin permeation and in vivo immunization. In vitro skin permeation experiments and confocal laser scanning microscopy revealed that hollow microneedles had a superior enhancing effect on skin permeation compared with a solid microneedle patch and untreated skin by efficiently delivering ovalbumin-fluorescein conjugate into the deep skin layers. The flux and cumulative amount of ovalbumin-fluorescein conjugate at 8 h after administering with various conditions could be ranked as follows: hollow MN; high dose > medium dose > low dose > MN patch; high dose > medium dose > low dose > untreated skin; high dose > medium dose > low dose > without ovalbumin-fluorescein conjugate...
February 3, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28155135/influence-of-peroxide-impurities-in-povidone-on-the-stability-of-selected-%C3%AE-blockers-with-the-help-of-hplc
#16
Saklecha Prachi, Chaudhary Komal, Mehta J Priti
A present study was conducted to investigate compatibility of β-blocker drugs( like atenolol, labetalol hydrochloride, bisoprolol fumarate, metoprolol succinate, carvedilol and propranolol hydrochloride) with the pharmaceutical excipient povidone. To check the influence of peroxide impurity present in povidone on the stability of β-blockers, a binary mixture technique has been adopted. The binary mixtures (1:1) of β-blockers with povidone excipient were stored for the duration of 6 months at accelerated conditions (40°C and 75% RH) and analyzed with the technique of high-performance liquid chromatography (HPLC)...
February 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28138820/development-of-extended-release-oral-flexible-tablet-er-oft-formulation-for-pediatric-and-geriatric-compliance-an-age-appropriate-formulation
#17
Prabagaran Chandrasekaran, Ruckmani Kandasamy
Development of age-appropriate formulation suitable for pediatric and geriatric patients involves various challenges. The objective of this research was to develop extended-release oral flexible tablet (ER-OFT) formulation using carbamazepine (CBZ) as model drug for pediatric and geriatric compliance. ER-microparticles of carbamazepine, a BCS class 2, and narrow therapeutic index (NTI) drug, were prepared using ethyl cellulose as matrixing polymer and hypromellose as hydrophilic pore former. Microparticles were prepared using high-shear granulator fitted with an atomizing spray system...
January 30, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28127721/stabilization-and-amorphization-of-lovastatin-using-different-types-of-silica
#18
Mai Khanfar, Suhair Al-Nimry
Lovastatin (LOV), an antihyperlipidimic agent, is characterized by low solubility/poor dissolution and, thus, low bioavailability (<5%). A beneficial effect on its bioavailability could result from improving its dissolution. One of the most common methods used to enhance dissolution is the preparation of solid dispersions. Solid dispersions of LOV and silica with different surface areas were prepared. The effects of the type of silica, ratio of drug/silica, incubation period with silica, and the effect of surface area were all studied...
January 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28127720/dem-modelling-of-granule-rearrangement-and-fracture-behaviours-during-a-closed-die-compaction
#19
Ryoichi Furukawa, Kazunori Kadota, Tetsuro Noguchi, Atsuko Shimosaka, Yoshiyuki Shirakawa
The closed-die compaction behaviour of D-mannitol granules has been simulated by the discrete element method (DEM) to investigate the granule rearrangement and fracture behaviour during compaction which affects the compactibility of the tablet. The D-mannitol granules produced in a fluidized bed were modelled as agglomerates of primary particles connected by linear spring bonds. The validity of the model granule used in the DEM simulation was demonstrated by comparing to the experimental results of a uniaxial compression test...
January 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28124212/skin-delivery-of-egcg-and-silibinin-potential-of-peptide-dendrimers-for-enhanced-skin-permeation-and-deposition
#20
Pallavi Krishna Shetty, Jyothsna Manikkath, Karnaker Tupally, Ganesh Kokil, Aswathi R Hegde, Sushil Y Raut, Harendra S Parekh, Srinivas Mutalik
The aim of the present study was to evaluate the ability of the peptide dendrimers to facilitate transdermal delivery of antioxidants, silibinin, and epigallocatechin-3-gallate (EGCG). Drug-peptide dendrimer complexes were prepared and evaluated for their ability to permeate across the skin. The data revealed the ready formation of complexes between drug and peptide dendrimer in a molar ratio of 1:1. In vitro permeation studies using excised rat skin and drug-peptide dendrimer complexes showed highest values for cumulative drug permeation at the end of 12 h (Q12), with corresponding permeability coefficient (Kp) and enhancement ratio values also determined at this time point...
January 25, 2017: AAPS PharmSciTech
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