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https://www.readbyqxmd.com/read/28771055/the-use-of-albumin-solid-dispersion-to-enhance-the-solubility-of-unionisable-drugs
#1
Mouhamad Khoder, Hamdy Abdelkader, Amr ElShaer, Ayman Karam, Mohammad Najlah, Raid G Alany
In this study, solid dispersions of prednisolone (PRD) and bovine serum albumin (BSA) were prepared by spray drying and freeze drying methods using a PRD:BSA solution (20:1 Molar Ratio (MR)). PRD-BSA dispersed mixtures were characterised by scanning electron microscopy (SEM), and powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). PRD-BSA physical and dispersed mixtures showed significantly higher solubility in water than that of unprocessed drug. Enhancement factor of six was obtained in both physical mixture and solid dispersion solubility studies...
August 3, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28762740/in-situ-characterization-of-pharmaceutical-formulations-by-dynamic-nuclear-polarization-enhanced-mas-nmr
#2
Qing Zhe Ni, Fengyuan Yang, Thach V Can, Ivan V Sergeyev, Suzanne M D'Addio, Sudheer K Jawla, Yongjun Li, Maya P Lipert, Wei Xu, Robert Thomas Williamson, Anthony Leone, Robert G Griffin, Yongchao Su
A principle advantage of magic angle spinning (MAS) NMR spectroscopy lies in its ability to determine molecular structure in a non-invasive and quantitative manner. Accordingly, MAS should be widely applicable to studies of the structure of active pharmaceutical ingredients (API) and formulations. However, the low sensitivity encountered in spectroscopy of natural abundance API's present at low concentration has limited the success of MAS experiments. Dynamic nuclear polarization (DNP) enhances NMR sensitivity and can be used to circumvent this problem provided that suitable paramagnetic polarizing can be incorporated into the system without altering the integrity of solid dosages...
August 1, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28759638/influence-of-the-microwave-technology-on-solid-dispersions-of-mefenamic-acid-and-flufenamic-acid
#3
Sultan Alshehri, Faiyaz Shakeel, Mohamed Ibrahim, Ehab Elzayat, Mohammad Altamimi, Gamal Shazly, Kazi Mohsin, Musaed Alkholief, Bader Alsulays, Abdullah Alshetaili, Abdulaziz Alshahrani, Bander Almalki, Fars Alanazi
The present studies were undertaken to develop solvent-free solid dispersions (SDs) for poorly soluble anti-inflammatory drugs mefenamic acid (MA) and flufenamic acid (FFA) in order to enhance their in vitro dissolution rate and in vivo anti-inflammatory effects. The SDs of MA and FFA were prepared using microwaves irradiation (MW) technique. Different carriers such as Pluronic F127® (PL), Eudragit EPO® (EPO), polyethylene glycol 4000 (PEG 4000) and Gelucire 50/13 (GLU) were used for the preparation of SDs...
2017: PloS One
https://www.readbyqxmd.com/read/28746834/development-of-an-analytical-method-for-crystalline-content-determination-in-amorphous-solid-dispersions-produced-by-hot-melt-extrusion-using-transmission-raman-spectroscopy-a-feasibility-study
#4
L Netchacovitch, E Dumont, J Cailletaud, J Thiry, C De Bleye, P-Y Sacré, M Boiret, B Evrard, Ph Hubert, E Ziemons
The development of a quantitative method determining the crystalline percentage in an amorphous solid dispersion is of great interest in the pharmaceutical field. Indeed, the crystalline Active Pharmaceutical Ingredient transformation into its amorphous state is increasingly used as it enhances the solubility and bioavailability of Biopharmaceutical Classification System class II drugs. One way to produce amorphous solid dispersions is the Hot-Melt Extrusion (HME) process. This study reported the development and the comparison of the analytical performances of two techniques, based on backscattering and transmission Raman spectroscopy, determining the crystalline remaining content in amorphous solid dispersions produced by HME...
July 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28741140/melt-extrusion-for-a-high-melting-point-compound-with-improved-solubility-and-sustained-release
#5
Jiannan Lu, Sakae Obara, Fei Liu, Wanyi Fu, Wen Zhang, Shingo Kikuchi
The objective of the current study was to develop an amorphous solid dispersion for a high melting point compound, griseofulvin (GRF), with an enhanced solubility and a controlled release pattern utilizing hot melt extrusion (HME) technology. Hypromellose acetate succinate (HPMCAS, Shin-Etsu AQOAT®, medium particle size) was explored as the polymeric carrier, while hypromellose (HPMC, Metolose® SR) was chosen as the release rate control agent. GRF presented an HPMCAS grade-dependent solubility: AS-HMP > AS-MMP > AS-LMP...
July 24, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28733828/thermosensitive-in-situ-gel-based-on-solid-dispersion-for-rectal-delivery-of-ibuprofen
#6
Yangdan Liu, Xin Wang, Youping Liu, Xin Di
The objective of this study was to develop a thermosensitive in situ gel based on solid dispersions (SDs) for rectal delivery of ibuprofen (IBU). Thermosensitive (poloxamer 407) and mucoadhesive (hydroxypropylmethyl cellulose E5 and sodium alginate) polymers were used to prepare the in situ gel and the sol-gel transition temperature (T sol-gel) and gel strength were optimized. The in vitro release performance and in vivo pharmacokinetic properties of the in situ gel after their rectal administration to rabbits were investigated...
July 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28721630/in-situ-salification-in-polar-solvents-a-paradigm-for-enabling-drug-delivery-of-weakly-ionic-drugs-as-amorphous-solid-dispersion
#7
Rashmi Nair, Ioorika Lamare, Nirbhay Kumar Tiwari, Punna Rao Ravi, Raviraj Pillai
Solubility challenge for a poorly water-soluble drug gets further intensified when it is weakly ionic because the most common solubility enhancement technique, salt formation, becomes less feasible. Salt screening for such drugs often concludes with either a difficult to crystalize salt or an unstable salt, leading the scientists to explore other solubility enhancement technique like amorphous solid dispersions which is comparatively costlier, time-consuming and may require use of hazardous organic solvents...
July 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28720535/effect-of-polymer-type-on-the-surface-energy-of-acetaminophen-solid-dispersions-prepared-by-melt-method
#8
Tereza Školáková, Jan Patera, Petr Zámostný
Many newly developed active pharmaceutical ingredients (APIs) have very low solubility in aqueous media. The preparation of solid dispersions (SDs) is one way of avoiding this problem. However, compound wettability and thus solubility are influenced by surface energy. In this study, we used inverse gas chromatography (IGC) to evaluate the surface energies of prepared SDs, and compared them with those obtained for physical mixtures (PMs). SDs containing different weight ratios of crystalline acetaminophen and one of three polymers (Kollidon(®) 12 PF, Kollidon(®) VA 64 or Soluplus(®)) were prepared by the melt-quenching of corresponding PMs...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28711592/producing-amorphous-solid-dispersions-via-co-precipitation-and-spray-drying-impact-to-physicochemical-and-biopharmaceutical-properties
#9
Amanda K P Mann, Luke Schenck, Athanas Koynov, Alfred C F Rumondor, Xiaoling Jin, Melanie Marota, Chad Dalton
Many small molecule active pharmaceutical ingredients (APIs) exhibit low aqueous solubility, and benefit from generation of amorphous dispersions of the API and polymer to improve their dissolution properties. Spray drying and hot melt extrusion are two common methods to produce these dispersions; however, for some systems these approaches may not be optimal, and it would be beneficial to have an alternative route. Herein, amorphous solid dispersions of Compound A, a low solubility weak acid, and copovidone were made by conventional spray drying and co-precipitation...
July 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28705623/water-induced-phase-separation-of-miconazole-poly-vinylpyrrolidone-co-vinyl-acetate-amorphous-solid-dispersions-insights-with-confocal-fluorescence-microscopy
#10
Sugandha Saboo, Lynne S Taylor
The aim of this study was to evaluate the utility of confocal fluorescence microscopy (CFM) to study the water-induced phase separation of miconazole-poly (vinylpyrrolidone-co-vinyl acetate) (mico-PVPVA) amorphous solid dispersions (ASDs), induced during preparation, upon storage at high relative humidity (RH) and during dissolution. Different fluorescent dyes were added to drug-polymer films and the location of the dyes was evaluated using CFM. Orthogonal techniques, in particular atomic force microscopy (AFM) coupled with nanoscale infrared spectroscopy (AFM-nanoIR), were used to provide additional analysis of the drug-polymer blends...
July 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28689964/improving-the-solubility-of-nilotinib-through-novel-spray-dried-solid-dispersions
#11
Maikel Herbrink, Jan H M Schellens, Jos H Beijnen, Bastiaan Nuijen
The tyrosine kinase inhibitor nilotinib has a very low aqueous solubility and a low and variable oral bioavailability. A pharmaceutical formulation with an improved solubility may enhance the bioavailability and reduce the variability thereof and of the pharmacokinetics. The aim of this study was to enhance the solubility of nilotinib by developing a spray dried solid dispersion. A broad selection of polymer excipients were tested for solubilizing properties. The spray drying technique was used to produce solid dispersions of nilotinib hydrochloride (NH) in matrices of the best performing polymers...
July 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28687987/evaluation-of-the-crystallization-tendency-of-commercially-available-amorphous-tacrolimus-formulations-exposed-to-different-stress-conditions
#12
Niraj S Trasi, Hitesh S Purohit, Lynne S Taylor
PURPOSE: Tacrolimus, an immunosuppressant, is a poorly water soluble compound whereby the commercially available capsule formulations contain the drug in amorphous form. The goal of this study was to evaluate the robustness of the innovator product and five generic formulations to crystallization following storage at stress conditions. METHODS: Products were purchased from a pharmacy and stored at 40°C/75% relative humidity (RH), open dish conditions. Crystallinity was determined using X-ray diffraction...
July 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28681332/association-of-silver-nanoparticles-and-curcumin-solid-dispersion-antimicrobial-and-antioxidant-properties
#13
Thais Francine Alves, Marco V Chaud, Denise Grotto, Angela Faustino Jozala, Raksha Pandit, Mahendra Rai, Carolina Alves Dos Santos
The last century, more precisely after 1945, was marked by major advances in the treatment of infectious diseases which promoted a decrease in mortality and morbidity. Despite these advances, currently the development of antimicrobial resistance has been growing drastically and therefore there is a pressing need to search for new compounds. Silver nanoparticles (AgNps) have been demonstrating good antimicrobial activity against different bacteria, viruses, and fungi. Curcumin (CUR) extracted from rhizomes of Curcuma longa has a variety of applications including antiinflammatory, antioxidant, and antibacterial agent...
July 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28677032/molecular-mechanism-of-polymer-assisting-supersaturation-of-poorly-water-soluble-loratadine-based-on-experimental-observations-and-molecular-dynamic-simulations
#14
Shenwu Zhang, Mengchi Sun, Yongshan Zhao, Xuyang Song, Zhonggui He, Jian Wang, Jin Sun
Polymers have been usually used to retard nucleation and crystal growth in order to maintain supersaturation, yet their roles in inhibition of nucleation and crystal growth are poorly understood. In our work, the polymer-based supersaturation performances and molecular mechanisms of poorly aqueous soluble loratadine were investigated. Two common hydrophilic polymers (hydroxylpropylmethyl cellulose acetate succinate (HPMC-AS) and poly(vinylpyrrolidone-co-vinyl-acetate) (PVP-VA)) were used. It was found that HPMC-AS was a better polymer to prevent drug molecules from aggregation and to maintain the supersaturated state in solution than PVP-VA...
July 5, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28673860/3d-printing-of-tablets-using-inkjet-with-uv-photoinitiation
#15
Elizabeth A Clark, Morgan R Alexander, Derek J Irvine, Clive J Roberts, Martin J Wallace, Sonja Sharpe, Jae Yoo, Richard J M Hague, Chris J Tuck, Ricky D Wildman
Additive manufacturing (AM) offers significant potential benefits in the field of drug delivery and pharmaceutical/medical device manufacture. Of AM processes, 3D inkjet printing enables precise deposition of a formulation, whilst offering the potential for significant scale up or scale out as a manufacturing platform. This work hypothesizes that suitable solvent based ink formulations can be developed that allow the production of solid dosage forms that meet the standards required for pharmaceutical tablets, whilst offering a platform for flexible and personalized manufacture...
June 30, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28672810/development-and-characterization-of-an-amorphous-solid-dispersion-of-furosemide-in-the-form-of-a-sublingual-bioadhesive-film-to-enhance-bioavailability
#16
Viviana De Caro, Alessia Ajovalasit, Flavia Maria Sutera, Denise Murgia, Maria Antonietta Sabatino, Clelia Dispenza
Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent solubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and evaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing a good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed that the film prepared using the solvent casting method entrapped FUR in the amorphous state...
June 24, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28665158/dissolution-and-bioavailability-enhancement-of-alpha-asarone-by-solid-dispersions-via-oral-administration
#17
Li Deng, Yu Wang, Tao Gong, Xun Sun, Zhi-Rong Zhang
Alpha (α)-asarone (1-propenyl-2,4,5-methoxybenzol) (ARE) has been extensively used to treat chronic obstructive pulmonary diseases (COPD), bronchial asthma, pneumonia and epilepsy. Due to its poor solubility and bioavailability, ARE was clinically administered via intravenous injection. However, severe allergies were often reported due to the presence of solublizers in the injection formulation. In our study, we sought to explore the biopharmaceutical classification of ARE, elucidate the mechanisms behind ARE absorption, and to develop a viable formulation to improve the oral bioavailability of ARE...
June 30, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28663037/freeze-dried-solid-dispersion-of-exemestane-a-way-to-negate-an-aqueous-solubility-and-oral-bioavailability-problems
#18
Shamandeep Kaur, Sunil K Jena, Sanjaya K Samal, Vaishali Saini, Abhay T Sangamwar
This study was envisaged to demonstrate the potential of exemestane loaded phospholipid/sodium deoxycholate solid dispersions (EXE-PL/SDC-SDs) on the solubility and oral bioavailability of EXE. Initial studies were performed to screen the best suitable phospholipid among lysophosphatidylcholine, Phospholipon® P80H and Lipoid® E80S for solid dispersion preparation. Further studies were carried out to optimize the molar concentration of phospholipid and sodium deoxycholate (SDC) for EXE-PL/SDC-SDs preparation...
June 27, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28661679/viewing-molecular-and-interface-interactions-of-curcumin-amorphous-solid-dispersions-for-comprehending-dissolution-mechanisms
#19
Jing Li, Xin Wang, Chang Li, Na Fan, Jian Wang, Zhonggui He, Jin Sun
Tautomeric curcumin amorphous solid dispersions (Cur ASDs) formulated with various typical polymers (polyethylene glycol 6000 (PEG), polyvinylpyrrolidone K30 (PVP), Eudragit EPO (EuD), EuD/hydroxypropylmethyl cellulose E50 (HPMC), and PVP/EuD) were probed using in situ Raman imaging plus spectroscopy and molecular modeling techniques, and dissolution mechanism of Cur ASDs were revealed mainly through molecular and interfacial interactions formed between Cur and polymer. The results demonstrated that Cur of keto form existed in Cur-PEG, Cur of enol form was shown in Cur-PVP, while Cur-EuD or Cur ASDs formulated with EuD as component had Cur of keto form and enol form...
August 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28648863/two-phase-amorphous-amorphous-solid-drug-dispersion-with-enhanced-stability-solubility-and-bioavailability-resulting-from-ultrasonic-dispersion-of-an-immiscible-system
#20
Luz María Martínez, Marcelo Videa, Tania López Silva, Samuel Castro, Adolfo Caballero, Víctor J Lara-Díaz, Fabiola Castorena-Torres
Amorphization of active pharmaceutical ingredients (APIs) and the preparation of solid dispersions are strategies that can be synergized to improve the solubility of oral drugs. Immiscibility between an API and a carrier in the molten state that could be perceived as a problem in the preparation of solid dispersions, may actually introduce an advantage. In the present work, a two-phase amorphous-amorphous solid dispersion (AASD) was prepared by ultrasonicating a molten immiscible mixture of indomethacin (IND) and glucose (GLU) prior quenching...
June 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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