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https://www.readbyqxmd.com/read/28343348/process-analytical-techniques-for-hot-melt-extrusion-and-their-application-to-amorphous-solid-dispersions
#1
REVIEW
Patrick Hitzer, Tim Bäuerle, Tobias Drieschner, Edwin Ostertag, Katharina Paulsen, Holger van Lishaut, Günter Lorenz, Karsten Rebner
Newly developed active pharmaceutical ingredients (APIs) are often poorly soluble in water. As a result the bioavailability of the API in the human body is reduced. One approach to overcome this restriction is the formulation of amorphous solid dispersions (ASDs), e.g., by hot-melt extrusion (HME). Thus, the poorly soluble crystalline form of the API is transferred into a more soluble amorphous form. To reach this aim in HME, the APIs are embedded in a polymer matrix. The resulting amorphous solid dispersions may contain small amounts of residual crystallinity and have the tendency to recrystallize...
March 25, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28342789/enhanced-gastric-stability-of-esomeprazole-by-molecular-interaction-and-modulation-of-microenvironmental-ph-with-alkalizers-in-solid-dispersion
#2
Hien Van Nguyen, Namhyun Baek, Beom-Jin Lee
Due to the instability of esomeprazole magnesium dihydrate (EPM), a proton pump inhibitor, in gastric fluid, enteric-coated dosage form is commonly used for therapeutic application. In this study, we prepared new gastric fluid resistant solid dispersions (SDs) containing alkalizers. Then, new mechanistic evidence regarding the effects of pharmaceutical alkalizers on the aqueous stability of EPM in simulated gastric fluid was investigated. The alkalizer-loaded SD were prepared by dissolving or dispersing EPM, hydroxypropyl methylcellulose (HPMC) 6 cps, and an alkalizer, in ethanol 50% (v/v) followed by spray drying...
March 22, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28330645/design-of-fixed-dose-combination-and-physicochemical-characterization-of-enteric-coated-bilayer-tablet-with-circadian-rhythmic-variations-containing-telmisartan-and-pravastatin-sodium
#3
Daoqi Luo, Joo Hee Kim, Chulhun Park, Euichaul Oh, Jun Bum Park, Jing-Hao Cui, Qing-Ri Cao, Beom-Jin Lee
The aim of this study was to investigate a fixed dose combination (FDC) of telmisartan (TEL) and pravastatin sodium (PRA) in enteric-coated bilayer tablets, which was designed for once-daily bedtime dose in order to match circadian rhythmic variations of hypertension and cholesterol synthesis and optimize the patient friendly dosing treatment. Due to the poor aqueous solubility of TEL, a ternary solid dispersions (SD) consisting of TEL, polyethylene glycol 6000 (PEG 6000) and magnesium oxide (MgO) were designed to enhance its dissolution rate in intestinal fluid...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28324691/comparison-of-three-different-types-of-cilostazol-loaded-solid-dispersion-physicochemical-characterization-and-pharmacokinetics-in-rats
#4
Omer Mustapha, Kyung Soo Kim, Shumaila Shafique, Dong Shik Kim, Sung Giu Jin, Youn Gee Seo, Yu Seok Youn, Kyung Taek Oh, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
The aim of this research was to compare three different types of cilostazol-loaded solid dispersion system including solvent-evaporated, solvent-wetted and surface-attached solid dispersion. The effect of polymers and surfactants on the aqueous solubility of cilostazol was investigated, leading to the selection of polyvinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS). Employing a spray-drying technique, numerous surface-attached, solvent-evaporated and solvent-wetted solid dispersions were prepared with various amounts PVP and SLS using water, 90% ethanol and acetone, respectively...
March 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28322164/solubilization-and-enhancement-of-ex-vivo-vaginal-delivery-of-progesterone-using-solid-dispersions-inclusion-complexes-and-micellar-solubilization
#5
Abeer S Hassan, Ghareb M Soliman, Mona M El-Mahdy, Gamal El-Din A El-Gindy
Progesterone (PG), a natural female sex hormone is used clinically in menopausal hormone replacement therapy and to control reproductive functions. Its very limited aqueous solubility of 7 µg/ml results in reduced oral bioavailability and low patient compliance when administered in high doses. The aim of this study was to enhance PG aqueous solubility and vaginal delivery using solid dispersion, inclusion complex and micellar solubilization techniques. PG solid dispersions and inclusion complexes were prepared by solvent evaporation method using different polymers, such as cyclodextrins, polyvinyl pyrrolidone (PVP), poly (ethylene glycol) 6000, Pluronic® F-127 and Pluronic® F-68...
March 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28296409/microfibrous-solid-dispersions-of-poorly-water-soluble-drugs-produced-via-centrifugal-spinning-unexpected-dissolution-behaviour-on-recrystallization
#6
Stefania Marano, Susan Anne Barker, Shahrzad Missaghi, Ali Rajabi-Siahboomi, Bahijja Tolulope Raimi-Abraham, Abil E Aliev, Duncan Q M Craig
Temperature-controlled, solvent-free centrifugal spinning may be used as a means of rapid production of amorphous solid dispersions in the form of drug-loaded sucrose microfibers. However, due to the high content of amorphous sucrose in the formulations, such microfibers may be highly hygroscopic and unstable on storage. In this study, we explore both the effects of water uptake of the microfibers and the consequences of deliberate recrystallization for the associated dissolution profiles. The stability of sucrose microfibers loaded with three selected BCS class II model drugs (itraconazole (ITZ), olanzapine (OLZ) and piroxicam (PRX)) was investigated under four different relative humidity conditions (11, 33, 53 and 75% RH) at 25°C for 8 months, particularly focusing on the effect of the highest level of moisture (75% RH) on the morphology, size, drug distribution, physical state and dissolution performance of microfibers...
March 15, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28286079/multifractal-and-mechanical-analysis-of-amorphous-solid-dispersions
#7
Camille Adler, Alexandra Teleki, Martin Kuentz
The formulation of lipophilic and hydrophobic compounds is a challenge for the pharmaceutical industry and it requires the development of complex formulations. Our first aim was to investigate hot-melt extrudate microstructures by means of multifractal analysis using scanning electron microscopy imaging. Since the microstructure can affect solid dosage form performance such as mechanical properties, a second objective was to study the influence of the type of adsorbent and of the presence of an amorphous compound on extrudate hardness...
March 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28282989/sustained-release-ivermectin-loaded-solid-lipid-dispersion-for-subcutaneous-delivery-in-vitro-and-in-vivo-evaluation
#8
Mengmeng Lu, Dan Xiong, Weiwei Sun, Tong Yu, Zixia Hu, Jiafeng Ding, Yunpeng Cai, Shizhuang Yang, Baoliang Pan
This work aimed to develop a sustained release solid dispersion of ivermectin (IVM-SD) in a lipid matrix (hydrogenated castor oil, HCO) for subcutaneous delivery. Solvent-melting technology was employed to prepare IVM-SDs using HCO. The physicochemical properties of the IVM-SDs were evaluated by scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and Fourier transform infrared spectroscopy (FTIR). The release of IVM from IVM-SDs was evaluated with HPLC in vitro. Pharmacokinetics of IVM was studied in rabbits following a single subcutaneous administration of IVM-SD formulations...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28277846/study-of-a-novel-disintegrable-oleanolic-acid-polyvinylpolypyrrolidone-solid-dispersion
#9
Weiqin Wang, Changchang Cui, Mengying Li, Zhenhai Zhang, Huixia Lv
Novel solid dispersions of oleanolic acid-Polyvinylpolypyrrolidone (OLA-PVPP SDs) were designed and prepared to improve the apparent solubility of drug, as well as to improve the stability, fluidity and compressibility of SDs. Disintegrable OLA-PVPP SDs were then evaluated both in vitro and in vivo. DSC, XRD, IR and SEM analysis proved the formation of OLA-PVPP SD and its amorphous state. The results of fluidity study, moisture absorption test and stability test showed that OLA-PVPP SD with good fluidity and qualified stability was successfully obtained...
March 2, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28260895/biodegradable-polymeric-micelles-coencapsulating-paclitaxel-and-honokiol-a-strategy-for-breast-cancer-therapy-in-vitro-and-in-vivo
#10
Ning Wang, Zhihan Wang, Shihong Nie, Linjiang Song, Tao He, Suleixin Yang, Xi Yang, Cheng Yi, Qinjie Wu, Changyang Gong
The combination of chemotherapy drugs attracts more attention in clinical cancer trials. However, the poor water solubility of chemotherapeutic drugs restricts their anticancer application. In order to improve antitumor efficiency and reduce side effects of free drugs, we prepared paclitaxel (PTX) and honokiol (HK) combination methoxy poly(ethylene glycol)-poly(caprolactone) micelles (P-H/M) by solid dispersion method against breast cancer. The particle size of P-H/M was 28.7±2.5 nm, and transmission electron microscope image confirmed that P-H/M were spherical in shape with small particle size...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28259831/melt-extrusion-vs-spray-drying-the-effect-of-processing-methods-on-crystalline-content-of-naproxen-povidone-formulations
#11
Abbe Haser, Tu Cao, Joe Lubach, Tony Listro, Larry Acquarulo, Feng Zhang
Our hypothesis is that melt extrusion is a more suitable processing method than spray drying to prepare amorphous solid dispersions of drugs with a high crystallization tendency. Naproxen-povidone K25 was used as the model system in this study. Naproxen-povidone K25 solid dispersions at 30% and 60% drug loadings were characterized by modulated DSC, powder X-ray diffraction, FT-IR, and solid-state (13)C NMR to identify phase separation and drug recrystallization during processing and storage. At 30% drug loading, hydrogen bond (H-bond) sites of povidone K25 were not saturated and the glass transition (Tg) temperature of the formulation was higher...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28257881/dual-mechanism-gastroretentive-drug-delivery-system-loaded-with-an-amorphous-solid-dispersion-prepared-by-hot-melt-extrusion
#12
Anh Q Vo, Xin Feng, Manjeet Pimparade, Xinyou Ye, Dong Wuk Kim, Scott T Martin, Michael A Repka
In the present study, we aimed to prepare a gastroretentive drug delivery system that would be both highly resistant to gastric emptying via multiple mechanisms and would also potentially induce in situ supersaturation. The bioadhesive floating pellets, loaded with an amorphous solid dispersion, were prepared in a single step of hot-melt extrusion technology. Hydroxypropyl cellulose (Klucel™ MF) and hypromellose (Benecel™ K15M) were used as matrix-forming polymers, and felodipine was used as the model drug...
February 28, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28257818/novel-alternating-current-electrospinning-of-hydroxypropylmethylcellulose-acetate-succinate-hpmcas-nanofibers-for-dissolution-enhancement-the-importance-of-solution-conductivity
#13
Attila Balogh, Balázs Farkas, Ádám Pálvölgyi, András Domokos, Balázs Démuth, György Marosi, Zsombor Kristóf Nagy
Novel high-yield alternating current electrospinning (ACES) as well as direct current (DCES) methods were investigated to prepare high quality hydroxypropylmethylcellulose acetate succinate (HPMCAS) fibers for the dissolution enhancement of poorly soluble spironolactone (SPIR). Although HPMCAS is of great pharmaceutical importance as a carrier of marketed solid dispersion-based products, it was found to be unprocessable using electrospinning. Addition of small amounts of polyethylene oxide as aid polymer provided smooth fibers with DCES but strongly beaded products with ACES...
February 28, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28241116/molecular-factors-governing-the-liquid-and-glassy-states-recrystallization-of-celecoxib-in-binary-mixtures-with-excipients-of-different-molecular-weights
#14
K Grzybowska, K Chmiel, J Knapik, A Grzybowski, K Jurkiewicz, M Paluch
Transformation of poorly water-soluble crystalline pharmaceuticals to the amorphous form is one of the most promising strategies to improve their oral bioavailability. Unfortunately, the amorphous drugs are usually thermodynamically unstable and may quickly return to their crystalline form. A very promising way to enhance the physical stability of amorphous drugs is to prepare amorphous compositions of APIs with certain excipients which can be characterized by significantly different molecular weights, such as polymers, acetate saccharides, and other APIs...
February 27, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28235625/mathematical-model-to-analyze-the-dissolution-behavior-of-metastable-crystals-or-amorphous-drug-accompanied-with-a-solid-liquid-interface-reaction
#15
Daiki Hirai, Yasunori Iwao, Shin-Ichiro Kimura, Shuji Noguchi, Shigeru Itai
Metastable crystals and the amorphous state of poorly water-soluble drugs in solid dispersions (SDs), are subject to a solid-liquid interface reaction upon exposure to a solvent. The dissolution behavior during the solid-liquid interface reaction often shows that the concentration of drugs is supersaturated, with a high initial drug concentration compared with the solubility of stable crystals but finally approaching the latter solubility with time. However, a method for measuring the precipitation rate of stable crystals and/or the potential solubility of metastable crystals or amorphous drugs has not been established...
February 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28217547/a-study-of-the-formation-of-magnetically-active-solid-dispersions-of-phenacetin-using-atomic-and-magnetic-force-microscopy
#16
Liana Stanislavovna Usmanova, Marat Akhmedovich Ziganshin, Valery Vilenovich Gorbatchuk, Sufia Askhatovna Ziganshina, Dmitry Anatolevich Bizyaev, Anastas Akhmetovich Bukharaev, Timur Anvarovich Mukhametzyanov, Alexander Vladimirovich Gerasimov
A lot of pharmaceutical substances have a poor solubility that limits their absorption and distribution to the targeted sites to elicit the desired action without causing untoward effects on healthy cells or tissues. For such drugs, new modes of delivery have to be developed for efficient and effective delivery of the drug to the target site. Formation of magnetically active solid dispersion of such drugs could be a useful approach to addressing this problem because they combine targeted delivery and good solubility...
January 2017: Journal of Advanced Pharmaceutical Technology & Research
https://www.readbyqxmd.com/read/28208830/cefdinir-solid-dispersion-composed-of-hydrophilic-polymers-with-enhanced-solubility-dissolution-and-bioavailability-in-rats
#17
Hyun-Jong Cho, Jun-Pil Jee, Ji-Ye Kang, Dong-Yeop Shin, Han-Gon Choi, Han-Joo Maeng, Kwan Hyung Cho
The aim of this work was to develop cefdinir solid dispersions (CSDs) prepared using hydrophilic polymers with enhanced dissolution/solubility and in vivo oral bioavailability. CSDs were prepared with hydrophilic polymers such as hydroxypropyl-methylcellulose (HPMC; CSD1), carboxymethylcellulose-Na (CMC-Na; CSD2), polyvinyl pyrrolidone K30 (PVP K30; CSD3) at the weight ratio of 1:1 (drug:polymer) using a spray-drying method. The prepared CSDs were characterized by aqueous solubility, differential scanning calorimetry (DSC), powder X-ray diffraction (p-XRD), scanning electron microscopy (SEM), aqueous viscosity, and dissolution test in various media...
February 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28208662/characterization-molecular-docking-and-in-vitro-dissolution-studies-of-solid-dispersions-of-20-s-protopanaxadiol
#18
Qi Zhang, Yiqiong Pu, Bing Wang, Yuqin Wang, Tina Tingxia Dong, Tao Guo, Tong Zhang, Zhenzhen Cai
In this study, we prepared solid dispersions (SDs) of 20(S)-protopanaxadiol (PPD) using a melting-solvent method with different polymers, in order to improve the solubility and dissolution performance of drugs with poor water solubility. The SDs were characterized via differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and molecular docking and dynamics study. DSC and PXRD results indicated that PPD crystallinity in SDs was significantly reduced, and that the majority of PPD is amorphous...
February 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28204967/advantageous-solubility-permeability-interplay-when-using-amorphous-solid-dispersion-asd-formulation-for-the-bcs-class-iv-p-gp-substrate-rifaximin-simultaneous-increase-of-both-the-solubility-and-the-permeability
#19
Avital Beig, Noa Fine-Shamir, David Lindley, Jonathan M Miller, Arik Dahan
Rifaximin is a BCS class IV (low-solubility, low-permeability) drug and also a P-gp substrate. The aims of this work were to assess the efficiency of different rifaximin amorphous solid dispersion (ASDs) formulations in achieving and maintaining supersaturation and to investigate the consequent solubility-permeability interplay. Spray-dried rifaximin ASDs were prepared with different hydrophilic polymers and their ability to achieve and maintain supersaturation was assessed. Then, rifaximin's apparent intestinal permeability was investigated as a function of increasing supersaturation both in vitro using the parallel artificial membrane permeability assay (PAMPA) and in vivo using the single-pass rat intestinal perfusion (SPIP) model...
February 15, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28201965/preparation-and-characterization-of-silymarin-synchronized-and-sustained-release-dropping-pill
#20
Zhi-Hong Liu, Xue-Jing Li, Ai-Wen Huang, Jing Zhang, Hong-Tao Song
PURPOSE: This study aimed to develop a synchronized and sustained-release silymarin dropping pill, and to evaluate its pharmacokinetic characteristics. METHODS: Polyoxyethylene stearate, glyceryl monostearate, and stearic acid were used to prepare the dropping pills. X-ray powder diffraction, differential scanning calorimetry, and release were used to evaluate its physicochemical properties. The plasma concentration of silybin in beagle dogs after oral administration of silymarin dropping pills and silymarin capsule was determined by RP-HPLC...
February 13, 2017: Current Drug Delivery
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