Read by QxMD icon Read

"solid dispersion"

Giovanna C R M Schver, Dajun D Sun, Salvana P M Costa, Keyla E R Silva, Jamerson F Oliveira, Larissa Araujo Rolim, Mônica Camelo Pessôa de Azevedo Albuquerque, André de Lima Aires, Maria do Carmo A Lima, Ivan R Pitta, Ping I Lee, Pedro J Rolim-Neto
Drug candidate LPSF/FZ4 with promising schistosomicidal properties in vitro was previously synthesized. However, LPSF/FZ4 has limited aqueous solubility (<1 μg/mL), leading to ineffective dissolution and, therefore, no meaningful in vivo comparative studies could be pursued. This study was aimed to develop a proper amorphous solid dispersion (SD) to enhance the solubility and dissolution rate of LPSF/FZ4 such that its biological activity could be investigated. To better understand its physiological behavior, the pKa of LPSF/FZ4, a monoprotic weak acid with NH group at the imidazolidine ring, was first determined to be 8...
January 10, 2018: European Journal of Pharmaceutical Sciences
G H Meletharayil, H A Patel, L E Metzger, C Marella, T Huppertz
Innovative clean label processes employed in the manufacture of acid gels are targeted to modify the structure of proteins that contribute to rheological properties. In the present study, CO2-treated milk protein concentrate powder with 80% protein in dry matter (TMPC80) was mixed with nonfat dry milk (NDM) in different ratios for the manufacture of acid gels. Dispersions of NDM and TMPC80 that provided 100, 90, 70, and 40% of protein from NDM were reconstituted to 4.0% (wt/wt) protein and 12.0% (wt/wt) total solids...
January 10, 2018: Journal of Dairy Science
Benjamin Schammé, Nicolas Couvrat, Vincent Tognetti, Laurent Delbreilh, Valérie Dupray, Eric Dargent, Gérard Coquerel
The effect of low molecular weight excipients on drug-excipient interactions, molecular mobility and propensity to recrystallization of an amorphous active pharmaceutical ingredient is investigated. Two structurally related excipients (α-Pentaacetylglucose and β-Pentaacetylglucose), five different drug:excipient ratios (1:5, 1:2, 1:1, 2:1 and 5:1, w/w) and three different solid state characterization tools (Differential Scanning Calorimetry, X-Ray Powder Diffraction and Dielectric Relaxation Spectroscopy) were selected for the present research...
January 12, 2018: Molecular Pharmaceutics
Jens Wesholowski, Sebastian Prill, Andreas Berghaus, Markus Thommes
Hot-melt extrusion on co-rotating twin screw extruders is a focused technology for the production of pharmaceuticals in the context of Quality by Design. Since it is a continuous process, the potential for minimizing product quality fluctuation is enhanced. A typical application of hot-melt extrusion is the production of solid dispersions, where an active pharmaceutical ingredient (API) is distributed within a polymer matrix carrier. For this dosage form, the product quality is related amongst others to the drug content...
January 11, 2018: Drug Delivery and Translational Research
Tu Van Duong, Bart Goderis, Jan Van Humbeeck, Guy Van den Mooter
The microstructure of pharmaceutical semicrystalline solid dispersions has attracted extensive attention due to its complexity that might result in the diversity in physical stability, dissolution behavior and pharmaceutical performance of the systems. Numerous factors have been reported that dictate the microstructure of semicrystalline dispersions. Nevertheless, the importance of the complicated conformation of the polymer has never been elucidated. In this study, we investigate the microstructure of dispersions of polyethylene glycol and active pharmaceutical ingredients by small angle X-ray scattering and high performance differential scanning calorimetry...
January 10, 2018: Molecular Pharmaceutics
Jeffrey M Ting, William W Porter, Jodi M Mecca, Frank S Bates, Theresa M Reineke
Synthetic polymers have enabled amorphous solid dispersions (ASDs) to emerge as an oral delivery strategy for overcoming poor drug solubility in aqueous environments. Modern ASD products noninvasively treat a range of chronic diseases (for example, hepatitis C, cystic fibrosis, and HIV). In such formulations, polymeric carriers generate and maintain drug supersaturation upon dissolution, increasing the apparent drug solubility to enhance gastrointestinal barrier absorption and oral bioavailability. In this Review, we outline several approaches in designing polymeric excipients to drive interactions with active pharmaceutical ingredients (APIs) in spray-dried ASDs, highlighting polymer-drug formulation guidelines from industrial and academic perspectives...
January 10, 2018: Bioconjugate Chemistry
Silvina Orlandi, Josefina Priotti, Hermínio P Diogo, Dario Leonardi, Claudio J Salomon, Teresa G Nunes
Praziquantel (PZQ) is the recommended, effective, and safe treatment against all forms of schistosomiasis. Solid dispersions (SDs) in water-soluble polymers have been reported to increase solubility and bioavailability of poorly water-soluble drugs like PZQ, generally due to the amorphous form stabilization. In this work, poloxamer (PLX) 237 and poly(vinylpyrrolidone) (PVP) K30 were evaluated as potential carriers to revert PZQ crystallization. Binary and ternary SDs were prepared by the solvent evaporation method...
January 8, 2018: AAPS PharmSciTech
Eirini Palazi, Evangelos Karavas, Panagiotis Barmpalexis, Margaritis Kostoglou, Stavroula Nanaki, Evi Christodoulou, Dimitrios N Bikiaris
The purpose of the present study was to use commercial available polymers like PVP/PEG, soluplus® and kollidon® SR to prepare immediate and sustained release formulations of felodipine by hot melt mixing method. Solid dispersions containing 5, 10, 20 and 30wt% drug have been prepared in a Haake-Buchler Reomixer at melt temperatures 130°C and mixing times 10min. As was found from DSC and XDR studies completely amorphous and miscible solid dispersions can be prepared. In all cases a single glass transition was recorded, which is depending from the used drug amount...
January 3, 2018: European Journal of Pharmaceutical Sciences
Kristin Lehmkemper, Samuel O Kyeremateng, Matthias Degenhardt, Gabriele Sadowski
PURPOSE: The oral bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs) can be improved by the preparation of amorphous solid dispersions (ASDs) where the API is dissolved in polymeric excipients. Desired properties of such ASDs like storage stability, dissolution behavior, and processability can be optimized by additional excipients. In this work, the influence of so-called low-molecular-weight excipients (LMWEs) on the phase behavior of ASDs was investigated...
January 5, 2018: Pharmaceutical Research
Kamil Wlodarski, Feng Zhang, Tongzhou Liu, Wieslaw Sawicki, Thomas Kipping
PURPOSE: The first objective is to evaluate the feasibility of melt-extruding polyvinyl alcohol-based amorphous solid dispersions for oral drug delivery. The second objective is to investigate the miscibility between polyvinyl alcohol 4-88 and copovidone, and to characterize the properties of ternary itraconazole amorphous solid dispersions comprising both polymers. METHODS: Samples were prepared using a co-rotating, twin-screw extruder. A solution precipitation study was conducted to compare the precipitation inhibition of polyvinyl alcohol against other commonly used polymers for amorphous solid dispersions...
January 5, 2018: Pharmaceutical Research
Chengyu Liu, Zhengsheng Liu, Yuejie Chen, Zhen Chen, Huijun Chen, Yipshu Pui Feng Qian
The aim of this paper was to compare the in vitro dissolution and in vivo bioavailability of three solubility enhancement technologies for β-lapachone (LPC), a poorly water soluble compound with extremely high crystallization propensity. LPC cocrystal was prepared by co-grinding LPC with resorcinol. LPC crystalline and amorphous solid dispersions (CSD and ASD) were obtained by spray drying with Poloxamer 188 and HPMC-AS, respectively. The cocrystal structure was solved by single crystal x-ray diffraction. All formulations were characterized by WAXRD, DSC, POM and SEM...
January 2, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Jian Guan, Qiaoyu Liu, Xiaofei Zhang, Yeli Zhang, Rina Chokshi, Haiyang Wu, Shirui Mao
The objective of this study was to explore the feasibility of using alginate as a promising diphase solid dispersion carrier to enhance dissolution rate of BCS II drugs with improved stability. Taking lovastatin and indomethacin as model drugs, solvent evaporation method was used to prepare solid dispersions. The drug/polymer compatibility was predicted by Hansen solubility parameter and the drug/polymer ratio was screened based on dissolution study, drug existing state in solid dispersion was characterized by DSC and XRPD...
January 2, 2018: European Journal of Pharmaceutical Sciences
Qihong Zhang, Nikolay E Polyakov, Yulia S Chistyachenko, Mikhail V Khvostov, Tatjana S Frolova, Tatjana G Tolstikova, Alexandr V Dushkin, Weike Su
An amorphous solid dispersion (SD) of curcumin (Cur) with disodium glycyrrhizin (Na2GA) was prepared by mechanical ball milling. Curcumin loaded micelles were self-formed by Na2GA when SD dissolved in water. The physical properties of Cur SD in solid state were characterized by differential scanning calorimetry, X-ray diffraction studies, and scanning electron microscope. The characteristics of the sample solutions were analyzed by reverse phase HPLC, UV-visible spectroscopy, 1H NMR spectroscopy, gel permeation LC, and transmission electron microscopy...
November 2018: Drug Delivery
Jinping Fu, Lin Cui, Congbin Yang, Hui Xiong, Guobin Ren, Xingyuan Ma, Qiufang Jing, Fuzheng Ren
The solvent-shift method was used to identify appropriate polymers that inhibit the growth of felodipine crystals by monitoring particle size in supersaturated drug solutions in the presence of different polymers. We speculated that there would be an intermolecular interaction between the selected polymer (zein) and felodipine by extrapolating the inhibitory effect on crystal growth and then used the selected polymer as a carrier to prepare solid dispersions. The formulations were characterized by crystalline properties, thermodynamics of mixing, dissolution behavior, and physical stability...
January 4, 2018: AAPS PharmSciTech
Lizhen Cheng, Ting Li, Ling Dong, Xiaoyu Wang, Qiye Huo, Haoyu Wang, Zhujun Jang, Xinyu Shan, Weisan Pan, Xinggang Yang
In this study, a bi-layer osmotic pump tablet (OPT) of Flurbiprofen (FP) solid dispersions (SDs) was developed to increase the solubility of the poorly soluble drug and control drug release at a constant rate. Based on the thermodynamic properties investigation of the drug, the carrier and the calculation of the solubility parameters, the FP-SD was prepared by hot melt extrusion (HME) technique with the carrier of PVPVA64. Then central composite design-response surface methodology (CCD-RSM) was used to evaluate the influence of factors on the responses...
December 29, 2017: Journal of Pharmaceutical Sciences
Sunita Metre, Sumit Mukesh, Sanjaya K Samal, Mahesh Chand, Abhay T Sangamwar
Rivaroxaban (RXB) is an orally active direct inhibitor of the activated serine protease Factor Xa, given as monotherapy in the treatment of venous thromboembolism (VTE). It has been characterized in-vitro as a substrate for the active, non-saturable efflux via P-gp transporter, limiting its high permeability. Therefore, role of P-gp inhibiting polymers in enhancing the biopharmaceutical performance of RXB by preparing polymeric amorphous solid dispersion and subsequent improvement in solubility and permeability was investigated...
December 29, 2017: Molecular Pharmaceutics
Christopher J Winslow, Brittany L B Nichols, Diana C Novo, Laura I Mosquera-Giraldo, Lynne S Taylor, Kevin J Edgar, Andrew P Neilson
The efficacy of rifapentine, an oral antibiotic used to treat tuberculosis, may be reduced due to degradation at gastric pH and low solubility at intestinal pH. We hypothesized that delivery properties would be improved in vitro by incorporating rifapentine into pH-responsive amorphous solid dispersions (ASDs) with cellulose derivatives including: hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate suberate (CASub), and 5-carboxypentyl hydroxypropyl cellulose (CHC). ASDs generally reduced rifapentine release at gastric pH, with CASub affording >31-fold decrease in area under the curve (AUC) compared to rifapentine alone...
February 15, 2018: Carbohydrate Polymers
Sharif Md Abuzara, Sang-Min Hyun, Jun-Hee Kim, Hee Jun Park, Min-Soo Kim, Jeong-Sook Park, Sung-Joo Hwang
Poor water solubility and poor bioavailability are problems with many pharmaceuticals. Increasing surface area by micronization is an effective strategy to overcome these problems, but conventional techniques often utilize solvents and harsh processing, which restricts their use. Newer, green technologies, such as supercritical fluid (SCF)-assisted particle formation, can produce solvent-free products under relatively mild conditions, offering many advantages over conventional methods. The antisolvent properties of the SCFs used for microparticle and nanoparticle formation have generated great interest in recent years, because the kinetics of the precipitation process and morphologies of the particles can be accurately controlled...
December 23, 2017: International Journal of Pharmaceutics
Divya Dheer, Jyoti, Prem N Gupta, Ravi Shankar
From the current trends, tacrolimus (TAC) has become an important therapeutic option for the optimal individualization of immunosuppressive therapy especially in case of transplant recipients. TAC is used most frequently in comparison to other immunosuppressants because it offers better safety profile with increased long-term survival in patients especially in children and adolescents. This drug has developed an immense interest in the research field owing to its potential pharmacological scope but due to its poor water solubility, need of concomitant steroids and higher incidences of nephrotoxicity, there comes a need for future research to minimize such limitations and decipher maximum use of the drug...
December 22, 2017: European Journal of Pharmaceutical Sciences
Jong Hyuck Park, Dong Shik Kim, Omer Mustapha, Abid Mehmood Yousaf, Jung Suk Kim, Dong Wuk Kim, Chul Soon Yong, Yu Seok Youn, Kyung Taek Oh, Soo-Jeong Lim, Jong Oh Kim, Han-Gon Choi
The aim of this research was to compare three strategies for enhancing the solubility of poorly water-soluble revaprazan hydrochloride: solid dispersion, solid SNEDDS and inclusion compound. The influence of polymers, surfactants and oils on the drug solubility was assessed, and via the chosen carriers, the three types of formulations were prepared utilising spray drying technique. Their physicochemical properties, solubility, dissolution and pharmacokinetics in rats were performed compared with revaprazan powder...
December 12, 2017: Colloids and Surfaces. B, Biointerfaces
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"