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"solid dispersion"

Hiroyuki Takabe, Zachary N Warnken, Yajie Zhang, Daniel A Davis, Hugh D C Smyth, John G Kuhn, Steve Weitman, Robert O Williams Iii
Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain...
May 19, 2018: Pharmaceutics
Matthias E Lauer, Reto Maurer, Anne T De Paepe, Cordula Stillhart, Laurence Jacob, Rajesh James, Yuki Kojima, Rene Rietmann, Tom Kissling, Joost A van den Ende, Sabine Schwarz, Olaf Grassmann, Susanne Page
Hot-melt extrusion is an option to fabricate amorphous solid dispersions and to enhance oral bioavailability of poorly soluble compounds. The selection of suitable polymer carriers and processing aids determines the dissolution, homogeneity and stability performance of this solid dosage form. A miniaturized extrusion device (MinEx) was developed and Hypromellose acetate succinate type L (HPMCAS-L) based extrudates containing the model drugs neurokinin-1 (NK1) and cholesterylester transfer protein (CETP) were manufactured, plasticizers were added and their impact on dissolution and solid-state properties were assessed...
May 19, 2018: Pharmaceutics
Yipshu Pui, Yuejie Chen, Huijun Chen, Shan Wang, Chengyu Liu, Wouter Tonnis, Linc Chen, Peter Serno, Stefan Bracht, Feng Qian
Amorphous solid dispersion (ASD) is one of the most versatile supersaturating drug delivery system to improve the dissolution rate and oral bioavailability of poorly water soluble drugs. PVP based ASD formulation of nimodipine (NMD) has been marketed and effectively used in clinic for nearly 30 years, yet the mechanism by which PVP maintains the supersaturation and subsequently improves the bioavailability of NMD was rarely investigated. In this research, we first studied the molecular interactions between NMD and PVP by solution NMR using CDCl3 as the solvent, and drug-polymer Flory-Huggins interaction parameter...
May 21, 2018: Molecular Pharmaceutics
Lindsay A Smith, Dolores Remedios Serrano, Marion Mauger, Francisco Bolás-Fernández, Maria Auxiliadora Dea-Ayuela, Aikaterini Lalatsa
Nano-enabled lipid based drug delivery systems offer a platform to overcome challenges encountered with current failed leads in the treatment of parasitic and infectious diseases. When prepared with FDA or EMA approved excipients, they can be readily translated without the need for further toxicological studies, while they remain affordable and amenable to scale-up. Buparvaquone (BPQ), a hydroxynapthoquinone with in vitro activity in the nanomolar range, failed to clinically translate as a viable treatment for visceral leishmaniasis due to its poor oral bioavailability limited by its poor aqueous solubility (BCS Class II drug)...
May 15, 2018: Molecular Pharmaceutics
Nizar Al-Zoubi, Faten Odah, Wasfy Obeidat, Ahmad Al-Jaberi, Ioannis Partheniadis, Ioannis Nikolakakis
Solid dispersions of spironolactone with Soluplus® and PVP were prepared by spray drying according to a mixture experimental design and evaluated for moisture content, particle size, drug solubility, crystallinity (PXRD and DSC) and physicochemical interactions (FTIR, Raman). In vitro dissolution was evaluated for the spray dried product itself and after compression into tablets and prediction models were derived using multiple linear regression analysis. The spray dried products consisted of amorphous drug, indicated by the absence of crystalline PXRD peaks...
May 9, 2018: Journal of Pharmaceutical Sciences
Dave A Miller
No abstract text is available yet for this article.
May 8, 2018: AAPS PharmSciTech
Jiali Chen, Yuqi Chen, Wencong Huang, Hanning Wang, Yang Du, Subin Xiong
The objectives of this study were to explore sodium dodecyl sulfate (SDS) and Soluplus on the crystallization inhibition and dissolution of felodipine (FLDP) extrudates by bottom-up and top-down approaches. FLDP extrudates with Soluplus and/or SDS were prepared by hot melt extrusion (HME), and characterized by PLM, DSC and FT-IR. Results indicated that Soluplus inhibited FLDP crystallization and the whole amorphous solid dispersions (ASDs) were binary FLDP-Soluplus (1:3) and ternary FLDP-Soluplus-SDS(1:2:0...
May 5, 2018: Journal of Pharmaceutical Sciences
Alberto Berardi, Lorina Bisharat, Hatim S AlKhatib, Marco Cespi
Zein is the main storage protein of corn and it has several industrial applications. Mainly in the last 10-15 years, zein has emerged as a potential pharmaceutical excipient with unique features. Zein is a natural, biocompatible and biodegradable material produced from renewable sources. It is insoluble, yet due to its amphiphilic nature, it has self-assembling properties, which have been exploited for the formation of micromicroparticle and nanoparticle and films. Moreover, zein can hydrate so it has been used in swellable matrices for controlled drug release...
May 7, 2018: AAPS PharmSciTech
Daniel Sironi, Jörg Rosenberg, Annette Bauer-Brandl, Martin Brandl
Here we report first experiences with the novel in vitro dissolution/permeation setup PermeaLoop™. It was designed to overcome current limitations of in vivo predictive dissolution testing of enabling formulations, such as lack of relevant absorptive drag to allow for meaningful interplay between dissolution and permeation, as it is occurring in vivo. We propose a novel setup with a high area-to-volume ratio and report as a model case the dissolution/permeation behavior of an enabling formulation of the poorly soluble and poorly permeable drug ABT-869...
April 28, 2018: Journal of Pharmaceutical and Biomedical Analysis
Yoshiki Kojo, Hiroki Suzuki, Kouki Kato, Yuuki Kaneko, Kayo Yuminoki, Naofumi Hashimoto, Hideyuki Sato, Yoshiki Seto, Satomi Onoue
The present study aimed to clarify the applicability of a self-micellizing solid dispersion of tranilast (SMSD/TL) to the treatment of inflammatory bowel diseases (IBD) using an experimental colitis model. SMSD/TL with several loading amounts ranging from 10 to 50% was prepared using a wet-milling system. The physicochemical properties of SMSD/TL were evaluated in terms of the dissolution behavior, morphology, and particle size distribution. Animal studies were conducted to evaluate oral bioavailability in rats and anti-inflammatory effects in a rat model of chemically induced colitis...
April 24, 2018: International Journal of Pharmaceutics
K P Safna Hussan, Mohamed Shahin Thayyil, S K Deshpande, T V Jinitha, K Manoj, K L Ngai
In this paper, a stable amorphous solid dispersion of an antihypertensive drug, amlodipine besylate (AMB) was prepared by entrapping it in a polymer matrix, polyvinyl pyrrollidone, in different weight ratios (AMB/PVP 05:95, 10:90, 20:80, 30:70). The glass forming ability of all binary dispersions were studied by means of differential scanning calorimetry and found good correlation between experimental Tg and Fox Flory's prediction. By considering the daily dosage limit of 5 mg, a weight ratio of 05:95 was further considered for the study...
April 24, 2018: European Journal of Pharmaceutical Sciences
Tapan Parikh, Abu T M Serajuddin
PURPOSE: The purpose of this study was to explore the feasibility of developing amorphous solid dispersion (ASD) by inducing acid-base interaction at an elevated temperature using hot melt extrusion. METHODS: Itraconazole and glutaric acid, which do not form salt with each other, were selected as, respectively, model basic drug and weak organic acid. A 1:4:1w/w mixture of itraconazole, glutaric acid and a polymer, Kollidon®VA64, was melt extruded at 95°C. The ground extrudate was characterized by DSC and PXRD and then tested for dissolution at pH 1...
April 25, 2018: Pharmaceutical Research
Disang Feng, Tingting Peng, Zhengwei Huang, Vikramjeet Singh, Yin Shi, Ting Wen, Ming Lu, Guilan Quan, Xin Pan, Chuanbin Wu
The rapid release of poorly water-soluble drugs from amorphous solid dispersion (ASD) is often associated with the generation of supersaturated solution, which provides a strong driving force for precipitation and results in reduced absorption. Precipitation inhibitors, such as polymers and surfactants, are usually used to stabilize the supersaturated solution by blocking the way of kinetic or thermodynamic crystal growth. To evaluate the combined effect of polymers and surfactants on maintaining the supersaturated state of itraconazole (ITZ), various surfactants were integrated with enteric polymer hydroxypropyl methylcellulose acetate succinate (HPMC AS) to develop polymer⁻surfactant based solid dispersion...
April 24, 2018: Pharmaceutics
Casey J Smith, Scott R Griffin, Gregory S Eakins, Fengyuan Deng, Julia K White, Satyanarayana Thirunahari, Srividya Ramakrishnan, Atanu Sangupta, Si-Wei Zhang, Julie Novak, Zhen Liu, Timothy A Rhodes, Garth J Simpson
Triboluminescence (TL) is shown to enable selective detection of trace crystallinity within nominally amorphous solid dispersions (ASDs). ASDs are increasingly used for the preparation of pharmaceutical formulations, the physical stability of which can be negatively impacted by trace crystallinity introduced during manufacturing or storage. In the present study, TL measurements of a model ASD consisting of griseofulvin in polyethylene glycol produced limits of detection of 140 ppm. Separate studies of the particle size dependence of sucrose crystals and the dependence on polymorphism in clopidogrel bisulphate particles are both consistent with a mechanism for TL closely linked to the piezoelectric response of the crystalline fraction...
April 25, 2018: Analytical Chemistry
(no author information available yet)
[This corrects the article on p. 142 in vol. 7.].
October 2017: International Journal of Pharmaceutical Investigation
Albert Nguessan Ngo, Danielle Thomas, James Murowchick, Navid J Ayon, Archana Jaiswal, Bi-Botti Celestin Youan
It is hypothesized that a novel crystalline solid dispersion (CSD) of docetaxel (C-DXT) can be engineered by dispersing native docetaxel (DXT, a class II drug) in sodium acetate crystal (SA). DXT is dissolved in glacial acetic/SA solution and freeze-dried. The C-DXT is characterized by differential scanning calorimetry (DSC), powder X-ray analysis (PXRD), LC-MS/MS, scanning electron microscopy (SEM), transmission electron microscopy (TEM), Quartz crystal microbalance with dissipation monitoring (QCM-D) and dynamic light scattering (DLS)...
April 21, 2018: International Journal of Pharmaceutics
Mark T Davis, Catherine B Potter, Gavin M Walker
Downstream processing aspects of a stable form of amorphous itraconazole exhibiting enhanced dissolution properties were studied. Preparation of this ternary amorphous solid dispersion by either spray drying or hot melt extrusion led to significantly different powder processing properties. Particle size and morphology was analysed using scanning electron microscopy. Flow, compression, blending and dissolution were studied using rheometry, compaction simulation and a dissolution kit. The spray dried material exhibited poorer flow and reduced sensitivity to aeration relative to the milled extrudate...
April 21, 2018: International Journal of Pharmaceutics
Xia Lin, Yang Hu, Lei Liu, Lili Su, Na Li, Jing Yu, Bo Tang, Ziyi Yang
PURPOSE: Amorphous solid dispersions (ASDs) have been widely used in the pharmaceutical industry for solubility enhancementof poorly water-soluble drugs. The physical stability, however, remainsone of the most challenging issues for the formulation development.Many factors can affect the physical stability via different mechanisms, and therefore an in-depth understanding on these factors isrequired. METHODS: In this review, we intend to summarize the physical stability of ASDsfrom a physicochemical perspective whereby factors that can influence the physical stability areclassified into thermodynamic, kinetic and environmental aspects...
April 23, 2018: Pharmaceutical Research
Camila Bezerra Melo Figueirêdo, Daniela Nadvorny, Amanda Carla Quintas de Medeiros Vieira, Giovanna Christinne Rocha de Medeiros Schver, José Lamartine Soares Sobrinho, Pedro José Rolim Neto, Ping I Lee, Monica Felts de La Roca Soares
Posaconazole (PCZ) and benznidazole (BNZ) are known to show synergetic effect in treating the acute and chronic phases of Chagas disease, a neglected parasitic disease. However, as both compounds are poorly water soluble, the development of amorphous solid dispersions (ASDs) of a PCZ/BNZ fixed-dose combination in a water-soluble polymer becomes an attractive option to increase their apparent solubility and dissolution rate, potentially improving their oral bioavailability. The initial approach was to explore solvent evaporated solid dispertion (SD) systems for a PCZ/BNZ 50:50 (wt%) combination at several total drug loading levels (from SD with 10% to 50% drug loading) in water-soluble carriers, including polyvinylpyrrolidone (PVP K-30) and vinylpyrrolidone-vinyl acetate copolymer (PVPVA 64)...
April 18, 2018: European Journal of Pharmaceutical Sciences
Frank Theil, Johanna Milsmann, Sankaran Anantharaman, Holger van Lishaut
The preparation of an amorphous solid dispersion (ASD) by dissolving a poorly water-soluble active pharmaceutical ingredient (API) in a polymer matrix can improve the bioavailability by orders of magnitude. Crystallization of the API in the ASD, though, is an inherent threat for bioavailability. Commonly, the impact of crystalline API on the drug release of the dosage form is studied with samples containing spiked crystallinity. These spiked samples possess implicit differences compared to native crystalline samples, regarding size and spatial distribution of the crystals as well as their molecular environment...
April 12, 2018: Molecular Pharmaceutics
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