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https://www.readbyqxmd.com/read/29145748/application-of-hot-melt-extrusion-for-improving-bioavailability-of-artemisinin-a-thermolabile-drug
#1
C Kulkarni, A L Kelly, T Gough, V Jadhav, K K Singh, A Paradkar
Hot melt extrusion has been used to produce a solid dispersion of the thermolabile drug artemisinin. Formulation and process conditions were optimized prior to evaluation of dissolution and biopharmaceutical performance. Soluplus(®), a low Tg amphiphilic polymer especially designed for solid dispersions enabled melt extrusion at 110 °C although some drug-polymer incompatibility was observed. Addition of 5% citric acid as a pH modifier was found to suppress the degradation. The area under plasma concentration time curve (AUC0-24h) and peak plasma concentration (Cmax) were four times higher for the modified solid dispersion compared to that of pure artemisinin...
November 16, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29136763/amorphous-solid-dispersions-of-hecogenin-acetate-using-different-polymers-for-enhancement-of-solubility-and-improvement-of-anti-hyperalgesic-effect-in-neuropathic-pain-model-in-mice
#2
Carlos Demócedes Luís de França Almeida Moreira, Jonas Gabriel de Oliveira Pinheiro, Walter Ferreira da Silva-Júnior, Euzébio Guimarães Barbosa, Zênia Maria Maciel Lavra, Erick Willyame Menezes Pereira, Marília Matos Resende, Eduardo Pereira de Azevedo, Lucindo José Quintans-Júnior, Adriano Antunes de Souza Araújo, Jullyana de Souza Siqueira Quintans, Ádley Antonini Neves de Lima
Hecogenin acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy...
November 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29133204/investigating-phase-separation-in-amorphous-solid-dispersions-via-raman-mapping
#3
Christian Luebbert, Christian Klanke, Gabriele Sadowski
The bioavailability of poorly-water-soluble active pharmaceutical ingredients (APIs) can be significantly improved by so-called amorphous solid dispersions (ASDs). However, the long-term stability of ASDs might be impaired by API recrystallization and/or amorphous phase separation (APS). So far, no methods have been reported to quantify APS in ASDs. In this work, phase-separation kinetics as well as the compositions of the two amorphous phases evolving due to APS were quantitatively determined for the first time using confocal Raman spectroscopy...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29128423/amorphous-solid-dispersions-and-nanocrystal-technologies-for-poorly-water-soluble-drug-delivery-an-update
#4
Scott V Jermain, Chris Brough, Robert O Williams
Poor water-solubility remains a typical property of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate, and bioavailability of these active ingredients belonging to biopharmaceutical classification system (BCS) II and IV classifications. Since the early 2000s, nanocrystal delivery and amorphous solid dispersions are more established techniques to overcome the limitations of poorly-water soluble drugs in FDA available products...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29125764/selective-acceleration-of-crystal-growth-of-indomethacin-polymorphs-by-low-concentration-poly-ethylene-oxide
#5
Qin Shi, Jie Zhang, Chen Zhang, Jing Jiang, Jun Tao, Dongshan Zhou, Ting Cai
Physical stability of pharmaceutical amorphous solid dispersions is one of the critical attributes to the successful development of the formulation. Herein, we studied the impact of low-concentration poly(ethylene oxide) (PEO) on the crystallization rates of three polymorphs of indomethacin (IMC, γ, α and δ-form). We observed that the addition of 3% w/w PEO significantly increased the crystal growth rates of γ-form and α-from of IMC, but had a negligible effect on the δ-form. The reduction of the activation energy for the crystal growth of IMC polymorphs after adding the PEO follows the order γ-form > α-form > δ-form, which is consistent with the trend toward the accelerating effects of PEO on the crystal growth rates of three polymorphs...
November 10, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29125700/bioavailability-and-pharmacokinetics-of-trpv1-antagonist-mavatrep-jnj-39439335-tablet-and-capsule-formulations-in-healthy-men-two-open-label-crossover-single-dose-phase-1-studies
#6
Prasarn Manitpisitkul, Kevin Shalayda, Lucille Russell, Panna Sanga, Yinka Williams, Bhavna Solanki, Joseph Caruso, John A Moyer
To improve room temperature stability and oral bioavailability of mavatrep (JNJ-39439335, a transient receptor potential vanilloid subtype-1 antagonist), various formulations were initially developed and evaluated in 2 phase 1 open-label, randomized, 3-way crossover studies in healthy participants. Study 1 evaluated 2 new overencapsulated tablet formulations (formulations B and C) relative to an overencapsulated early tablet formulation (formulation A), using mavatrep HCl salt form. Because these tablets were still not room-temperature stable, in study 2: two free-base solid dispersion amorphous formulations (formulations D and E) were evaluated relative to the best encapsulated formulation from study 1 (formulation C) and also food effect...
November 10, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29124978/sustained-release-solid-dispersion-of-pelubiprofen-using-the-blended-mixture-of-aminoclay-and-ph-independent-polymers-preparation-and-in-vitro-in-vivo-characterization
#7
Yeo-Song Lee, Jae Guen Song, Sang Hoon Lee, Hyo-Kyung Han
The present study aimed to develop the sustained-release oral dosage form of pelubiprofen (PEL) by using the blended mixture of 3-aminopropyl functionalized-magnesium phyllosilicate (aminoclay) and pH-independent polymers. The sustained-release solid dispersion (SRSD) was prepared by the solvent evaporation method and the optimal composition of SRSD was determined as the weight ratio of drug: Eudragit® RL PO: Eudragit® RS PO of 1:1:2 in the presence of 1% of aminoclay (SRSD(F6)). The dissolution profiles of SRSD(F6) were examined at different pHs and in the simulated intestinal fluids...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/29120370/amorphous-solid-dispersion-of-epigallocatechin-gallate-for-enhanced-physical-stability-and-controlled-release
#8
Yizheng Cao, Jing Teng, Jon Selbo
Epigallocatechin gallate (EGCG) has been recognized as the most prominent green tea extract due to its healthy influences. The high instability and low bioavailability, however, strongly limit its utilization in food and drug industries. This work, for the first time, develops amorphous solid dispersion of EGCG to enhance its bioavailability and physical stability. Four commonly used polymeric excipients are found to be compatible with EGCG in water-dioxane mixtures via a stepwise mixing method aided by vigorous mechanical interference...
November 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29117503/recent-strategies-in-spray-drying-for-the-enhanced-bioavailability-of-poorly-water-soluble-drugs
#9
REVIEW
Mark Davis
Poorly water-soluble drugs are a significant and ongoing issue for the pharmaceutical industry. An overview of recent developments for the preparation of spray-dried delivery systems is presented. Examples include amorphous solid dispersions, spray dried dispersions, microparticles, nanoparticles, surfactant systems and self-emulsifying drug delivery systems. Several aspects of formulation are considered, such as pre-screening, choosing excipient(s), the effect of polymer structure on performance, formulation optimisation, ternary dispersions, fixed-dose combinations, solvent selection and component miscibility...
November 5, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29113805/octenylsuccinate-hydroxypropyl-phytoglycogen-enhances-the-solubility-and-in-vitro-antitumor-efficacy-of-niclosamide
#10
Ying Xie, Yuan Yao
Niclosamide is a promising antitumor agent, but its low aqueous solubility places limit on its antitumor efficacy. The aim of this study was to improve the solubility and dissolution of niclosamide through using octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer. The niclosamide-OHPP solid dispersion (niclo-OHPP SD) was prepared and characterized in terms of crystallinity, molecular interactions, solubility and dissolution profile, in-vitro antitumor efficacy, and in-vitro transdermal amount...
November 4, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29111751/extraordinary-long-term-stability-in-kinetically-stabilized-amorphous-solid-dispersions-of-fenofibrate
#11
Frank Theil, Johanna Milsmann, Samuel O Kyeremateng, Sankaran Anantharaman, Jörg Rosenberg, Holger van Lishaut
Inhibition of recrystallization of the drug substance in kinetically stabilized amorphous solid dispersions (ASDs) within and beyond shelf life is still a matter of debate. Generally, these ASD systems are considered to be prone to recrystallization, but examples of their long term stability are emerging in the literature. Since, in some cases, the formation of crystals may impact bioavailability, recrystallization may present a relevant risk for patients as it potentially lowers the effective dose of the formulation...
November 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29107047/moisture-induced-amorphous-phase-separation-of-amorphous-solid-dispersions-molecular-mechanism-microstructure-and-its-impact-on-dissolution-performance
#12
Huijun Chen, Yipshu Pui, Chengyu Liu, Zhen Chen, Ching-Chiang Su, Michael Hageman, Munir Hussain, Roy Haskell, Kevin Stefanski, Kimberly Foster, Olafur Gudmundsson, Feng Qian
Amorphous phase separation (APS) is commonly observed in amorphous solid dispersions (ASD) when exposed to moisture. The objective of this study was to investigate: 1) the phase behavior of amorphous solid dispersions composed of a poorly water-soluble drug with extremely low crystallization propensity, BMS-817399, and PVP, following exposure to different relative humidity (RH), and 2) the impact of phase separation on the intrinsic dissolution rate of amorphous solid dispersion. Drug-polymer interaction was confirmed in ASDs at different drug loading using Infrared (IR) spectroscopy and water vapor sorption analysis...
October 26, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29103508/octenylsuccinate-hydroxypropyl-phytoglycogen-a-dendrimer-like-biopolymer-solubilizes-poorly-water-soluble-active-pharmaceutical-ingredients
#13
Ying Xie, Yuan Yao
Effective solubilizers for poorly water-soluble active pharmaceutical ingredients (APIs) are highly desirable. This study introduced an amphiphilic dendrimer-like biopolymer, octenylsuccinate hydroxypropyl phytoglycogen (OHPP) as a new solubilizer. The molar substitution degree of octenylsuccinate and hydroxypropyl groups of OHPP was 0.51 and 1.69, respectively. The weight-average molecular weight, Z-average root mean square radius, and Zeta-potential of OHPP were 1.507×10(7)g/mol, 22.6nm, and -23.6mV, respectively...
January 15, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29098883/solid-dispersion-adsorbate-technique-for-improved-dissolution-and-flow-properties-of-lurasidone-hydrochloride-characterization-using-3-2-factorial-design
#14
Ashok Mahajan, Naazneen Surti, Pooja Koladiya
The aim of the present investigation was to improve the dissolution and flow properties of Lurasidone hydrochloride by solid dispersion adsorbate technique. Solid dispersions of Lurasidone hydrochloride were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate). A 3(2) factorial design was employed to quantify the effect of two independent variables, namely ratio of carrier (Poloxamer 188) and Lurasidone hydrochloride in solid dispersion and ratio of adsorbent (Florite) to solid dispersion...
November 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29097142/exploring-the-feasibility-of-the-use-of-biopolymers-as-a-carrier-in-the-formulation-of-amorphous-solid-dispersions-part-i-gelatin
#15
Timothy Pas, Bjorn Vergauwen, Guy Van den Mooter
Biopolymers have rarely been used so far as carriers in the formulation of amorphous solid dispersions (ASD) to overcome poor solubility of active pharmaceutical ingredients (APIs). In an attempt to enlarge our knowledge on this topic, gelatin, type 50PS was selected. A screening study was initiated in which twelve structurally different poorly soluble biopharmaceutical classification system (BCS) Class II drugs (carbamazepine, cinnarizine, diazepam, itraconazole, nifedipine, indomethacin, darunavir (ethanolate), ritonavir, fenofibrate, griseofulvin, ketoconazole and naproxen) were selected for evaluation...
October 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29082762/application-of-scco2-technology-for-preparing-coq10-solid-dispersion-and-sfc-ms-ms-for-analyzing-in-vivo-bioavailability
#16
Rujie Yang, Yingchao Li, Jing Li, Cuiru Liu, Ping Du, Tianhong Zhang
OBJECTIVE: In this study, solid dispersion (SD) for oral delivery of a poorly water-soluble drug, coenzyme Q10 was developed by supercritical fluid technology and characterized in vitro and in vivo. METHODS: Dissolution was used to optimize the formulations of CoQ10-SD. The physicochemical properties of SD were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The supercritical fluid chromatography-electrospray ionization tandem mass spectrometry (SFC-ESI-MS/MS) was used for the in vivo study...
October 30, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29080855/rheological-analysis-of-itraconazole-polymer-mixtures-to-determine-optimal-melt-extrusion-temperature-for-development-of-amorphous-solid-dispersion
#17
Nayan Solanki, Simerdeep Singh Gupta, Abu T M Serajuddin
The objective of this investigation was to develop a systematic method for the determination of optimal processing temperatures of drug-polymer mixtures for the development of amorphous solid dispersion (ASD) by melt extrusion. Since melt extrusion is performed at high temperature, it is essential that the processing temperature should be as low as possible to minimize degradation of drug and polymer, and yet the temperature should be high enough that the drug-polymer mixture attains certain viscosity that is extrudable and the drug dissolves in the molten polymer...
October 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29074389/different-effects-of-silica-added-internal-or-external-on-in-vitro-dissolution-of-indomethacin-hot-melt-extrudates
#18
Yulong Xia, Meng Yuan, Yueyang Deng, Xue Ke, Tianyuan Ci
The purpose of this work was to investigate the effect on the dissolution behavior when silica was added in different ways. The solid dispersion was prepared by hot-melt extrusion (HME) using indomethacin (IND) as a model drug and Kollidon VA64 as a carrier. In order to change the dissolution behavior, the silica was added during or after the HME respectively, to obtain the corresponding silica internal-added solid dispersion (InSD) and silica external-added solid dispersion (ExSD). According to the results, the internal-added silicon dioxide could reduce the dissolution rate from 66...
October 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29074381/drug-solubilization-by-means-of-a-surface-modified-edible-biopolymer-enabled-by-hot-melt-extrusion
#19
Hwee Jing Ong, Rodolfo Pinal
A formulation/processing combination approach for increasing the solubility of poorly-soluble drugs using solid dispersions (SDs) is presented, whereby the API retains its crystalline state. The approach utilizes a biopolymer naturally produced as dendrimeric nanoparticles that has been surface-modified to act as a solubilizing agent. The solubilizing agent is enabled by hot melt extrusion to produce the SDs. Four APIs, phenytoin (PHT), griseofulvin (GSF), ibuprofen (IBU) and loratadine (LOR) were used as model compounds to evaluate solubility enhancement...
October 23, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29069712/optimization-and-evaluation-of-lyophilized-fenofibrate-nanoparticles-with-enhanced-oral-bioavailability-and-efficacy
#20
Ahmed H Ibrahim, Hany M Ibrahim, Hatem R Ismael, Ahmed M Samy
The objective of this study was to enhance physiochemical properties as well as oral bioavailability of the poorly water soluble drug fenofibrate (FB), through preparation of amorphous solid dispersions (ASDs). ASDs were prepared via freeze drying using polyvinylpyrrolidone (PVP) K30 and poloxamer 188 as hydrophilic carriers. Formulations were optimized by 3(2) full factorial design (FFD) with PVP-K30 level (X1) and poloxamer 188 level (X2) as independent variables and particle size (Y1), zeta potential (Y2), drug content (Y3) and dissolution rate (T90, [Y4]) as dependent variables...
March 1, 2017: Pharmaceutical Development and Technology
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