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Pharmaceutical cocrystals

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https://www.readbyqxmd.com/read/29132223/comparison-of-the-relative-stability-of-pharmaceutical-cocrystals-consisting-of-paracetamol-and-dicarboxylic-acids
#1
Naoto Suzuki, Masatoshi Kawahata, Kentaro Yamaguchi, Toyofumi Suzuki, Kazuo Tomono, Toshiro Fukami
OBJECTIVE: The aim of this study is to evaluated evaluated the relative stability of pharmaceutical cocrystals consisting of paracetamol (APAP) and oxalic acid (OXA) or maleic acid (MLA). SIGNIFICANCE: These observations of cocrystal stability under various conditions are useful coformer criteria when cocrystals are selected as the API in drug development. METHOD: The relative stability was determined from the preferentially formed cocrystals under various conditions...
November 13, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29103527/preface-engineering-of-pharmaceutical-cocrystals-salts-and-polymorphs-advances-and-challenges
#2
EDITORIAL
Dennis Douroumis, Ali Nokhodchi
No abstract text is available yet for this article.
August 1, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29097226/understanding-the-differences-between-cocrystal-and-salt-aqueous-solubilities
#3
Katie L Cavanagh, Chinmay Maheshwari, Naír Rodríguez-Hornedo
This work challenges the popular notion that pharmaceutical salts are more soluble than cocrystals. There are cocrystals that are more soluble than salt forms of a drug and vice-versa. It all depends on the interplay between the chemistry of both the solid and solution phases. Aqueous solubility, pHmax, and supersaturation index (SA =SCC or Ssalt/SD) of cocrystals and salts of a basic drug, Lamotrigine (LTG), were determined, and mathematical models that predict the influence of cocrystal/salt Ksp and Ka were derived...
October 30, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29071222/pharmaceutical-cocrystal-of-piroxicam-design-formulation-and-evaluation
#4
Prabhakar Panzade, Giridhar Shendarkar, Sarfaraj Shaikh, Pavan Balmukund Rathi
Purpose: Cocrystallisation of drug with coformers is a promising approach to alter the solid sate properties of drug substances like solubility and dissolution. The objective of the present work was to prepare, formulate and evaluate the piroxicam cocrystal by screening various coformers. Methods: Cocrystals of piroxicam were prepared by dry grinding method. The melting point and solubility of crystalline phase was determined. The potential cocrystal was characterized by DSC, IR, XRPD. Other pharmaceutical properties like solubility and dissolution rate were also evaluated...
September 2017: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29055755/spectroscopic-investigation-on-structure-and-ph-dependent-cocrystal-formation-between-gamma-aminobutyric-acid-and-benzoic-acid
#5
Yong Du, Jiadan Xue, Qiang Cai, Qi Zhang
Vibrational spectroscopic methods, including terahertz absorption and Raman scattering spectroscopy, were utilized for the characterization and analysis of gamma-aminobutyric acid (GABA), benzoic acid (BA), and the corresponding GABA-BA cocrystal formation under various pH values of aqueous solution. Vibrational spectroscopic results demonstrated that the solvent GABA-BA cocrystal, similar as grinding counterpart, possessed unique characteristic features compared with that of starting parent compounds. The change of vibrational modes for GABA-BA cocrystal comparing with starting components indicates there is strong inter-molecular interaction between GABA and BA molecules during its cocrystallization process...
October 12, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28990387/mechanistic-insight-into-caffeine-oxalic-cocrystal-dissociation-in-formulations-role-of-excipients
#6
Naga Kiran Duggirala, Amber Vyas, Joseph F Krzyzaniak, Kapildev K Arora, Raj Suryanarayanan
Caffeine-oxalic acid cocrystal, widely reported to be stable under high humidity, dissociated in the presence of numerous pharmaceutical excipients. In cocrystal-excipient binary systems, the water mediated dissociation reaction occurred under pharmaceutically relevant storage conditions. Powder X-ray diffractometry was used to identify the dissociated products obtained as a consequence of coformer-excipient interaction. The proposed cocrystal dissociation mechanism involved water sorption, dissolution of cocrystal and excipient in the sorbed water, proton transfer from oxalic acid to the excipient, and formation of metal salts and caffeine hydrate...
November 6, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28987500/evaluating-suspension-formulations-of-theophylline-cocrystals-with-artificial-sweeteners
#7
Srinivasulu Aitipamula, Annie B H Wong, Parijat Kanaujia
Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evaluate suspension formulations of cocrystals of an antiasthmatic drug, theophylline, with 2 artificial sweeteners. Stability, solubility, drug release, and taste of the suspension formulations were evaluated...
October 5, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28981007/first-line-antituberculosis-drug-pyrazinamide-its%C3%A2-pharmaceutically-relevant-cocrystals-and-a-salt
#8
Kashyap Kumar Sarmah, Trishna Rajbongshi, Sourav Bhowmick, Ranjit Thakuria
A few pyrazinamide (Pyz) cocrystals involving hydroxybenzoic/cinnamic acid derivatives [2,4-dihydroxybenzoic acid (24DHBA); 2,6-dihydroxybenzoic acid (26DHBA); 3,5-dihydroxybenzoic acid (35DHBA) and nutraceutical molecule ferulic acid (FRA)] and the first example of a molecular salt with p-toluenesulfonic acid (pTSA) have been prepared and characterized using various solid-state techniques. A high-temperature cocrystal polymorph of Pyz·FRA has been characterized from the endothermic peaks observed using differential scanning calorimetry...
October 1, 2017: Acta Crystallographica Section B, Structural Science, Crystal Engineering and Materials
https://www.readbyqxmd.com/read/28978781/crystal-structure-of-pharmaceutical-cocrystals-of-2-6-diaminopyridine-with-piracetam-and-theophylline
#9
Melissa Hidekel Durán-Palma, Sonia Sanet Mendoza-Barraza, Nancy Evelyn Magaña-Vergara, Francisco Javier Martínez-Martínez, Juan Saulo González-González
Pharmaceutical cocrystals are crystalline solids formed by an active pharmaceutical ingredient and a cocrystal former. The cocrystals 2,6-diaminopyridine (DAP)-piracetam [PIR; systematic name: 2-(2-oxopyrrolidin-1-yl)acetamide] (1/1), C5H7N3·C6H10N2O2, (I), and 2,6-diaminopyridine-theophylline (TEO; systematic name: 1,3-dimethyl-7H-purine-2,6-dione) (1/1), C5H7N3·C7H8N4O2, (II), were prepared by the solvent-assisted grinding method and were characterized by IR spectroscopy and powder X-ray diffraction. Cocrystal (I) crystallized in the orthorhombic space group Pbca and showed a 1:1 stoichiometry...
October 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28931472/pharmaceutical-cocrystals-salts-and-polymorphs-advanced-characterization-techniques
#10
Edyta Pindelska, Agnieszka Sokal, Waclaw Kolodziejski
The main goal of a novel drug development is to obtain it with optimal physiochemical, pharmaceutical and biological properties. Pharmaceutical companies and scientists modify active pharmaceutical ingredients (APIs), which often are cocrystals, salts or carefully selected polymorphs, to improve the properties of a parent drug. To find the best form of a drug, various advanced characterization methods should be used. In this review, we have described such analytical methods, dedicated to solid drug forms. Thus, diffraction, spectroscopic, thermal and also pharmaceutical characterization methods are discussed...
September 18, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28917964/phenazopyridine-phthalimide-nano-cocrystal-release-rate-and-oral-bioavailability-enhancement
#11
Yu Huang, Jin-Mei Li, Zhi-Hui Lai, Jun Wu, Tong-Bu Lu, Jia-Mei Chen
Both cocrystal and nanocrystal technologies have been widely used in the pharmaceutical development for poorly soluble drugs. However, the synergistic effects due to the integration of these two technologies have not been well investigated. The aim of this study is to develop a nano-sized cocrystal of phenazopyridine (PAP) with phthalimide (PI) to enhance the release rate and oral bioavailability of PAP. A PAP-PI nano-cocrystal with particle diameter of 21.4±0.1nm was successfully prepared via a sonochemical approach and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and dynamic light scattering (DLS) analysis...
September 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28875033/exploring-the-salt-cocrystal-continuum-with-solid-state-nmr-using-natural-abundance-samples-implications-for-crystal-engineering
#12
Lalit Rajput, Manas Banik, Jayasubba Reddy Yarava, Sumy Joseph, Manoj Kumar Pandey, Yusuke Nishiyama, Gautam R Desiraju
There has been significant recent interest in differentiating multicomponent solid forms, such as salts and cocrystals, and, where appropriate, in determining the position of the proton in the X-H⋯A-YX(-)⋯H-A(+)-Y continuum in these systems, owing to the direct relationship of this property to the clinical, regulatory and legal requirements for an active pharmaceutical ingredient (API). In the present study, solid forms of simple cocrystals/salts were investigated by high-field (700 MHz) solid-state NMR (ssNMR) using samples with naturally abundant (15)N nuclei...
July 1, 2017: IUCrJ
https://www.readbyqxmd.com/read/28811184/experimental-cocrystal-screening-and-solution-based-scale-up-cocrystallization-methods
#13
REVIEW
Maria Malamatari, Steven A Ross, Dennis Douroumis, Sitaram P Velaga
Cocrystals are crystalline single phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates nor simple salts. If one of the components is an active pharmaceutical ingredient (API), the term pharmaceutical cocrystal is often used. There is a growing interest among drug development scientists in exploring cocrystals, as means to address physicochemical, biopharmaceutical and mechanical properties and expand solid form diversity of the API...
August 12, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28797789/dry-mechanochemical-synthesis-of-caffeine-oxalic-acid-cocrystals-and-their-evaluation-by-powder-x-ray-diffraction-and-chemometrics
#14
Yuta Otsuka, Akira Ito, Masaki Takeuchi, Hideji Tanaka
We report the effects of dry mechanochemical synthesis conditions on the crystallization of caffeine and oxalic acid 2:1 cocrystal. Caffeine anhydrate (CA) and oxalic acid (OX) dihydrate were grinded at various temperatures, rotation speeds and grinding time. The cocrystal was also synthesized by an organic solvent evaporation method, as a reference. The produced samples were measured by a powder X-ray diffraction (PXRD) analysis. The PXRD spectra suggest that the grinded cocrystal has a lower crystallinity than the evaporated one...
August 7, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28712924/advanced-methodologies-for-cocrystal-synthesis
#15
Dennis Douroumis, Steven A Ross, Ali Nokhodchi
Pharmaceutical cocrystals are multicomponent systems composed of two or more molecules and held together by H-bonding. Currently, cocrystals provide exciting opportunities in the pharmaceutical industry for the development and manufacturing of new medicines by improving poor physical properties of Active Pharmaceutical Ingredients (APIs) such as processability, solubility, stability and bioavailability. According to the recent reclassification, cocrystals are considered as drug polymorph rather a new API which has a significant impact on drug development, regulatory submissions and intellectual property protection...
July 14, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28699761/comparison-of-intermolecular-forces-in-anhydrous-sorbitol-and-solvent-cocrystals
#16
Teresa M Dierks, Timothy M Korter
The hygroscopicity of solid sorbitol is important for its utilization as a sweetener in the pharmaceutical and food industries. The molecular foundations of sorbitol hydration characteristics are explored here using two solvated cocrystals, sorbitol-water and sorbitol-pyridine. In this work, solid-state density functional theory and terahertz time-domain spectroscopy were used to evaluate the relative stabilities of these cocrystals as compared to anhydrous sorbitol in terms of conformational and cohesive energies...
July 21, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28690273/current-status-and-promising-future-of-pharmaceutical-cocrystals-in-development-of-oral-dosage-forms
#17
Toshiro Fukami
No abstract text is available yet for this article.
2017: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
https://www.readbyqxmd.com/read/28687528/selection-of-effective-cocrystals-former-for-dissolution-rate-improvement-of-active-pharmaceutical-ingredients-based-on-lipoaffinity-index
#18
Piotr Cysewski, Maciej Przybyłek
New theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification allowed to formulate quantitative criterions. Among considered 3679 molecular descriptors the relative value of lipoaffinity index, expressed as the difference between values calculated for active compound and excipient, has been found as the most appropriate measure suited for discrimination of positive and negative cases...
July 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28687273/pharmaceutical-aspects-of-salt-and-cocrystal-forms-of-apis-and-characterization-challenges
#19
Paolo Cerreia Vioglio, Michele R Chierotti, Roberto Gobetto
In recent years many efforts have been devoted to the screening and the study of new solid-state forms of old active pharmaceutical ingredients (APIs) with salification or co-crystallization processes, thus modulating final properties without changing the pharmacological nature. Salts, hydrates/solvates, and cocrystals are the common solid-state forms employed. They offer the intriguing possibility of exploring different pharmaceutical properties for a single API in the quest of enhancing the final drug product...
July 5, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28652091/investigating-therapeutic-usage-of-combined-ticagrelor-and-aspirin-through-solid-state-and-analytical-studies
#20
Hassane Sadou Yayé, Ivo B Rietveld, Maria Barrio, Philippe-Henri Secrétan, Antoine Faucheron, Maher Karoui, Patrick Tilleul, Najet Yagoubi, Bernard Do
The mainstay treatment for patients with acute coronary syndrome is an oral route dual antiplatelet therapy with a P2Y12-receptor antagonist and Aspirin (ASA). To improve patient adherence to such treatments, combination therapies (polypill) are envisioned. Physicochemical solid-state studies have been carried out to develop a preformulation strategy of ASA with the P2Y12-receptor antagonist Ticagrelor (TIC). The investigations were carried out using differential scanning calorimetry, liquid chromatography-high resolution-multistage mass spectrometry (LC-HR-MS(n)) and as complementary techniques Fourier transform infrared measurements and thermogravimetric analysis...
June 23, 2017: European Journal of Pharmaceutical Sciences
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