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Pharmaceutical cocrystals

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https://www.readbyqxmd.com/read/29680958/intermolecular-interaction-as-a-direct-measure-of-water-solubility-advantage-of-meloxicam-cocrystalized-with-carboxylic-acids
#1
Piotr Cysewski
The solubility advantage (SA) of meloxicam cocrystalized with mono- and dicarboxylic acids was expressed in terms of equilibrium constants involving active pharmaceutical ingredient and coformer in aqueous solutions. It is argued that SA can be quantified by concentration of pairs formed in water. The pH and concentration of dissolved components is included explicitly in the model. The alternative behavior of mono- and dicarboxylic acids was emphasized and addressed to different structural motifs. The structural and energetic properties of meloxicam and its complexes with carboxylic acids were characterized, including tautmerism and dissociation in aqueous media...
April 21, 2018: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/29678263/mid-infrared-spectroscopy-of-pharmaceutical-solids
#2
Harry G Brittain
It is now well established that infrared absorption spectroscopy is a powerful technique for the physical characterization of pharmaceutical solids. Besides being a preferred methodology for identification purposes, one can use trends in the energy values in the spectra as a means to study the solid-state properties of the system. FTIR spectra are often used to evaluate the type of polymorphism existing in a drug substance, can be very useful in studies of the water contained within a hydrate species, and are emerging as a technique of choice for the study of cocrystal systems...
2018: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/29550709/experimental-and-dft-simulation-study-of-a-novel-felodipine-cocrystal-characterization-dissolving-properties-and-thermal-decomposition-kinetics
#3
Caiqin Yang, Wei Guo, Yulong Lin, Qianqian Lin, Jiaojiao Wang, Jing Wang, Yanli Zeng
In this study, a new cocrystal of felodipine (Fel) and glutaric acid (Glu) with a high dissolution rate was developed using the solvent ultrasonic method. The prepared cocrystal was characterized using X-ray powder diffraction, differential scanning calorimetry, thermogravimetric (TG) analysis, and infrared (IR) spectroscopy. To provide basic information about the optimization of pharmaceutical preparations of Fel-based cocrystals, this work investigated the thermal decomposition kinetics of the Fel-Glu cocrystal through non-isothermal thermogravimetry...
March 8, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29524619/in-situ-monitoring-of-cocrystals-in-formulation-development-using-low-frequency-raman-spectroscopy
#4
Takashi Otaki, Yuta Tanabe, Takashi Kojima, Masaru Miura, Yukihiro Ikeda, Tatsuo Koide, Toshiro Fukami
In recent years, to guarantee a quality-by-design approach to the development of pharmaceutical products, it is important to identify properties of raw materials and excipients in order to determine critical process parameters and critical quality attributes. Feedback obtained from real-time analyses using various process analytical technology (PAT) tools has been actively investigated. In this study, in situ monitoring using low-frequency (LF) Raman spectroscopy (10-200 cm-1 ), which may have higher discriminative ability among polymorphs than near-infrared spectroscopy and conventional Raman spectroscopy (200-1800 cm-1 ), was investigated as a possible application to PAT...
May 5, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29512461/multicomponent-pharmaceutical-cocrystals-a-novel-approach-for-combination-therapy
#5
Zeeshan Fatima, Dipti Srivastava, Chanchal Deep Kaur
Cocrystallization is a technique for modifying the physicochemical and pharmacokinetic properties of an active pharmaceutical ingredient (API) embodying the concept of supramolecular synthon. Most of the examples cited in the literature are of cocrystals formed between an API and a coformer chosen from the generally recognized as safe (GRAS) substance list, however, few examples exist where a cocrystal consists of two or more APIs. These cocrystals are commonly known as multi API, multi drug or drug- drug cocrystals...
March 5, 2018: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/29473529/application-of-cocrystallization-approach-in-drug-development-recent-patents-review
#6
Kunti Abhishek Shah, Vijay Parmar
Cocrystals of active pharmaceutical ingredient have been of interest in the field of pharmaceutical research due to their potential for tailoring the physicochemical properties of pharmaceutical molecules. The increase in the number of cocrystals screening experiments being reported for numerous drug substances having less favorable physicochemical properties and simultaneously the draft guidelines issued from regulatory bodies on pharmaceutical cocrystals provide the evidence of the acceptance of cocrystals in the drug development...
February 21, 2018: Recent Patents on Nanotechnology
https://www.readbyqxmd.com/read/29462633/improved-stability-of-tuberculosis-drug-fixed-dose-combination-using-isoniazid-caffeic-acid-and-vanillic-acid-cocrystal
#7
Swapna Battini, M K Chaitanya Mannava, Ashwini Nangia
The classic fixed-dose combination (FDC) of 4 tuberculosis drugs, namely rifampicin (RIF), isoniazid (INH), pyrazinamide (PZA), and ethambutol dihydrochloride (EDH) has the twin issues of physical stability and RIF cross-reaction in the 4-FDC. The major reason for these quality issues is the interaction between RIF and INH to yield isonicotinyl hydrazone in drug tablets. Pharmaceutical cocrystals of INH with caffeic acid (CFA) (PZA + EDH + RIF + INH-CFA cocrystal) and vanillic acid (VLA) (PZA + EDH + RIF + INH-VLA cocrystal) are able to stabilize the FDC formulation compared with the reference batch (PZA + EDH + RIF + INH)...
February 17, 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29370068/pharmaceutical-cocrystals-new-solid-phase-modification-approaches-for-the-formulation-of-apis
#8
REVIEW
Anna Karagianni, Maria Malamatari, Kyriakos Kachrimanis
Cocrystals can be used as an alternative approach based on crystal engineering to enhance specific physicochemical and biopharmaceutical properties of active pharmaceutical ingredients (APIs) when the approaches to salt or polymorph formation do not meet the expected targets. In this article, an overview of pharmaceutical cocrystals will be presented, with an emphasis on the intermolecular interactions in cocrystals and the methods for their preparation. Furthermore, cocrystals of direct pharmaceutical interest, along with their in vitro properties and available in vivo data and characterization techniques are discussed, highlighting the potential of cocrystals as an attractive route for drug development...
January 25, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29347850/feasibility-of-electrospray-deposition-for-rapid-screening-of-the-cocrystal-formation-and-single-step-continuous-production-of-pharmaceutical-nanococrystals
#9
Shahram Emami, Mohammadreza Siahi-Shadbad, Mohammad Barzegar-Jalali, Khosro Adibkia
OBJECTIVES: This study employed electrospray deposition (ESD) for simultaneous synthesis and particle engineering of cocrystals. SIGNIFICANCE: Exploring new methods for the efficient production of cocrystals with desired particle properties is an essential demand. METHODS: The possibility of cocrystal formation by ESD was examined for indomethacin-saccharin, indomethacin-nicotinamide, naproxen-nicotinamide, and naproxen-iso-nicotinamide cocrystals...
June 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29305142/oral-bioavailability-enhancement-of-%C3%AE-lapachone-a-poorly-soluble-fast-crystallizer-by-cocrystal-amorphous-solid-dispersion-and-crystalline-solid-dispersion
#10
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...
March 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29303500/temperature-induced-pseudopolymorphism-of-molecular-salts-from-a-pyridyl-bis-urea-macrocycle-and-naphthalene-1-5-disulfonic-acid
#11
Bozumeh Som, Jessica R Shue, Mark D Smith, Linda S Shimizu
Molecular salts, often observed as cocrystals, play an important role in the fields of pharmaceutics and materials science, where salt formation is used to tune the properties of active pharmaceutical ingredients (APIs) and improve the stability of solid-state materials. Salt formation via a proton-transfer reaction typically alters hydrogen-bonding motifs and influences supramolecular assembly patterns. We report here the molecular salts formed by the pyridyl bis-urea macrocycle 3,5,13,15,21,22-hexaazatricyclo[15...
January 1, 2018: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/29278209/pharmaceutical-cocrystals-as-an-opportunity-to-modify-drug-properties-from-the-idea-to-application-a-review
#12
Agnieszka Sokal, Edyta Pindelska
The properties of many drugs which have been available on the pharmaceutical market for a long time still need to be improved. Cocrystals are the solid state drug modification which can improve such properties as low solubility, stability and mechanical properties (e.g. compressibility). In this paper examples how to use cocrystals to modify properties of API (Active Pharmaceutical Ingredient) will be reported. Additionally, in this review the way from an idea of the new cocrystal to drug dosage form registration will be shortly described...
December 26, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29241701/production-of-cocrystals-in-an-excipient-matrix-by-spray-drying
#13
David Walsh, Dolores R Serrano, Zelalem Ayenew Worku, Brid A Norris, Anne Marie Healy
Spray drying is a well-established scale-up technique for the production of cocrystals. However, to the best of our knowledge, the effect of introducing a third component into the feed solution during the spray drying process has never been investigated. Cocrystal formation in the presence of a third component by a one-step spray drying process has the potential to reduce the number of unit operations which are required to produce a final pharmaceutical product (e.g. by eliminating blending with excipient)...
January 30, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29196273/optimising-the-in-vitro-and-in-vivo-performance-of-oral-cocrystal-formulations-via-spray-coating
#14
Dolores R Serrano, David Walsh, Peter O'Connell, Naila A Mugheirbi, Zelalem Ayenew Worku, Francisco Bolas-Fernandez, Carolina Galiana, Maria Auxiliadora Dea-Ayuela, Anne Marie Healy
Engineering of pharmaceutical cocrystals is an advantageous alternative to salt formation for improving the aqueous solubility of hydrophobic drugs. Although, spray drying is a well-established scale-up technique in the production of cocrystals, several issues can arise such as sublimation or stickiness due to low glass transition temperatures of some organic molecules, making the process very challenging. Even though, fluidised bed spray coating has been successfully employed in the production of amorphous drug-coated particles, to the best of our knowledge, it has never been employed in the production of cocrystals...
March 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29166563/mechanochemical-synthesis-of-pharmaceutical-cocrystal-suspensions-via-hot-melt-extrusion-enhancing-cocrystal-yield
#15
Shu Li, Tao Yu, Yiwei Tian, Colette Lagan, David S Jones, Gavin P Andrews
Pharmaceutical cocrystals have attracted increasing attention over the past decade as an alternative way to modify the physicochemical properties and hence improve the bioavailability of a drug, without sacrificing thermodynamic stability. Our previous work has demonstrated the viability of in-situ formation of ibuprofen/isonicotinamide cocrystal suspensions within a matrix carrier via a single-step hot-melt extrusion (HME) process. The key aim of the current work is to establish optimised processing conditions to improve cocrystal yield within extruded matrices...
November 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29132223/comparison-of-the-relative-stability-of-pharmaceutical-cocrystals-consisting-of-paracetamol-and-dicarboxylic-acids
#16
Naoto Suzuki, Masatoshi Kawahata, Kentaro Yamaguchi, Toyofumi Suzuki, Kazuo Tomono, Toshiro Fukami
OBJECTIVE: The aim of this study is to evaluate 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 active pharmaceutical ingredient in drug development. METHOD: The relative stability was determined from the preferentially formed cocrystals under various conditions...
April 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29103527/preface-engineering-of-pharmaceutical-cocrystals-salts-and-polymorphs-advances-and-challenges
#17
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
#18
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 /SD 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...
January 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29071222/pharmaceutical-cocrystal-of-piroxicam-design-formulation-and-evaluation
#19
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
#20
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...
February 15, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
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