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Pharmaceutical cocrystals

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https://www.readbyqxmd.com/read/28625724/the-binary-system-of-ibuprofen-nicotinamide-under-nanoscale-confinement-from-cocrystal-to-coamorphous-state
#1
Yanping Bi, Deli Xiao, Shuai Ren, Shuyan Bi, Jianzhu Wang, Fei Li
Coamorphous systems have gained success in stabilizing amorphous drugs and improving their solubility and dissolution. Here we proposed to confine a binary mixture of drug and coformer (CF) within nanopores to obtain a nano-confined coamorphous (NCA) system. For proving feasibility of this proposal, a poorly water-soluble drug (ibuprofen, IBP) and a frequently used pharmaceutical CF (nicotinamide, NIC) were loaded into nanopores of mesoporous silica microspheres (MSMs). The solid state of NCA system was characterized by differential scanning calorimetry, X-ray powder diffraction, infrared spectrum and solid state nuclear magnetic resonance...
June 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28585942/progress-of-crystallization-in-microfluidic-devices
#2
REVIEW
Huan-Huan Shi, Yan Xiao, Steven Ferguson, Xin Huang, Na Wang, Hong-Xun Hao
Microfluidic technology provides a unique environment for the investigation of crystallization processes at the nano or meso scale. The convenient operation and precise control of process parameters, at these scales of operation enabled by microfluidic devices, are attracting significant and increasing attention in the field of crystallization. In this paper, developments and applications of microfluidics in crystallization research including: crystal nucleation and growth, polymorph and cocrystal screening, preparation of nanocrystals, solubility and metastable zone determination, are summarized and discussed...
June 6, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28579571/supramolecular-architectures-in-two-1-1-cocrystals-of-5-fluorouracil-with-5-bromothiophene-2-carboxylic-acid-and-thiophene-2-carboxylic-acid
#3
Marimuthu Mohana, Packianathan Thomas Muthiah, Colin D McMillen
In solid-state engineering, cocrystallization is a strategy actively pursued for pharmaceuticals. Two 1:1 cocrystals of 5-fluorouracil (5FU; systematic name: 5-fluoro-1,3-dihydropyrimidine-2,4-dione), namely 5-fluorouracil-5-bromothiophene-2-carboxylic acid (1/1), C5H3BrO2S·C4H3FN2O2, (I), and 5-fluorouracil-thiophene-2-carboxylic acid (1/1), C4H3FN2O2·C5H4O2S, (II), have been synthesized and characterized by single-crystal X-ray diffraction studies. In both cocrystals, carboxylic acid molecules are linked through an acid-acid R2(2)(8) homosynthon (O-H...
June 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28512568/acemetacin-cocrystal-structures-by-powder-x-ray-diffraction
#4
Geetha Bolla, Vladimir Chernyshev, Ashwini Nangia
Cocrystals of acemetacin drug (ACM) with nicotinamide (NAM), p-aminobenzoic acid (PABA), valerolactam (VLM) and 2-pyridone (2HP) were prepared by melt crystallization and their X-ray crystal structures determined by high-resolution powder X-ray diffraction. The powerful technique of structure determination from powder data (SDPD) provided details of molecular packing and hydrogen bonding in pharmaceutical cocrystals of acemetacin. ACM-NAM occurs in anhydrate and hydrate forms, whereas the other structures crystallized in a single crystalline form...
May 1, 2017: IUCrJ
https://www.readbyqxmd.com/read/28502182/isotope-edited-infrared-spectroscopy-for-efficient-discrimination-between-pharmaceutical-salts-and-cocrystals
#5
Kentaro Iwata, Masatoshi Karashima, Yukihiro Ikeda
Isotope-edited infrared spectroscopy using carboxylic acids selectively labeled with 13C is proposed herein for the efficient discrimination of pharmaceutical salts and cocrystals, whereby proton-transfer probe vibrations are highlighted by isotope shifts. This new technique can accurately discriminate even a confusing salt from a cocrystal for the traditional method, highlighting the diagnostic peaks and providing the OH in-plane bending vibrations corresponding to intermolecular hydrogen bonding at the carbonyl oxygens of the cocrystals...
May 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28403609/solid-state-nmr-characterization-of-ibuprofen-nicotinamide-cocrystals-and-new-idea-for-controlling-release-of-drugs-embedded-into-mesoporous-silica-particles
#6
Ewa Skorupska, Sławomir Kaźmierski, Marek J Potrzebowski
Grinding and melting methods were employed for synthesis of pharmaceutical cocrystals formed by racemic (R/S) and entiomeric (S) ibuprofen (IBU) and nicotinamide (NA) as coformer. Obtained (R/S)-IBU:NA and (S)-IBU:NA cocrystals were fully characterized by means of advanced one- and two-dimensional solid state nuclear magnetic resonance (SS NMR) techniques with very fast magic angle spinning (MAS) at 60 kHz. The distinction in molecular packing and specific hydrogen bonding pattern was clearly recognized by analysis of (1)H, (13)C, and (15)N spectra...
April 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28392495/cocrystal-solubility-product-analysis-dual-concentration-ph-mass-action-model-not-dependent-on-explicit-solubility-equations
#7
Alex Avdeef
A novel general computational approach is described to address many aspects of cocrystal (CC) solubility product (Ksp) determination of drug substances. The CC analysis program, pDISOL-X, was developed and validated with published model systems of various acid-base combinations of active pharmaceutical ingredients (APIs) and coformers: (i) carbamazepine cocrystal systems with 4-aminobenzoic acid, cinnamic acid, saccharin, and salicylic acid, (ii) for indomethacin with saccharin, (iii) for nevirapine with maleic acid, saccharin, and salicylic acid, and (iv) for gabapentin with 3-hydroxybenzoic acid...
April 6, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28355489/encapsulation-of-ibuprofen-in-cd-mof-and-related-bioavailability-studies
#8
Karel J Hartlieb, Daniel P Ferris, James M Holcroft, Irawati Kandela, Charlotte L Stern, Majed S Nassar, Youssry Y Botros, J Fraser Stoddart
Although ibuprofen is one of the most widely used nonsteroidal anti-inflammatory drugs (NSAIDs), it exhibits poor solubility in aqueous and physiological environments as a free acid. In order to improve its oral bioavailability and rate of uptake, extensive research into the development of new formulations of ibuprofen has been undertaken, including the use of excipients as well as ibuprofen salts, such as ibuprofen lysinate and ibuprofen, sodium salt. The ultimate goals of these studies are to reduce the time required for maximum uptake of ibuprofen, as this period of time is directly proportional to the rate of onset of analgesic/anti-inflammatory effects, and to increase the half-life of the drug within the body; that is, the duration of action of the effects of the drug...
April 12, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28344021/pharmaceutical-cocrystals-salts-and-multicomponent-systems-intermolecular-interactions-and-property-based-design
#9
REVIEW
David J Berry, Jonathan W Steed
As small molecule drugs become harder to develop and less cost effective for patient use, efficient strategies for their property improvement become increasingly important to global health initiatives. Improvements in the physical properties of Active Pharmaceutical Ingredients (APIs), without changes in the covalent chemistry, have long been possible through the application of binary component solids. This was first achieved through the use of pharmaceutical salts, within the last 10-15years with cocrystals and more recently coamorphous systems have also been consciously applied to this problem...
March 23, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28342786/pharmaceutical-solvates-hydrates-and-amorphous-forms-a-special-emphasis-on-cocrystals
#10
REVIEW
Anne Marie Healy, Zelalem Ayenew Worku, Dinesh Kumar, Atif M Madi
Active pharmaceutical ingredients (APIs) may exist in various solid forms, which can lead to differences in the intermolecular interactions, affecting the internal energy and enthalpy, and the degree of disorder, affecting the entropy. Differences in solid forms often lead to differences in thermodynamic parameters and physicochemical properties for example solubility, dissolution rate, stability and mechanical properties of APIs and excipients. Hence, solid forms of APIs play a vital role in drug discovery and development in the context of optimization of bioavailability, filing intellectual property rights and developing suitable manufacturing methods...
March 22, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28322394/self-assembly-of-magnesium-seamed-hexameric-pyrogallol-4-arene-nanocapsules
#11
Chen Zhang, Rahul S Patil, Tao Li, Charles L Barnes, Jerry L Atwood
The solvothermal synthesis of a metal-seamed hexameric nanocapsule from pyrogallol[4]arenes and magnesium is reported. The unique non-toxic and biocompatible nature of divalent magnesium cations in addition to the large inherent cavities make these nanocapsules promising for potential application in biomedicine. In addition, we show that these nanocapsules can form cocrystals with pyridine molecules through hydrogen bonding, which sheds light to cocrystallization of supramolecular nanocapsules with small pharmaceutics...
March 21, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28274662/pharmaceutical-properties-of-two-ethenzamide-gentisic-acid-cocrystal-polymorphs-drug-release-profiles-spectroscopic-studies-and-theoretical-calculations
#12
Agnieszka Sokal, Edyta Pindelska, Lukasz Szeleszczuk, Waclaw Kolodziejski
The aim of this study was to evaluate the stability and solubility of the polymorphic forms of the ethenzamide (ET) - gentisic acid (GA) cocrystals during standard technological processes leading to tablet formation, such as compression and excipient addition. In this work two polymorphic forms of pharmaceutical cocrystals (ETGA) were characterized by (13)C and (15)N solid-state nuclear magnetic resonance and Fourier transformed infrared spectroscopy. Spectroscopic studies were supported by gauge including projector augmented wave (GIPAW) calculations of chemical shielding constants...
March 6, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28257022/supramolecular-hydrogen-bonding-patterns-in-1-1-cocrystals-of-5-fluorouracil-with-4-methylbenzoic-acid-and-3-nitrobenzoic-acid
#13
Marimuthu Mohana, Packianathan Thomas Muthiah, Colin D McMillen
The design of a pharmaceutical cocrystal is based on the identification of specific hydrogen-bond donor and acceptor groups in active pharmaceutical ingredients (APIs) in order to choose a `complementary interacting' molecule that can act as an efficient coformer. 5-Fluorouracil (5FU) is a pyrimidine derivative with two N-H donors and C=O acceptors and shows a diversity of hydrogen-bonding motifs. Two 1:1 cocrystals of 5-fluorouracil (5FU), namely 5-fluorouracil-4-methylbenzoic acid (5FU-MBA), C4H3FN2O2·C8H8O2, (I), and 5-fluorouracil-3-nitrobenzoic acid (5FU-NBA), C4H3FN2O2·C7H5NO4, (II), have been prepared and characterized by single-crystal X-ray diffraction...
March 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28257018/a-13-c-solid-state-nmr-investigation-of-four-cocrystals-of-caffeine-and-theophylline
#14
Nicolas J Vigilante, Manish A Mehta
We report an analysis of the (13)C solid-state NMR chemical shift data in a series of four cocrystals involving two active pharmaceutical ingredient (API) mimics (caffeine and theophylline) and two diacid coformers (malonic acid and glutaric acid). Within this controlled set, we make comparisons of the isotropic chemical shifts and the principal values of the chemical shift tensor. The dispersion at 14.1 T (600 MHz (1)H) shows crystallographic splittings in some of the resonances in the magic angle spinning spectra...
March 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28257010/structure-and-physicochemical-characterization-of-a-naproxen-picolinamide-cocrystal
#15
Hannah E Kerr, Lorna K Softley, Kuthuru Suresh, Paul Hodgkinson, Ivana Radosavljevic Evans
Naproxen (NPX) is a nonsteroidal anti-inflammatory drug with pain- and fever-relieving properties, currently marketed in the sodium salt form to overcome solubility problems; however, alternative solutions for improving its solubility across all pH values are desirable. NPX is suitable for cocrystal formation, with hydrogen-bonding possibilities via the COOH group. The crystal structure is presented of a 1:1 cocrystal of NPX with picolinamide as a coformer [systematic name: (S)-2-(6-methoxynaphthalen-2-yl)propanoic acid-pyridine-2-carboxamide (1/1), C14H14O3·C6H6N2O]...
March 1, 2017: Acta Crystallographica. Section C, Structural Chemistry
https://www.readbyqxmd.com/read/28101455/pharmaceutical-cocrystals-regulatory-and-strategic-aspects-design-and-development
#16
REVIEW
Dipak Dilip Gadade, Sanjay Sudhakar Pekamwar
Cocrystal is a concept of the supramolecular chemistry which is gaining the extensive interest of researchers from pharmaceutical and chemical sciences and of drug regulatory agencies. The prominent reason of which is its ability to modify physicochemical properties of active pharmaceutical ingredients. During the development of the pharmaceutical product, formulators have to optimize the physicochemical properties of active pharmaceutical ingredients. Pharmaceutical cocrystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28092854/biopharmaceutical-characterization-of-praziquantel-cocrystals-and-cyclodextrin-complexes-prepared-by-grinding
#17
Martina Cugovčan, Jasna Jablan, Jasmina Lovrić, Dominik Cinčić, Nives Galić, Mario Jug
Mechanochemical activation using several different co-grinding additives was applied as a green chemistry approach to improve physiochemical and biopharmaceutical properties of praziquantel (PZQ). Liquid assisted grinding with an equimolar amount of citric acid (CA), malic acid (MA), salicylic acid (SA) and tartaric acid (TA) gained in cocrystal formation, which all showed pH-dependent solubility and dissolution rate. However, the most soluble cocrystal of PZQ with MA was chemically unstable, as seen during the stability testing...
April 15, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28070074/raman-spectroscopy-of-pharmaceutical-cocrystals-in-nanosized-pores-of-mesoporous-silica
#18
Ryuichi Ohta, Yuko Ueno, Katsuhiro Ajito
The Raman spectroscopy of pharmaceutical cocrystals based on caffeine and oxalic acid in nanosized pores of mesoporous silica has been demonstrated at various molar amounts. The Raman peak shifts of caffeine molecules express the existence of pharmaceutical cocrystals in mesoporous silica. The molar amount dependence of the peak shifts describes that caffeine and oxalic acid cocrystallized on the surface of the nanosized pores and piled up layer by layer. This is the first report that shows the Raman spectroscopy is a powerful tool to observe the synthesis of pharmaceutical cocrystals incorporated in the nanosized pores of mesoporous silica...
2017: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
https://www.readbyqxmd.com/read/28035627/supramolecular-cocrystals-of-gliclazide-synthesis-characterization-and-evaluation
#19
Renu Chadha, Dimpy Rani, Parnika Goyal
PURPOSE: To prepare the supramolecular cocrystals of gliclazide (GL, a BCS class II drug molecule) via mechanochemical route, with the goal of improving physicochemical and biopharmaceutical properties. METHODS: Two cocrystals of GL with GRAS status coformers, sebacic acid (GL-SB; 1:1) and α-hydroxyacetic acid (GL-HA; 1:1) were screened out using liquid assisted grinding. The prepared cocrystals were characterized using thermal and analytical techniques followed by evaluation of antidiabetic activity and pharmacokinetic parameters...
December 29, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27914793/challenges-in-translational-development-of-pharmaceutical-cocrystals
#20
Dnyaneshwar P Kale, Sandeep S Zode, Arvind K Bansal
The last 2 decades have witnessed increased research in the area of cocrystals resulting in deeper scientific understanding, increase in intellectual property landscape, and evolution in the regulatory environment. Pharmaceutical cocrystals have received significant attention as a new solid form on account of their ability to modulate poor physicochemical properties of drug molecules. However, pharmaceutical development of cocrystals could be challenging, thus limiting their translation into viable drug products...
February 2017: Journal of Pharmaceutical Sciences
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