Coamorphous System of Florfenicol-Oxymatrine for Improving the Solubility and Dissolution Rate of Florfenicol: Preparation,Characterization and Molecular Dynamics Simulation |
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| Authors: | Bin Li Yi Hu Yujie Guo Renjie Xu Xiaoping Fang Xuecheng Xiao Cuiping Jiang Shan Lu |
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| Affiliation: | 1. School of Pharmacy, Hubei University of Chinese Medicine, Wuhan 430065, PR China;2. School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, PR China |
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| Abstract: | ![]()
Coamorphous system has proved to be an effective approach to improve the solubility of BCSⅡ drugs. Florfenicol (FF) is a widely used veterinary antibiotic but has poor aqueous solubility. Therefore, the coamorphous system of florfenicol and oxymatrine (OMT) formulated at 1:1 and 1:2 M ratios were prepared by using solvent evaporation, followed by a series of characterization in terms of PXRD, DSC, FTIR and Raman spectroscopy. It was found that FF and OMT are miscible according to Hansen solubility parameters. The molecular electrostatic potential (MEP) and radial distribution function (RDF) analysis demonstrated the possible hydrogen bond interaction in coamorphous system, which was confirmed by FTIR and Raman spectra. The coamorphous FF-OMT (1:1) maintained stability for 60 days at 25 °C/0% RH and 30 days at 40 °C/75% RH, which may be attributed to better molecular miscibility of FF and OMT and the strong hydrogen bond of O–H (FF)?O–N (OMT) and N–H (FF)?O–N (OMT). In addition, the apparent solubility and permeability, dissolution and intrinsic dissolution rate (IDR) of the acquired coamorphous solids were obviously increased compared with crystalline FF. In conclusion, a drug-drug coamorphous formulation can be applied to improve the solubility and dissolution of crystalline FF. |
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| Keywords: | Coamorphous system Florfenicol Solubility Dissolution Hydrogen bond Molecular dynamics FF" },{" #name" :" keyword" ," $" :{" id" :" kwrd0045" }," $$" :[{" #name" :" text" ," _" :" florfenicol OMT" },{" #name" :" keyword" ," $" :{" id" :" kwrd0055" }," $$" :[{" #name" :" text" ," _" :" oxymatrine BCS" },{" #name" :" keyword" ," $" :{" id" :" kwrd0065" }," $$" :[{" #name" :" text" ," _" :" biopharmaceutical classification system PXRD" },{" #name" :" keyword" ," $" :{" id" :" kwrd0075" }," $$" :[{" #name" :" text" ," _" :" powder X-ray diffraction DSC" },{" #name" :" keyword" ," $" :{" id" :" kwrd0085" }," $$" :[{" #name" :" text" ," _" :" differential scanning calorimetry HPLC" },{" #name" :" keyword" ," $" :{" id" :" kwrd0095" }," $$" :[{" #name" :" text" ," _" :" high performance liquid chromatography MD" },{" #name" :" keyword" ," $" :{" id" :" kwrd0105" }," $$" :[{" #name" :" text" ," _" :" molecular dynamics MEP" },{" #name" :" keyword" ," $" :{" id" :" kwrd0115" }," $$" :[{" #name" :" text" ," _" :" molecular electrostatic potential RDF" },{" #name" :" keyword" ," $" :{" id" :" kwrd0125" }," $$" :[{" #name" :" text" ," _" :" radial distribution function FTIR" },{" #name" :" keyword" ," $" :{" id" :" kwrd0135" }," $$" :[{" #name" :" text" ," _" :" fourier transform infrared IDR" },{" #name" :" keyword" ," $" :{" id" :" kwrd0145" }," $$" :[{" #name" :" text" ," _" :" intrinsic dissolution rate RH" },{" #name" :" keyword" ," $" :{" id" :" kwrd0155" }," $$" :[{" #name" :" text" ," _" :" relative humidity |
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