scholarly journals Development and Characterization of Nanoemulsion-based Buccal Films of Atorvastatin Calcium for Enhancement of Hypolipidemic Effect

2021 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Moetaza Soliman ◽  
Fatma Bakr ◽  
Hassan Elsabbagh
Author(s):  
Rajesh Desai ◽  
Suresh Koradia

The objective of this study is to isolation and characterization of unknown degradation product of Atorvastatin calcium in combination formulation product with Ezetimibe by using modern techniques of separation and aracterization. An unknown impurity is generating during a forced degradation study of Atorvastatin and Ezetimibe fixed-dose combination tablets. By using the gradient reversed-phase high-pressure liquid chromatographic method, unknown degradation impurity was detected and quantified in the range of 0.05% to 0.2% of Atorvastatin. The impurity was enriched by extreme oxidation degradation of Atorvastatin and isolated through preparative HPLC. The structure of the impurity was characterized by mass and NMR spectrum.


2015 ◽  
Vol 44 (6) ◽  
pp. 1448-1456 ◽  
Author(s):  
Kritika Sharma ◽  
Supandeep Singh Hallan ◽  
Bharat Lal ◽  
Ankur Bhardwaj ◽  
Neeraj Mishra

2016 ◽  
Vol 45 (6) ◽  
pp. 1138-1145 ◽  
Author(s):  
Azin Jahangiri ◽  
Mohammad Barzegar-Jalali ◽  
Yousef Javadzadeh ◽  
Hamed Hamishehkar ◽  
Khosro Adibkia

2020 ◽  
Vol 28 (3) ◽  
pp. 266-273 ◽  
Author(s):  
Gamal M. Zayed ◽  
Saleh Abd-El Rasoul ◽  
Mohamed A. Ibrahim ◽  
Mohammed S. Saddik ◽  
Doaa H. Alshora

2019 ◽  
Vol 15 ◽  
pp. 2085-2091
Author(s):  
Jürgen Krauß ◽  
Monika Klimt ◽  
Markus Luber ◽  
Peter Mayer ◽  
Franz Bracher

Atorvastatin calcium (Lipitor®, Sortis®) is a well-established cholesterol synthesis enzyme (CSE) inhibitor commonly used in the therapy of hypercholesterolemia. This drug is known to be sensitive to acid treatment, but only little data has been published on the structures of the degradation products. Here we report the identification of two novel degradation products of atorvastatin, which are formed only under drastic acidic conditions. While treatment with conc. sulfuric acid led to a loss of the carboxanilide residue (accompanied by an expectable lactonization/dehydration process in the side chain), treatment with conc. aqueous hydrochloric acid gave a complex, bridged molecule under C–C-bond formation of the lactone moiety with the pyrrole, migration of the isopropyl group and loss of the carboxanilide residue. The novel degradation products were characterized by NMR spectroscopy, HRMS data and X-ray crystal structure analysis.


2011 ◽  
Vol 77 (2) ◽  
pp. 187-199 ◽  
Author(s):  
Javier O. Morales ◽  
Jason T. McConville
Keyword(s):  

2019 ◽  
Vol 19 (3) ◽  
pp. 660
Author(s):  
Yudi Wicaksono ◽  
Dwi Setyawan ◽  
Siswandono Siswandono ◽  
Tri Agus Siswoyo

Preparation and characterization of a novel cocrystal of atorvastatin calcium with succinic acid coformer were successfully performed. This research aims to modify the crystalline form of atorvastatin calcium through cocrystallization with succinic acid coformer. The cocrystal was prepared by a solvent evaporation method and characterized by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The atorvastatin calcium-succinic acid cocrystal has new crystalline peaks at 2θ of 12.9, 18.2 and 26.7° indicating the formation of a new crystalline phase. The cocrystal showed the melting point at 205.7 °C with an enthalpy of fusion 30.2 J/g which is different from the initial components. The FTIR spectra of cocrystal showed the shifting of absorption peaks of groups of initial components indicating of formation of atorvastatin calcium-succinic acid cocrystal through acid–amide intermolecular hydrogen bond interactions. The solubility and dissolution test showed that the cocrystal has solubility and dissolution rate significantly higher than the solubility and dissolution rate of pure atorvastatin calcium.


Symmetry ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 88
Author(s):  
Maram Diab ◽  
Al-Sayed Sallam ◽  
Imad Hamdan ◽  
Randa Mansour ◽  
Rohanah Hussain ◽  
...  

Insulin mucoadhesive buccal films (MBF) are a noninvasive insulin delivery system that offers an advantageous alternative route of administration to subcutaneous injection. One major concern in the formulation of insulin MBF is the preservation of an insulin secondary structure in the presence of the other film components. Buccal films were formulated using chitosan, glycerin, and L-arginine. The MBF-forming solutions (MBF-FS) and the films (MBF) were examined for their chemical and structural stability and for their in vivo activity. Enzyme-Linked Immunosorbent Assay (ELISA) of the insulin-loaded MBF showed that each individualized unit dose was at least loaded with 80% of the insulin theoretical dose. Results of Synchrotron Radiation Circular Dichroism (SRCD) measurements revealed that MBF-FS retained the α-helices and β–sheets conformations of insulin. Fourier transform infrared (FTIR)-microspectroscopy (FTIR-MS) examination of insulin MBF revealed the protective action of L-arginine on insulin structure by interacting with chitosan and minimizing the formation of an unordered structure and β-strand. A blood glucose-lowering effect of insulin MBF was observed in comparison with subcutaneous (S.C) injection using a rat model. As a result; chitosan-based MBFs were formulated and characterized using SRCD and FTIR-MS techniques. Furthermore, the results of in vivo testing suggested the MBFs as a promising delivery system for insulin.


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