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Polymer Bulletin
Published in: Polymer Bulletin 12/2020

18-12-2019 | Original Paper

Preparation and evaluation of pharmaceutical co-crystals for solubility enhancement of atorvastatin calcium

Authors: Afreen Naqvi, Mahmood Ahmad, Muhmmad Usman Minhas, Kifayat Ullah Khan, Fakhra Batool, Ali Rizwan

Published in: Polymer Bulletin | Issue 12/2020

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Abstract

Co-crystallization is one of the methods to enhance the solubility of hydrophobic drugs that belong to BCS class II. Preparation and characterization of atorvastatin calcium co-crystals by liquid-assisted grinding method using citric acid and nicotinamide as co-formers for solubility enhancement were the objective of the current research. All the prepared formulations were characterized by powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), zeta size analysis, dissolution and solubility studies. Solubility studies were performed in distilled water, pH 1.2 and pH 6.8. PXRD revealed the structural nature of the co-crystals formulations. FTIR, TGA and DSC confirmed the complex formation and have better thermal stability than individual components. SEM images exhibited the prism-like crystals with irregular and rough surfaces. Zeta size analysis showed the small particle size having large surface area that facilitates to improve the solubility. Dissolution and solubility studies of the formulations confirmed that solubility enhanced several folds in all media as compared to the solubility of available market drug. From all these studies, it can be concluded that co-crystallization technique enhanced the solubility of atorvastatin calcium by using liquid-assisted grinding method.
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Literature
1.
Junghanns J-UA, Müller RH (2008) Nanocrystal technology, drug delivery and clinical applications. Int J Nanomed 3(3):295
2.
Loh ZH, Samanta AK, Heng PWS (2015) Overview of milling techniques for improving the solubility of poorly water-soluble drugs. Asian J Pharm Sci 10(4):255–274CrossRef
3.
Kumar A et al (2011) Review on solubility enhancement techniques for hydrophobic drugs. Pharmacie Globale 3(3):001–007
4.
Vemula VR, Lagishetty V, Lingala S (2010) Solubility enhancement techniques. Int J Pharm Sci Rev Res 5(1):41–51
5.
Kim J-S et al (2008) Physicochemical properties and oral bioavailability of amorphous atorvastatin hemi-calcium using spray-drying and SAS process. Int J Pharm 359(1):211–219PubMedCrossRef
6.
Chaudhary A et al (2012) Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: a recent review. J Adv Pharm Educ Res 2(1):32–67
7.
8.
Williams HD et al (2013) Strategies to address low drug solubility in discovery and development. Pharmacol Rev 65(1):315–499PubMedCrossRef
9.
Shekhawat P, Pokharkar V (2017) Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles. Acta Pharm Sin B 7(3):260–280CrossRef
10.
Khadka P et al (2014) Pharmaceutical particle technologies: an approach to improve drug solubility, dissolution and bioavailability. Asian J Pharm Sci 9(6):304–316CrossRef
11.
Charoenchaitrakool M et al (2000) Micronization by rapid expansion of supercritical solutions to enhance the dissolution rates of poorly water-soluble pharmaceuticals. Ind Eng Chem Res 39(12):4794–4802CrossRef
12.
Kawabata Y et al (2011) Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications. Int J Pharm 420(1):1–10PubMedCrossRef
13.
14.
Arenas-García JI et al (2017) Interrelation of the dissolution behavior and solid-state features of acetazolamide cocrystals. Eur J Pharm Sci 96:299–308PubMedCrossRef
15.
Setyawan D et al (2014) Preparation and characterization of artesunate–nicotinamide co-crystal by solvent evaporation and slurry method. Asian J Pharm Clin Res 7(1):62–65
16.
Zaini E et al (2010) Cocrystalline phase transformation of binary mixture of trimethoprim and sulfamethoxazole by slurry technique. Asian J Pharm Clin Res 3(4):26–29
17.
Grossjohann C et al (2012) Characterisation, solubility and intrinsic dissolution behaviour of benzamide: dibenzyl sulfoxide cocrystal. Int J Pharm 422(1):24–32PubMedCrossRef
18.
Serrano DR et al (2016) Modelling and shadowgraph imaging of cocrystal dissolution and assessment of in vitro antimicrobial activity for sulfadimidine/4-aminosalicylic acid cocrystals. Eur J Pharm Sci 89:125–136PubMedCrossRef
19.
Bavishi DD, Borkhataria CH (2016) Spring and parachute: how cocrystals enhance solubility. Prog Cryst Growth Charact Mater 62(3):1–8CrossRef
20.
Drozd KV et al (2017) Drug-drug cocrystals of antituberculous 4-aminosalicylic acid: screening, crystal structures, thermochemical and solubility studies. Eur J Pharm Sci 99:228–239PubMedCrossRef
21.
Gozali D et al (2016) Virtual screening of coformers for atorvastatin co-crystallization and the characterizations of the co-crystals. Int J Pharm Sci Res 7(4):1450
22.
Wicaksono Y, Wisudyaningsih B, Siswoyo TA (2017) Cocrystal of atorvastatin calcium–malonic acid, pp 75–78
23.
Farajzadeh MA, Khorram P, Pazhohan A (2016) Simultaneous determination of atorvastatin and valsartan in human plasma by solid-based disperser liquid–liquid microextraction followed by high-performance liquid chromatography–diode array detection. J Chromatogr B 1017:62–69CrossRef
24.
Ramani K et al (2012) Design and development of atorvastatin calcium buccoadhesive bilayered devices for oral drug delivery. J Drug Deliv Sci Technol 22(6):505–510CrossRef
25.
Ahmed IS et al (2016) PD-PK evaluation of freeze-dried atorvastatin calcium-loaded poly-ε-caprolactone nanoparticles. Int J Pharm 504(1):70–79PubMedCrossRef
26.
Zhang H-X et al (2009) Micronization of atorvastatin calcium by antisolvent precipitation process. Int J Pharm 374(1):106–113PubMedCrossRef
27.
Kanoujia J et al (2016) Novel genipin crosslinked atorvastatin loaded sericin nanoparticles for their enhanced antihyperlipidemic activity. Mater Sci Eng, C 69:967–976CrossRef
28.
Choudhary A et al (2012) Development and characterization of an atorvastatin solid dispersion formulation using skimmed milk for improved oral bioavailability. Acta Pharm Sin B 2(4):421–428CrossRef
29.
Mukaida M et al (2015) Identification and physicochemical characterization of caffeine–citric acid co-crystal polymorphs. Eur J Pharm Sci 79:61–66PubMedCrossRef
30.
Ganesh M et al (2015) Chitosan cocrystals embedded alginate beads for enhancing the solubility and bioavailability of aceclofenac. Int J Biol Macromol 74:310–317PubMedCrossRef
31.
Cugovčan M et al (2017) Biopharmaceutical characterization of praziquantel cocrystals and cyclodextrin complexes prepared by grinding. J Pharm Biomed Anal 137:42–53PubMedCrossRef
32.
Hsu P-C et al (2012) Solid-state thermal behavior and stability studies of theophylline–citric acid cocrystals prepared by neat cogrinding or thermal treatment. J Solid State Chem 192:238–245CrossRef
33.
34.
Shimono K et al (2015) Kinetics of co-crystal formation with caffeine and citric acid via liquid-assisted grinding analyzed using the distinct element method. Eur J Pharm Sci 76:217–224PubMedCrossRef
35.
Tomaszewska I et al (2013) Pharmaceutical characterisation and evaluation of cocrystals: importance of in vitro dissolution conditions and type of coformer. Int J Pharm 453(2):380–388PubMedCrossRef
Metadata
Title
Preparation and evaluation of pharmaceutical co-crystals for solubility enhancement of atorvastatin calcium
Authors
Afreen Naqvi
Mahmood Ahmad
Muhmmad Usman Minhas
Kifayat Ullah Khan
Fakhra Batool
Ali Rizwan
Publication date
18-12-2019
Publisher
Springer Berlin Heidelberg
Published in
Polymer Bulletin / Issue 12/2020
Print ISSN: 0170-0839
Electronic ISSN: 1436-2449
DOI
https://doi.org/10.1007/s00289-019-02997-4

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