Preparation and Characterization of a Novel Cocrystal of Atorvastatin Calcium with Succinic Acid Coformer

Wicaksono, Yudi; Setyawan, Dwi; Siswandono, Siswandono; Siswoyo, Tri Agus

doi:10.22146/ijc.35801

Cited by 8 publications

(9 citation statements)

References 27 publications

(39 reference statements)

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“…That of crystalline AC shows sharp diffraction peaks of 2θ at 9.4, 10.2, 11.8, 17.0, 19.4, 21.6, and 23.7°. This indicates the presence of a crystalline solid, which agrees with previous reports [11,31]. The PXRD patterns of AC-INA and AC-MA indicated the absence of sharp diffraction peaks and the presence of typical halo patterns, which suggest amorphicity [21].…”

Section: Pxrd Diffractogramsupporting

confidence: 91%

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Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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Atorvastatin calcium (AC) is a statin drug used to lower cholesterol. Its crystalline form is usually found in the market with low solubility properties. The amorphization of crystalline AC is a technique used to increase its solubility however; the amorphous form has less thermodynamic stability. Therefore, to increase the solubility properties of its crystalline form, an AC coamorphous solid was prepared. This coamorphous solid was prepared using spray drying techniques, and coformers such as isonicotinamide (INA) and maleic acid (MA). Furthermore, characterization was carried out using powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy, and scanning electron microscopy, while the solubility properties test was conducted using the shake-flask and paddle method. The results showed that the spray-dried solids were coamorphous with single-phase homogeneous systems. Furthermore, the coamorphous solids, AC-INA and AC-MA were found to have a higher Tg than the melting points of other components, and formed intermolecular interactions between them. The higher Tg and presence of intermolecular interactions indicate that coamorphous solids are more stable than the amorphous form. Therefore, the results of the solubility and dissolution test showed that the coamorphous solid of AC-INA and AC-MA have better solubility properties compared to the AC crystalline form.

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Section: Pxrd Diffractogramsupporting

confidence: 91%

“…The PXRD patterns of AC-INA and AC-MA indicated the absence of sharp diffraction peaks and the presence of typical halo patterns, which suggest amorphicity [21]. These results show that spray dried solids of AC with INA and MA coformers forms a coamorphous solid system [19,20,31].…”

Section: Pxrd Diffractogrammentioning

confidence: 69%

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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“…The main objective of the application of pharmaceutical cocrystallization is to improve problematic properties such as solubility, dissolution rate, bioavailability and stability [18].…”

Section: Effect Of Cocrystal On Active Pharmaceutical Propertiesmentioning

confidence: 99%

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

et al. 2021

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Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.

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“…The identification of AVA was carried out by melting point determination, FTIR spectrometry and differential scanning calorimetry (DSC). Melting point determination was carried using Thiele tube method [31].DSC was carried out to study the thermal behaviour of the drug [19].The analytical method development was carried out using ultraviolet spectroscopic analysis. Calibration of AVA was performed in solvents namely methanol, pH 1.2 hydrochloric acid buffer and pH 6.8 phosphate buffer.…”

Section: Preformulation Studiesmentioning

confidence: 99%

“…SEM imaging of AVA, CCFs and cocrystals were performed by a scanning electron microscope (ZEISS EVO 18 Germany -Physics department, RTMNU, Nagpur) using electron beam for surface imaging [19].…”

Section: Scanning Electron Microscopymentioning

confidence: 99%

Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

Trivedi¹,

Borkar²,

Puranik³

2020

jrp

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The objective of the present work was to prepare cocrystals of poorly soluble drug Atorvastatin Calcium (AVA) with the aim of increasing its solubility and dissolution properties. Screening of 8 cocrystal formers (CCFs) was performed by Hansen solubility parameter (HSPs) using 4 methods-neat grinding, solvent drop grinding, solvent evaporation and sonocrystallization in equimolar ratio. Solubility of AVA cocrystal (1.9 fold increase) in comparison to plain AVA drug has been demonstrated with solubility experiments. FTIR spectra of AVA cocrystal showed disappearance of O-H group indicating the formation of hydrogen bond synthon between the drug and CCFs. DSC thermogram showed drastic reduction in melting point from 164.6°C to 71.9 °C indicating the reduction in cohesive energy and increase in solubility. XRD pattern showed new crystalline peaks at 2θ values of 9.858°, 15.201°, 22.907°, 25.407°, 29.496°. SEM analysis showed changes in the morphological characteristics as compared to drug and CCFs, indicating different crystalline nature. Experimental design was applied to optimize AVA cocrystal IR tablet for concentration of aerosil (X1) and MMC 102 (X2) and were evaluated for drug release (Y1) and friability (Y2). It was found that as the concentration of aerosil and MMC 102 increased friability decreased and %drug release increased. A drug release of 98.54±1.163% and friability of 0.515±0.090 % was obtained for optimized batch. Ex vivo diffusion study was carried out by isolating rat stomach tissue, exhibiting higher drug release (95.71±0.98 %) than plain AVA and marketed tablet. Thus formulating AVA cocrystal and its subsequent formulation in optimized IR tablet gives a promising opportunity for manufacturing a drug with increased bioavailability.

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Preparation and Characterization of a Novel Cocrystal of Atorvastatin Calcium with Succinic Acid Coformer

Cited by 8 publications

References 27 publications

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Systematic Review: Cocrystal as Efforts to Improve Physicochemical and Bioavailability Properties of Oral Solid Dosage Form

Experimental design approach for development of cocrystals and immediate release cocrystal tablet of atorvastatin calcium for enhancement of solubility and dissolution

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