Influence of Preparation Methods on Physicochemical and Pharmacokinetic Properties of Co-amorphous Formulations: The Case of Co-amorphous Atorvastatin: Naringin

Nair, Athira R; Varma, Raghava; Gourishetti, Karthik; Bhat, Krishnamurthy; Dengale, Swapnil J.

doi:10.1007/s12247-019-09381-9

Cited by 34 publications

(13 citation statements)

References 49 publications

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“…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]. These results show that spray dried solids of AC with INA and MA coformers forms a coamorphous solid system [19,20,31].…”

Section: Pxrd Diffractogramsupporting

confidence: 90%

“…DSC is a technique used to analyze thermal events related to the phase transitions of solid materials [18,32]. Therefore, the phase transitions obtained from DSC thermograms can be used to strengthen the alleged amorphicity [21]. DSC can also be used to estimate the phase solubility of amorphous materials.…”

Section: Dsc Thermogrammentioning

confidence: 99%

“…The Tg of co-amorphous AC-INA and AC-MA showed higher temperatures than the melting point of crystalline AC. Therefore, the relatively higher Tg of the coamorphous system indicates that intermolecular interactions such as hydrogen bonding between functional groups of drug and coformers were occurring [21]. In general, the intermolecular interactions within the coamorphous system increase its stability and reduces crystallization tendency [13].…”

Section: Dsc Thermogrammentioning

confidence: 99%

“…Creating coamorphous solids in order to improve the solubility of AC can been carried out using the solvent evaporation and cooling method [20,21]. However, there is a limitation to these methods, given that they are both difficult to make on a commercial scale [22,23].…”

Section: Introductionmentioning

confidence: 99%

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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: 90%

Section: Dsc Thermogrammentioning

confidence: 99%

Section: Dsc Thermogrammentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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 and irbesartan were chosen as model compounds to formulate the co-amorphous system. There have been several attempts to improve the solubility of ATR and IRB by both solid dispersion [ 3 , 5 , 28 , 29 , 30 , 31 ] and co-amorphous formulation [ 27 , 32 , 33 , 34 , 35 ]. ATR and IRB were chosen as model compounds for several reasons.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Characterization of a Co-Amorphous Atorvastatin-Irbesartan System with a Potential Application in Fixed-Dose Combination Therapy

et al. 2021

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The aim of this study was to characterize a 1:1 molar ratio of a pharmacologically relevant co-amorphous atorvastatin-irbesartan (ATR-IRB) system obtained by quench cooling of the crystalline ATR/IRB physical mixture for potential use in the fixed-dose combination therapy. The system was characterized by employing standard differential scanning calorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), and intrinsic dissolution rate studies. Quantum mechanical calculations were performed to obtain information regarding intermolecular interactions in the studied co-amorphous ATR-IRB system. The co-amorphous formulation showed a significant improvement in the intrinsic dissolution rate (IDR) of IRB over pure crystalline as well as its amorphous counterpart. An unusual behavior was observed for ATR, as the IDR of ATR in the co-amorphous formulation was slightly lower than that of amorphous ATR alone. Short-term physical aging studies of up to 8 h proved that the ATR-IRB co-amorphous system remained in the amorphous form. Furthermore, no physical aging occurred in the co-amorphous system. FT-IR, density functional theory calculations, and analysis of Tg value of co-amorphous system using the Couchman–Karasz equation revealed the presence of molecular interactions between APIs, which may contribute to the increased physical stability.

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Breaking barriers: enhancing solubility and dissolution of efonidipine using co-amorphous formulations

Jadav,

Dudhat

2024

Naunyn-Schmiedeberg's Arch Pharmacol

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Influence of Preparation Methods on Physicochemical and Pharmacokinetic Properties of Co-amorphous Formulations: The Case of Co-amorphous Atorvastatin: Naringin

Cited by 34 publications

References 49 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

Physicochemical Characterization of a Co-Amorphous Atorvastatin-Irbesartan System with a Potential Application in Fixed-Dose Combination Therapy

Breaking barriers: enhancing solubility and dissolution of efonidipine using co-amorphous formulations

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