Solubility Enhancement of BCS Classified II/IV Drug – Solid Dispersion of Apixaban by Solvent Evaporation

Asati, Amit; Salunkhe, Kishor S.; Chavan, Machindra J.; Chintamani, Ravindra; Singh, Rudra Pratap

doi:10.5530/ijpi.2020.4.76

Cited by 4 publications

(5 citation statements)

References 7 publications

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“…The solution was sifted through a 0.45µm filter and diluted with purified water and analysed using a UV-spectrophotometer at 278nm (Shimadzu 1800). 1,2…”

Section: Solubilitymentioning

confidence: 99%

“…The absorbance of the sample was taken at 278nm. 1,2 The drug content was determined by the formula: Drug content (%) = Weight of drug in co-crystal/ Total weight of sample X 100…”

Section: Drug Contentmentioning

confidence: 99%

“…The accomplishment of these approaches is totally dependent on the particular physico-chemical properties of the molecules being studied. 2 Over last few years there has been an enhanced interest in the design and development of pharmaceutical cocrystals emerging as a potential method for enhancing the bioavailability of drugs with low aqueous solubility.…”

Section: Introductionmentioning

confidence: 99%

“…Apixaban is a direct inhibitor of blood clotting factor Xa (FXa) that has been approved in many countries for several indications. 1,2 It is poorly soluble in water (0.028 mg/mL at 24°C) and possesses a lower bioavailability (about 50% for a single 10 mg dose). 4 The aim of the present research work is to improve the solubility of the Apixaban by using co-crystal approach.…”

Section: Introductionmentioning

confidence: 99%

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Co-crystals: A Novel Approach to Improve the Solubility of Apixaban

Asati¹,

Salunkhe²,

Rajput³

et al. 2023

Int J. Pharm. Investigation

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Objectives: The current study work was aimed to improve the solubility of Apixaban by forming co-crystals. Materials and Methods: Two solvents mainly Dimethyl Sulphoxide (DMSO) and 2,2,2-trifluoroethanol were tried during the formulation of co-crystals. The other chemicals oxalic acid, adipic acid and L-Tartaric acid were used. Results: From the different trials it was concluded that oxalic acid and DMSO combination with the drug gave the better results for improvement in the solubility. Hence the batch F3 was analysed further. The melting point of F3 was found lower than pure drug. Drug content was found optimum as 95.06 ±0.65%. FTIR-spectra demonstrated the combined peaks of drug and oxalic acid. DSC thermogram showed the sharp endothermic peak similar to pure drug. SEM and XRD spectra confirmed the formation of co-crystals. Conclusion: It was found that formation of co-crystals of apixaban and oxalic acid was satisfactory and it was beneficial to improve the solubility of the apixaban.

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“…The solution was sifted through a 0.45µm filter and diluted with purified water and analysed using a UV-spectrophotometer at 278nm (Shimadzu 1800). 1,2…”

Section: Solubilitymentioning

confidence: 99%

“…The absorbance of the sample was taken at 278nm. 1,2 The drug content was determined by the formula: Drug content (%) = Weight of drug in co-crystal/ Total weight of sample X 100…”

Section: Drug Contentmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Co-crystals: A Novel Approach to Improve the Solubility of Apixaban

Asati¹,

Salunkhe²,

Rajput³

et al. 2023

Int J. Pharm. Investigation

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“…The discrepancy between BCS and APX absolute physicochemical properties was because dose is considered in the classification of solubility [ 9 ]. There have been studies about the enhancement of APX solubility, ultimately to enhance its oral bioavailability [ 10 , 11 , 12 ]. Notably, solid dispersion (SD) has been employed in studies by Zhoye Y.Y and Asati et al; APX SD with mannitol and several hydrophilic polymers were prepared showing improvement of APX in aqueous solution [ 11 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Apixaban Solid Dispersion for the Enhancement of Apixaban Solubility and Permeability

Lee

et al. 2023

Pharmaceutics

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(1) Background: Solid dispersion (SD) can help increase the bioavailability of poorly water-soluble drugs. Meanwhile, apixaban (APX)—a new anticoagulation drug—has low water solubility (0.028 mg/mL) and low intestinal permeability (0.9 × 10−6 cm/s across Caco-2 colonic cells), thus resulting in a low oral bioavailability of <50%; (2) Methods: To solve the drawbacks of conventional APX products, a novel SD of APX in Soluplus® was prepared, characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR) spectroscopy techniques and evaluated for its solubility, intestinal permeability and pharmacokinetic performance. (3) Results: The crystallinity of the prepared APX SD was confirmed. The saturation solubility and apparent permeability coefficient increased 5.9 and 2.54 times compared to that of raw APX, respectively. After oral administration to the rats, the bioavailability of APX SD was improved by 2.31-fold compared to that of APX suspension (4) Conclusions: The present study introduced a new APX SD that potentially exhibits better solubility and permeability, thus increasing APX’s bioavailability.

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