Supercritical Process for Preparation of Nanomedicine: Oxaprozin Case Study

Khoshmaram, Aliakbar; Zabihi, Samyar; Pelalak, Rasool; Pishnamazi, Mahboubeh; Marjani, Azam; Shirazian, Saeed

doi:10.1002/ceat.202000411

Cited by 19 publications

(10 citation statements)

References 27 publications

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“…The density of solvent is reduced with increasing temperature because of higher energy of molecules which results in free movement of solvent molecules. The second phenomenon could be recognized as the change of solid sublimation pressure that can cause a positive influence on the solubility of drug in the solvent 4 , 12 , 18 , 30 . As such, the net effect of these two competing phenomena will determine whether the temperature has an increasing or decreasing effect on the drug solubility 4 .…”

Section: Resultsmentioning

confidence: 99%

“…These thermodynamic models have been well examined owing to their acceptable accuracy and simplicity which utilize only three fitting factors along with temperature, and density of CO 2 which can be accurately estimated. The worth mentioning point in using these models for correlating decitabine solubility in SC-CO 2 is that the models possess different fitting parameters because each one has been derived based on specific theory 30 .…”

Section: Methodsmentioning

confidence: 99%

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Experimental and thermodynamic modeling decitabine anti cancer drug solubility in supercritical carbon dioxide

Pishnamazi

Zabihi

Jamshidian³

et al. 2021

Sci Rep

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Design and development of efficient processes for continuous manufacturing of solid dosage oral formulations is of crucial importance for pharmaceutical industry in order to implement the Quality-by-Design paradigm. Supercritical solvent-based manufacturing can be utilized in pharmaceutical processing owing to its inherent operational advantages. However, in order to evaluate the possibility of supercritical processing for a particular medicine, solubility measurement needs to be carried out prior to process design. The current work reports a systematic solubility analysis on decitabine as an anti-cancer medicine. The solvent is supercritical carbon dioxide at different conditions (temperatures and pressures), while gravimetric technique is used to obtain the solubility data for decitabine. The results indicated that the solubility of decitabine varies between 2.84 × 10–05 and 1.07 × 10–03 mol fraction depending on the temperature and pressure. In the experiments, temperature and pressure varied between 308–338 K and 12–40 MPa, respectively. The solubility of decitabine was plotted against temperature and pressure, and it turned out that the solubility had direct relation with the pressure due to the effect of pressure on solvating power of solvent. The effect of temperature on solubility was shown to be dependent on the cross-over pressure. Below the cross-over pressure, there is a reverse relation between temperature and solubility, while a direct relation was observed above the cross-over pressure (16 MPa). Theoretical study was carried out to correlate the solubility data using several thermodynamic-based models. The fitting and model calibration indicated that the examined models were of linear nature and capable to predict the measured decitabine solubilities with the highest average absolute relative deviation percent (AARD %) of 8.9%.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Experimental and thermodynamic modeling decitabine anti cancer drug solubility in supercritical carbon dioxide

Pishnamazi

Zabihi

Jamshidian³

et al. 2021

Sci Rep

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“…Various predictive models in this research have been investigated and developed based on the experimental investigation of Khoshmaram et al They experimentally measured the solubility of Oxaprozin using the combination of static and gravimetric techniques via a pressure–volume-temperature (PVT) cell 14 . This system can be filled with up to 0.4 L Oxaprozin and supercritical liquid.…”

Section: Methodsmentioning

confidence: 99%

“…Supercritical carbon dioxide (SC-CO 2 ) is being frequently applied to fractionate the precious components in pharmaceutical processes due to possessing noteworthy properties such as abundancy, colorless nature, cost-effectiveness, and environmentally benign characteristic 13 . Due to the importance of solubility in SC-CO 2 for the design and development of novel drugs, the conduction of experimental investigation for evaluating the solubility of these drugs is of great importance 14 . Despite the great importance for obtaining the solubility of drugs, the existence of some economic/operational problems such as difficulty in solute–solvent interactions in SC-CO 2 system and high cost have limited the conduction of experimental investigation.…”

Section: Introductionmentioning

confidence: 99%

Design of predictive model to optimize the solubility of Oxaprozin as nonsteroidal anti-inflammatory drug

Alshehri

Alqarni

Namazi

et al. 2022

Sci Rep

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These days, many efforts have been made to increase and develop the solubility and bioavailability of novel therapeutic medicines. One of the most believable approaches is the operation of supercritical carbon dioxide fluid (SC-CO2). This operation has been used as a unique method in pharmacology due to the brilliant positive points such as colorless nature, cost-effectives, and environmentally friendly. This research project is aimed to mathematically calculate the solubility of Oxaprozin in SC-CO2 through artificial intelligence. Oxaprozin is a nonsteroidal anti-inflammatory drug which is useful in arthritis disease to improve swelling and pain. Oxaprozin is a type of BCS class II (Biopharmaceutical Classification) drug with low solubility and bioavailability. Here in order to optimize and improve the solubility of Oxaprozin, three ensemble decision tree-based models including random forest (RF), Extremely random trees (ET), and gradient boosting (GB) are considered. 32 data vectors are used for this modeling, moreover, temperature and pressure as inputs, and drug solubility as output. Using the MSE metric, ET, RF, and GB illustrated error rates of 6.29E−09, 9.71E−09, and 3.78E−11. Then, using the R-squared metric, they demonstrated results including 0.999, 0.984, and 0.999, respectively. GB is selected as the best fitted model with the optimal values including 33.15 (K) for the temperature, 380.4 (bar) for the pressure and 0.001242 (mole fraction) as optimized value for the solubility.

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“…From the processing point of view, it is also of great importance to obtain the API solubilities in a wide range of operational conditions, so that the solubility can be obtained as a function of the process parameters 14–18. Hazaveie et al 19 and Sodeifian et al 20, 21 studied the correlation of drug solubility, using different empirical correlations in the SC state.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Supercritical Technology for the Preparation of Nanomedicine: Etoricoxib Analysis

Pishnamazi

Zabihi

Jamshidian³

et al. 2021

Chem Eng & Technol

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The solubility of etoricoxib in supercritical CO2 was measured using a gravimetric method in a wide range of pressures and temperatures. A pressure‐volume‐temperature (PVT) cell was designed and used. Different solubility values were obtained between 2.34 × 10−5 and 7.96 × 10−4 mol mol−1, depending on the applied pressure and temperature. Analyzing the solubility curves revealed that the pressure had a direct effect on the solubility of etoricoxib at all temperatures, while the effect of the temperature was dependent on the crossover point in the solubility curve. Indeed, before reaching the crossover point, the solubility decreased with increasing temperature, and after the crossover point, a direct relationship was observed between the solubility and the temperature. As such, the lowest solubility was obtained at 120 bar and 338 K.

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Supercritical Process for Preparation of Nanomedicine: Oxaprozin Case Study

Cited by 19 publications

References 27 publications

Experimental and thermodynamic modeling decitabine anti cancer drug solubility in supercritical carbon dioxide

Experimental and thermodynamic modeling decitabine anti cancer drug solubility in supercritical carbon dioxide

Design of predictive model to optimize the solubility of Oxaprozin as nonsteroidal anti-inflammatory drug

Evaluation of Supercritical Technology for the Preparation of Nanomedicine: Etoricoxib Analysis

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