Abstract:The solubility of loxoprofen as a nonsteroidal anti-inflammatory drug (NSAID) is measured at various temperatures (308, 318, 328, and 338 K) and pressures (12,16,20,24,28,32,36, and 40 MPa) in supercritical carbon dioxide (SC-CO 2 ). The solubility data were measured using a gravimetric-based approach and revealed the solubility range of 1.35 × 10 −5 to 1.28 × 10 −3 based on the mole fraction of loxoprofen. The results revealed that solubility can be significantly enhanced from 1.04 × 10 −5 to 1.28 × 10 −3 (… Show more
“…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%
“…It should be pointed out that one of the attractive advantages of the currently designed setup and method for solubility measurements is its simplicity, because this method only requires an accurate digital balance with a minimum accuracy of 0.1 mg and high-pressure and high-temperature vessel with known volume. So, it would be easier than the other available methods to measure the solubility of different APIs in SC-CO 2 as a function of pressure and temperature 4 , 11 , 12 , 16 , 18 . Figure 1 The supercritical based solubility apparatus used in this study.…”
Section: Methodsmentioning
confidence: 99%
“…The models rely on density of solvent and can be easily fitted to the experimental data using regression techniques. These models have been used and validated in our previous studies for solubility of different types of API in supercritical CO 2 4 , 12 , 13 , 16 , 18 . The models for predicting the solubility of decitabine in this work include: Chrastil 26 , Garlapati and Madras 20 , Mendez-Santiago and Teja (MST) 27 , Bartle et al 28 , and Kumar and Johnston (K–J) 29 models.…”
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%.
“…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%
“…It should be pointed out that one of the attractive advantages of the currently designed setup and method for solubility measurements is its simplicity, because this method only requires an accurate digital balance with a minimum accuracy of 0.1 mg and high-pressure and high-temperature vessel with known volume. So, it would be easier than the other available methods to measure the solubility of different APIs in SC-CO 2 as a function of pressure and temperature 4 , 11 , 12 , 16 , 18 . Figure 1 The supercritical based solubility apparatus used in this study.…”
Section: Methodsmentioning
confidence: 99%
“…The models rely on density of solvent and can be easily fitted to the experimental data using regression techniques. These models have been used and validated in our previous studies for solubility of different types of API in supercritical CO 2 4 , 12 , 13 , 16 , 18 . The models for predicting the solubility of decitabine in this work include: Chrastil 26 , Garlapati and Madras 20 , Mendez-Santiago and Teja (MST) 27 , Bartle et al 28 , and Kumar and Johnston (K–J) 29 models.…”
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%.
“…Recently, this technique has been applied to measure the solubility of different APIs in supercritical CO 2 (SC-CO 2 ) at different temperatures and pressures [13][14][15][16]. Considering the advantages of supercritical technology in manufacturing nanomedicine, in this work the solubility of an NSAID, i.e., oxaprozin, in supercritical CO 2 at temperatures between 308 and 338 K and pressures between 120 and 400 bar using a simple gravimetric method is determined.…”
The solubility of oxaprozin was determined in supercritical carbon dioxide as solvent under different temperatures and pressures using the gravimetric technique. The measured solubility data revealed that the solubility of this medication varies by changing the pressure and temperature. The oxaprozin/supercritical solvent possesses a crossover pressure at 200 bar where the influence of temperature on the solubility changes. Furthermore, the experimental data was correlated using several semi‐empirical models. The best result was stated for the Kumar and Johnston model, whereas the other examined models introduced higher deviations.
“…In this way, several works have been done for measuring solubility of potential drugs in supercritical carbon dioxide such as phenylepherin hydrochloride 12 , sulindac 13 , fluoxetine hydrochloride 14 , trioctylmethyl ammonium 15 , piroxicam 16 , etc. [17][18][19][20][21] . Unfortunately, since measuring the experimental values of the solubility for all of the substances at the wide range of temperature and pressure is impossible, it is highly required to utilize models and correlations which can simulate solubility values of them under various pressures and temperatures such as equations of state (EOS) 22,23 , artificial neural network 24,25 , and, semi-empirical density based correlations 26,27 .…”
Tolmetin is a non-steroidal anti-inflammatory drug being used to decrease the level of hormones which are the reasons for pain, swelling, tiredness, and stiffness for osteoarthritis and rheumatoid arthritis cases. We evaluated its solubility in supercritical carbon dioxide (SC-CO2) with the aim of drug nanonization, considering temperature and pressure variations between 120 and 400 bar and 308–338 K, in the experiments. In this way, a PVT solubility cell based on static solubility approach coupled with a simple gravimetric procedure was utilized to evaluate the solubility of tolmetin. The solubility values between 5.00 × 10−5 and 2.59 × 10−3 mol fraction were obtained for tolmetin depending on the pressure and temperature of the cell. The measured data demonstrated a direct correlation between pressure and solubility of tolmetin, while the effect of temperature was a dual effect depending on the crossover pressure (160 bar). The calculated solubility data were modeled using several semi-empirical correlations, and the fitting parameters were calculated using the experimental data via appropriate optimization method. The correlated solubility data revealed that the KJ model was the most accurate one with an average absolute relative deviation percent (AARD%) of 6.9. Moreover, the carried out self-consistency analysis utilizing these correlations illustrated great potential of these models to extrapolate the solubility of tolmetin beyond the measured conditions.
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