Study of biopharmaceutical solubility of quercetin and its solid dispersions
Keywords:biopharmaceutical solubility, quercetin, solid dispersion, spectrophotometric determination method
Topicality. Quercetin is a natural flavonoid, which has a variety of pharmacological properties, such as anti-inflammatory, antioxidant, anti-allergic, chemo-preventive, antiaggregate, etc. Despite the breadth of the pharmacological profile, its use is limited due to low solubility. Solid dispersions are widely used to increase the solubility of poorly soluble substances.
Aim. To determine the biopharmaceutical solubility of quercetin and its solid dispersions.
Materials and methods. The subjects of the study were the substance quercetin, its solid dispersion (SD) with macrogol-6000, which also included microcrystalline cellulose and neusilin. Samples of solid dispersions were obtained by liquid phase method. The ratio of AFI and carrier is as 1 : 2. Biopharmaceutical solubility of the samples was determined by the method of shaking the maximum single dose of quercetin 100 mg at a constant temperature (37 ±1 °C) for 24 hours in 250 ml of buffer solutions with a physiological pH value (1.2; 4.5; 6.8). Quantitative determination was carried out by spectrophotometric standard method. The statistical processing of the results of the experiment was carried out using the Microsoft Office Excel 2007 package.
Results and discussion. It was found that the adsorption spectra of quercetin solutions in buffer solutions with pH 1.2, 4.5, 6.8 contain a wide inclined absorption band at a maximum of 365 nm, which can be used to determine the concentration of quercetin solutions by the one-component single-wave spectrophotometry method according to the standard. It has been established that light absorption of quercetin solutions at λ 365 nm is linear and obeys Beer-Lambert Law. It has been proved that macrogol-6000, used in the preparation of solid dispersions, does not affect the adsorption spectrum of quercetin solutions in buffer solutions with pHs of 1.2, 4.5, and 6.8. It was established that according to the solubility parameters in water buffer solutions with pH of 1.2, 4.5 and 6.8, quercetin refers to practically insoluble substances. Creating solid dispersions can increase the solubility ratios from 8 to 40 times depending on the pH of the buffer solution. The maximum solubility value is observed at pH 4.5.
Conclusions. Thus, the use of solid dispersions significantly increases the value of quercetin biopharmaceutical solubility in a dose of 100 mg, and at a dose of 50 mg it is close to normal when using pH of 4.5. The obtained results allow concluding that it is expedient to create enteric-soluble coated medicines.
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