DOI: https://doi.org/10.24959/ubphj.19.209

Study of biopharmaceutical solubility of quercetin and its solid dispersions

I. Kovalevska, O. Ruban, V. Grudko

Abstract


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.


Keywords


biopharmaceutical solubility; quercetin; solid dispersion; spectrophotometric determination method

Full Text:

PDF

References


Bajaj, S., Khan. A. (2012). Antioxidants and diabetes. Indian Journal of Endocrinology and Metabolism, 16, 267–271.

Ioku, K., Tsushida, T., Takei, Y., Nakatani, N., & Terao, J. (1995). Antioxidative activity of quercetin and quercetin monoglucosides in solution and phospholipid bilayers. Biochimica et Biophysica Acta (BBA) – Biomembranes, 1234 (1), 99–104. https://doi.org/10.1016/0005-2736(94)00262-n

Kovalevska, I. V. (2014). Aktualni pytannia farmatsevtychnoi i medychnoi praktyky, 1, 9–11.

Kovalevska, I., & Ruban, O. (2018). Development of the methodological approach of obtaining preparations based on solid dispersions. ScienceRise: Pharmaceutical Science, 4 (14), 4–8. https://doi.org/10.15587/2519-4852.2018.140756

Kovalevska, I. V., Ruban, E. A., Kutsenko, S. A., Kutova, O. V., Kovalenko, S. V. (2017). Study of physical and chemical properties of solid dispersions of quercetin. Asian Journal of Pharmaceutics, 11 (4), 805–809. https://doi.org/10.22377/ajp.v11i04.1719

Derzhavna Farmakopeya Ukraini: v 3 t. (2015). Derzhavne pidprimstvo “Ukrains’kij naukovij farmakopejnij centr yakosti likars’kih zasobiv”. – 2-e vid. – Kharkiv: Derzhavne pidprimstvo “Ukrains’kij naukovij farmakopejnij centr yakosti likars’kih zasobiv”, 1, 1128.

Ramenskaia, G. V., Shokhin, I. E., Savchenko, A. Iu., Kulinich, Iu. I., & Davydova, K. S. (2011). Farmatciia, 5, 3–11.

Ramenskaia, G. V., Shokhin, I. E., Kulinich, Iu. I. (2012). Vestn. VGU, seriia: khimiia. biologiia. Farmatciia, 1, 213–215.


GOST Style Citations


1. Bajaj, S. Antioxidants and diabetes/ S. Bajaj, A. Khan // Indian J. of Endocrinol. and Metabolism. – 2012. – Vol. 16. – P. 267–271.

2. Antioxidative activity of quercetin and quercetin monoglucosides in solution and phospholipid bilayers / K. Ioku, T. Tsushida, Y. Takei et al. // Biochim. Biophys. Acta. – 1995. – Vol. 1234. – P. 99–104. https://doi.org/10.1016/0005-2736(94)00262-n

3. Ковалевська, І. В. Визначення фізико-хімічних характеристик кверцетину / І. В. Ковалевська // Акт. питання фарм. і мед. практики. – 2014. – № 1. – C. 9–11.

4. Kovalevska, I. Development of the methodological approach of obtaining preparations based on solid dispersions / I. Kovalevska, O. Ruban // ScienceRise: Pharm. Sci. – 2018. – № 4 (14). – P. 4–8. https://doi.org/10.15587/2519-4852.2018.140756

5. Study of physical and chemical properties of solid dispersions of quercetin / I. V. Kovalevska, E. A. Ruban, S. A. Kutsenko et al. // Asian J. of Pharmaceutics. – 2017. – Vol. 11 (4). – P. 805–809. https://doi.org/10.22377/ajp.v11i04.1719

6. Державна фармакопея України : в 3-х т. / Державне підприємство «Український науковий фармакопейний центр якості лікарських засобів». – 2-е вид. – Х. : Державне підприємство «Український науковий фармакопейний центр якості лікарських засобів», 2015. – Т. 1. – 1128 с

7. Биофармацевтическая классификация жизненно необходимых и важнейших лекарственных средств / Г. В. Раменская, А. Ю. Савченко, И. Е. Шохин и др. // Фармация. – 2011. – № 5. – C. 3–11.

8. Раменская, Г. В. Классификации лекарственных веществ по их биофармацевтическим свойствам – БКС и BDDCS / Г. В. Раменская, И. Е. Шохин, Ю. И. Кулинич // Вестн. ВГУ, серия: химия. биология. Фармация. – 2012. – № 1. – C. 213–215.




Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 International License.

Abbreviated key title: Ukr. bìofarm. ž.

ISSN 2519-8750 (Online), ISSN 2311-715X (Print)