Influence of solid dispersions on the solubility of tamsulosin hydrochloride
- Авторлар: Stantsov M.I.1, Krasnyuk I.I.1, Krasnyuk I.I.1, Belyatskaya A.V.1, Stepanova O.I.1, Grikh V.V.1, Bakhrushina E.O.1, Bokov D.O.1
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Мекемелер:
- Sechenov First Moscow State Medical University (Sechenov University)
- Шығарылым: Том 74, № 2 (2025)
- Беттер: 38-45
- Бөлім: Technology of medicines
- URL: https://journal-vniispk.ru/0367-3014/article/view/290960
- DOI: https://doi.org/10.29296/25419218-2025-02-05
- ID: 290960
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Аннотация
Introduction. The solubility rate is a critical aspect of the physicochemical parameters of a pharmaceutical substance that determines the bioavailability profile during the development of a drug formulation. Limited solubility slows down the absorption process and release rates, resulting in insufficient active concentration for a pronounced clinical effect. An innovative solution to improve the pharmacokinetic parameters and therapeutic profile of a substance is the method of "solid dispersions." Solid dispersions of tamsulosin with hydrophilic polymers are a promising direction in the development of new drug formulations with improved characteristics.
Objective. To investigate the effect of solid dispersions prepared with polyethylene glycol-1500 (PEG) on the solubility of tamsulosin hydrochloride in aqueous media.
Material and methods. The object of the study was tamsulosin hydrochloride. Polyethylene glycol-1500 (PEG-1500) was used as the matrix polymer. Solid dispersions of tamsulosin were prepared by the solvent evaporation method.
Results. The developed solid dispersions with tamsulosin increase the solubility and dissolution rate of tamsulosin hydrochloride in water. They enhance the solubility of tamsulosin from PEG-1500-based solid dispersion by 2.92 times compared to the original substance. A comprehensive analysis using various physicochemical methods–UV-spectrophotometry, crystal structure analysis, and optical properties analysis of the Faraday–Kendall effect in the developed solutions-reveals that the increased solubility of tamsulosin from solid dispersions can be attributed to the loss of crystalline structure and the formation of a "solid solution" with the polymer matrix. Upon dissolving the solid dispersion in water, a stable colloidal solution is formed.
Conclusion. The solid dispersions obtained with the hydrophilic polymer PEG-1500 facilitate enhanced dissolution of tamsulosin in water. It is planned to utilize these results for developing fast-dissolving drug forms and enteric-coated capsules of tamsulosin with increased bioavailability and controlled release.
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##article.viewOnOriginalSite##Авторлар туралы
Maxim Stantsov
Sechenov First Moscow State Medical University (Sechenov University)
Хат алмасуға жауапты Автор.
Email: stantsov_m_i@staff.sechenov.ru
ORCID iD: 0000-0002-6686-8166
SPIN-код: 2916-9833
assistant professor at the Department of Analytical, Physical, and Colloid Chemistry of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Ivan Krasnyuk
Sechenov First Moscow State Medical University (Sechenov University)
Email: krasnyuk.79@mail.ru
ORCID iD: 0000-0001-8557-8829
SPIN-код: 1746-8595
ScD in pharmaceutical sciences, professor, professor at the Department of Analytical, Physical, and Colloid Chemistry of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Ivan Krasnyuk
Sechenov First Moscow State Medical University (Sechenov University)
Email: krasnyuki@mail.ru
ORCID iD: 0000-0002-7242-2988
SPIN-код: 9865-8758
ScD in pharmaceutical sciences, professor, professor at the Department of Pharmaceutical Technology of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Anastasia Belyatskaya
Sechenov First Moscow State Medical University (Sechenov University)
Email: av.beliatskaya@mail.ru
ORCID iD: 0000-0002-8214-4483
SPIN-код: 2477-4321
PhD in pharmaceutical sciences, associate professor at the Department of Pharmaceutical Technology of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Olga Stepanova
Sechenov First Moscow State Medical University (Sechenov University)
Email: o.i.nikulina@mail.ru
ORCID iD: 0000-0002-9885-3727
SPIN-код: 1645-9092
PhD in pharmaceutical sciences, associate professor at the Department of Pharmacology of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Victoria Grikh
Sechenov First Moscow State Medical University (Sechenov University)
Email: grikh_v_v_1@staff.sechenov.ru
ORCID iD: 0000-0003-1614-1070
SPIN-код: 8479-0344
PhD in pharmaceutical sciences, associate professor at the Department of Analytical, Physical, and Colloid Chemistry of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Elena Bakhrushina
Sechenov First Moscow State Medical University (Sechenov University)
Email: bakhrushina_e_o@staff.sechenov.ru
ORCID iD: 0000-0001-8695-0346
SPIN-код: 9537-1297
ScD in pharmaceutical sciences, associate professor at the Department of Pharmaceutical Technology of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Dmitry Bokov
Sechenov First Moscow State Medical University (Sechenov University)
Email: bokov_d_o@staff.sechenov.ru
ORCID iD: 0000-0003-2968-2466
SPIN-код: 7523-5909
PhD in pharmaceutical sciences, associate professor at the Department of Analytical, Physical, and Colloid Chemistry of Nelyubin Institute of Pharmacy
Ресей, Trubetskaya str., 8/2, Mosсow, 119991Әдебиет тізімі
- Zhang H.L., Huang Z.G., Qiu Y., Cheng X., Zou X.Q., Liu T.T. Tamsulosin for treatment of lower urinary tract symptoms in women: a systematic review and meta-analysis. Int J. Impot Res. 2017; 29 (4): 148–56. doi: 10.1038/ijir.2017.12.
- Ban M.S., Kim Y.K., Kim B., Jung J., Kim Y.I., Oh J., Yu K.S. Evaluation of the pharmacokinetics and food effects of a novel formulation tamsulosin 0.4 mg capsule compared with a 0.2 mg capsule in healthy male volunteers. Transl Clin Pharmacol. 2020; 28 (4): 181–8. doi: 10.12793/tcp.2020.28.e17.
- Beliatskaya A.V., Elagina A.O., Krasnyuk I.I. (Jr.), Krasnyuk I.I., Stepanova O.I., Kashlikova I.M., Vorob’yev A.N., Iskenderova S.G., Kuzmenko A.N., Kannieva D.R. Study of the solubility of furazolidone from solid dispersions with polyvinylpyrrolidone. Moscow university chemistry bulletin. 2020; 75 (1): 43–6. doi: 10.3103/S0027131420010046.
- Krasnyuk I.I., Stepanova O.I., Beliatskaya A.V., Kuzmenko A.N., Kasimovskaya N.A., Lucenko S.V., Matyushin A.A., Vorob’yev A.N., Mazyarkin E.V., Nesterenko E.P. Influence of polymers on the physicochemical properties of benzonal in solid dispersions Moscow university chemistry bulletin. 2020; 75 (6): 388–90. doi: 10.3103/S0027131420060127.
- Kosenkova S.I., Belyatskaya A.V., Krasnyuk I.I., Stepanova O.I., Mazyarkin E.V., Li Tianlong., Korochkina T.V., Novikov V.V., Fateeva T.V. Antimycotic activity of naftifine hydrochloride solution in combination with polyethylene glycols. Pharmaceutical chemistry J. 2020; 54 (3): 310–1. doi: 10.1007/s11094-020-02196-w.
- Belyatskaya A.V., Krasnyuk I.I., Kashlikova I.M., Krasnyuk I.I. (Jr.), Vorob’ev A.N., Stepanova O.I. Development of compositions and production technology for gels with a solid dispersal of nitrofural. Pharmaceutical chemistry J. 2020; 53 (10): 981–5. doi: 10.1007/s11094-020-02109-x.
- Krasnyuk I.I. (Jr.), Stepanova O.I., Ovsyannikova L.V., Belyatskaya A.V., Grikh V.V., Krasnyuk I.I., Kosheleva T.M., Skovpen Y.V., Kozin D.A. Development of dosage forms containing solid dispersion of diclofenac Pharmaceutical chemistry J. 2018; 52 (4): 357–60. doi: 10.1007/s11094-018-1821-6.
- Krasnyuk I.I. (Jr), Krasnyuk I.I., Beliatskaya A.V., Stepanova O.I., Valeeva A.M., Korol L.A., Grikh V.V., Kosheleva T.M., Ovsyannikova L.V. Effect of solid dispersions on the dissolution of ampicillin. BioNanoScience. 2017; 7 (2): 340–4. doi: 10.1007/s12668-016-0342-6.
- Krasnyuk I.I. (Jr.), Belyatskaya A.V., Kosheleva T.M., Krasnyuk I.I., Skovpen Y.V., Stepanova O.I., Ovsyannikova L.V., Grikh V.V. Effect of solid dispersions with polyethylene glycol 1500 on the solubility of indomethacin. Pharmaceutical chemistry J. 2018; 52 (3): 241–4. doi: 10.1007/s11094-018-1799-0.
- Siepmann J. Clas S.D., Faham A., Boydd B.J., Bernkop-Schnürchf A., Jannine V., Zhaog H., Evansh J.C., Lecommandouxg S., Allenh C., Costabilei G., Merkeli O.M., Alexanderj M.R., Robertsj C.J., Wildmank R.D., Leroux J.C. Lipids and polymers in pharmaceutical technology: lifelong companions. International journal of pharmaceutics. 2019; 558: 128–42. doi: 10.1016/j.ijpharm.2018.12.080.
- Younis M.A. Solid dispersion technology, a contemporary overview on a well established technique. Universal J. of pharmaceutical research. 2017; 2 (3): 15–9. doi: 10.22270/ujpr.v2i3.RW1
- Huang Y., Dai W.G. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Actapharmaceuticasinica B. 2013; 4 (1): 18–25. doi: 10.1016/j.apsb.2013.11.001.
- Teodorescu M., Morariu S., Bercea M. Biomaterials of PVA and PVP in medical and pharmaceutical applications: Perspectives and challenges. Biotechnology advances. 2018; 37 (1): 109–31. doi: 10.1016/j.biotechadv.2018.11.008.
- Krasnyuk I.I. (Jr.), Krasnyuk I.I., Beliatskaya A.V., Stepanova O.I., Lucenko S.V., Kuzmenko A.N., Kasimovskaya N.A., Mazyarkin E.V., Matyushin A.A., Nesterenko E., Vorob`yov A.N. Influence of polymers on the physicochemical properties of benzonal in solid dispersions. Moscow university chemistry bulletin. 2021; 75 (6): 388–90. doi: 10.3103/S0027131420060127
- Beliatskaya A.V., Krasnyuk I.I. (Jr.), Krasnyuk I.I., Elagina A.O., Kashlikova I.M., Vorob’yov A.N., Stepanova O.I., Kuzmenko A.N., Kannievaa D.R., Iskenderova S.G. Study of the solubility of furazolidone from solid dispersions with polyvinylpyrrolidone. Moscow university chemistry bulletin. 2020; 75 (1): 43–6. doi: 10.3103/S0027131420010046.
- Silaeva Yu., Slivkin A.I., Belenova A.S., Chupandina E.E., Krasnyuk I.I. (Jr.), Naryshkin S.R., Krasnyuk I.I. Use of solid dispersion systems in pharmacy. Condensed matter and interphases. 2020; 22 (2): 173–81. doi: 10.17308/kcmf.2020.22/2820.
- Chen X., Partheniadis I., Al-Obaidi H., Nikolakakis I. Solubility improvement of progesterone from solid dispersions prepared by solvent evaporation and co-milling. Polymers. 2020; 12 (4): 854. doi: 10.3390/polym12040854.
- Hou H.H., Pandya K.M., Rajesh A., Lubach J.W., Yost E., Muliadi A., Jia W., Nagapudi K. Impact of method of preparation of amorphous solid dispersions on mechanical properties: comparison of coprecipitation and spray drying. J. of pharmaceutical sciences. 2019; 108 (2): 870–9. doi: 10.1016/j.xphs.2018.09.008.
- Parker A.S., Stewart A.A., Gilpin C.J., Taylor L.S., Beaudoin S.P. Dissolution of indomethacin crystals into a polymer melt: role of diffusion and fragmentation. Crystal growth and design. 2019; 19 (6): 3315–28. DOI: 0000-0001-6986-8252.
- Luebbert C., Sadowski G., Klanke C. Investigating phase separation in amorphous solid dispersions via raman mapping. International J. of pharmaceutics. 2018; 535 (1–2): 245–52. doi: 10.1016/j.ijpharm.2017.11.014.
- Okada K., Hayashi Y., Hirai D., Shungo Kumada, Yoshinori Onuki, Atsushi Kosugi A novel approach to evaluate amorphous-to-crystalline transformation of active pharmaceutical ingredients in solid dispersion using time-domain NMR. Chem pharm bull (Tokyo). 2019; 67 (3): 265–70. doi: 10.1248/cpb.c18-00887.
- Singh A., Van den Mooter G. Spray drying formulation of amorphous solid dispersions. Advanced drug delivery reviews. 2016; 100: 27–50. doi: 10.1016/j.addr.2015.12.010.
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