Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions
Само за регистроване кориснике
2019
Аутори
Đuriš, JelenaMilovanović, Stoja
Medarević, Đorđe
Dobričić, Vladimir
Dapčević, Aleksandra
Ibrić, Svetlana
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Solid dispersions production is one of the substantial approaches for improvement of poor drug solubility. Additionally, supercritical fluid assisted method for preparation of solid dispersions can offer many advantages in comparison to the conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance for selection of the most appropriate polymeric carrier for dispersion of the drug of interest. In addition to the increased drug release rate, solid dispersions should have proper mechanical attributes in order to be successfully formulated in the final solid dosage form such as tablet. Therefore, several pharmaceutical grade polymers have been selected for development of BCS Class II drug carvedilol (CARV) solid dispersions. They were compared based on behavior in supercritical CO2 and affinity towards CARV calculated from the miscibility analysis. By utilization of the supercritical CO2 assisted method, solid dispersions of CARV with the selected ...(co) polymers (polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus (R) and Eudragit (R)) were obtained. Properties of the prepared CARV-polymer dispersions were observed by the polarizing and scanning electron microscopy and analyzed by differential scanning calorimetry and Fourier transform infrared spectroscopy. CARV was additionally characterized by X-ray powder diffraction. Furthermore, in vitro dissolution studies and dynamic compaction analysis were performed on the selected samples of solid dispersions. Among the studied polymers, PVP and HPMC have been identified as polymers with the highest affinity towards CARV, based on the calculated delta(p) values. This has been also confirmed with the highest dissolution efficiency of CARV-PVP and CARV-HPMC solid dispersions. Solid state characterization indicated that CARV was dispersed either molecularly, or in the amorphous form, depending on interactions with each polymer. Determination of CARV-PVP and CARV-HPMC mechanical properties revealed that CARV-PVP solid dispersion has superior compactibility and tabletability. Therefore, CARV-PVP solid dispersion has been highlighted as the most appropriate for the further development of tablets as the final dosage form. Presented study provides an example for efficient approach for development of poorly soluble drug solid dispersion with satisfactory tableting properties.
Кључне речи:
Carvedilol / Supercritical CO2 / Solid dispersion / Improved dissolution / TabletabilityИзвор:
International Journal of Pharmaceutics, 2019, 554, 190-200Издавач:
- Elsevier Science Bv, Amsterdam
Финансирање / пројекти:
- Развој производа и технологија које обезбеђују жељено ослобађање лековитих супстанци из чврстих фармацеутских облика (RS-MESTD-Technological Development (TD or TR)-34007)
- Функционални физиолошки активни биљни материјали са додатом вредношћу за примену у фармацеутској и прехрамбеној индустрији (RS-MESTD-Integrated and Interdisciplinary Research (IIR or III)-45017)
- 0-3D наноструктуре за примену у електроници и обновљивим изворима енергије: синтеза, карактеризација и процесирање (RS-MESTD-Integrated and Interdisciplinary Research (IIR or III)-45007)
Напомена:
- Peer-reviewed manuscript: http://technorep.tmf.bg.ac.rs/handle/123456789/5030
Повезане информације:
- Верзија документа
http://technorep.tmf.bg.ac.rs/handle/123456789/5030
DOI: 10.1016/j.ijpharm.2018.11.015
ISSN: 0378-5173
PubMed: 30414899
WoS: 000454421400019
Scopus: 2-s2.0-85056454143
Институција/група
Tehnološko-metalurški fakultetTY - JOUR AU - Đuriš, Jelena AU - Milovanović, Stoja AU - Medarević, Đorđe AU - Dobričić, Vladimir AU - Dapčević, Aleksandra AU - Ibrić, Svetlana PY - 2019 UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/4335 AB - Solid dispersions production is one of the substantial approaches for improvement of poor drug solubility. Additionally, supercritical fluid assisted method for preparation of solid dispersions can offer many advantages in comparison to the conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance for selection of the most appropriate polymeric carrier for dispersion of the drug of interest. In addition to the increased drug release rate, solid dispersions should have proper mechanical attributes in order to be successfully formulated in the final solid dosage form such as tablet. Therefore, several pharmaceutical grade polymers have been selected for development of BCS Class II drug carvedilol (CARV) solid dispersions. They were compared based on behavior in supercritical CO2 and affinity towards CARV calculated from the miscibility analysis. By utilization of the supercritical CO2 assisted method, solid dispersions of CARV with the selected (co) polymers (polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus (R) and Eudragit (R)) were obtained. Properties of the prepared CARV-polymer dispersions were observed by the polarizing and scanning electron microscopy and analyzed by differential scanning calorimetry and Fourier transform infrared spectroscopy. CARV was additionally characterized by X-ray powder diffraction. Furthermore, in vitro dissolution studies and dynamic compaction analysis were performed on the selected samples of solid dispersions. Among the studied polymers, PVP and HPMC have been identified as polymers with the highest affinity towards CARV, based on the calculated delta(p) values. This has been also confirmed with the highest dissolution efficiency of CARV-PVP and CARV-HPMC solid dispersions. Solid state characterization indicated that CARV was dispersed either molecularly, or in the amorphous form, depending on interactions with each polymer. Determination of CARV-PVP and CARV-HPMC mechanical properties revealed that CARV-PVP solid dispersion has superior compactibility and tabletability. Therefore, CARV-PVP solid dispersion has been highlighted as the most appropriate for the further development of tablets as the final dosage form. Presented study provides an example for efficient approach for development of poorly soluble drug solid dispersion with satisfactory tableting properties. PB - Elsevier Science Bv, Amsterdam T2 - International Journal of Pharmaceutics T1 - Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions EP - 200 SP - 190 VL - 554 DO - 10.1016/j.ijpharm.2018.11.015 ER -
@article{ author = "Đuriš, Jelena and Milovanović, Stoja and Medarević, Đorđe and Dobričić, Vladimir and Dapčević, Aleksandra and Ibrić, Svetlana", year = "2019", abstract = "Solid dispersions production is one of the substantial approaches for improvement of poor drug solubility. Additionally, supercritical fluid assisted method for preparation of solid dispersions can offer many advantages in comparison to the conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance for selection of the most appropriate polymeric carrier for dispersion of the drug of interest. In addition to the increased drug release rate, solid dispersions should have proper mechanical attributes in order to be successfully formulated in the final solid dosage form such as tablet. Therefore, several pharmaceutical grade polymers have been selected for development of BCS Class II drug carvedilol (CARV) solid dispersions. They were compared based on behavior in supercritical CO2 and affinity towards CARV calculated from the miscibility analysis. By utilization of the supercritical CO2 assisted method, solid dispersions of CARV with the selected (co) polymers (polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus (R) and Eudragit (R)) were obtained. Properties of the prepared CARV-polymer dispersions were observed by the polarizing and scanning electron microscopy and analyzed by differential scanning calorimetry and Fourier transform infrared spectroscopy. CARV was additionally characterized by X-ray powder diffraction. Furthermore, in vitro dissolution studies and dynamic compaction analysis were performed on the selected samples of solid dispersions. Among the studied polymers, PVP and HPMC have been identified as polymers with the highest affinity towards CARV, based on the calculated delta(p) values. This has been also confirmed with the highest dissolution efficiency of CARV-PVP and CARV-HPMC solid dispersions. Solid state characterization indicated that CARV was dispersed either molecularly, or in the amorphous form, depending on interactions with each polymer. Determination of CARV-PVP and CARV-HPMC mechanical properties revealed that CARV-PVP solid dispersion has superior compactibility and tabletability. Therefore, CARV-PVP solid dispersion has been highlighted as the most appropriate for the further development of tablets as the final dosage form. Presented study provides an example for efficient approach for development of poorly soluble drug solid dispersion with satisfactory tableting properties.", publisher = "Elsevier Science Bv, Amsterdam", journal = "International Journal of Pharmaceutics", title = "Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions", pages = "200-190", volume = "554", doi = "10.1016/j.ijpharm.2018.11.015" }
Đuriš, J., Milovanović, S., Medarević, Đ., Dobričić, V., Dapčević, A.,& Ibrić, S.. (2019). Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions. in International Journal of Pharmaceutics Elsevier Science Bv, Amsterdam., 554, 190-200. https://doi.org/10.1016/j.ijpharm.2018.11.015
Đuriš J, Milovanović S, Medarević Đ, Dobričić V, Dapčević A, Ibrić S. Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions. in International Journal of Pharmaceutics. 2019;554:190-200. doi:10.1016/j.ijpharm.2018.11.015 .
Đuriš, Jelena, Milovanović, Stoja, Medarević, Đorđe, Dobričić, Vladimir, Dapčević, Aleksandra, Ibrić, Svetlana, "Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions" in International Journal of Pharmaceutics, 554 (2019):190-200, https://doi.org/10.1016/j.ijpharm.2018.11.015 . .