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Improvement of dissolution and tabletability of carbamazepine solid dispersions with high drug loading prepared by hot-melt extrusion.
Pharmazie. 2019 09 01; 74(9):523-528.P

Abstract

Solid dispersions (SDs) have made great progress in the improvement of dissolution for poorly soluble drugs, however the low drug loading still limits their wide application. In the present paper, high carbamazepine (CBZ) loaded SDs with excellent dissolution and tabletability were prepared and characterized. The CBZ SDs were prepared with Eudragit EPO as carrier by hot-melt extrusion (HME) in the drug: carrier ratio of 4:1. Powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy and powder dissolution was carried out to characterize the SDs. The results showed that the crystalline form the polymorph of CBZ in SDs was transformed into form I from form III after extruded at 140 °C. Wettability and microstructure of CBZ SDs were improved by the HME process, which promoted the dissolution significantly. More than 85 % drug dissolved within 5 min from CBZ SDs with even only 20 % Eudragit EPO as carrier. CBZ SDs tablets were prepared by direct tableting with a universal material testing machine at various compaction pressures. Compactibility and tabletability were enhanced significantly by the HME process. All of these results showed the CBZ SDs prepared by HME with 80 % CBZ and 20 % Eudragit EPO could improve the dissolution and tabletability significantly.

Authors

No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31484591

Citation

Feng, Zilin, et al. "Improvement of Dissolution and Tabletability of Carbamazepine Solid Dispersions With High Drug Loading Prepared By Hot-melt Extrusion." Die Pharmazie, vol. 74, no. 9, 2019, pp. 523-528.
Feng Z, Li M, Wang W. Improvement of dissolution and tabletability of carbamazepine solid dispersions with high drug loading prepared by hot-melt extrusion. Pharmazie. 2019;74(9):523-528.
Feng, Z., Li, M., & Wang, W. (2019). Improvement of dissolution and tabletability of carbamazepine solid dispersions with high drug loading prepared by hot-melt extrusion. Die Pharmazie, 74(9), 523-528. https://doi.org/10.1691/ph.2019.9008
Feng Z, Li M, Wang W. Improvement of Dissolution and Tabletability of Carbamazepine Solid Dispersions With High Drug Loading Prepared By Hot-melt Extrusion. Pharmazie. 2019 09 1;74(9):523-528. PubMed PMID: 31484591.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improvement of dissolution and tabletability of carbamazepine solid dispersions with high drug loading prepared by hot-melt extrusion. AU - Feng,Zilin, AU - Li,Mengting, AU - Wang,Wenxi, PY - 2019/9/6/entrez PY - 2019/9/6/pubmed PY - 2020/7/15/medline SP - 523 EP - 528 JF - Die Pharmazie JO - Pharmazie VL - 74 IS - 9 N2 - Solid dispersions (SDs) have made great progress in the improvement of dissolution for poorly soluble drugs, however the low drug loading still limits their wide application. In the present paper, high carbamazepine (CBZ) loaded SDs with excellent dissolution and tabletability were prepared and characterized. The CBZ SDs were prepared with Eudragit EPO as carrier by hot-melt extrusion (HME) in the drug: carrier ratio of 4:1. Powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy and powder dissolution was carried out to characterize the SDs. The results showed that the crystalline form the polymorph of CBZ in SDs was transformed into form I from form III after extruded at 140 °C. Wettability and microstructure of CBZ SDs were improved by the HME process, which promoted the dissolution significantly. More than 85 % drug dissolved within 5 min from CBZ SDs with even only 20 % Eudragit EPO as carrier. CBZ SDs tablets were prepared by direct tableting with a universal material testing machine at various compaction pressures. Compactibility and tabletability were enhanced significantly by the HME process. All of these results showed the CBZ SDs prepared by HME with 80 % CBZ and 20 % Eudragit EPO could improve the dissolution and tabletability significantly. SN - 0031-7144 UR - https://www.unboundmedicine.com/medline/citation/31484591/Improvement_of_dissolution_and_tabletability_of_carbamazepine_solid_dispersions_with_high_drug_loading_prepared_by_hot_melt_extrusion_ L2 - https://www.ingentaconnect.com/openurl?genre=article&issn=0031-7144&volume=74&issue=9&spage=523&aulast=Feng DB - PRIME DP - Unbound Medicine ER -