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Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method.
Pharm Dev Technol. 2018 Dec; 23(10):1007-1015.PD

Abstract

The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SDs) of artemether were prepared using artemether and polyethylene glycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESDs) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESDs were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3). Each of these preparations was formulated using physical mixing and the solvent evaporation method. Aqueous solubility of artemether improved 11-, 95- and 102-fold, while dissolution (in simulated gastric fluid) increased 3-, 13- and 14-fold, for formulation groups 1, 2 and 3, respectively. X-ray diffraction patterns of SDs indicated a decrease in peak intensities at 10° implying reduced artemether crystallinity. Scanning electron micrographs invariably revealed embedment of artemether by various excipients and a glassy appearance for solvent evaporated mixtures for all three formulation Groups. Our findings indicate improved hydrophilic interactions for drug particles yield greater solubility and dissolution in the following order for artemether formulating methods: solvent evaporation mixtures > physical mixtures > pure artemether.

Authors+Show Affiliations

a Department of Pharmacy , Bahauddin Zakariya University , Multan , Pakistan.a Department of Pharmacy , Bahauddin Zakariya University , Multan , Pakistan.a Department of Pharmacy , Bahauddin Zakariya University , Multan , Pakistan.b De Montfort University , Leicester , UK.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27885872

Citation

Tayyab Ansari, Muhammad, et al. "Improvement of Solubility, Dissolution and Stability Profile of Artemether Solid Dispersions and Self Emulsified Solid Dispersions By Solvent Evaporation Method." Pharmaceutical Development and Technology, vol. 23, no. 10, 2018, pp. 1007-1015.
Tayyab Ansari M, Arshad MS, Hussain A, et al. Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method. Pharm Dev Technol. 2018;23(10):1007-1015.
Tayyab Ansari, M., Arshad, M. S., Hussain, A., & Ahmad, Z. (2018). Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method. Pharmaceutical Development and Technology, 23(10), 1007-1015. https://doi.org/10.1080/10837450.2016.1265554
Tayyab Ansari M, et al. Improvement of Solubility, Dissolution and Stability Profile of Artemether Solid Dispersions and Self Emulsified Solid Dispersions By Solvent Evaporation Method. Pharm Dev Technol. 2018;23(10):1007-1015. PubMed PMID: 27885872.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method. AU - Tayyab Ansari,Muhammad, AU - Arshad,Muhammad Sohail, AU - Hussain,Altaf, AU - Ahmad,Zeeshan, Y1 - 2016/12/08/ PY - 2016/11/26/pubmed PY - 2019/1/10/medline PY - 2016/11/26/entrez KW - Artemether KW - dissolution KW - self-emulsified solid dispersions KW - solid dispersions KW - solubility KW - stability SP - 1007 EP - 1015 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 23 IS - 10 N2 - The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SDs) of artemether were prepared using artemether and polyethylene glycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESDs) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESDs were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3). Each of these preparations was formulated using physical mixing and the solvent evaporation method. Aqueous solubility of artemether improved 11-, 95- and 102-fold, while dissolution (in simulated gastric fluid) increased 3-, 13- and 14-fold, for formulation groups 1, 2 and 3, respectively. X-ray diffraction patterns of SDs indicated a decrease in peak intensities at 10° implying reduced artemether crystallinity. Scanning electron micrographs invariably revealed embedment of artemether by various excipients and a glassy appearance for solvent evaporated mixtures for all three formulation Groups. Our findings indicate improved hydrophilic interactions for drug particles yield greater solubility and dissolution in the following order for artemether formulating methods: solvent evaporation mixtures > physical mixtures > pure artemether. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/27885872/Improvement_of_solubility_dissolution_and_stability_profile_of_artemether_solid_dispersions_and_self_emulsified_solid_dispersions_by_solvent_evaporation_method_ L2 - https://www.tandfonline.com/doi/full/10.1080/10837450.2016.1265554 DB - PRIME DP - Unbound Medicine ER -