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Physicochemical characterization of artemether solid dispersions with hydrophilic carriers by freeze dried and melt methods.
Arch Pharm Res. 2010 Jun; 33(6):901-10.AP

Abstract

Solid dispersions of artemether (ARM), a poorly soluble drug, were prepared using polyvinylpyrrolidone (PVPK25, MW 25000) and polyethyleneglycol (PEG4000, MW 4000) as excipients. These dispersions were studied by physical mixture, freeze-drying, and melting methods. They were characterized by X-ray diffraction pattern, fourier transform infrared spectrophotometry, differential scanning calorimetery, and dissolution studies. X-ray diffraction pattern revealed the complete crystalline nature of artemether, whereas physical mixtures, melt mixtures (MM), and freeze-dried solid dispersions (FDSD) of ARM-PVP and ARM-PEG showed reduced peak intensities with increased PVP/PEG content. PEG showed lower decreases in intensity than PVP preparations. Differential scanning calorimetery also confirmed this finding by showing either a small or absent endotherm. Red shifts in O-H stretching vibrations of ARM were higher in the MM of ARM-PVP than its FDSD as exhibited by fourier transform infrared spectrophotometry. The carbonyl peak of PEG was blue shifted in MM and FDSD, whereas the C=O peak of PVP was red shifted in FDSD and MM, indicating different H-bonding by PEG and PVP with ARM. The rate of dissolution (phosphate buffer at pH 4.5) was improved up to 4-fold in MM and FDSD compared to artemether, and up to 50% compared to physical mixtures. The preparation of solid dispersions influenced the rate of dissolution at various drug-carrier ratios, i.e., the dissolution order of 1:1-1:4 ratio was MM > FDSD; FDSD > MM at 1:6-1:8 ratios of both ARM-PVP and ARM-PEG; and FDSD of ARM-PEG > FDSD of ARM-PVP > MM of ARM-PEG > MM of ARM-PVP at a 1:10 ratio.

Authors+Show Affiliations

Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan. Ansari.Muhammad@gmail.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20607495

Citation

Ansari, Muhammad Tayyab, et al. "Physicochemical Characterization of Artemether Solid Dispersions With Hydrophilic Carriers By Freeze Dried and Melt Methods." Archives of Pharmacal Research, vol. 33, no. 6, 2010, pp. 901-10.
Ansari MT, Karim S, Ranjha NM, et al. Physicochemical characterization of artemether solid dispersions with hydrophilic carriers by freeze dried and melt methods. Arch Pharm Res. 2010;33(6):901-10.
Ansari, M. T., Karim, S., Ranjha, N. M., Shah, N. H., & Muhammad, S. (2010). Physicochemical characterization of artemether solid dispersions with hydrophilic carriers by freeze dried and melt methods. Archives of Pharmacal Research, 33(6), 901-10. https://doi.org/10.1007/s12272-010-0613-7
Ansari MT, et al. Physicochemical Characterization of Artemether Solid Dispersions With Hydrophilic Carriers By Freeze Dried and Melt Methods. Arch Pharm Res. 2010;33(6):901-10. PubMed PMID: 20607495.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characterization of artemether solid dispersions with hydrophilic carriers by freeze dried and melt methods. AU - Ansari,Muhammad Tayyab, AU - Karim,Shahid, AU - Ranjha,Nazar Muhammad, AU - Shah,Nisar Hussain, AU - Muhammad,Sher, Y1 - 2010/07/06/ PY - 2009/10/12/received PY - 2010/02/16/accepted PY - 2010/02/08/revised PY - 2010/7/8/entrez PY - 2010/7/8/pubmed PY - 2010/11/17/medline SP - 901 EP - 10 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 33 IS - 6 N2 - Solid dispersions of artemether (ARM), a poorly soluble drug, were prepared using polyvinylpyrrolidone (PVPK25, MW 25000) and polyethyleneglycol (PEG4000, MW 4000) as excipients. These dispersions were studied by physical mixture, freeze-drying, and melting methods. They were characterized by X-ray diffraction pattern, fourier transform infrared spectrophotometry, differential scanning calorimetery, and dissolution studies. X-ray diffraction pattern revealed the complete crystalline nature of artemether, whereas physical mixtures, melt mixtures (MM), and freeze-dried solid dispersions (FDSD) of ARM-PVP and ARM-PEG showed reduced peak intensities with increased PVP/PEG content. PEG showed lower decreases in intensity than PVP preparations. Differential scanning calorimetery also confirmed this finding by showing either a small or absent endotherm. Red shifts in O-H stretching vibrations of ARM were higher in the MM of ARM-PVP than its FDSD as exhibited by fourier transform infrared spectrophotometry. The carbonyl peak of PEG was blue shifted in MM and FDSD, whereas the C=O peak of PVP was red shifted in FDSD and MM, indicating different H-bonding by PEG and PVP with ARM. The rate of dissolution (phosphate buffer at pH 4.5) was improved up to 4-fold in MM and FDSD compared to artemether, and up to 50% compared to physical mixtures. The preparation of solid dispersions influenced the rate of dissolution at various drug-carrier ratios, i.e., the dissolution order of 1:1-1:4 ratio was MM > FDSD; FDSD > MM at 1:6-1:8 ratios of both ARM-PVP and ARM-PEG; and FDSD of ARM-PEG > FDSD of ARM-PVP > MM of ARM-PEG > MM of ARM-PVP at a 1:10 ratio. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/20607495/Physicochemical_characterization_of_artemether_solid_dispersions_with_hydrophilic_carriers_by_freeze_dried_and_melt_methods_ L2 - https://dx.doi.org/10.1007/s12272-010-0613-7 DB - PRIME DP - Unbound Medicine ER -