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Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.33 no.6, 2010년, pp.901 - 910   SCIE 피인용횟수: 1
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Physicochemical Characterization of Artemether Solid Dispersions with Hydrophilic Carriers by Freeze Dried and Melt Methods

Ansari, Muhammad Tayyab    (Department of Pharmacy, Bahauddin Zakariya University   ); Karim, Shahid    (Department of Pharmacy, Bahauddin Zakariya University   ); Ranjha, Nazar Muhammad    (Department of Pharmacy, Bahauddin Zakariya University   ); Shah, Nisar Hussain    (Department of Pharmacy, Bahauddin Zakariya University   ); Muhammad, Sher    (Department of Pharmacy, University of Sargodha  );
  • 초록

    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.


  • 주제어

    Artemether .   Solid dispersions .   Polyvinylpyrrolidone .   Polyethyleneglycol .   Differential scanning calorimetery .   Dissolution rate.  

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  • 이 논문을 인용한 문헌 (1)

    1. 2011. "" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, 34(5): 757~765     

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