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Amorphous Solid Dispersion of Meloxicam Enhanced Oral Absorption in Rats With Impaired Gastric Motility  Hiroki Suzuki, Keisuke Yakushiji, Saori Matsunaga,

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Presentation on theme: "Amorphous Solid Dispersion of Meloxicam Enhanced Oral Absorption in Rats With Impaired Gastric Motility  Hiroki Suzuki, Keisuke Yakushiji, Saori Matsunaga,"— Presentation transcript:

1 Amorphous Solid Dispersion of Meloxicam Enhanced Oral Absorption in Rats With Impaired Gastric Motility  Hiroki Suzuki, Keisuke Yakushiji, Saori Matsunaga, Yukinori Yamauchi, Yoshiki Seto, Hideyuki Sato, Satomi Onoue  Journal of Pharmaceutical Sciences  Volume 107, Issue 1, Pages (January 2018) DOI: /j.xphs Copyright © 2018 American Pharmacists Association® Terms and Conditions

2 Figure 1 Chemical structure of meloxicam.
Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

3 Figure 2 Micrographs of (i) crystalline MEL, (ii) ASD-MEL/HPMC, and (iii) ASD-MEL/EUD. (a) SEM and (b) PLM images of MEL samples. White and black bars represent 25 and 50 μm, respectively. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

4 Figure 3 XRPD analysis of MEL samples including (i) crystalline MEL, (ii) physical mixture (MEL and HPMC), (iii) ASD-MEL/HPMC, and (iv) ASD-MEL/EUD. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

5 Figure 4 Photochemical characterizations of MEL samples. (a) Generation of singlet oxygen (open column) and superoxide (filled column) from MEL, naproxen (positive control), and sulisobenzone (negative control) under exposure to simulated sunlight (250 W/m2) for 1 h. (b) Photodegradation of MEL samples, including crystalline MEL, MEL solution, and ASD-MEL samples with HPMC (ASD-MEL/HPMC) and EUD (ASD-MEL/EUD). Each sample was exposed to UV/VIS (750 W/m2) for 1 h, and the purity (% of remaining) was determined by UPLC-ESI/MS. Data represent mean ± SD of 3 experiments. #p <0.01 with respect to crystalline MEL. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

6 Figure 5 Dissolution profiles of MEL samples in acidic solution (pH 1.2). ■, Crystalline MEL; ●, ASD-MEL/HPMC; and △, ASD-MEL/EUD. Degrees of supersaturation were expressed as the measured concentration of dissolved MEL (C) versus equilibrium solubility of MEL (Ceq). Data represent mean ± SE of 3 experiments. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

7 Figure 6 Plasma MEL concentration-time profiles in (a) normal and (b) PPT-pretreated rats after oral administration of MEL samples. ■, Crystalline MEL; ●, ASD-MEL/HPMC; and △, ASD-MEL/EUD. Data represent mean ± SE of 4-6 experiments. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

8 Figure 7 Baseline-corrected and normalized IR spectra of samples after Kubelka-Munk conversion, including (i) HPMC, (ii) ASD-MEL/EUD, (iii) crystalline MEL, (iv) ASD-MEL/EUD, and (v) EUD. Journal of Pharmaceutical Sciences  , DOI: ( /j.xphs ) Copyright © 2018 American Pharmacists Association® Terms and Conditions

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