Comparison of Dissolution Rates of Different Crystalline Phases of Fluprednisolone by In Vitro and In Vivo Methods

1971 ◽  
Vol 60 (10) ◽  
pp. 1488-1491 ◽  
Author(s):  
John K. Haleblian ◽  
Robert T. Koda ◽  
John A. Biles
Keyword(s):  
Dissolution Rates ◽  
Crystalline Phases

In vivo-in vitro correlations of salicylate saliva levels and continuous flow cell dissolution rates

1983 ◽  
Vol 15 (2) ◽  
pp. 167-175 ◽  
Author(s):  
Hartmut Derendorf ◽  
Gertrude Drehsen ◽  
Peter Rohdewald
Keyword(s):  
Continuous Flow ◽  
Flow Cell ◽  
Dissolution Rates

Liquid crystalline phases of monoolein and water for topical delivery of cyclosporin A: Characterization and study of in vitro and in vivo delivery

2006 ◽  
Vol 63 (2) ◽  
pp. 146-155 ◽  
Author(s):  
Luciana B. Lopes ◽  
João L.C. Lopes ◽  
Dionéia C.R. Oliveira ◽  
José A. Thomazini ◽  
M. Tereza J. Garcia ◽  
...  
Keyword(s):  
Cyclosporin A ◽  
Liquid Crystalline ◽  
Topical Delivery ◽  
Crystalline Phases ◽  
Liquid Crystalline Phases ◽  
In Vivo Delivery

scholarly journals Two Novel Palbociclib-Resorcinol and Palbociclib-Orcinol Cocrystals with Enhanced Solubility and Dissolution Rate

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 23
Author(s):  
Chenxin Duan ◽  
Wenwen Liu ◽  
Yunwen Tao ◽  
Feifei Liang ◽  
Yanming Chen ◽  
...  
Keyword(s):  
Water Solubility ◽  
Cancer Drug ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Intrinsic Dissolution ◽  
X Ray ◽  
Enhanced Solubility

Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly restricted due to poor bioavailability (resulting from extremely low water solubility) and serious adverse reactions. In this study, two cocrystals of PAL with resorcinol (RES) or orcinol (ORC) were prepared by evaporation crystallization to enhance their solubility. The cocrystals were characterized by single crystal X-ray diffraction, Hirshfeld surface analysis, powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared and scanning electron microscopy. The intrinsic dissolution rates of the PAL cocrystals were determined in three different dissolution media (pH 1.0, pH 4.5 and pH 6.8), and both cocrystals showed improved dissolution rates at pH 1.0 and pH 6.8 in comparison to the parent drug. In addition, the cocrystals increased the solubility of PAL at pH 6.8 by 2–3 times and showed good stabilities in both the accelerated stability testing and stress testing. The PAL-RES cocrystal also exhibited an improved relative bioavailability (1.24 times) than PAL in vivo pharmacokinetics in rats. Moreover, the in vitro cytotoxicity assay of PAL-RES showed an increased IC50 value for normal cells, suggesting a better biosafety profile than PAL. Co-crystallization may represent a promising strategy for improving the physicochemical properties of PAL with better pharmacokinetics.

Invite Article: The Liquid-Crystalline Phases of Double-Stranded Nucleic Acids in Vitro and in Vivo

1988 ◽  
Vol 3 (11) ◽  
pp. 1443-1459 ◽  
Author(s):  
Yu M. Yevdokimov ◽  
S. G. Skuridin ◽  
V. I. Salyanov
Keyword(s):  
Nucleic Acids ◽  
Liquid Crystalline ◽  
Crystalline Phases ◽  
Liquid Crystalline Phases

scholarly journals Evaluation of the Solid Dispersion System Engineered from Mesoporous Silica and Polymers for the Poorly Water Soluble Drug Indomethacin: In Vitro and In Vivo

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 144 ◽  
Author(s):  
Ziyue Xi ◽  
Wei Zhang ◽  
Yali Fei ◽  
Mingshu Cui ◽  
Luyao Xie ◽  
...  
Keyword(s):  
Mesoporous Silica ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Membrane Penetration ◽  
Artificial Membrane ◽  
Dissolution Rates

This work explored absorption efficacy via an in vivo imaging system and parallel artificial membrane penetration in indomethacin (IMC) solid dispersion (SD) systems. Two different polymer excipients—hydroxypropyl methylcellulose (HPMC) and Kollicoat IR as precipitation inhibitors (PIs)—combined with mesoporous silica nanoparticles (MSNs) as carriers were investigated. The IMC–SDs were prepared using the solvent evaporation method and characterized by solubility analysis, infrared (IR) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), and differential scanning calorimetry (DSC). It was confirmed that IMC successfully changed into an amorphous state after loading into the designed carriers. The in vitro release and stability experiments were conducted to examine the in vitro dissolution rates of IMC–SDs combined with HPMC and Kollicoat IR as PIs which both improved approximately three-fold to that of the pure drug. Finally, in vivo studies and in vitro parallel artificial membrane penetration (PAMPA) experiments ensured the greater ability of enhancing the dissolution rates of pure IMC in the gastrointestinal tract by oral delivery. In brief, this study highlights the prominent role of HPMC and Kollicoat IR as PIs in MSN SD systems in improving the bioavailability and gastrointestinal oral absorption efficiency of indomethacin.

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