scholarly journals In Situ Lipolysis and Synchrotron Small-Angle X-ray Scattering for the Direct Determination of the Precipitation and Solid-State Form of a Poorly Water-Soluble Drug During Digestion of a Lipid-Based Formulation

2016 ◽  
Vol 105 (9) ◽  
pp. 2631-2639 ◽  
Author(s):  
Jamal Khan ◽  
Adrian Hawley ◽  
Thomas Rades ◽  
Ben J. Boyd
Keyword(s):  
Direct Determination ◽  
Water Soluble ◽  
X Ray ◽  
X Ray Scattering ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
State Form ◽  
Poorly Water Soluble Drug

scholarly journals Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics

2021 ◽  
Vol 71 (5) ◽  
pp. 393-409
Author(s):  
Earle Radha-Rani ◽  
Gadela Venkata-Radha
Keyword(s):  
Benzoic Acid ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
X Ray Diffraction ◽  
X Ray ◽  
Water Soluble Drug ◽  
Novel Approach ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were compared with the products formed by neat grinding (NG) and liquid assisted grinding (LAG) in their enhancement of solubility. The formation of CCs was confirmed by the IR spectroscopy, powder X-ray diffraction and thermal analysis methods. The saturation solubility studies indicate that the aqueous solubility of PPD-BA and PPD-PABA CCs was significantly improved to 1.343±0.162mg/ml and 1.964±0.452mg/ml, respectively, in comparison with the PPD solubility of 0.473mg/ml. This increase in solubility is 2.83-and 3.09-fold, respectively. PPD exhibited a poor dissolution of 37.8% in 60min, while the dissolution of the CCs improved tremendously to 96.07% and 89.65% in 60min. CCs of PPD with BA and PABA present a novel approach to overcome the solubility challenges of poorly water-soluble drug PPD.

DISSOLUTION ENHANECEMENT OF AN ANTIHYPERTENSIVE AGENT BY SOLID DISPERSION

2013 ◽  
pp. 21-24
Author(s):  
Keyword(s):  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
X Ray Diffraction ◽  
Peg 6000 ◽  
X Ray ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: To evaluate dissolution enhancement of IS, a poorly water-soluble drug, by PEG 6000-based solid dispersion and investigate mechanism of dissolution enhancement from the solid dispersion. Methods: Solid dispersion was prepared by melting method. Dissolution test was performed at pH 6.8. Powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR) were used to investigate the drug crystallinity as well as the interaction between drug and polymer. Results: Dissolution rate of IS from the solid dispersion was significantly increased at pH 6.8 as compared to the pure drug. Drug crystallinity was reduced. FTIR showed the interaction between polymer and IS in the solid dispersion. Conclusions: PEG 6000 was successfully used to increase the dissolution of IS. Moreover, mechanism of the dissolution enhancement was fully explained in the study. Key words: poorly water-soluble drug, dissolution, solid dispersion.

scholarly journals Formulation of Orally Disintegrating Films as an Amorphous Solid Solution of a Poorly Water-Soluble Drug

Membranes ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 376
Author(s):  
Pattaraporn Panraksa ◽  
Pratchaya Tipduangta ◽  
Kittisak Jantanasakulwong ◽  
Pensak Jantrawut
Keyword(s):  
Mechanical Strength ◽  
Amorphous State ◽  
Strength Properties ◽  
Water Soluble ◽  
Disintegration Time ◽  
Surface Ph ◽  
X Ray ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The objective of the present study was to develop an orally disintegrating film (ODF) for a poorly water-soluble drug, phenytoin (PHT), using the cosolvent solubilization technique to achieve the amorphization of the drug, followed by the preparation of ODFs. Eleven formulations were prepared with different polymers, such as polyvinyl alcohol (PVA) and high methoxyl pectin (HMP) by the solvent casting method. The prepared films were subjected to characterization for weight variations, thickness, surface pH, disintegration time and mechanical strength properties. Then, differential scanning calorimetry, X-ray diffraction analysis and the drug release patterns of the selected films were evaluated. Among the prepared formulations, the formulation composed of 1% w/w of PVA, 0.04% w/w of sodium starch glycolate with polyethylene glycol 400, glycerin and water as cosolvents (PVA-S4) showed promising results. The physical appearance and mechanical strength properties were found to be good. The PVA-S4 film was clear and colorless with a smooth surface. The surface pH was found to be around 7.47 and the in vitro disintegration time was around 1.44 min. The drug content of the PVA-S4 film was 100.27%. X-ray diffractometry and thermal analysis confirmed the transition of phenytoin in the PVA-S4 film into a partially amorphous state during film preparation using the cosolvent solubilization approach. The resulting PVA-S4 film showed a higher dissolution rate in comparison to the film without a cosolvent. Overall, this study indicated the influence of cosolvents on enhancing the solubility of a poorly water-soluble drug and its film dissolution.

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