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      Glucosamine-paracetamol spray-dried solid dispersions with maximized intrinsic dissolution rate, bioavailability and decreased levels of in vivo toxic metabolites

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          Abstract

          Purpose

          This study is aimed at preparing and testing physicochemical, pharmacokinetic and levels of toxic metabolites of paracetamol and glucosamine solid dispersions intended for multiple deliveries via the parenteral or per oral route.

          Methods

          Solid dispersions were prepared using the spray drying technique at different molar ratios of paracetamol and glucosamine. Characterization of the solid dispersions was carried out using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), equilibrium solubility and intrinsic dissolution rate. In vivo pharmacokinetics and toxic metabolites of the prepared dispersions were evaluated and compared to those of pure drugs and physical mixtures.

          Results

          Instant water solubility and more than 7-fold increase in dissolution rate led to significantly high plasma drug concentration (>6.5-fold) compared to paracetamol alone. More than 2-fold increase in area under the curve from 0 to 24 h from the dispersions was noticed on the third day of oral dosing to animals. Lower number and concentration followed by the complete disappearance of toxic pathway metabolites were observed on second and third days of dosing with solid dispersions and physical mixtures, respectively.

          Conclusions

          The spray-dried dispersions support safer and more effective delivery of multiple doses of paracetamol, leading to an acceleration of its analgesic actions. Synergism between the analgesic actions of paracetamol and joint protective actions of glucosamine in this combination is expected to facilitate effective treatment of persistent pain-related illnesses such as osteoarthritis.

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          Most cited references 35

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          An infrared investigation in relation with chitin and chitosan characterization

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            Solubility parameters as predictors of miscibility in solid dispersions.

            This paper reports interactions and possible incompatibilities in solid dispersions of hydrophobic drugs with hydrophilic carriers, with solubility parameters employed as a means of interpreting results. Systems containing ibuprofen (IB) and xylitol (XYL) in varying proportions and systems of IB with other sugars and a sugar polymer were produced using solvent evaporation and fusion methods. Additionally, bridging agents were employed with IB/XYL systems to facilitate the production of a solid dispersion. Results show that IB formed no interactions with any of the sugar carriers but interacted with all the bridging agents studied. The bridging agents were immiscible with XYL in the liquid state. Results of other reported drug/carrier systems and those from the systems studied in this paper were interpreted using Hildebrand solubility parameters. A trend between differences in drug/carrier solubility parameters and immiscibility was identified with incompatibilities evidence when large solubility parameter differences exist between drug and carrier. It was concluded that Hildebrand parameters give an indication of possible incompatibilities between drugs and carriers in solid dispersions, but that the use of partial solubility parameters may provide a more accurate prediction of interactions in and between materials and could provide more accurate indications of potential incompatibilities.
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              Recent advances in co-amorphous drug formulations.

              Co-amorphous drug delivery systems have recently gained considerable interest in the pharmaceutical field because of their potential to improve oral bioavailability of poorly water-soluble drugs through drug dissolution enhancement as a result of the amorphous nature of the material. A co-amorphous system is characterized by the use of only low molecular weight components that are mixed into a homogeneous single-phase co-amorphous blend. The use of only low molecular weight co-formers makes this approach very attractive, as the amount of amorphous stabilizer can be significantly reduced compared with other amorphous stabilization techniques. Because of this, several research groups started to investigate the co-amorphous formulation approach, resulting in an increasing amount of scientific publications over the last few years. This study provides an overview of the co-amorphous field and its recent findings. In particular, we investigate co-amorphous formulations from the viewpoint of solid dispersions, describe their formation and mechanism of stabilization, study their impact on dissolution and in vivo performance and briefly outline the future potentials.
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                Author and article information

                Journal
                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                1177-8881
                2018
                21 September 2018
                : 12
                : 3071-3084
                Affiliations
                [1 ]Department of Pharmaceutics, Faculty of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia, a.mali@ 123456tu.edu.sa
                [2 ]Department of Pharmaceutics, Beni-Suef University, Beni-Suef, Egypt, a.mali@ 123456tu.edu.sa
                [3 ]Department of Clinical Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia
                [4 ]Department of Pharmaceutics, Umm Al-Qura University, Makkah, Kingdom of Saudi Arabia
                [5 ]Department of Pharmaceutics, Minia University, Minia, Egypt
                Author notes
                Correspondence: Ahmed Mahmoud Abdelhaleem Ali, Department of Pharmaceutics, Taif University, College of Pharmacy, PO Box 888, Taif-Al-Haweiah 21974, Kingdom of Saudi Arabia, Tel +966 2 727 2020, Fax +966 2 727 4299, Email a.mali@ 123456tu.edu.sa
                Article
                dddt-12-3071
                10.2147/DDDT.S176099
                6157577
                © 2018 Ali et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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                Original Research

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