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      Gastroretentive behavior of orally administered radiolabeled tamarind seed formulations in rabbits validated by gamma scintigraphy

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          Abstract

          This study aimed to formulate floating gastroretentive tablets containing metformin hydrochloric acid (HCl), using various grades of hydrogel such as tamarind powders and xanthan to overcome short gastric residence time of the conventional dosage forms. Different concentrations of the hydrogels were tested to determine the formulation that could provide a sustained release of 12 h. Eleven formulations with different ratios of tamarind seed powder/tamarind kernel powder (TKP):xanthan were prepared. The physical parameters were observed, and in vitro drug-release studies of the prepared formulations were carried out. Optimal formulation was assessed for physicochemical properties, thermal stability, and chemical interaction followed by in vivo gamma scintigraphy study. MKP3 formulation with a TKP:xanthan ratio of 3:2 was found to have 99.87% release over 12 h. Furthermore, in vivo gamma scintigraphy study was carried out for the optimized formulation in healthy New Zealand White rabbits, and the pharmacokinetic parameters of developed formulations were obtained. 153Sm 2O 3 was used to trace the profile of release in the gastrointestinal tract of the rabbits, and the drug release was analyzed. The time ( T max) at which the maximum concentration of metformin HCl in the blood ( C max) was observed, and it was extended four times for the gastroretentive formulation in comparison with the formulation without polymers. C max and the half-life were found to be within an acceptable range. It is therefore concluded that MKP3 is the optimal formulation for sustained release of metformin HCl over a period of 12 h as a result of its floating properties in the gastric region.

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          Most cited references 43

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          Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention.

           H. Kim,  J. B. Singh (2000)
          In recent years scientific and technological advancements have been made in the research and development of rate-controlled oral drug delivery systems by overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying times (GET). Several approaches are currently utilized in the prolongation of the GRT, including floating drug delivery systems (FDDS), also known as hydrodynamically balanced systems (HBS), swelling and expanding systems, polymeric bioadhesive systems, modified-shape systems, high-density systems, and other delayed gastric emptying devices. In this review, the current technological developments of FDDS including patented delivery systems and marketed products, and their advantages and future potential for oral controlled drug delivery are discussed.
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            Pharmaceutical applications of various natural gums, mucilages and their modified forms.

            A large number of plant based pharmaceutical excipients are available today. Gums and mucilages are the most commonly available plant ingredients with a wide range of applications in pharmaceutical and cosmetic industries. They are being used due to their abundance in nature, safety and economy. They have been extensively explored as pharmaceutical excipients. They are biocompatible, cheap and easily available. Natural materials have advantages over synthetic ones since they are chemically inert, nontoxic, less expensive, biodegradable and widely available. They can also be modified in different ways to obtain tailor-made materials for drug delivery systems and thus can compete with the available synthetic excipients. Recent trend toward the use of plant based and natural products demands the replacement of synthetic additives with natural ones. In this review, we describe the pharmaceutical applications of various natural gums, mucilages and their modified forms for the development of various drug delivery systems.
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              Optimisation of floating matrix tablets and evaluation of their gastric residence time.

              The present investigation concerns the development of the floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. The importance of the composition optimisation, the technological process development for the preparation of the floating tablets with a high dose of freely soluble drug and characterisation of those tablets (crushing force, floating properties in vitro and in vivo, drug release) was examined. Tablets containing hydroxypropyl methylcellulose (HPMC), drug and different additives were compressed. The investigation shows that tablet composition and mechanical strength have the greatest influence on the floating properties and drug release. With the incorporation of a gas-generating agent together with microcrystalline cellulose, besides optimum floating (floating lag time, 30 s; duration of floating, >8 h), the drug content was also increased. The drug release from those tablets was sufficiently sustained (more than 8 h) and non-Fickian transport of the drug from tablets was confirmed. Radiological evidence suggests that, that the formulated tablets did not adhere to the stomach mucus and that the mean gastric residence time was prolonged (>4 h).
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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
                2017
                19 December 2016
                : 11
                : 1-15
                Affiliations
                [1 ]Department of Pharmacy
                [2 ]University Malaya Research Imaging Centre and Department of Biomedical Imaging, Faculty of Medicine
                [3 ]Center for Natural Product Research and Drug Discovery (CENAR)
                [4 ]Department of Obstetrics & Gynaecology
                [5 ]Shimadzu-UMMC Centre for Xenobiotics Studies, Pharmacology Department, Faculty of Medicine, University of Malaya
                [6 ]Malaysian Institute of Pharmaceuticals and Nutraceuticals (IPharm), National Institutes of Biotechnology Malaysia, Ministry of Science, Technology and Innovation, Penang, Malayasia
                Author notes
                Correspondence: Mahboubeh Razavi; Mohamed Ibrahim Noordin, Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia, Tel +60 3 7967 3194, Fax +60 3 7967 4964, Email mahbobehrazavi@ 123456gmail.com ; ibrahimn@ 123456um.edu.my
                Article
                dddt-11-001
                10.2147/DDDT.S115466
                5182038
                © 2017 Razavi 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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