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Optimization for glimepiride dissolution enhancement utilizing different carriers and techniques

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Abstract

The present work is a comparative study that matches between carriers and techniques used to prepare solid mixtures with glimepiride. The study is directed towards elucidation of the most promising carrier capable of highly improving drug dissolution along with the most successful technique used for drug formulation. Mixtures were tested for drug content and dissolution. The most optimum formulae were characterized by DSC, IR and XRPD. Kinetic treatment of dissolution data was performed for physical and co-ground mixtures, solid dispersions and their adsorbates, triple solid dispersions and their adsorbates, microwave generated or treated solid dispersions. Results revealed that enhancing effect mostly reached maximum with ternary solid dispersion adsorbate (TSDads). The latter technique demonstrated a dramatic increase in drug dissolution rate which was reflected in the shortest half-life for most carriers at variable degrees. The highest dissolution rate was attained with pregelatinized starch and decreased to variable degrees with remaining carriers. Differences were ascribed to chemical nature as well as relative water solubility of carriers. The combined effects of incorporating surfactants, polymers and adsorbents to glimepiride contributed together to improve wetting, reduce crystallinity and caused substantial increase in the surface area which made TSDads the most promising technique for enhancing dissolution of glimepiride.

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Abbreviations

PM:

Physical mixtures

CGM:

Co-ground mixtures

SD:

Solid dispersions

SDads:

Solid dispersion adsorbate

TSD:

Triple solid dispersion

TSDads:

Triple solid dispersion adsorbate

MwGSD:

Microwave generated solid dispersion

MwTSD:

Microwave treated solid dispersion

PreGelSt:

Pregelatinized starch

CP:

Crospovidone

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Acknowledgments

The authors are grateful for the members of Pharmaceutics Department in National Research Center in Dokki, Cairo, Egypt for their continuous help and support in terminating the experimental work.

Conflict of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

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Authors and Affiliations

  1. Faculty of Pharmacy, Ahram Canadian University, 6th October City, Egypt

    Rana R. Makar & Ehab A. Hosni

  2. Faculty of Pharmacy, Cairo University, 47 Maamal El Alban Street, Khalafawi, Shoubra, Cairo, 11241, Egypt

    Randa Latif

  3. Faculty of Pharmacy, Cairo University, Cairo, Egypt

    Omaima N. El Gazayerly

Authors
  1. Rana R. Makar
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  2. Randa Latif
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  3. Ehab A. Hosni
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  4. Omaima N. El Gazayerly
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Corresponding author

Correspondence to Randa Latif.

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Makar, R.R., Latif, R., Hosni, E.A. et al. Optimization for glimepiride dissolution enhancement utilizing different carriers and techniques. Journal of Pharmaceutical Investigation 43, 115–131 (2013). https://doi.org/10.1007/s40005-013-0061-8

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  • DOI: https://doi.org/10.1007/s40005-013-0061-8

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