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Co-processing of nateglinide with meglumine for enhanced dissolution rate: in vitro and in vivo evaluation

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dc.contributor.authorBazeed, A.Y.
dc.contributor.authorEssa, E.A.
dc.contributor.authorNouh, A.
dc.contributor.authorEl Maghraby, G.M.
dc.date.issued2020
dc.description.abstractObjective: The aim of this work was to investigate dry co-grinding of nateglinide with meglumine for enhanced dissolution rate of nateglinide. The study was extended to investigate the effect of this dissolution enhancement on the hypoglycemic effect of the drug in diabetic rats. Methods: Nateglinide was subjected to dry co-grinding with increasing proportions of meglumine to prepare products containing the drug with meglumine at 1:1, 1:2, and 1:3 molar ratios. These products were evaluated using combined instrumental analysis which employed Fourier transform infrared spectroscopy (FTIR), differential thermal analysis (DTA), and X-ray diffraction (XRD). Drug dissolution was also monitored before and after processing with and without meglumine. The optimum ratio was used to assess the effect of dissolution enhancement on the hypoglycemic effect of nateglinide on diabetic rats. The unprocessed nateglinide was used as control. Results: Co-grinding of nateglinide resulted in changes in the FTIR spectral patterns of nateglinide and meglumine. The changes suggested the formation of amide bond between both compounds at 1:1 molar ratio. The new species was confirmed by DTA and XRD. This species exhibited fast dissolution of nateglinide after incorporation of higher proportions of meglumine. Co-grinding was essential as indicated from slower dissolution from physical mixture containing the highest proportion of meglumine. Enhanced dissolution was reflected in vivo as improved rate and extent of hypoglycemia. Conclusion: Dry co-grinding of nateglinide with meglumine developed new species which liberated nateglinide rapidly and enhanced the rate and extent of hypoglycemia of nateglinide.
dc.identifier.citationDrug Development and Industrial Pharmacy, 2020; 46(10):1676-1683
dc.identifier.doi10.1080/03639045.2020.1820035
dc.identifier.issn0363-9045
dc.identifier.issn1520-5762
dc.identifier.urihttps://hdl.handle.net/11541.2/33586
dc.language.isoen
dc.publisherTaylor and Francis
dc.rightsCopyright 2020 Informa UK Limited, trading as Taylor & Francis Group
dc.source.urihttps://doi.org/10.1080/03639045.2020.1820035
dc.subjectdissolution rate
dc.subjecthypoglycemic effect
dc.subjectmeglumine
dc.subjectNateglinide
dc.subjectsalt formation
dc.titleCo-processing of nateglinide with meglumine for enhanced dissolution rate: in vitro and in vivo evaluation
dc.typeJournal article
pubs.publication-statusPublished
ror.mmsid9916727922901831

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