Development of Mannitol-Corn Starch Co-processed Direct Compression Excipient Using Lactitol as Binder
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Abstract
Direct compression is the simplest and most economic method to produce tablets that ingredients are thoroughly mixed and then compressed into tablets. The important role of this process is the good and effective direct compression excipient. Objective: The aim of this study was to develop a new co-processed direct compression excipient from mannitol and corn starch using wet granulation method. Methods: The direct compression excipients were prepared by co-processing mannitol with corn starch in a ratio of 2:1 using lactitol (0 - 15% on dry basis) as a binder. The resulted granules were evaluated for physical properties. These excipients were used to prepared placebo tablets to characterize tabletability, disintegration time and lubricant sensitivity ratio. All excipients were used to formulate hydrochlorothiazide (HCTZ) tablets. Dissolution profiles of the HCTZ tablets were compared to the original product using similarity factor (f2). Results: The 2:1 mannitol-corn starch co-processed granules containing lactitol as binder (0%, 10% and 15% named as MCL00, MCL10 and MCL15, respectively) performed good to excellent flowability with relatively low %moisture contents (1.60 ± 0.17-1.63 ± 0.06). The median diameter (d0.5) of MCL00, MCL10 and MCL15 were 445, 610 and 595 mm, respectively. Tensile strength of placebo tablets from MCL excipients increased with the increase amount of lactitol (ANOVA, Tukey post-hoc, p<0.01). Lubricant sensitivity ratios were between 0.29-0.53. Placebo tablets from MCL10 and MCL15 met the acceptance criteria according to pharmaceutical compendia. HCTZ tablets (50 mg/tab) produced from MCL10 without or with superdisintegrant at 2-4% offered good physical characteristics and complied with the dissolution test. The similarity factors calculated from dissolution profiles and compared to that of the original product were 51-60. Conclusion: Lactitol was an effective binder for co-processed mannitol-corn starch granules. Both MCL10 and MCL15 exhibited good flowability and high tabletability and suited for direct compression excipient. In the present study, MCL10 was the most suitable excipient to deal with such a very slightly soluble drug like HCTZ. The adding of superdisintegrant might need to attain the desired disintegration time and drug release.
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