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23 Factorial Design and Optimization of Effervescent Floating Matrix Tablet of Neratinib

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An Author Correction to this article was published on 01 July 2021

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Abstract

Purpose

The main objective of the research was to formulate an effervescent floating matrix tablet (EFMT) of a potential anticancer drug neratinib employed in breast cancer therapy. The drug shows poor aqueous solubility at higher pH leading to reduce therapeutic efficacy, thereby resulting in poor bioavailability. Hence, an EFMT is designed to extend the gastric residence time (GRT) of drugs, which can remain several hours in the gastric region and enhance bioavailability. Further 23 factorial design employed.

Methods

The EFMT of neratinib are prepared by direct compression using hydroxyl propyl methylcellulose, Carbopol 940, microcrystalline cellulose, sodium bicarbonate, talc, and lactose. Polymer concentrations were selected as independent variables, whereas hardness, percentage swelling, floating, and percentage drug release were the dependent variables. Pre- and post-compression measurements, swelling studies, in vitro buoyancy, FTIR, scanning electron microscopy (SEM), in vitro release, kinetic, and mechanism of drug release studies have been characterized for preparing floating matrix tablets

Results

The results showed that pre-and post-compression parameters are within the limit of USP. The buoyancy lag time and total buoyancy time are less than 2 min and > 12 h, respectively, with good swelling characteristics. Fourier transform infrared (FTIR) spectrum showed that no interaction was found between drug and polymers. The optimized formulation (F9) showed 100% drug release at 8 h, which shows a Fickian diffusion.

Conclusion

The developed novel neratinib floating matrix tablet could enhance the solubility and residence time of neratinib at upper GIT because of the combined effect of the polymers.

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Funding

The Deanship of Scientific Research at King Khalid University provided funding for this work through research groups program under grant number R.G.P. 168-42.

Author information

Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, King Khalid University, Guraiger, Abha, 61421, Saudi Arabia

    Mohamed Rahamathulla, Umme Hani & Yasmin Begum M

  2. Department of Pharmacology, College of Pharmacy, King Khalid University, Guraiger, Abha, 61421, Saudi Arabia

    Ali Alqahtani & Kumarappan Chidambaram

  3. Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysore, 570015, India

    Gangadharappa. H.V

  4. Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia

    Mohammed Jafar

  5. Department of Biosciences and Bioengineering, Indian Institute of Technology Bombay (IITB), Mumbai, 400076, India

    Riyaz Ali M. Osmani

  6. Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail, Saudi Arabia

    Afrasim Moin

  7. Department of Pharmaceutics, Vivekananda College of Pharmacy, Dr. Rajkumar Road, Rajajinagar 2nd Stage, Bengaluru, 56005, India

    S. J. Shankar

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  1. Mohamed Rahamathulla
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  4. Gangadharappa. H.V
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Correspondence to Mohamed Rahamathulla.

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The original version of this article unfortunately contained a mistake in the name and affiliation of one co-author. The correct name Dr. Mohammed is "Mohammed Jafar" with the affiliation "Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia."

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Rahamathulla, M., Hani, U., Alqahtani, A. et al. 23 Factorial Design and Optimization of Effervescent Floating Matrix Tablet of Neratinib. J Pharm Innov 17, 1451–1462 (2022). https://doi.org/10.1007/s12247-021-09563-4

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