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Preparation and Optimization of Fast-Disintegrating Tablet Containing Naratriptan Hydrochloride Using D-Optimal Mixture Design

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A Correction to this article was published on 16 July 2018

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Abstract

Optimization of a lyophilized fast-disintegrating tablet (LFDT) formulation containing naratriptan hydrochloride, an antimigraine drug, was the foremost objective of the study, aiming in achieving fast headache pain relief. The Design-Expert® v10 software was used to generate formulations using D-optimal mixture design with four components: gelatin (X1), hydrolyzed gelatin (X2), glycine (X3), and mannitol (X4) of total solid material (TSM) w/w. The effect of the relative proportion of each component was determined on friability (Y1), hardness (Y2), and in vitro disintegration time (Y3), which was then applied for formulation optimization. In addition, their effect on tablet porosity was determined via scanning electron microscopy (SEM). Drug-excipient interaction was evaluated using differential scanning calorimetry (DSC). A comparative dissolution study against the conventional tablets was studied. Accelerated stability study was carried out in (Al/Al) and (Al/PVC) blister packs. An in vivo pharmacokinetic study was carried out to compare the optimized formulation and the conventional tablets. The optimized formulation’s responses were 0.30%, 3.4 kg, and 6.12 s for Y1, Y2, and Y3, respectively. No drug-excipient interaction was specified via DSC. The optimized formulation exhibited porous structure as determined via SEM. Dissolution study demonstrated complete dissolution within 1.5 min. Study indicated stability for 78 months in (Al/Al) blister packs. In vivo pharmacokinetic study demonstrated that Cmax, AUClast, and AUCinf were significantly higher for the developed formulation. As well, the Tmax was 1 h earlier than that of convenient tablet. An LFDT would achieve a faster onset of action for naratriptan compared to other formulations.

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Change history

  • 16 July 2018

    During the production process, an editorial error occurred where the typesetter placed the ± symbol on the right side of the values in Table IV, whereas the symbol should be placed on the left side. The original article has been corrected.

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Authors and Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmacy, Helwan University, Cairo, Egypt

    Samia M. Omar & Noha M. Abdelgawad

  2. Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University (ACU), Giza, Egypt

    Samia M. Omar

  3. Department of Pharmaceutics, Faculty of Pharmacy, Al Azhar University, Cairo, Egypt

    Fathy I. AbdAlla

  4. Department of Pharmaceutics and Pharmaceutical Technology, Egyptian Russian University (ERU), Badr, Egypt

    Fathy I. AbdAlla

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  1. Samia M. Omar
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  2. Fathy I. AbdAlla
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  3. Noha M. Abdelgawad
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Correspondence to Samia M. Omar.

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Additional information

The original version of this article was revised: During the production process, an editorial error occurred where the typesetter placed the ± symbol on the right side of the values in Table IV, whereas the symbol should be placed on the left side. Also in Table IV, the AI/PVC was changed from 3.39d to 3.32d in month 5 after publication. In Table IV and Table V the < sign was omitted during the production process.

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Omar, S.M., AbdAlla, F.I. & Abdelgawad, N.M. Preparation and Optimization of Fast-Disintegrating Tablet Containing Naratriptan Hydrochloride Using D-Optimal Mixture Design. AAPS PharmSciTech 19, 2472–2487 (2018). https://doi.org/10.1208/s12249-018-1061-9

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  • DOI: https://doi.org/10.1208/s12249-018-1061-9

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