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. 2023 Oct 12:12:1325.
doi: 10.12688/f1000research.140607.1. eCollection 2023.

Enteric-coating film effect on the delayed drug release of pantoprazole gastro-resistant generic tablets

Mosab Arafat  1 , Molham Sakkal  1 , Mohammad F Bostanudin  1 , Othman Abdulrahim Alhanbali  2 , Priya Yuvaraju  3 , Rami Beiram  3 , Bassem Sadek  3 , Amal Akour  3 , Salahdein AbuRuz  3   4
Affiliations

Enteric-coating film effect on the delayed drug release of pantoprazole gastro-resistant generic tablets

Mosab Arafat et al. F1000Res. .

Abstract

Background: Enteric coating films in acidic labile tablets protect the drug molecule from the acidic environment of the stomach. However, variations in the excipients used in the coating formulation may affect their ability to provide adequate protection. This study is the first to investigate the potential effects of coating materials on the protective functionality of enteric coating films for pantoprazole (PNZ) generic tablets after their recall from the market. Methods: A comparative analysis was conducted between generic and branded PNZ products, using pure drug powder for identification. The in vitro release of the drug was evaluated in different pH media. The study also utilized various analytical and thermal techniques, including differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier-transform infrared (FTIR), and confocal Raman microscopy. Results: The in vitro assessment results revealed significant variations in the release profile for the generic product in acidic media at 120 min. DSC and TGA thermal profile analyses showed slight variation between the two products. XRD analysis exhibited a noticeable difference in peak intensity for the generic sample, while SEM revealed smaller particle sizes in the generic product. The obtained spectra profile for the generic product displayed significant variation in peaks and band intensity, possibly due to impurities. These findings suggest that the excipients used in the enteric coating film of the generic product may have affected its protective functionality, leading to premature drug release in acidic media. Additionally, the presence of polysorbate 80 (P-80) in the brand product might improve the properties of the enteric coating film due to its multi-functionality. Conclusions: In conclusion, the excipients used in the brand product demonstrated superior functionality in effectively protecting the drug molecule from acidic media through the enteric coating film, as compared to the generic version.

Keywords: Enteric Coating Film; Pantoprazole; In vitro Drug Release; Analytical Techniques; Differential Scanning Calorimetry; Thermogravimetric Analysis; Generic Drug; Polysorbate 80..

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Conflict of interest statement

No competing interests were disclosed.

Figures

Figure 1.
Figure 1.. Comparison of dissolution profiles for the brand and generic products of Pantoprazole (PNZ in three dissolution media (pH 1.2, pH 5, and pH 6.8) after 60 min at 37°C.
Values are expressed as means ± S.D. (n=6).
Figure 2.
Figure 2.. Comparison of dissolution profiles for the brand and generic products of PNZ in three dissolution media (pH 1.2, pH 5, and pH 6.8) after 120 min at 37°C.
Values are expressed as means ± S.D. (n=6).
Figure 3.
Figure 3.. DSC Thermal analytical spectra of the pure powder of PNZ, the brand product of PNZ, and the generic product of PNZ.
Figure 4.
Figure 4.. Thermal gravimetric analysis/DTG analytical spectra for the pure powder of PNZ, the brand product of PNZ, and the generic product of PNZ.
Figure 5.
Figure 5.. X-ray diffraction analytical spectra for the brand product of PNZ, the pure powder of PNZ, and the generic product of PNZ.
Figure 6.
Figure 6.. SEM images for (A) generic tablet PNZ, (B) branded tablet of PNZ, and (C) pure powder of PNZ.
Caliper indicates 5-20 μm. Images were obtained under x850-5000 - magnifications operating at 20 kV.
Figure 7.
Figure 7.. Fourier transform infrared analytical spectra for the generic product of PNZ, the brand product of PNZ, and the pure powder of PNZ.
Figure 8.
Figure 8.. Chemical structure of Pantoprazole.
Figure 9.
Figure 9.. Raman spectroscopy of the pure powder of PNZ, the brand product of PNZ, and the generic product of PNZ.
See this image and copyright information in PMC

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