¬Formulation and Evaluation of Metoprolol Fast Disintegrating Tablets Using Coprocessed Excipients

Abstract

Metoprolol is a medication primarily used for managing conditions like high blood pressure, chest pain (angina), irregular heart rhythms, and heart attacks. This study aimed to develop fast-dissolving tablets of metoprolol using coprocessedsuperdisintegrants, consisted of sodium starch glycolate (SSG) with either crospovidone (CP) or croscarmellose sodium (CCS) in different ratios (1:1 and 1:2).The study investigated the effects of these coprocessedsuperdisintegrants on various aspects of the tablets, such as wetting time, disintegrating time, drug content, and release of the medication in laboratory tests. The pre-compression parameters, which assess the properties of the materials before tablet formation, were within the recommended limits, suggesting that the materials flowed well during the manufacturing process. Al the parameters met the acceptable limits specified by the Indian Pharmacopoeia (IP), indicating satisfactory tablet quality.The in-vitro disintegration time, which measures how quickly the tablets break down in a simulated environment, ranged from 8±4 to 86±14 seconds. Notably, the addition of coprocessedsuperdisintegrants significantly reduced the disintegration time, indicating their effectiveness.The tablets achieved complete drug release in 6 minutes for formulation F6 and 8 minutes for formulation F5, respectively. Among all the formulations, the tablets containing a combination of SSG and CP in a 1:1 ratio demonstrated the highest drug release, reaching 99.79% within 4 minutes.Based on the findings of this study, it was observed that the coprocessedsuperdisintegrants consisting of SSG and CP were more superior compared to SSG and CCS. Increasing the concentration of coprocessedsuperdisintegrants resulted in longer disintegration time and decreased drug release for both combinations. In conclusion, the researchers determined that the tablets formulated with SSG and CP in a 1:1 ratio exhibited the most favorable properties in terms of disintegration time and drug release.

Introduction

Oral disintegrating tablets (ODTs) are gaining popularity for their rapid drug action, ease of swallowing, improved patient compliance, and convenience, especially for populations like children and seniors. ODTs dissolve quickly in the mouth, enhancing bioavailability by bypassing first-pass metabolism. Co-processed super disintegrants (combinations of excipients like sodium starch glycolate (SSG), crospovidone (CP), and croscarmellose sodium (CCS)) are used in ODT formulations to improve disintegration and dissolution rates, providing better moisture resistance and stability.

This study focused on developing fast-disintegrating metoprolol tablets using different ratios and concentrations of co-processed super disintegrants (SSG:CP and SSG:CCS) via direct compression. Metoprolol is a cardioselective beta-blocker with variable oral bioavailability due to first-pass metabolism.

Materials and Methods:
Co-processed super disintegrants were prepared by solvent evaporation in specified ratios and incorporated into tablets with metoprolol and other excipients. Tablets were evaluated for pre-compression properties (flow, density) and post-compression attributes such as weight variation, hardness, friability, drug content, disintegration time, wetting time, in vitro dispersion, and dissolution.

Results:

• All formulations exhibited good flow and mechanical properties within pharmacopeial limits.

• Increasing super disintegrant concentration generally reduced disintegration time but excessive amounts sometimes slowed it due to gel formation.

• The best performing formulation (F6: 10% SSG:CP at 1:1 ratio) showed rapid disintegration (~8 seconds), quick wetting (~62 seconds), and almost complete drug release within 6 minutes.

• SSG:CP combinations outperformed SSG:CCS in disintegration and dissolution efficiency.

• FTIR analysis confirmed no chemical interaction between drug and excipients.

Conclusion

Metoprolol, a cardio-selective beta-blocker, is commonly utilized for treating hypertension, angina pectoris, heart rhythm disorders, and heart attacks. In this study, fast-dissolving atenolol tablets were created using a combination of co-processed super disintegrants – SSG with CP and SSG with CCS – in various proportions (1:1 and 1:2 at 5% and 10% concentrations). The metoprolol tablets with co-processed super disintegrants displayed rapid disintegration and enhanced drug dissolution. This research suggests that combining SSG and CP as co-processed super disintegrants proves to be more effective than mixing SSG and CCS.

References

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Copyright

Copyright © 2025 V. Himabindu, M. Mounika, M. Manasa, Rakibul Islam, Rasidul Islam. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.