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Purpose <p>Crohn’s disease (CD) and ulcerative colitis (UC), the two main forms of inflammatory bowel disease (IBD), are commonly treated with mesalamine (5-ASA). Among its oral dosage forms, time-dependent prolonged-release granules (PRGs) enable targeted drug delivery throughout the gastrointestinal tract. Developing generic versions of these time-dependent PRGs is challenging due to complex formulation strategies and extensive patent protection. This study functions as a systematic technical diligence, offering a structured patent landscape, clinical data analysis, and design-around strategies to uncover innovation trends, regulatory barriers, and formulation approaches relevant to generic product development.</p> Methods <p>An extensive patent landscape analysis was conducted, and over 50 relevant granted patents, PCT publications, and patent applications (filed between 1983 and 2023) were analysed using major global databases, including USPTO, Espacenet, WIPO, Lens.org, and Google Patents. Granted patents, PCT publications, and patent applications were categorized by legal status, geography, and International Patent Classification (IPC) codes to uncover formulation and process innovation trends. Additionally, 12 clinical studies and formulary data complemented the landscape. The study also examined claim strategies, design-around approaches, and bioequivalence (BE) challenges relevant to generic development.</p> Results <p>The analysis revealed a progression from early sustained-release tablets to multiparticulate PRGs employing advanced granulation and coating technologies. Innovations in granulation, coating techniques, and excipient selection, such as the use of polymers with defined viscosity grades and optimised curing conditions, pose significant hurdles for generic development. Design-around strategies in non-innovator patents often involved excipient substitutions or process modifications.</p> Conclusion <p>The development of generic time-dependent 5-ASA PRGs is challenged by complex formulation designs and layered patent protections. This analysis underscores the importance of understanding patent clusters, critical quality attributes, and regulatory timelines. Such insights can guide the formulation of effective design-around and optimization strategies, supporting the development of bioequivalent alternatives and expanding treatment options for IBD.</p> Graphical abstract <p></p>

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Patent Landscaping of Time-dependent Mesalamine Prolonged-release Granules: A Case Study for Generic Formulation Development

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Ayush Rohila,
  • Ankit Kumar,
  • Prakash Kumar Sirvi,
  • Sadhana Dhyagala,
  • Sakshi Kunjir,
  • Rajkumar Malayandi

摘要

Purpose

Crohn’s disease (CD) and ulcerative colitis (UC), the two main forms of inflammatory bowel disease (IBD), are commonly treated with mesalamine (5-ASA). Among its oral dosage forms, time-dependent prolonged-release granules (PRGs) enable targeted drug delivery throughout the gastrointestinal tract. Developing generic versions of these time-dependent PRGs is challenging due to complex formulation strategies and extensive patent protection. This study functions as a systematic technical diligence, offering a structured patent landscape, clinical data analysis, and design-around strategies to uncover innovation trends, regulatory barriers, and formulation approaches relevant to generic product development.

Methods

An extensive patent landscape analysis was conducted, and over 50 relevant granted patents, PCT publications, and patent applications (filed between 1983 and 2023) were analysed using major global databases, including USPTO, Espacenet, WIPO, Lens.org, and Google Patents. Granted patents, PCT publications, and patent applications were categorized by legal status, geography, and International Patent Classification (IPC) codes to uncover formulation and process innovation trends. Additionally, 12 clinical studies and formulary data complemented the landscape. The study also examined claim strategies, design-around approaches, and bioequivalence (BE) challenges relevant to generic development.

Results

The analysis revealed a progression from early sustained-release tablets to multiparticulate PRGs employing advanced granulation and coating technologies. Innovations in granulation, coating techniques, and excipient selection, such as the use of polymers with defined viscosity grades and optimised curing conditions, pose significant hurdles for generic development. Design-around strategies in non-innovator patents often involved excipient substitutions or process modifications.

Conclusion

The development of generic time-dependent 5-ASA PRGs is challenged by complex formulation designs and layered patent protections. This analysis underscores the importance of understanding patent clusters, critical quality attributes, and regulatory timelines. Such insights can guide the formulation of effective design-around and optimization strategies, supporting the development of bioequivalent alternatives and expanding treatment options for IBD.

Graphical abstract