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Development of Novel High Density Gastroretentive Multiparticulate Pulsatile Tablet of Clopidogrel Bisulfate Using

Nilesh Desai1, Ravindra Purohit2

  • 1Department of Quality Assurance Techniques, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune, 411038, India.

AAPS Pharmscitech
|May 28, 2017
PubMed

Insights

A novel high-density tablet delivers clopidogrel bisulfate (CLB) with pulsatile release, ideal for morning heart attack prevention. This chronotherapy approach ensures sustained drug delivery for improved patient outcomes.

Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Cardiovascular Medicine

Background:

  • Myocardial infarction (heart attack) is a growing global health concern, with many events occurring in the morning due to platelet aggregation.
  • Chronotherapy, timing medication to the body's natural rhythms, is crucial for managing morning cardiovascular events.
  • Clopidogrel bisulfate (CLB), an antiplatelet drug, is vital for heart attack prevention but requires acidic pH for solubility and has a narrow absorption window, necessitating prolonged gastric residence.

Purpose of the Study:

  • To develop a novel high-density tablet formulation for pulsatile delivery of clopidogrel bisulfate (CLB).
  • To achieve a delayed and targeted drug release profile for effective chronotherapy of myocardial infarction.
  • To ensure prolonged gastric retention of the CLB formulation for enhanced therapeutic efficacy.

Main Methods:

  • Multiparticulate pellets of CLB were prepared using extrusion-spheronization and coated for pulsatile release.
  • High-density tablets (2.2 g cm⁻³) containing the coated pellets were formulated.
  • Quality by Design (QbD) principles were employed for process optimization.
  • In vitro dissolution studies determined drug release profiles, and in vivo X-ray studies in rabbits assessed gastric retention.

Main Results:

  • The developed pulsatile system exhibited a significant lag time of 6 hours, followed by a burst release of up to 94% of the drug within 1 hour.
  • The high-density tablets demonstrated prolonged gastric retention for 8 hours in rabbit models.
  • The tablet's density (2.2 g cm⁻³) ensured it remained at the stomach's bottom, floating on gastric fluid.

Conclusions:

  • A high-density pulsatile drug delivery system for CLB was successfully developed, demonstrating effective gastric retention and chronotherapeutic release.
  • This formulation offers a promising approach for drugs requiring prolonged gastric residence and targeted release for conditions like myocardial infarction.
  • The study highlights the potential of high-density pulsatile systems for optimizing chronotherapy and improving drug efficacy in cardiovascular medicine.

Keywords:
clopidogrel bisulfatehigh density tabletmultiparticulate pulsatile systemquality by design

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