Microsphere-based once-daily modified release matrix tablets for oral administration in angina pectoris
Ceyda T Sengel-Türk1, Canan Hasçicek, Nurşin Gönül
1Faculty of Pharmacy, Department of Pharmaceutical Technology, University of Ankara, Tandogan, Ankara, Turkey.
Journal of Microencapsulation
|May 10, 2008
Summary
This study developed diltiazem hydrochloride (DH) modified-release tablets using microspheres for once-daily dosing. These novel formulations offer improved convenience for angina pectoris patients.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Diltiazem hydrochloride (DH) is a calcium channel blocker for angina pectoris.
- Current DH formulations require multiple daily doses, impacting patient compliance.
Purpose of the Study:
- To develop once-daily modified-release tablet formulations of diltiazem hydrochloride (DH).
- To create a convenient oral dosage form for angina pectoris management.
Main Methods:
- DH-loaded microspheres were prepared using the solvent evaporation technique with Eudragit RS 100.
- The influence of drug/polymer ratio on microsphere characteristics was assessed.
- Microspheres were formulated into tablets using direct tableting agents like Compritol 888 ATO, Ludipress, and Cellactose 80.
Main Results:
- Successful development of DH-loaded microspheres with controlled physical and release properties.
- Optimized microspheres were formulated into stable modified-release tablets.
- The developed tablets demonstrated potential for once-daily administration.
Conclusions:
- Modified-release diltiazem hydrochloride microsphere tablets were successfully designed.
- These formulations offer a promising once-daily alternative to multiple daily doses for angina pectoris.
- The study highlights the potential of microsphere technology for improving drug delivery and patient compliance.
Related Concept Videos
01:26Oral Drug Delivery Systems: Continuous-Release Systems
Continuous-release drug delivery systems offer a strategic approach to maintaining therapeutic drug levels over extended periods following oral administration. By modulating the release rate of active pharmaceutical ingredients, these systems minimize fluctuations in plasma concentrations, which enhances clinical efficacy and reduces the need for frequent dosing. Such characteristics make them particularly advantageous in managing chronic diseases where patient adherence and stable drug...
01:16Antianginal Drugs: Nitrates and β-Blockers
In cardiovascular health, antianginal drugs combat angina pectoris — a condition marked by chest pain owing to diminished blood flow to the heart.
Organic nitrates, such as nitroglycerin, play a pivotal role. Once metabolized, they liberate nitric oxide, a molecular marvel. Nitric oxide triggers guanylyl cyclase and augments cGMP production. This biochemical cascade orchestrates the relaxation of vascular smooth muscles, ushering in vasodilation and enhancing coronary blood flow. Administered...
Organic nitrates, such as nitroglycerin, play a pivotal role. Once metabolized, they liberate nitric oxide, a molecular marvel. Nitric oxide triggers guanylyl cyclase and augments cGMP production. This biochemical cascade orchestrates the relaxation of vascular smooth muscles, ushering in vasodilation and enhancing coronary blood flow. Administered...
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
01:26Angina IV: Management
IntroductionThe management of angina requires a comprehensive approach that includes pharmacological therapies, medical procedures, and lifestyle modifications.Pharmacological TherapiesAntiplatelet agents, such as aspirin, clopidogrel, prasugrel, and ticagrelor, play a pivotal role in preventing thrombus formation in patients with angina. These medications inhibit platelet aggregation and reduce the likelihood of myocardial infarction and other cardiovascular events.Anticoagulants, including...
01:25Antianginal Drugs: Calcium Channel Blockers and Ranolazine
Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management.
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
01:20Modified-Release Drug Delivery Systems: Influencing Factors
Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...