Related Experiment Video
Updated: May 5, 2026
09:11
Alternating Magnetic Field-Responsive Hybrid Gelatin Microgels for Controlled Drug Release
Published on: February 13, 2016
9.3K
Sustained-release pellets of nifedipine using microcrystals combined with MCC-based matrix
Jinlong Ma1, Juan Wang, Zhibo Cheng
1Department of Pharmaceutics, Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
Drug Development and Industrial Pharmacy
|December 11, 2013
Summary
This study developed sustained-release nifedipine pellets (NSPs) using microcrystalline cellulose (MCC) and enhanced dissolution via wet-milling with HPMC. The resulting NSPs demonstrated effective sustained release and bioequivalence in beagle dogs.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Nifedipine is a widely used calcium channel blocker for cardiovascular conditions.
- Developing sustained-release formulations improves patient compliance and therapeutic efficacy.
- Microcrystalline cellulose (MCC) is a common excipient for matrix-based drug delivery systems.
Purpose of the Study:
- To prepare sustained-release nifedipine pellets (NSPs) utilizing an MCC matrix.
- To investigate the drug release mechanism and influencing factors.
- To evaluate the stability and bioequivalence of the developed NSPs.
Main Methods:
- Wet-milling and extrusion-spheronization techniques were employed.
- Co-grinding nifedipine with Hydroxypropyl Methylcellulose (HPMC) to create microcrystals.
- Differential Scanning Calorimetry (DSC), X-ray powder diffraction, and microscopy for characterization.
- In vitro dissolution studies and in vivo bioequivalence study in beagle dogs.
Main Results:
- Wet-milling reduced nifedipine particle size to 5 μm, enhancing dissolution rate.
- Nifedipine release from MCC-based NSPs followed the Korsmeyer model, indicating diffusion-controlled release.
- The prepared NSPs exhibited sustained release over 8 hours.
- High stability was confirmed after a 6-month accelerated stability test.
- Bioequivalence was established between the developed NSPs and a commercial product.
Conclusions:
- Sustained-release nifedipine pellets (NSPs) can be effectively prepared using MCC and a co-ground mixture (CGM) of nifedipine with HPMC.
- The formulation process is convenient, scalable, and yields a stable product with favorable pharmacokinetic properties.
- This approach offers a promising alternative for nifedipine sustained-release drug delivery.
More Related Videos
Related Concept Videos
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
137
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...
137
01:26Oral Drug Delivery Systems: Continuous-Release Systems
308
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...
308
01:22Modified-Release Drug Delivery Systems: Rate-Programmed I
172
Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
172
01:11Oral Drug Delivery Systems: Delayed-Release Systems
222
Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
222
01:22Modified-Release Drug Delivery Systems: Drug Release Characteristics
257
Drug release from modified-release dosage forms is designed to achieve specific therapeutic effects by controlling the rate and extent of drug release. The classification of these drug release systems is based on key pharmacokinetic assumptions: drug disposition follows first-order kinetics, drug release is the rate-limiting step in absorption, and the released drug is rapidly and completely absorbed.There are four major models of drug release patterns. The first model is the slow zero-order...
257
01:21Intrauterine Drug Delivery Systems
168
Controlled-release systems for intravaginal and intrauterine drug delivery have been developed primarily for the administration of contraceptive steroid hormones. These delivery routes circumvent first-pass hepatic metabolism, thereby enhancing bioavailability and allowing for reduced systemic dosages compared to oral administration. Such approaches contribute to improved therapeutic efficacy and patient compliance, particularly in long-term contraceptive regimens.Intravaginal Drug Delivery...
168