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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...
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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,...
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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...
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Alternating Magnetic Field-Responsive Hybrid Gelatin Microgels for Controlled Drug Release
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Published on: February 13, 2016

The development of Eudragit® NM-based controlled-release matrix tablets.

Kateřina Dvořáčková1, Rasa Kalėdaitė, Jan Gajdziok

  • 1Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Czech Republic.

Medicina (Kaunas, Lithuania)
|July 28, 2012
PubMed
Summary

Eudragit® NM combined with microcrystalline cellulose is effective for controlled-release tablets of freely soluble drugs. This formulation is best suited for a 1:1 drug-to-filler ratio, ensuring optimal sustained release.

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Materials Science

Background:

  • Controlled-release drug formulations are crucial for optimizing therapeutic efficacy and patient compliance.
  • Eudragit® NM, a polymer, and microcrystalline cellulose, an insoluble filler, were explored for their potential in matrix tablet formulation.
  • Understanding the influence of drug solubility on release kinetics from such matrices is essential.

Purpose of the Study:

  • To investigate Eudragit® NM as a matrix former with microcrystalline cellulose for controlled-release tablets.
  • To evaluate the impact of drug-to-filler ratios and polymer amounts on drug release profiles.
  • To assess the performance of these formulations with model drugs of varying solubility (diltiazem hydrochloride and caffeine).

Main Methods:

  • Preparation of matrix tablets with Eudragit® NM and microcrystalline cellulose at different drug-to-filler ratios (1:1, 2:1, 4:1).
  • Incorporation of freely soluble diltiazem hydrochloride and sparingly soluble caffeine as model drugs.
  • In vitro dissolution testing at a constant pH (6.8) and under changing pH conditions to simulate physiological environments.

Main Results:

  • Matrix tablets exhibited excellent mechanical properties and met European Pharmacopoeia standards.
  • The 1:1 drug-to-filler ratio formulation demonstrated optimal sustained release for the freely soluble drug, minimizing burst effect.
  • Dissolution profiles were significantly influenced by drug-to-filler ratio and polymer content, confirmed by similarity factor analysis.
  • Faster release was observed for diltiazem hydrochloride under changing pH due to its solubility.
  • Prolonged release was not achieved for the sparingly soluble drug, with a tendency towards rapid disintegration.

Conclusions:

  • The combination of Eudragit® NM and microcrystalline cellulose is suitable for controlled-release formulations of freely soluble drugs.
  • Optimal performance is achieved when the drug and insoluble filler are present in similar amounts (1:1 ratio).
  • This formulation approach is less effective for sparingly soluble drugs, necessitating alternative strategies for prolonged release.