Related Experiment Video
Updated: May 30, 2026
11:27
A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
Published on: August 9, 2022
Design of prolonged release tablets using new solid acrylic excipients for direct compression.
J C O Villanova1, E Ayres, R L Oréfice
1Universidade Federal de Minas Gerais - UFMG, Escola de Engenharia, Departamento de Engenharia de Materiais, Belo Horizonte, MG, Brazil. pharmacotecnica@yahoo.com.br
Summary
New polymeric excipients developed from acrylic monomers enable sustained drug release for over 12 hours. These novel excipients, prepared via suspension polymerization, show promise for extended-release tablets and are non-toxic to gingival fibroblasts.
Area of Science:
- Polymer Chemistry
- Pharmaceutical Sciences
- Materials Science
Background:
- Developing novel excipients is crucial for achieving prolonged drug release and improved therapeutic outcomes.
- Acrylic monomers offer a versatile base for creating new polymeric excipients for pharmaceutical applications.
Purpose of the Study:
- To synthesize and characterize new polymeric excipients from acrylic monomers (ethyl acrylate, methyl methacrylate, butyl methacrylate) for direct compression (DC).
- To evaluate the micromeritic, mechanical, and drug release properties of tablets formulated with these novel excipients.
- To assess the in vitro biocompatibility of the developed polymeric excipients.
Main Methods:
- Polymeric excipients synthesized using suspension and emulsion polymerization.
- Characterization included FTIR, SEM, particle size analysis, and density measurements.
- Micromeritic properties (Carr index, Hausner ratio) and compactability were assessed.
- Tablets formulated with propranolol hydrochloride (PHCl) using direct compression.
- Tablet quality (weight, hardness, friability) and drug release profiles were evaluated.
Main Results:
- Excipients from suspension polymerization (NWCB, PECB) facilitated PHCl release exceeding 12 hours, attributed to superior micromeritic properties.
- Increased polymer content and compression time enhanced tablet hardness and reduced drug release rate.
- In vitro tests confirmed the non-toxicity of the developed polymeric excipients on gingival fibroblasts.
Conclusions:
- Novel polymeric excipients based on acrylic monomers can be effectively prepared for direct compression.
- Suspension-polymerized excipients demonstrate significant potential for creating extended-release drug delivery systems.
- The developed excipients exhibit favorable properties for tablet formulation and are biocompatible.
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
01:11Oral Drug Delivery Systems: Delayed-Release Systems
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...
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...
01:27Drug Delivery Systems: Different Types
Conventional oral drug products, termed immediate-release (IR) formulations, are engineered to promptly release their active pharmaceutical ingredient (API) upon ingestion, typically in tablets or capsules. This rapid release often results in swift drug absorption and consequent pharmacodynamic effects, although the timing and intensity can vary depending on the drug's properties. Prodrugs within these formulations require metabolic conversion to activate their pharmacodynamic effects,...
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...
01:22Modified-Release Drug Delivery Systems: Rate-Programmed I
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,...