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Related Concept Videos

Drug Delivery Systems: Different Types01:27

Drug 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,...
Modified-Release Drug Delivery Systems: Overview01:19

Modified-Release Drug Delivery Systems: Overview

Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
Modified-Release Drug Delivery Systems: Rate-Programmed I01:22

Modified-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,...
Oral Drug Delivery Systems: Delayed-Release Systems01:11

Oral 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...
Oral Drug Delivery Systems: Continuous-Release Systems01:26

Oral 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...
Intrauterine Drug Delivery Systems01:21

Intrauterine Drug Delivery Systems

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...

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Microwave-driven Synthesis of Iron Oxide Nanoparticles for Fast Detection of Atherosclerosis
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Risedronate-loaded Eudragit S100 microparticles formulated into tablets.

Aline A Velasquez1, Juliane Mattiazzi, Luana M Ferreira

  • 1Department of Industrial Pharmacy, Federal University of Santa Maria , Santa Maria , Brazil.

Pharmaceutical Development and Technology
|March 20, 2013
PubMed
Summary

This study developed risedronate-loaded microparticles and tablets to improve oral drug delivery. The novel formulation enhances risedronate release in the intestine, potentially improving patient compliance for osteoporosis treatment.

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Materials Science

Background:

  • Risedronate, an osteoporosis medication, suffers from poor patient compliance due to gastrointestinal side effects and complex dosing.
  • Developing alternative oral dosage forms is crucial to enhance patient adherence and therapeutic outcomes.

Purpose of the Study:

  • To prepare and characterize risedronate-loaded Eudragit® S100 microparticles.
  • To develop a stable and effective tablet formulation using these microparticles for improved oral administration.
  • To evaluate the in vitro release profile of risedronate from the developed dosage form.

Main Methods:

  • Risedronate-loaded Eudragit® S100 microparticles were prepared using spray-drying technology.
  • Microparticles were characterized for yield, encapsulation efficiency, particle size, moisture content, morphology, and flowability.
  • Microparticles were compressed into tablets using direct tableting excipients, including varying concentrations of polyvinylpyrrolidone.
  • Tablet properties such as weight variation, hardness, friability, disintegration time, and drug content were assessed.
  • In vitro drug release studies were conducted in simulated gastric (pH 1.2) and intestinal (pH 6.8) media.

Main Results:

  • Spray-dried microparticles exhibited high encapsulation efficiency (>90%) and a mean diameter of 3.3 µm.
  • Microparticles showed pH-dependent release, with minimal drug release in acidic conditions and rapid release at pH 6.8.
  • The compressed tablets demonstrated consistent physical properties, low friability, and rapid disintegration (<15 min).
  • Tableted microparticles provided sustained risedronate release over 240 minutes in intestinal medium, with limited release (<16%) in acidic conditions.
  • The developed formulation showed promising characteristics for oral risedronate delivery.

Conclusions:

  • Risedronate-loaded Eudragit® S100 microparticles can be successfully prepared and formulated into tablets.
  • The tableted microparticle formulation offers a potential strategy to mitigate gastrointestinal side effects and improve risedronate delivery.
  • This novel dosage form holds promise for enhancing patient compliance in osteoporosis management.