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Related Concept Videos

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...
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Modified-Release Drug Delivery Systems: Stimuli-Activated

Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also called...
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Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
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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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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...
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Solid-state Graft Copolymer Electrolytes for Lithium Battery Applications
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Drug-organic electrolyte complexes as controlled release systems.

Rajesh Vadlapatla1, E Kim Fifer, Cherng-Ju Kim

  • 1College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA.

Drug Development and Industrial Pharmacy
|November 11, 2008
PubMed
Summary
This summary is machine-generated.

A novel water-insoluble complex of diltiazem HCl and sodium deoxycholate enables sustained drug release (>24 h). Incorporating this complex into hydroxypropylmethylcellulose carriers shifts release control from diffusion to polymer erosion, ensuring consistent kinetics for various cationic and anionic drugs.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery Systems

Background:

  • Sustained release dosage forms are crucial for improving therapeutic efficacy and patient compliance.
  • Developing stable drug complexes that exhibit predictable release profiles remains a significant challenge in pharmaceutical formulation.

Purpose of the Study:

  • To prepare and characterize a water-insoluble complex of diltiazem hydrochloride (HCl) and sodium deoxycholate for sustained release applications.
  • To investigate the drug release kinetics from tablets and hydroxypropylmethylcellulose (HPMC) carrier systems incorporating the diltiazem complex.
  • To evaluate the influence of pH, polymer viscosity, drug solubility, and drug amine type on the release characteristics.

Main Methods:

  • Preparation of a water-insoluble diltiazem HCl-sodium deoxycholate complex.
  • Physicochemical characterization using differential scanning calorimetry, (1)H-nuclear magnetic resonance, and Fourier transform infrared spectroscopy.
  • In vitro dissolution studies of drug-complex tablets and HPMC-based formulations across various pH conditions and polymer grades.

Main Results:

  • The formation of an ionic complex between diltiazem HCl and sodium deoxycholate was confirmed by spectroscopic and thermal analyses.
  • Drug release from drug-complex/HPMC formulations was sustained (>24 h), with pH dependence minimized at neutral pH and reduced at acidic pH.
  • Drug release kinetics became linear or near-linear, irrespective of HPMC viscosity, due to a shift from drug diffusion to polymer erosion as the primary release mechanism.
  • Release profiles were consistent across various cationic and anionic drugs, indicating broad applicability of the complexation approach.

Conclusions:

  • The diltiazem HCl-sodium deoxycholate complex effectively facilitates sustained drug release.
  • Incorporation into HPMC carriers transforms the release mechanism to polymer erosion, ensuring predictable and linear release kinetics.
  • This complexation strategy offers a versatile platform for developing sustained release formulations for a wide range of drugs.