Related Experiment Video
Updated: Dec 21, 2025
09:11
Alternating Magnetic Field-Responsive Hybrid Gelatin Microgels for Controlled Drug Release
Published on: February 13, 2016
10.1K
Robustness of Controlled Release Tablets Based on a Cross-linked Pregelatinized Potato Starch Matrix
D Elgaied-Lamouchi1,2, N Descamps2, P Lefèvre2
1University of Lille, Inserm, CHU Lille, U1008, 59000, Lille, France.
AAPS Pharmscitech
|May 22, 2020
Summary
Cross-linked potato starch shows promise as a controlled-release tablet matrix former. It maintains tablet integrity and exhibits stable drug release across various conditions, similar to hydroxypropyl methylcellulose (HPMC).
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery Systems
Background:
- Controlled-release drug delivery systems are crucial for optimizing therapeutic efficacy and patient compliance.
- Matrix formers play a vital role in modulating drug release profiles.
- Hydrogels, including modified starches and cellulose derivatives, are commonly used as matrix formers.
Purpose of the Study:
- To evaluate the potential of cross-linked pregelatinized potato starch (PREGEFLO® PI10) as a matrix former for controlled-release tablets.
- To compare its performance against hydroxypropyl methylcellulose (HPMC) grades.
- To assess drug release kinetics under diverse physiological and environmental conditions.
Main Methods:
- Tablets containing diprophylline, diltiazem HCl, or theophylline (20-50% drug content) were prepared by direct compression using PREGEFLO® PI10 or HPMC.
- Drug release studies were conducted in various media, including acidic, buffered, and simulated physiological fluids (gastric, intestinal, colonic).
- Release experiments utilized USP apparatuses I, II, and III, with optional simulation of mechanical stress.
Main Results:
- Cross-linked potato starch tablets demonstrated drug release kinetics largely unaffected by environmental variations, similar to HPMC tablets.
- Starch-based tablets maintained structural integrity (increased size, minimal erosion) in release media, unlike HPMC tablets which showed more pronounced swelling.
- Water penetration into the starch matrix was significantly less pronounced compared to HPMC.
Conclusions:
- Cross-linked pregelatinized potato starch (PREGEFLO® PI10) is a viable matrix former for controlled-release tablets.
- It offers comparable drug release stability to HPMC but with superior structural integrity and reduced water uptake.
- This starch derivative presents an interesting alternative for developing robust controlled-release formulations.
Related Concept Videos
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
137
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
137
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
329
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...
329
01:18Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules
122
Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
122
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
101
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
101
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
595
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
595
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
415
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
415