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Enteric coated HPMC capsules designed to achieve intestinal targeting
Ewart T Cole1, Robert A Scott, Alyson L Connor
1Capsugel Division of Pfizer Inc., Fabrikmattenweg 2, CH-4144 Arlesheim, Basel, Switzerland. ewart.cole@pfizer.com
International Journal of Pharmaceutics
|November 24, 2001
Summary
Hydroxypropyl methylcellulose (HPMC) capsules with enteric coatings demonstrated controlled drug release. Eudragit L 30 D-55 provided small bowel release, while Eudragit FS 30 D ensured colonic delivery of paracetamol.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Hydroxypropyl methylcellulose (HPMC) is a common capsule material.
- Developing controlled-release drug delivery systems is crucial for therapeutic efficacy.
Purpose of the Study:
- To evaluate the enteric coating properties of HPMC capsules using Eudragit polymers.
- To determine the gastrointestinal release profiles of paracetamol from coated HPMC capsules.
Main Methods:
- Capsules were coated with Eudragit L 30 D-55 and Eudragit FS 30 D.
- Coating uniformity was assessed using optical and scanning electron microscopy.
- In vitro dissolution studies were performed at pH 1.2 and pH 6.8.
- In vivo disintegration was visualized using gamma scintigraphy.
Main Results:
- Microscopy confirmed uniform coatings and good adhesion due to HPMC's rough surface.
- Eudragit L 30 D-55 coated capsules showed gastroresistance for 2 hours at pH 1.2.
- Eudragit FS 30 D coated capsules exhibited resistance for an additional hour at pH 6.8.
- In vivo studies showed small bowel release at 2.4 hours for Eudragit L 30 D-55 and colonic release at 6.9 hours for Eudragit FS 30 D.
Conclusions:
- HPMC capsules can be effectively enteric-coated with Eudragit polymers.
- Eudragit L 30 D-55 facilitates predominantly small intestinal drug release.
- Eudragit FS 30 D enables targeted drug delivery to the colon.