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Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquacoat ECD.
Int J Pharm. 2006 Aug 02; 318(1-2):124-31.IJ

Abstract

The objective of this study was to develop and evaluate a pulsatile multiparticulate drug delivery system (DDS), coated with aqueous dispersion Aquacoat ECD. A rupturable pulsatile drug delivery system consists of (i) a drug core; (ii) a swelling layer, comprising a superdisintegrant and a binder; and (iii) an insoluble, water-permeable polymeric coating. Upon water ingress, the swellable layer expands, resulting in the rupturing of outer membrane with subsequent rapid drug release. Regarding the cores, the lag time was shorter, when 10% (w/w) theophylline was layered on sugar cores compared with cores consisting of 100% theophylline. Regarding swelling layer, the release after lag time was fast and complete, when cross-linked carboxymethyl cellulose (AcDiSol) was used as a swelling agent. In contrast, a sustained release was achieved after the lag time, when low-substituted hydroxypropyl cellulose (L-HPC) and sodium starch glycolate (Explotab) were used as swelling agents. The optimal level of AcDiSol to achieve a fast and complete release after the lag time was 26% (w/w) (based on the weight of the coated pellets) for poorly soluble theophylline and 48% (w/w) for highly soluble propranolol HCl. The lag time can be controlled by the coating level of an outer membrane and increased with increasing coating level of the outer membrane. Outer membrane, formed using aqueous dispersion Aquacoat ECD was brittle and ruptured sufficiently to ensure fast drug release, compared to ethylcellulose membrane formed using organic solution. The addition of talc led to increase brittleness of membrane and was very advantageous because of (i) reduced sensitivity of lag time on variations in the coating level and (ii) fast and complete drug release. Drug release starts only after rupturing of outer membrane, which was illustrated by microscopical observation of pellet during release.

Authors+Show Affiliations

Mohamad A
College of Pharmacy, Department of Pharmaceutical Technology, Kelchstrasse 31, 12169 Berlin, Germany. dashevsk@zedat.fu-berlin.de
Dashevsky A
No affiliation info available

MeSH

Adrenergic beta-AntagonistsAlgorithmsBronchodilator AgentsCelluloseDrug Delivery SystemsMembranes, ArtificialPermeabilityPolymersPropranololTheophylline

Pub Type(s)

Journal Article

Language

eng

PubMed ID

16759827

Citation

Mohamad, Ahmad, and Andrei Dashevsky. "Development of Pulsatile Multiparticulate Drug Delivery System Coated With Aqueous Dispersion Aquacoat ECD." International Journal of Pharmaceutics, vol. 318, no. 1-2, 2006, pp. 124-31.
Mohamad A, Dashevsky A. Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquacoat ECD. Int J Pharm. 2006;318(1-2):124-31.
Mohamad, A., & Dashevsky, A. (2006). Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquacoat ECD. International Journal of Pharmaceutics, 318(1-2), 124-31.
Mohamad A, Dashevsky A. Development of Pulsatile Multiparticulate Drug Delivery System Coated With Aqueous Dispersion Aquacoat ECD. Int J Pharm. 2006 Aug 2;318(1-2):124-31. PubMed PMID: 16759827.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquacoat ECD. AU - Mohamad,Ahmad, AU - Dashevsky,Andrei, Y1 - 2006/04/03/ PY - 2006/01/11/received PY - 2006/03/08/revised PY - 2006/03/22/accepted PY - 2006/6/9/pubmed PY - 2007/1/31/medline PY - 2006/6/9/entrez SP - 124 EP - 31 JF - International journal of pharmaceutics JO - Int J Pharm VL - 318 IS - 1-2 N2 - The objective of this study was to develop and evaluate a pulsatile multiparticulate drug delivery system (DDS), coated with aqueous dispersion Aquacoat ECD. A rupturable pulsatile drug delivery system consists of (i) a drug core; (ii) a swelling layer, comprising a superdisintegrant and a binder; and (iii) an insoluble, water-permeable polymeric coating. Upon water ingress, the swellable layer expands, resulting in the rupturing of outer membrane with subsequent rapid drug release. Regarding the cores, the lag time was shorter, when 10% (w/w) theophylline was layered on sugar cores compared with cores consisting of 100% theophylline. Regarding swelling layer, the release after lag time was fast and complete, when cross-linked carboxymethyl cellulose (AcDiSol) was used as a swelling agent. In contrast, a sustained release was achieved after the lag time, when low-substituted hydroxypropyl cellulose (L-HPC) and sodium starch glycolate (Explotab) were used as swelling agents. The optimal level of AcDiSol to achieve a fast and complete release after the lag time was 26% (w/w) (based on the weight of the coated pellets) for poorly soluble theophylline and 48% (w/w) for highly soluble propranolol HCl. The lag time can be controlled by the coating level of an outer membrane and increased with increasing coating level of the outer membrane. Outer membrane, formed using aqueous dispersion Aquacoat ECD was brittle and ruptured sufficiently to ensure fast drug release, compared to ethylcellulose membrane formed using organic solution. The addition of talc led to increase brittleness of membrane and was very advantageous because of (i) reduced sensitivity of lag time on variations in the coating level and (ii) fast and complete drug release. Drug release starts only after rupturing of outer membrane, which was illustrated by microscopical observation of pellet during release. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16759827/Development_of_pulsatile_multiparticulate_drug_delivery_system_coated_with_aqueous_dispersion_Aquacoat_ECD_ DB - PRIME DP - Unbound Medicine ER -