Basic drug--enterosoluble polymer coevaporates: development of oral controlled release systems

Ramprakash Govindarajan; Mangal S Nagarsenker

doi:10.1081/DDC-200034572

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Basic drug--enterosoluble polymer coevaporates: development of oral controlled release systems

Journal article

Peer reviewed

Basic drug--enterosoluble polymer coevaporates: development of oral controlled release systems

Ramprakash Govindarajan and Mangal S Nagarsenker

Drug development and industrial pharmacy, Vol.30(8), pp.847-857

09/2004

DOI: 10.1081/DDC-200034572

PMID: 15521330

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Abstract

Precipitation of basic drugs within oral prolonged release systems, at the higher pH values of the intestine, would affect drug release. Coevaporates of a model basic drug verapamil HCl, in single or mixed polymer systems, containing Eudragit L100 (L100) and ethyl cellulose or Eudragit RS100, were prepared from ethanolic solution. XRD and DSC indicated loss of crystallinity of the drug in the coevaporates. The presence of the enterosoluble polymer in the system was found to aid in faster dissolution of the drug at higher pH values. This was affected by the presence and type of retarding polymer present in the system. Compression of the coevaporates resulted in either very slow release of the drug or undesirable changes in the release profile. Pelletization of a coevaporate containing drug and L100 yielded systems, which released the drug uniformly when studied by the buffer change method in simulated gastric (SGF) and intestinal (SIF) fluids. The presence of L100 in intimate contact with the drug was found to be essential for the desirable drug release properties of the system. The drug release occurred predominantly by diffusion in SGF and by a combination of diffusion and polymer dissolution/erosion in SIF. Appropriate choice of release modifiers and formulation variables and development of suitable formulations can yield systems which compensate for the reduced solubility of the drug in the higher pH environments of the intestine.

Chemistry, Pharmaceutical - methods

Excipients - pharmacokinetics

Delayed-Action Preparations - chemistry

Plasticizers - chemistry

Gastric Juice - physiology

Cellulose - chemistry

Excipients - chemistry

Volatilization

Delayed-Action Preparations - pharmacokinetics

Cellulose - pharmacokinetics

Cellulose - analogs & derivatives

Administration, Oral

Gastric Juice - drug effects

Crystallization

Intestinal Secretions - physiology

Verapamil - pharmacokinetics

Technology, Pharmaceutical - methods

Polymethacrylic Acids - chemistry

Diffusion - drug effects

Particle Size

Plasticizers - pharmacokinetics

Intestinal Secretions - drug effects

Polymers - pharmacokinetics

Polymethacrylic Acids - pharmacokinetics

Polymers - chemistry

Hydrogen-Ion Concentration

Details

Title: Subtitle: Basic drug--enterosoluble polymer coevaporates: development of oral controlled release systems
Creators: Ramprakash Govindarajan - Bombay College of Pharmacy, Mumbai, India
Mangal S Nagarsenker
Resource Type: Journal article
Publication Details: Drug development and industrial pharmacy, Vol.30(8), pp.847-857
Publisher: England
DOI: 10.1081/DDC-200034572
PMID: 15521330
ISSN: 0363-9045
eISSN: 1520-5762
Language: English
Date published: 09/2004
Academic Unit: Pharmaceutical Sciences and Experimental Therapeutics
Record Identifier: 9984065693002771

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3 Times Cited - Web of Science