Home About us Editorial board Search Ahead of print Current issue Archives Submit article Instructions Subscribe Contacts Login 
    Users Online: 419
Home Print this page Email this page Small font size Default font size Increase font size
Year : 2012  |  Volume : 1  |  Issue : 3  |  Page : 143-150

Formulation and characterization of colon specific drug delivery system of prednisolone

1 Department of Pharmaceutics, K.L.E. University's College of Pharmacy, Vidyanagar, Hubli, Karnataka, India
2 Research Student, Department of Pharmaceutics, K.L.E. University's College of Pharmacy, Vidyanagar, Hubli, Karnataka, India
3 Department of Pharmacognosy, K.L.E. University's College of Pharmacy, Vidyanagar, Hubli, Karnataka, India
4 Department of Pharmacy, Fenny Pharmacy, New Jersey, USA

Correspondence Address:
Fatima Sanjeri Dasankoppa
Department of Pharmaceutics, K.L.E. University's College of Pharmacy, Vidyanagar, Hubli, Karnataka
Login to access the Email id

Source of Support: None, Conflict of Interest: None

DOI: 10.4103/2278-0521.106084

Rights and Permissions

Background: Enteric-coated systems are most commonly used for colonic drug delivery and constitute a majority of commercially available preparations for colon targeting. This pH variation in different segments of gastrointestinal has been exploited for colon-specific delivery. Coating the drug core with pH-sensitive polymers, these polymers are insoluble in acidic media, but dissolves at a pH of 6 or more, thereby providing protection to the drug core in the stomach and to some extent in the SI releasing the drug in the colon. Aim: The present study aimed to statistically optimize a colon-specific drug delivery system of prednisolone for the treatment of inflammatory bowel disease. Materials and Methods: A 3 2 full factorial design was used for optimization. The independent variables employed were amount of hydroxyethyl guar (HEG) and % CWG each at three levels. The dependent variables were % CDR at 5 hours, % CDR at 12 hours, and t50% (time required for 50% drug release). The tablets were prepared by the wet granulation method using novel guar gum derivative HEG as a polysaccharide. The formulated tablets were evaluated for weight variation, thickness, hardness, friability, drug content, and swelling index. The tablets were coated with 10% w/v solution of Eudragit L100 and Eudragit S100 (1:4) in IPA using 20% w/w triethyl citrate as plasticizer. The coated tablets were evaluated for in vitro dissolution studies in different pH media mimicking the transit of tablet from stomach to colon. Results and Conclusions: Differential scanning calorimetry studies showed no incompatibility of drug with other excipients. The optimized formulation F9 containing 30% HEG and 9% CWG showed 10.09% drug release after 5 hours (lag phase) and 60.76% drug release after 12 hours. Drug release was accelerated in the presence of rat caecal contents and indicated the degradation of polysaccharide by colonic microflora. The optimized formulation was subjected to an in vivo X-ray imaging study in albino rabbit to trace the movement and behavior of the tablet in gastrointestinal tract. A short-term stability study of the optimized formulation showed no significant changes in physical appearance, drug content, and in vitro dissolution profile when stored at 40 ± 2°C/75 ± 5% RH for 3 months. The designed system can be potentially used as a carrier for colon delivery of prednisolone by regulating drug release in stomach and small intestine.

Print this article     Email this article
 Next article
 Previous article
 Table of Contents

 Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
 Citation Manager
 Access Statistics
 Reader Comments
 Email Alert *
 Add to My List *
 * Requires registration (Free)

 Article Access Statistics
    PDF Downloaded660    
    Comments [Add]    
    Cited by others 2    

Recommend this journal