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Statistical optimization and in vivo evaluation of colon specific delivery system of herbal rhubarb extract

Biraju Patel*, Dhaval Patel, Jayant Chavda, Ravi Manek, Dhaval Mori   

  1. 1. Department of Pharmaceutics, Smt. R.B.Patel Mahila Pharmacy College, Rajkot, Gujarat, India
    2. Department of Pharmaceutics, B.K. Mody Govt. Pharmacy College, Rajkot, Gujarat, India
  • 收稿日期:2013-04-01 修回日期:2013-05-07 出版日期:2013-11-15 发布日期:2014-01-22
  • 通讯作者: Biraju Patel*

Statistical optimization and in vivo evaluation of colon specific delivery system of herbal rhubarb extract

Biraju Patel*, Dhaval Patel, Jayant Chavda, Ravi Manek, Dhaval Mori   

  1. 1. Department of Pharmaceutics, Smt. R.B.Patel Mahila Pharmacy College, Rajkot, Gujarat, India
    2. Department of Pharmaceutics, B.K. Mody Govt. Pharmacy College, Rajkot, Gujarat, India
  • Received:2013-04-01 Revised:2013-05-07 Online:2013-11-15 Published:2014-01-22
  • Contact: Biraju Patel*

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摘要：

The present research effort was aimed to develop colon targeted drug delivery system (CTDDS) of rhubarb, herbal drug using a mixed film of pectin and ethyl cellulose (EC). Pectin and ethyl cellulose were mixed in various proportions to coat the core tablet to target colon. The methanolic extract of rhubarb was used and the dose of the extract in each formulation was finalized by estimating the emodin content in it by high performace thin layer chromatography (HPTLC). In vitro drug release, erosion study in presence and absence of pectinase enzyme and release constant (K) of zero order was measured for each formulation. The formulation was optimized by using 32 full factorial design. Formulation having 50% pectin as a coating polymer with 12% coat weight was selected as an optimized formulation (OF) on the basis of % similarity with maximum desirability but this formulation was not able to retard the release of drug in stomach and upper intestine fully. So it was further coated with Eudragit S100 (ES) (3% coat weight). The optimized formulation, coated with ES indicated significant laxative activity on loperamide induced constipation in rats. The results revealed that CTDDS of rhubarb using two combined approaches of biodegrable microflora-activated system and pH-sensitive system exhibited a promising colon targeting performance.

关键词: Rhubarb, Pectin, Ethyl cellulose, Eudragit S100, 32 Full factorial design, Y360 min

Abstract:

The present research effort was aimed to develop colon targeted drug delivery system (CTDDS) of rhubarb, herbal drug using a mixed film of pectin and ethyl cellulose (EC). Pectin and ethyl cellulose were mixed in various proportions to coat the core tablet to target colon. The methanolic extract of rhubarb was used and the dose of the extract in each formulation was finalized by estimating the emodin content in it by high performace thin layer chromatography (HPTLC). In vitro drug release, erosion study in presence and absence of pectinase enzyme and release constant (K) of zero order was measured for each formulation. The formulation was optimized by using 32 full factorial design. Formulation having 50% pectin as a coating polymer with 12% coat weight was selected as an optimized formulation (OF) on the basis of % similarity with maximum desirability but this formulation was not able to retard the release of drug in stomach and upper intestine fully. So it was further coated with Eudragit S100 (ES) (3% coat weight). The optimized formulation, coated with ES indicated significant laxative activity on loperamide induced constipation in rats. The results revealed that CTDDS of rhubarb using two combined approaches of biodegrable microflora-activated system and pH-sensitive system exhibited a promising colon targeting performance.

Key words: Rhubarb, Pectin, Ethyl cellulose, Eudragit S100, 32 Full factorial design, Y360 min

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*Corresponding author. Tel.: +91-9979022666

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