ABSTRACT
Sodium carboxymethyl cellulose is an excellent pharmaceutical excipient. It possesses good filmability, mucoadhesiv-ity, viscolising capacity and bindability. The current aim of our research work is to synthesize a novel colon targeting polymer by using sodium carboxymethyl cellulose and glycine for colon targeting and to screen its colon specificity by in-vitro release model. Sodium carboxymethyl cellulose was subjected for synthesizing its derivative with glycine using azo linkage. The azo polymeric conjugate was evaluated for its color, solubility, Rf value, melting point, IR and 1HNMR spectral analysis. It was further subjected for evaluating its colon targeting property by in-vitro method using rat fecal matter. The research study revealed that the sodium carboxymethyl cellulose azo derivative showed promising colon specificity for a period of 120 minutes in a controlled manner along with modified solubility. So it can serve as a potential colon targeting polymer.
ABSTRACT
Sodium carboxymethyl cellulose is an excellent pharmaceutical excipient. It possesses good filmability, mucoadhesiv-ity, viscolising capacity and bindability. The current aim of our research work is to synthesize a novel colon targeting polymer by using sodium carboxymethyl cellulose and glycine for colon targeting and to screen its colon specificity by in-vitro release model. Sodium carboxymethyl cellulose was subjected for synthesizing its derivative with glycine using azo linkage. The azo polymeric conjugate was evaluated for its color, solubility, Rf value, melting point, IR and 1HNMR spectral analysis. It was further subjected for evaluating its colon targeting property by in-vitro method using rat fecal matter. The research study revealed that the sodium carboxymethyl cellulose azo derivative showed promising colon specificity for a period of 120 minutes in a controlled manner along with modified solubility. So it can serve as a potential colon targeting polymer.
ABSTRACT
AIM: To explore the transport and delivery of active drug from dexamethasone-angelica sinensis polysaccharides prodrug in the gastrointestinal tract of rats. METHODS: Dexamethasone and the prodrug were orally administered to rats at the dose of 1.96 mg?kg~ -1 (calculated by carried dexamethasone). The drugs in the plasma and contents of different parts of the rats' gastrointestinal tract were determined by high performance liquid chromatography (HPLC). RESULTS: Dexamethasone carried by the prodrug was mainly released in the contents and mucosa of cecum and colon after oral administration of the prodrug. The absorption of released dexamethasone was reduced significantly. The peak time, peak concentration and AUC were 7.2 h , 42 ?g?L~ -1 and 334 ?g?h?L~ -1 , respectively. However, free dexamethasone was found mainly in the contents and mucosa of the stomach, proximal and distal small intestine after oral administration. The peak time, peak concentration and AUC were 2.2 h, 2 120 ?g?L~ -1 and 11 875 ?g?h?L~ -1 , respectively. CONCLUSION: Dexamethasone can be specifically delivered to the cecum and colon by using dexamethasone- angelica sinensis polysaccharides prodrug. The absorption of dexamethasone was reduced significantly and the drug concentration in colon was increased significantly. The prodrug has a potential in the treatment of colitis.