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Influence of Poloxamer188 on the Intestinal Transport of Diltiazem Hydrochloride

Abstract

Background: Many Excipients are known to interact with P - gp and CYP enzyme system thereby limiting the oral bioavailability. The present study was aimed to investigate the influence of polox amer 188(with different concentrations) pretreatment on the intestinal transp ort of Diltiazem Hydrochloride. Methods: The transport of Diltiazemacross different parts of rat intestine was studied by everted and non - everted sac methods. The control and poloxamer 188 (0.25%, 0.5% and 1% for 7 days) pre - treated rats were sacrificed an d isolated the intestine. The sacs of intestine were prepared, treated with Diltiazemsolution and then placed i n dulbeccos buffer. Samples were collected periodically and the drug content was estimated using HPLC. Results and conclusion: The results show that there was a significant (p<0.05) difference in the transport of Diltiazem from the intestinal sacs of pretreated with poloxamer 188 and control. Pretreatment with Poloxamer d ecreased drug exsorption in everted studies and increased transport in non ev erted studies compared to control indicating the inhibition of P - gp transporter and CYP3A enzyme respectively.

Hafsa Rana, Sunitha B , Shravan Kumar Y* , Avinash M

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