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Determination Of Pyrrole-imidazole Polyamide By HPLC And The Study Of Its Release Character In Drug Eluting Stents

Posted on:2012-09-04Degree:MasterType:Thesis
Country:ChinaCandidate:X R LinFull Text:PDF
GTID:2154330335982424Subject:Biochemistry and Molecular Biology
Abstract/Summary:PDF Full Text Request
Pyrrole-Imidazole Polyamides are small synthetic molecules composed of the aromatic rings of N-methyylimidazole and N-methylpyrrole amino acid, it's synthetic procedures are complicated and the post-synthesis purification work is quiet difficule. In this paper, PIP were used as the materials for the following researches:1 The recovery of Pyrrole-Imidazole Polyamide; 2 Determination of Pyrrole-Imidazole Polyamides by high-performance liquid chromatographic; 3 The release characteristic of PIP Drug eluting stents; 4 Determination of PIP in mouse vascular tissue. The main results were as follows:1 The deliquescent experiment indicated that:①The solubility of PIP was not obvious in water, methanol or acetonitrile solvent system, with ultrasound, rapid mixing and other external forces, there were still some PIP not completely dissolved.②The solubility of PIP in dimethyl sulfoxide was very obvious, it showed that the reconstructed PIP were steady by HPLC analysis, after a period of time(14d), the solution was still clear and transparent, and DMSO had no reservation in the symmetry C18 column, finally the study used 0.1% DMSO solution for PIP recovery.2 The chromatographic conditions for PIP analysis was:reversed-phase Waters symmetry C18 maintained at 35℃, the mobile phase solvent B was acetonitrile and the solvent C was 0.1%TFA(0→20min, B:23.5%→25.5%). The flow rate was 1.0 ml/min. The detection wavelength was set at 310nm. Quantitated PIP sample with external standard method, according to response signal(peak area), set up the curve of concentration as:Y = 0.0378X - 0.0956, R2 = 0.9996.3 In full release system, the PIP release content was determined as 100.75μg/ml, the release ratio >90%, while in the slow-release system, PIP can be released completely within 12 h, among them, the 1~2h period's release was 33.26μg/ml, accounted for 35.6% of total.4 Put the PIP drug eluting stents to use in the artificial lesion treated mice arterial tissue and continued to train regularly(2 weeks and 4 weeks), take part of vascular tissue to section observation, and another part for the homogenate extraction, by HPLC detected and pattern analysed, it displayed that PIP can exist in vascular tissue stably, and the main PIP peak height down from the two-week 0.0257(AU) to four-week 0.010(AU).
Keywords/Search Tags:Pyrrole-Imidazole Polyamide, high performance liquid chromatography, Drug eluting stents
PDF Full Text Request
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