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Study On Inclusion Compound Of Cyclodextrin Derivatives And Paeonol

Posted on:2010-03-04Degree:MasterType:Thesis
Country:ChinaCandidate:R F ZhangFull Text:PDF
GTID:2121360275474833Subject:Pharmaceutical Engineering
Abstract/Summary:PDF Full Text Request
Paeonol has the function of anticancer, analgesia, antiphlogistic ,cholesterol lowering and so on.It has strong activity, it was used to treatment many diseases. it has widely clinical applications and development Prospect.But paeonol has disadvantages of more volatile and poor stability slightly soluble in water ,dissolution rate was Lower and Bioavailability was not high and so on..It could not be solving basic problems of paeonol has poor water solubility and high volatility by traditional pharmaceutical adjuvant.Cyclodextrins inclusion complex technique was comprehensively applied in medicine area. Included into the cavities of cyclodextrins, the stability and dissolution of the included drugs were improved, therefore the bioavailability was increased. Moreover, some deliquescent or volatile drugs could be powderized, thus the stimulation, toxicity or the bad odor could be compromised by this technique.Therefore, people have pay more and more attention to increase the stability and solubility of drugs, and this has become an important topic in pharmaceutical research. Recently,β-CD is widely used. However, its anomalous low aqueous solubility, renal toxicity and hemoylsis serious forbid its wider utilization. So, on account of solubility, easier to form inclusion compound, and safety of drugs, it becomes necessary to modify or reconstructβ-CD.Paeonol is the object in this work. paeonol-β-cyclodextrin andβ-CD derivative inclusion complex and inclusion tablets have been prepared, the character of SPE7-β-CD inclusion tablets and paeonol bulk drug tablets was also compared.The content and result of this study as follows:①Method of continue change of molar concentration has been used to ensure the ratio of CD and paeonol. Six inclusion compounds of Pae-β-CD, Pae-M-β-CD, Pae-HP-β-CD, Pae-SPE1-β-CD,Pae-SPE4-β-CD and Pae-SPE7-β-CD were prepared by using ultrasonic method. Inclusion rate, dosage of drug in inclusion compounds, yield and dissolution rate have been researched, and inclusion rate and dissolution rate were regarded as the main factor to value the compounds, and the six inclusion compounds have been valued. It showed that the inclusion result was as follows: SPE7-β-CD> SPE4-β-CD > SPE1-β-CD> M-β-CD>HP-β-CD>β-CD.②The phase-solubilization data of Pae toβ-CD,M-β-CD,HP-β-CD,SPE1-β-CD SPE4-β-CD and SPE7-β-CD were determined under the temperature of 25℃, 37℃and 45℃. The result indicated that the solubilization of Pae inβ-CD,M-β-CD,HP-β-CD,SPE1-β-CD,SPE4-β-CD and SPE7-β-CD was improved notably, of which SPE7-β-CD was the best.③the orthogonal design was adopted to screen the formulation of troche preparation of paeonol and paeonol SPE7-β-CD, and the optimum formation was: paeonol- SPE7-β-CD 106.2g, lactose 48.7g, dry starch 6.0g, 10% starch paste 3.0g, octadecanoic magnesium 0.1g. inclusion tablets were prepared; comparing with the Pae tables which have been prepared using the same prescription, the inclusion tablets dissolved obviously better.④In vitro pharmaceutical properties of inclusion tablets were determined and compared with Pae tablets. The results indicated that the dissolution property of the inclusion tablets were superior to the Pae tablets.
Keywords/Search Tags:Paeonol, SPE-β-CD, Inclusion Complexes, Phase-solubilization, orthogonal design
PDF Full Text Request
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