Font Size: a A A

Synthesis And Characterization Of Designed Pharmaceutical Cocrystal

Posted on:2014-03-12Degree:MasterType:Thesis
Country:ChinaCandidate:L BianFull Text:PDF
GTID:2181330422468316Subject:Chemical Engineering
Abstract/Summary:PDF Full Text Request
In recent decades, more and more people are concerned about pharmaceuticalcocrystal, which is synthesized by self-assembled as a new solid form.This article is based on the synthesis of new pharmaceutical cocrystal as astarting point, it mainly introduces the application of prepared targetingpharmaceutical cocrystal of active pharmaceutical ingredient and coformers bydesigning. Here we use mechanochemical method to screen cocrystal,mechanochemical method is the preferred method of cocrystal screen. The reasons ofselecting piracetam and lamotrigine as active pharmaceutical ingredients are those:we need employ synthetic pharmaceutical cocrystal method to improve the quality ofdrugs because ofpiracetam’s poor stability. Lamotrigine needs the crystal engineeringto design solid form in order to solve the problem of poor solubility and dissolutionrate.In this paper, we describe the application of mechanochemical method to screenpiracetam with some aliphatic diacids.1:1piracetam-glutaric acid cocrystal wassuccessfully screened and identified by powder X-ray diffraction and differentialscanning calorimetry results. Followed by solution crystallization,1:1cocrystal ofpiracetam and glutaric acid was reproduced. To better understand the mechanism ofpiracetam cocrystal formation in solution crystallization, process analyticaltechnologies including Focussed Beam Reflectance Measurement, Attenuated TotalReflectance-Fourier Transform Infra-red, Particle Vision Measurement were used toinvestigate the cocrystallization process of piracetam with glutaric acid.Based on the screen cocrystal method of piracetam system, Here we firstlysynthesize2:1lamotrigine-4,4’-dipyridyl cocrystal by mechanochemical method.Followed by the powder X-ray diffraction, differential scanning calorimetry, thermalgravimetric analysis, Fourier transform infrared spectroscopy characterization havebeen used to prove the formation of the cocrystal. The same cocrystal has beenobtained through reactive crystallization, in order to further understand themechanism of the formation of lamotrigine cocrystal, Process analytical technologies are also used to on-line monitor the solution mediated phase transition between asingle component and cocrystal. Through characterization The solubility anddissolution rate are significantly improved, when compared to the pure activepharmaceutically ingredient.This paper studies how the grinding time, the amount of solvent, the kind ofsolvent affect preparation cocrystal by mechanochemical method, which has somereference value for improving the purity of the cocrystal.
Keywords/Search Tags:pharmaceutical cocrystal, piracetam, glutaric acid, lamotrigine, 4,4’-dipyridyl
PDF Full Text Request
Related items