Preparation And Characterization Of Novel Pharmaceutical Co-crystal

Preparation and characterization of novel pharmaceutical co-crystalIn recent decades, with the rapid development of crystal engineering, supramolecular chemistry and the pharmaceutical co-crystal, more and more people are concerned about the development of new solid crystalline form which is synthesized by self-assembled. This article mainly introduces the application of designed and prepared targeting pharmaceutical co-crystal by API and CCF. Pharmaceutical co-crystal has a wide range of application in the pharmaceutical sciences, nonlinear chemistry, biochemistry, pharmacology direction of science and so on. Pharmaceutical co-crystal which is mostly based by hydrogen bond and its advantages has been gradually revealed. Through hydrogen bonds form pharmaceutical co-crystal do not need to form a new covalent bonds or destroy covalent bonds, and it can be greatly modified a series of chemical properties and pharmacological properties of drugs. Therefore, the advantage of pharmaceutical co-crystal has been gradually revealed in the pharmaceutical industry.This thesis is based on synthesizing new drugs, the synthetic methods including traditional slow solvent evaporation method, solvothermal synthesis and grinding etc. pharmaceutical co-crystal is a new solid form of drugs, it can improve physical and chemical properties of drugs, such as stability, melting point, solubility, cited moist, metabolic stability, dispersion rate, dissolution rate, drug release, mechanical properties and bioavailability. It becomes the international forefront of crystal engineering and focus at the present stage. The reparation of the pharmaceutical co-crystal has been applied to synthesize new drugs through API and CCF. Specific contents are as follows:This thesis selects phenytoin (PHT) and acetaminophen as the drug API and uses 4,4'-bipyridine as the precursor to synthesize phenytoin co-crystal and acetaminophen co-crystal. Phenytoin is an anticonvulsant drug, it has anti-spasm and anti-epileptic effect, with a stable mood, expansion of peripheral blood vessels and lower blood pressure, also is effects for the epilepsy and the excessive force heart rate which is caused by digitalis. Phenytoin is a common and safe drug, but it isn't stability and we can improve the stability by preparing pharmaceutical co-crystal. Acetaminophen has antipyretic and analgesic for fever, uses for pain, neuralgia, migraine, cancer pain and pain after surgery etc. Acetaminophen is recognized as the United States "generally regarded as safe "(GRAS) by internationally.4,4'-bipyridine is a common pharmaceutical intermediates, has a double-based rigid linear ligand with no fork chain, sterically hindered and better bridge force. Acetaminophen is often used for synthesizing new drugs co-crystal.There are many methods for preparing drug co-crystal, the phenytoin co-crystal is used by slow solvent evaporation method and grinding method, the eutectic of acetaminophen is used in solvothermal method and grinding method. We can obtain identical crystal structure by different methods; this paper highlights the using of grinding method. The method is simple, greatly reducing the experimental period, easy to promote it in the pharmaceutical industry and avoid the tedious process. It is pharmaceutical co-crystal that has great practical value and suits with factory application.In summary, plenty of methods and principles described in the text has been significantly improving medication melting point, solubility, dissolution rate, dissolution, thermodynamic stability, chemical stability, cited moist, physical and chemical characteristics etc. Also, the preparing of pharmaceutical co-crystal can get more innovative, practical and creative drugs. At the present stage, series of relative drug cocrystal studies has been totally started; I believe the pharmaceutical co-crystal will be on the market just around the corner.