Phospholipid complex (Phytosome) is a relatively stable compound or complex formed by charge migration between drugs and phospholipid molecules. It can change the physical and chemical properties of the parent drug, improve bioavailability, and has a simple preparation method and low cost. In recent years, its application in pharmaceutical preparations has gradually increased, especially in the research of traditional Chinese medicine phospholipid complexes. It has made great achievements J. This article reviews the current research status of phospholipid complexes in traditional Chinese medicine as follows.
The formation mechanism and basic characteristics of phospholipid complexes
In the phospholipid structure, the oxygen atom in the hydroxyl group on the phosphorus atom has a strong tendency to gain electrons, while the nitrogen atom has a strong tendency to lose electrons. Electronic tendencies, so under certain conditions, it can form complexes with drug molecules of a certain structure. For example, in the structure of scutellarin, the oxygen on the carboxyl group and the oxygen on the phenolic hydroxyl group are both negatively charged, and can generate dipole-dipole interactions with the positively charged quaternary ammonium nitrogen in lecithin to form a complex; Puerarin and lecithin combine through van der Waals forces between polar sites to form phospholipid complex J. After the drug forms a complex with the phospholipid, the physical and chemical properties, biological activity, etc. will be greatly changed, showing many characteristics that are different from the parent drug. Changes in physical and chemical properties such as fat solubility are significantly enhanced, melting point, absorption coefficient, spectral characteristics, etc. will also be significantly changed. Changes in biological activity, such as the activity of phospholipid complexes, are generally stronger, more bioavailable, and less toxic and side effects than the parent drug.
Preparation and identification of phospholipid complexes
There have been many research reports on the preparation of phospholipid complexes. The usual method is to place drugs and phospholipids in aprotic solvents such as aromatic hydrocarbons, Halogen derivatives or some cyclic ethers (such as tetrahydrofuran, chloroform, methanol, diethyl ether, dioxane, etc.) are prepared by heating, stirring, refluxing and other means. The prepared complex can be obtained by evaporation or removal of the solvent under vacuum, or can be isolated by freeze-drying or non-solvent precipitation. Factors such as the selection of reaction solvent, reaction time, reaction temperature, concentration of reactants, and the ratio of drug to phospholipid will affect the binding rate of the drug. The optimal preparation formula and process can be screened through experiments.