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Objective::To study the degradation of salvianolate lyophilized injection (SLI) and establish a stability-indicating analysis method. Method::UPLC-Q-TOF-MS/MS was used to conduct a qualitative study on the main components of SLI, and a stability-indicating analysis method was established for simultaneous determination of the original components of SLI and its degradation products. The stability of SLI were systematically assessed under physicochemical conditions of high temperature, oxidation, metal ions. Result::Totally 13 main active ingredients in SLI were identified, and a semi-quantitative analysis was performed. Under the conditions of high temperature, oxidation, light, trivalent ion and divalent ion, 6, 4, 3, 4 and 1 new degradation products were added respectively. The established stability-indicating analysis method can simultaneously determine the degradation products of the main components and their active components in SLI, with a good separation effect. Conclusion::According to the degradation mechanism of the main ingredients in SLI, macromolecular polyphenol acid compounds are degraded into small molecular compounds, such as tanshinol and protocatechu aldehyde by a series of reactions, like benzofuran open-loop, hydrolysis of ester bond and removal of DSS. The stability-indicating analysis method can be used for the stability quality control of traditional Chinese medicine Salvianolate Lyophilized Injection (SLI).
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Objective: Biopharmaceutics classification system (BCS) of five main pharmacological/toxic components (gallic acid, emodin, stilbene glycoside, physcion, and emodin-8-O-β-D-glucoside) of Polygoni Multiflori Radix Praeparata (PMRP) were carried out. Methods: The solubility and permeability of each representative component were studied by equilibrium solubility method and everted intestinal sac method, respectively. Using two softwares (Pipeline Pilot 7.5, ChemDraw 7.0) to predict the solubility and permeability parameters of each component. Classical BCS classification of measured and predicted values of representative components was conducted according to Food and Drug Administration (FDA) standards, and their correlation was evaluated. Results: The emodin, emodin-8-O-β-D-glucoside, and physcion in PMRP was preliminary determined as BCS IV drugs. THSG and gallic acid belong to BCS III drugs, and permeability was the main limiting factor in their absorption process. There was software which predicts false positives of anthraquinone in BCS classification studies. Conclusion: In this study, five main pharmacodynamic/toxic components of PMRP were classified by BCS method, which provided data support and technical reference for in vivo absorption prediction and in vitro safety evaluation of traditional Chinese medicine.
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Objective To synthesize amino-modified Fe3O4 nanoparticles (MNP-NH2) and study the adsorption of flavonoids and organic acids by MNP-NH2. Methods MNP-NH2 were synthesized and characterized by transmission electron microscopy, scanning electron microscopy, Fourier transform infrared spectroscopy, and vibrating sample magnetometer analysis; The adsorption rule of MNP-NH2 was discussed by studying the adsorption properties of 12 monomers. The adsorption properties of MNP-NH2 were assessed under conditions of different ultrasonic time, temperature, ionic strength, and pH. The final elution conditions were determined by L9(34) orthogonal test and the recycling performance was also considered. Results MNP-NH2 synthesized in this study have stable structure, uniform distribution, and good magnetic properties. Adsorption of 12 monomers by MNP-NH2 showed that the mechanism of adsorption was related to the number of ortho-phenolic hydroxyl groups. Ions concentration and temperature had little effect on adsorption for different compounds except pH. The optimized adsorption conditions were extraction for 40 min at 30 ℃ and the final elution conditions were determined to be 5 mL of 20% glacialacetic acid (methanol-water 60∶40) and ultrasonication for 40 min. Conclusion MNP-NH2 can be utilized to extract the effective components of Lonicerae Japonicae Flos and maintain a high adsorption rate of flavonoids. Moreover, MNP-NH2 had great recycling and reproducibility, providing new ideas for the utilization of extracting chemical compounds from complex traditional Chinese medicine and natural medicines.