ABSTRACT
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).
ABSTRACT
The biopharmaceutical properties (solubility, permeability, etc.) of active pharmaceutical ingredients are playing an important role in understanding of disposition of drugs in the body, screening of drugs and evaluation of drug delivery system. The active ingredients of Chinese materia medica (CMM) are various and complex, the research on biopharmaceutics provides a train of thought and practical method for the prediction and research on the process of active ingredients from CMM in vivo. The multi-components system is one of the main differences between CMM and chemical medicine, and the study on biopharmaceutics of active ingredients in CMM under multi-components system has become a hot topic. The progress on biopharmaceutics of active ingredients in CMM under multi-components system was reviewed in this article, which may provide the reference for data integration, theoretical induction and system construction in this field, and provide new train of thought for the research on CMM theories and the development of CMM in the perspective of biopharmaceutics.
ABSTRACT
Nuciferin is the main active ingredients in Nelumbinis Folium， which was proved to have good hypolipidemic， antioxidative and anti-inflammatory bioactivities. Currently， pharmacokinetic studies of nuciferin showed different results based on different animal models. evaluation experiments were low-cost， stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable simulation method to evaluate the bioavailability of oral drugs. It was a scientific framework for classifying drugs or active pharmaceutical ingredients(API) according to their solubility and impermeability . In the study， BCS was applied in an active ingredient in traditional Chinese medicine(TCM)， which was consisted of numerous chemical components. To study the equilibrium solubility of nuciferine， ideal solution model， Ape blat model and polynomial model were adopted. The permeability was measured based on partition coefficient(logP) and distribution coefficient(logD). Besides， apparent permeabilities of Caco-2 cells and murine intestine tissues were evaluated. Nuciferine was classified as BCSⅠ， since it had a good solubility and permeability in all methods under acidic conditions. However， in neutral and alkaline environments， nuciferine was classified as BCSⅣ by using everted intestinal sac. It indicated that the species of experimental animals has a significant influence on the absorption of nuciferine. This experiment can provide data support to the prediction in a complex environment(medicinal materials and absorbed parts). The application of BCS on TCM ingredients provided a new method to evaluate and screen out the druggability of TCM ingredients.
Subject(s)
Animals , Humans , Mice , Aporphines , Chemistry , Biological Availability , Biological Products , Classification , Biopharmaceutics , Caco-2 Cells , Intestinal Absorption , Nelumbo , Chemistry , Permeability , Plant Leaves , Chemistry , SolubilityABSTRACT
AIM To investigate the effect of β-cyclodextrin-assisted extraction on Cassiae Semen.METHODS The chemical constituents in aqueous extract and β-cyclodextrin extract determined and analyzed by UPLC and principal component analysis had their antioxidant activities tested by six methods (protective effects on lipid peroxidation injuries induced by spontaneous liver,CCl4,H2 O2,FeSO4-vitamin C,and scavenging effects on DPPH,hydroxyl free radicals).RESULTS Compared with aqueous extract,the component content and antioxidant activity of β-cyclodextrin extract were increased by 10.476％ and 80.88％,respectively.CONCLUSION β-Cyclodextrin can effectively enhance the component extraction rate and antioxidant activity of Cassiae Semen.