ABSTRACT
OBJECTIVE: To study the influence and mechanism of bioactive ingredients of Ligusticum chuanxiong Hort. on the transport of gastrodin based on cell culture model in vitro. METHODS: Cell toxicity of gastrodin, ligustilide, senkyunolide I and senkyunolide A were detected by MTT assay. The transport mechanism of gastrodin and the influence of ligustilide, senkyunolide I and senkyunolide A on the transport of gastrodin were studied in MDCK-MDR1 monolayer cells. The changed expressions of P-gp caused by ligustilide, senkyunolide I and senkyunolide A were analyzed by Western blotting. RESULTS: Gastrodin showed relatively poor absorption in MDCK-MDR1 cells for its apparent permeability coefficients were less than 1×10-6 cm·s-1. P-gp inhibitor made the Papp(B→A)/Papp(A→B) of gastrodin reduced from 1.29 to 0.79, which indicated that the transport of gastrodin was influenced by P-gp. In the presence of ligustilide(30 μg·mL-1) or senkyunolide I(120 μg·mL-1), the Papp(A→B) of gastrodin in MDCK-MDR1 were significantly increased(P<0.01). In the presence of senkyunolide A(120 μg·mL-1), the Papp(A→B) of gastrodin in MDCK-MDR1 were markedly increased(P<0.05). High, medium and low dose of ligustilide, senkyunolide A and senkyunolide I could significantly inhibit the expression of P-gp protein. CONCLUSION: The results indicate that the transport mechanism of gastrodin might be passive diffusion as the dominating process with the active transportation mediated mechanism involved. Ligustilide, senkyunolide A and senkyunolide I increase the transport of gastrodin attribute to down-regulate P-gp expression.
ABSTRACT
Aromatic traditional Chinese medicines have a long history in China, with wide varieties. Volatile oils are active ingredients extracted from aromatic herbal medicines, which usually contain tens or hundreds of ingredients, with many biological activities. Therefore, volatile oils are often used in combined prescriptions and made into various efficient preparations for oral administration or external use. Based on the sources from the database of Newly Edited National Chinese Traditional Patent Medicines (the second edition), the author selected 266 Chinese patent medicines containing volatile oils in this paper, and then established an information sheet covering such items as name, dosage, dosage form, specification and usage, and main functions. Subsequently, on the basis of the multidisciplinary knowledge of pharmaceutics, traditional Chinese pharmacology and basic theory of traditional Chinese medicine, efforts were also made in the statistics of the dosage form and usage, variety of volatile oils and main functions, as well as the status analysis on volatile oils in terms of the dosage form development, prescription development, drug instruction and quality control, in order to lay a foundation for the further exploration of the market development situations of volatile oils and the future development orientation.
Subject(s)
Humans , Databases, Pharmaceutical , Drug Therapy , Medicine, Chinese Traditional , Nonprescription Drugs , Oils, Volatile , Classification , Therapeutic Uses , Outcome Assessment, Health Care , Phytotherapy , Plant Oils , Classification , Therapeutic UsesABSTRACT
Responsive drug delivery system can release drug at specific time and sites, and effectively overcome the drug resistance of organisms. With such advantages as drug protection, local targeting, inhibition of enzymatic activity, memory and expression, it has good prospect of application. So far, many chemical preparations have been launched in the market. This article mainly summarizes the advance in studies on establishment methods of responsive drug delivery system, while proposing research ideas for the traditional Chinese medicine component-based responsive drug delivery system according to the multi-component, multi-link and multi-target characteristics, in the expectation of providing reference and thought for the development of the drug delivery system.
Subject(s)
Animals , Humans , Drug Delivery Systems , Methods , Drugs, Chinese Herbal , ChemistryABSTRACT
To determine the concentration of gastrodigenin in tissue homogenates with high performance liquid chromatography (HPLC) , in order to study the changes of the distribution of gastrodigenin before and after combined application in rat tissues, including heart, liver, spleen, lung, kidney and brain tissues. The study showed that gastrodigenin could be found in kidney, liver, heart, lungs, spleen and brain tissues. After the combined application of Gastrodiae Rhizoma and Ligustici Wallichii Rhizoma, the content of gastrodigenin decreased in kidney and liver to varying degrees, while increasing in lung and brain. This indicated that Ligustici Wallichii Rhizoma had certain impact on the in vivo distribution of gastrodigenin, an active ingredient in Gastrodiae Rhizoma, because it could improve gastrodigenin's distribution in lung and brain tissues. The study provides scientific basis for the combined application of Gastrodiae Rhizoma and Ligustici Wallichii Rhizoma in treating brain diseases.
Subject(s)
Animals , Female , Male , Rats , Benzyl Alcohols , Metabolism , Pharmacokinetics , Brain , Metabolism , Chromatography, High Pressure Liquid , Gastrodia , Chemistry , Kidney , Metabolism , Ligusticum , Chemistry , Liver , Metabolism , Lung , Metabolism , Spleen , MetabolismABSTRACT
Nanocrystal suspensions drug delivery system is used to solve the delivery difficulty of poorly soluble drug. However, the physical stability of liquid nanocrystal suspensions is very bad. Solid nanocrystal delivery system as a novel technology, can improve the thermokinetics stability of nanocrystal suspensions and have good clinical compliance, which can achieve stabilization of nanocrystal suspension systems as an ideal delivery system. In this paper, we reviewed the research progress of nanotechnology and solidification technology of solid nanocrystal suspension delivery system, which will give the new mirrors and thoughts on the development of solid nanocrystal delivery system.
Subject(s)
Drug Delivery Systems , Nanoparticles , Nanotechnology , Methods , Pharmaceutical Preparations , ChemistryABSTRACT
The free membrane of Eudragit L100/S100 which is pH-sensitive, colon-specific was prepared by plane casting films. The film humidity, species and amount of plasticizers, the ratio of membrane material was investigated. The rate of membrane permeability and mechanical properties were used as indicators of orthogonal experiment, and its related properties were studied. The results show that the mechanical properties of the membrane and phragmoid capacity are the best when 30% TEC was used as plasticizer; the ratio of membrane material have little effect on the rate of membrane permeability and mechanical properties. By adjusting the species and amount of plasticizers, the ratio of Eudragit L100/S100, the free membrane which is colon-specific can be obtained.
Subject(s)
Citrates , Chemistry , Humidity , Hydrogen-Ion Concentration , Permeability , Phthalic Acids , Chemistry , Plasticizers , Chemistry , Polymethacrylic Acids , Chemistry , Technology, Pharmaceutical , Methods , Tensile Strength , Transition Temperature , Triacetin , ChemistryABSTRACT
The release kinetics research of sustained-release formulations of traditional Chinese medicines (TCM) is an inalienable part of the chain of TCM modernization, which plays an important role in the development of modern compound TCM preparation. However, the research method or pattern in line with the specific characteristics of TCM, i.e., multi-component and multi-target, is still lacking. On the basis of material rough set theory, this paper reviewed the advantages and disadvantages of the existing evaluation patterns and methods, a tentative idea about the "total amount" release characteristics evaluation on TCM compound sustained-release preparation has suggested so as to evaluate the release kinetics and to promote the development of evaluation methodology on TCM sustained-release preparations.
Subject(s)
Algorithms , Delayed-Action Preparations , Drug Combinations , Drug Delivery Systems , Drugs, Chinese Herbal , Pharmacokinetics , Kinetics , Medicine, Chinese Traditional , Plants, Medicinal , ChemistryABSTRACT
Objective: To investigate and optimize the formulation of sophoridine liposomes. Methods: Sophoridine liposomes were prepared by ammonium sulfate transmembrane gradient method. On the basis of single factor experiments, the effects of influence factors, such as entrapment efficiency, drug loading, and comprehensive indexes, were investigated by using central composite design and response surface method. The influence factors included the concentration of drug and ammonium sulfate. The data were imitated using multi-linear equation and second-order polynomial equation. Results: The latter was prior to the former considering from multiple correlation coefficients. Under the optimal conditions, the entrapment efficiency and drug loading of sophoridine liposomes were 51.81% and 5.39%. Conclusion: The optimized preparation technique for sophoridine liposomes is stable and feasible.