20 (S) - Protopanaxadiol And Ginsenoside -Rh ₂ , Rg ₃ Hydroxypropyl-β-cyclodextrin Inclusion Complexes

Ginseng saponin is the main active ingredient of ginseng and American ginseng, of which 20 (S/R)-Protopanaxadiol as aglycone ginsenosides have some significant non-cytotoxic anti-tumor effect. More research protopanaxdiol ginsenosides have:20 (S)-Protopanaxadiol on the liver, lung, stomach and prostate cancer was significantly inhibited, Rh2 can anti-colon cancer, lung cancer, breast cancer, leukemia and nasopharyngeal cancer, Rg3 in anti-liver cancer, stomach cancer, lung cancer, melanoma, cervical cancer, and esophageal cancer has a significant effect, has been developed as "a reference capsule" as the first-line anticancer drugs for clinical application. But the three caught both insoluble in water and insoluble in oil, very low oral bioavailability, direct using, can not give full play to its efficacy, changing the mode of administration, dosaging form appropriate preparation, is a top priority. Hydroxypropyl-β-cyclodextrin (HP-β-CD) is used to increase the solubility of hydrophobic drugs in the surrounding material, the interior cavity sized to fit a lot of guest molecules, water solubility, safety, and soluble in aqueous alcohol, kidney toxicity is low, hardly gastrointestinal absorption after oral administration, distribution of blood and urine rarely, mostly excreted with the feces, when parenteral administration, form complexes with the drug, the drug has release promoting effect, make rapid release of the drug in the body, which is then excreted in the urine, low surfactant essentially no hemolytic and irritating, is considered to be potentially useful pharmaceutical auxiliaries and food additives. However,20 (S)--protopanoxadiol, ginsenoside Rh2 and Rg3 hydroxypropyl-β-cyclodextrin inclusion much success, especially 20 (S)-Protopanaxadiol inclusion study uncommon reported.One main purpose of this paper is 20 (S)--protopanoxadiol, ginsenoside Rh2 and Rg3 were inclusion, inclusion and preferably the best condition; the other is the inclusion of the three conditions systematically comparative analysis to investigate the influence factor of carbohydrate side chains, in order to find a certain law, for other ginsenosides hydroxypropyl-β-cyclodextrin to provide some reference. The third, established a better system of quality assessment and analytical testing methods for hydroxypropyl-β-cyclodextrin inclusion.In this paper, inclusion compound was prepared by a magnetic stirrering methed. The encapsulation efficiency was measured by HPLC, choosing the optimum condition for inclusion by orthogonal test, obtained the optimum condition of 20 (S)-Protopanaxadiol-hydroxypropyl-β-cyclodextrin inclusion which was 20 (S)-protopanaxadiol hydroxypropyl-β-cyclodextrin molar ratio of 1:1, inclusion time was 2h, temperature 40℃, about 34 times solubility increased after inclusion; the best inclusion condition of ginsenoside Rh2 was Rh2 and hydroxypropyl-β-cyclodextrin molar ratio of 1:3, the temperature was 50 ℃, inclusion time was 3h,about 47 times solubility increased after inclusion; The optimum condition of ginsenoside Rg3 inclusion compound was Rg3 and hydroxypropyl-β-cyclodextrin molar ratio of 1:25, inclusion time was 3h, temperature was 40 ℃, about 19 times solubility increased after inclusion.The 20 (S)-protopanoxadiol, ginsenoside Rh2 and Rg3 has the same structure, the only difference is the number of different glycosidic bonds, the encapsulation efficiency as a index, this thesis made a comparative study of the three inclusion under the same condition, as well as literature, suggesting an important factor affecting the inclusion condition difference may be the number of glycosidic bonds, and the inclusion of the amount of material used from less to more followed:no glycosidic bond< glycosidic bond containing one<glycosidic linkages containing two. However, this study is only preliminary exploration, the broad-spectrum law also requires in-depth, systematic experiment.By the standard curve, stability test, precision test, repeatability and processing recovery test, established determination of the content of the sample and evaluation system, then by DSC analysis, TLC, IR and X-ray diffraction and other analytical techniques were identified for inclusion compound, determining the formation of inclusion complexes.This paper established the method of the inclusion preparation, test methods and the verification methods, the process is simple, accurate, and on Study of 20 (S)--protopanoxadiol, ginsenoside Rh2 and Rg3 have some help, the inclusion preparation of other ginsenosides hydroxylpropyl-β-cyclodextrin also have some reference value.