betadex and cryptotanshinone

1. The study aimed to investigate the pharmacokinetics of cryptotanshinone in a hydroxylpropyl-beta-cyclodextrin-included complex in dogs and rats. 2. Animals were administrated the inclusion complex of cryptotanshinone and the concentrations of cryptotanshinone and its major metabolite tanshinone IIA were determined by a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. 3. Cryptotanshinone in inclusion complex was absorbed slowly after an oral dose, and the C(max) and AUC(0-)(t) were dose-proportional. The bioavailability of cryptotanshinone in rats was (6.9% +/- 1.9%) at 60 mg kg(-1) and (11.1% +/- 1.8%) in dogs at 53.4 mg kg(-1). The t(1/2) of the compound in rats and dogs was 5.3-7.4 and 6.0-10.0 h, respectively. Cryptotanshinone showed a high accumulation in the intestine, lung and liver after oral administration, while the lung, liver and heart had the highest level following intravenous dose. Excretion data in rats showed that cryptotanshinone and its metabolites were mainly eliminated from faeces and bile, and the dose recovery rate was 0.02, 2.2, and 14.9% in urine, bile, and faeces, respectively. 4. The disposition of cryptotanshinone in an inclusion complex was dose-independent and the bioavailability was increased compared with that without cyclodextrin used to formulate the drug. Cryptotanshinone was distributed extensively into different organs. Excretion of cryptotanshinone and its metabolites into urine was extremely low, and they were mainly excreted into faeces and bile.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Abietanes; Administration, Oral; Animals; beta-Cyclodextrins; Cardiovascular Agents; Dogs; Drugs, Chinese Herbal; Drugs, Investigational; Female; Male; Phenanthrenes; Phenanthrolines; Rats; Salvia miltiorrhiza; Tissue Distribution

To prepare cryptotanshinone (CT)-cyclodextrin inclusion compound and improve dissolution of CT.. Inclusion ratio was determined by plotting the phase solubility curve of CT versus hydroxypropyl-beta-cyclodextrin (HPCD). CT-cyclodextrin inclusion compound was made by wet grinding method. Properties of the inclusion compound was investigated by in vitro dissolution test, DTA and IR spectrum.. Inclusion ratio of CT versus HPCD was 1:1. Dissolution of CT-HPCD inclusion compound at 45 min was 21.6 times of material drug.. Dissolution of CT was improved remarkably in CT-HPCD inclusion compound. The complexation force of the inclusion compound was hydrogen bond formed by carbonyl group of CT and hydroxyl group of HPCD.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; beta-Cyclodextrins; Biological Availability; Drug Carriers; Drugs, Chinese Herbal; Phenanthrenes; Salvia miltiorrhiza; Solubility; Technology, Pharmaceutical; Time Factors

The inclusion complexes of beta-cyclodextrin (beta-CD) and HP-beta-cyclodextrin (HP-beta-CD) with a kind of tanshinone, cryptotanshinone (CTan) were investigated by using spectrophotometry. Stable inclusion complexes were established in solution and in solid state and were characterized by UV, IR and 1H NMR spectra, respectively. The optimum pH for inclusion is about 7.5. Stoichiometry of the inclusion complex is 1:1. The stabilities of beta-CD and HP-beta-CD to CTan were in the order: beta-CD

Topics: 2-Hydroxypropyl-beta-cyclodextrin; beta-Cyclodextrins; Cyclodextrins; Hydrogen-Ion Concentration; Magnetic Resonance Spectroscopy; Phenanthrenes; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet; Thermodynamics