Pharmacokinetics and tissue distribution of cantharidin after oral administration of aqueous extracts from Mylabris in rats.

A sensitive gas chromatography-mass spectroscopy method was established for the determination of cantharidin (CTD) in rat plasma and liver homogenates. During the experiment, rats were randomly divided into two groups (low, high) and were administered aqueous extract of Mylabris compound for 7 days. Then, plasma and tissue samples were taken at different time points to study the pharmacokinetics and tissue distribution of CTD in rats. The selected reaction monitoring transitions for CTD and clofibrate (internal standard) were m/z 128 → 85 and m/z 169 → 141, respectively. The calibration curve ranged from 10.26 to 3,078 ng/ml for plasma and from 10.26 to 246.24 ng/ml for liver homogenates. The lower limits of quantification were 10.26 ng/ml for both plasma and liver. The intra- and inter-day precision and accuracy were <20% for both plasma and liver homogenates. Extraction recovery ranged from 89.21 to 103.61% for CTD in rat plasma and liver and from 83.79 to 102.74% for IS in rat plasma and liver. Matrix effects ranged from 93.06 to 110.44% for CTD and from 91.65 to 110.80% for IS.

[Study on the change of the content of cantharidin in Mylabris befere and after biortransfermation].

OBJECTIVE: To compare the change of the content of cantharidin in Mylabris before and after biotransformation. METHODS: The content of cantharidin was determined by gas chromatography (GC). The conditions of GC were as follows: HP-5 column, vanillin as internal standard, the column temperature maintained at 175 degrees for 5 min, rised to 240 degrees C at the speed of 4 degrees C/min and the remained for 5 min. RESULTS: The GC method was good reproducibility. The content of cantharidin in Myabris before and after botransformation was 0.7% and 1.29% respectively. After biotranformation, the content of cantharidin was increased. CONCLUSION: Mylabris fermentated with Trametes cinnabarina has great significance for increasing the content of cantharidn and provides experimentd basis for efficient use of Mylabris.

Determination of trace cantharidin in plasma and pharmacokinetic study in beagle dogs using gas chromatography-mass spectrometry.

The blister beetle is traditional Chinese medicine that was first discovered and used as anticancer drug in China, and cantharidin proved to be its principal active ingredient. Cantharidin-based pharmaceutical preparations are now widely used in clinics in China with good therapeutic efficacy. As a toxic anticancer drug, the therapeutic dose of cantharidin is low, and no method to determine the blood cantharidin concentration under the therapeutic dose has so far been reported. Here, we present a simple, sensitive, and reliable gas chromatography-mass spectrometry (GC-MS) method to monitor the plasma cantharidin and perform the pharmacokinetic study of cantharidin in beagle dogs. After protein precipitation by hydrochloric acid, a liquid-liquid extraction procedure using ethyl acetate was applied to extract cantharidin from plasma. An elastic quartz capillary GC column DB-5MS was used in GC-MS, the temperature was kept at 60 degrees C for 1 min, then increased to 220 degrees C at the rate of 6 degrees C/min, held there for 1 min, and then to 280 degrees C at the rate of 20 degrees C/min, held for 3 min. The extraction recovery was over 80% for all the tested specimens. The linearity ranged from 2.14 to 314.2 ng/mL, the intra- and interday precisions were both below 20%, the limit of detection was 0.5 ng/mL, and the limit of quantification was 2.14 ng/mL. Cantharidin in plasma proved to be stable during the whole period of storage, treatment, and analysis. Cantharidin demonstrated as one-compartment model after i.v. administration with an elimination half-life of 0.69 +/- 0.03 h and area under curve of 204 +/- 24 h.ng/mL. This GC-MS assay proved to have high precision, accuracy, reliability, and sensitivity, and it was suitable for determination of trace cantharidin in plasma.

[The determination of cantharidin in AIDI liquid injection by gas chromatography].

A method for the determination of cantharidin in AIDI liquid injection with gas chromatography is described. The cantharidin was extracted with dichloromethane and then determined by gas chromatography with OV-17 packed column and FID detector. Its distribution constant between dichloromethane and water was 480. The extraction recoveries of cantharidin were 99%-102%. The calibration curve was Y = -113 + 35,900X, r = 0.9999 and the detection limit was 0.02 mg/L in liquid injection. As the results showed, the method is simple, rapid, sensitive and precise for determining cantharidin in AIDI liquid injection.

A fatality due to the use of cantharides from Mylabris phalerata as an abortifacient.

A fatal case of attempting to procure abortion by the ingestion of the crude extract of cantharides from over 200 dried Mylabris phalerata is presented. The quantification of catharidin in blood, urine and liver by gas chromatography using trichloroacetic acid in the extraction process and butobarbitone as the internal standard is described. Ante- and post-mortem blood levels were found to be 0.27 and 0.11 micrograms/ml respectively. To conclude, the lack of legislative control in Hong Kong over Chinese herbal medicines is highlighted.

[Ultraviolet spectrophotometric determination of cantharidin in Mylabris].

In this study the content of cantharidin in Mylabris was analyzed quantitatively by UV. Analytical results thus obtained agree well with those by the neutralization method set forth in ChP. The average recovery of cantharidin is 99.98% and the coefficient of variation is 0.719%.