There is ongoing controversy about potential differences in the influence of the anti-thyroid drugs propylthiouracil (PTU) and methimazole (MMI) on radioiodine treatment of Graves' hyperthyroidism. This retrospective study investigated the influence of PTU and MMI pre-treatment, individually or sequentially, on the outcome of iodine-131 ((131)I) therapy in 199 patients with Graves' disease who had been treated with (131)I for the first time and followed up at 3 and 6 months after treatment. Pre-treatment with PTU, or sequential PTU and MMI pre-treatment, increased the failure rate of (131)I therapy and reduced the rate of hypothyroidism. MMI pre-treatment alone had no significant influence on the results of (131)I therapy. Logistic regression analyses indicated that PTU pre-treatment and having a thyroid gland of > 60 g were both significantly related to (131)I therapy failure.
Cantharidin (CA) is partially water-soluble. Solid dispersion of CA (CA-SD) in polyethylene glycol 4000 (PEG 4000) was carried out by a solvent-fusion method to increase its dissolution rate and oral bioavailability. The physicochemical properties of this solid dispersion (SD) were evaluated immediately after preparation by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM), and the oral in vivo bioavailability was studied. In in vitro experiments CA was analyzed by high-pressure liquid chromatography (HPLC) and by gas chromatography-mass spectrometry (GC-MS) in in vivo experiments. The solubility and dissolution rate of CA were improved by the SD technique. A comparison of the pharmacokinetics between CA-SD and free CA was performed in rats. The results showed that CA-SD had a higher bioavailability than free CA after oral dosing. By comparing the AUC(0-t) of CA and CA-SD, the relative bioavailability of CA-SD to free CA was 295.4%. From these observations it could be concluded that the CA-SD has a higher absorption than pure CA and this corresponds with the dissolution result in vitro.
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