Bis (1-aziridinyl)(hexahydro-1H-azepin-1-yl)phosphine sulfide, an active anticancer agent with low hematopoietic toxicity in animals and man, was recommended several years ago for breast cancer adjuvant chemotherapy as an alternate drug to thiotepa. This hope had led to the syntheses of aziridinylallylaminophosphine oxides or sulfides (compounds I-XVII) in our laboratories. The resurgent interest in this area of cancer chemotherapy encouraged us to report our synthetic work as well as their evaluation as both anticancer agents and insect chemosterilants. Based on observed antitumor activity in animals, low chemosterilant activity in female species (insects and rats), and histochemical observation of tissue toxicity in rat testes but not in ovaries, these new agents are of potential interest to the breast cancer adjuvant chemotherapy program.
Background:
Abiraterone acetate is a derivative of steroidal progesterone, used as a first-line therapy for metastatic castration of prostate cancer.
Objective:
The present study encompasses the design of an experiment approach for developing a simple, reliable, and rapid RP-HPLC method for the estimation of abiraterone acetate.
Method:
The chromatographic separation was efficiently conducted on a Hypersil Gold C18 (50 x 4.6 mm, 5 µm) HPLC column, using the mobile phase composition of acetonitrile: dibasic potassium phosphate (0.01 mM) in the ratio of 80:20 (%v/v) at pH 6.5 with an isocratic elution mode. Furthermore, the different force degradation study including hydrolysis, oxidation, thermal, and photolytic was performed for abiraterone acetate.
Result:
The dynamic linearity was established in the concentration range of 0.5-10 µg/mL with r2 of 0.9998. Furthermore, the limit of detection and the limit of quantitation were 0.0978 µg/mL and 0.3260 µg/mL. The degradation of abiraterone acetate was shown in both acidic (54.16 ± 0.247 after 24 hrs) and basic conditions (35.06 ± 0.458 after 24 hrs). Furthermore, the developed method was successfully employed to quantify abiraterone acetate in bulk powder and the solid dispersion did not show any change in the retention time.
Conclusion:
The developed method was validated according to the ICH Q2 (R1) specification, which was found to be sensitive, accurate, precise, robust, linear, and selective compared to the reported chromatographic method.
Antimetabolites have been used for some time in the treatment of malignant disorders. properties for this compound in transplanted fibrosarcoma in Swiss mice (2-4). Since the compound showed promising results in experimental cancer, it was decided to inves tigate some of its pharmacological actions.Dicetol was found to produce marked pharmacodynamic effects in experimental ani mals. Various aspects of this problem are presented in this paper.
MATERIALS AND METHODSAll experiments were carried out with mice (Swiss strain), rats (Wistar strain) and cats. Dicetol in N/250 sodium bicarbonate (pH 8) was administered in varying doses intravenously (i.v.) in mice and rats and the effects were noted. The fluid injected did not exceed 0.2 ml. It was previously ascertained that the same volume of the solvent did not produce any effects in mice. On the basis of the effect seen, the dose causing convulsions in 50% of the animals (CD,,) was calculated by the method of Litchfield and \Vilcoxon (5). The effects of dicetol on pentobarbital and ether induced sleeping time were also noted. Dicetol was injected in varying doses, i.v., followed 30 minutes later by pentobarbital sodium, 50 mg/kg, intraperitoneally (i.p.). In the ether hypnosis experiments, dicetol was injected i.v. in a dose of 40 mg/kg and 30 minutes later, the animals were placed individually under a beaker of 500 ml capacity and exposed for 2 minutes to 2 ml of ether.Since dicetol caused convulsions in mice, the effect of reserpine on dicetol induced convulsions was also studied. Reserpine was administered in a dose of 2.5 mg/kg i.p. for two consecutive days and dicetol injected 24 hours after the last dose of reserpine.
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