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Antiandrogens
Published in Sarah H. Wakelin, Howard I. Maibach, Clive B. Archer, Handbook of Systemic Drug Treatment in Dermatology, 2015
Antiandrogens are a group of drugs that block the action of androgens by two broad mechanisms: Competitive inhibition of binding of androgens (testosterone and dihydrotestosterone [DHT]) to the androgen receptor (androgen receptor antagonists).Inhibition of the enzyme 5α-reductase that converts testosterone to DHT.Androgen receptor antagonists include drugs, such as the steroidal antiandrogens, spironolactone and cyproterone acetate, which also have direct inhibitory effects on androgen synthesis, and the non-steroidal or ‘pure’ antiandrogens, flutamide and bicalutamide.
Spherical agglomeration to improve dissolution and micromeritic properties of an anticancer drug, Bicalutamide
Published in Drug Development and Industrial Pharmacy, 2019
Hitesh Dalvadi, Komal Parmar, Suryabali Yadav
Bicalutamide (BCT) is a nonsteroidal antiandrogen that is used widely in the treatment therapy of prostate cancer. It stops testosterone from reaching the cancer cells. It is not reported to cause any side effects associated with steroidal antiandrogens like cyproterone acetate and shows the absence of any known progestational activities. Elimination half-life of BCT is about one week and thus is compatible with once-daily dosing. BCT is a lipophilic drug with log P octanol/water value of 2.92, where P is the partition coefficient and depicts a very low solubility in water (<5 mg/L). Various researchers have investigated different approaches to improve the dissolution properties of BCT [16–18]. Heretofore, there is no work reported whereby micromeritic and dissolution properties of BCT have been improved by spherical crystal agglomeration technique. Hence, the authors endeavor to study the influence of processing conditions and formulation parameters on the formation of BCT agglomerates and its properties viz. micromeritic and dissolution. Principal component analysis and Box-Behnken experimental design were utilized to optimize the prepared agglomerates of BCT.