Topical corticosteroid creams and ointments

Weaker topical steroids are utilized for thin- skinned and sensitive areas, especially areas under occlusion, such as the armpit, groin, buttock crease, breast folds. Weaker steroids are used on the face, eyelids, diaper area, perianal skin, and intertrigo of the groin or body folds. Moderate steroids are used for atopic dermatitis , nummular eczema , xerotic eczema , lichen sclerosis et atrophicus of the vulva , scabies (after scabiecide) and severe dermatitis . Strong steroids are used for psoriasis , lichen planus , discoid lupus , chapped feet, lichen simplex chronicus , severe poison ivy exposure, alopecia areata , nummular eczema, and severe atopic dermatitis in adults. [1]

Pharmacokinetic studies in men with Topicort® (desoximetasone) Ointment % with tagged desoximetasone showed no detectable level (limit of sensitivity: μg/mL) in 1 subject and and μg/mL in the remaining 2 subjects in the blood when it was applied topically on the back followed by occlusion for 24 hours. The extent of absorption for the ointment was 7% based on radioactivity recovered from urine and feces . Seven days after application, no further radioactivity was detected in urine or feces. Studies with other similarly structured steroids have shown that predominant metabolite reaction occurs through conjugation to form the glucuronide and sulfate ester.

Lewis Sarett of Merck & Co. was the first to synthesize cortisone, using a 36-step process that started with deoxycholic acid, which was extracted from ox bile . [43] The low efficiency of converting deoxycholic acid into cortisone led to a cost of US $200 per gram. Russell Marker , at Syntex , discovered a much cheaper and more convenient starting material, diosgenin from wild Mexican yams . His conversion of diosgenin into progesterone by a four-step process now known as Marker degradation was an important step in mass production of all steroidal hormones, including cortisone and chemicals used in hormonal contraception . [44] In 1952, . Peterson and . Murray of Upjohn developed a process that used Rhizopus mold to oxidize progesterone into a compound that was readily converted to cortisone. [45] The ability to cheaply synthesize large quantities of cortisone from the diosgenin in yams resulted in a rapid drop in price to US $6 per gram, falling to $ per gram by 1980. Percy Julian's research also aided progress in the field. [46] The exact nature of cortisone's anti-inflammatory action remained a mystery for years after, however, until the leukocyte adhesion cascade and the role of phospholipase A2 in the production of prostaglandins and leukotrienes was fully understood in the early 1980s.

In summary, the three bioequivalence approaches that are currently consistently accepted by regulatory authorities are bioequivalence studies with clinical endpoints, in-vivo pharmacodynamic studies (in particular VCA for topical corticosteroid products), and waivers for topical solutions. Also, most require pharmacokinetic studies if there are safety concerns relating to systemic exposure. However, it is refreshing to see that the regulatory authorities are giving credence to alternative science-based methods for demonstration of bioequivalence, rather than insistence on clinical endpoint studies.

Topical corticosteroid creams and ointments

topical corticosteroid creams and ointments

In summary, the three bioequivalence approaches that are currently consistently accepted by regulatory authorities are bioequivalence studies with clinical endpoints, in-vivo pharmacodynamic studies (in particular VCA for topical corticosteroid products), and waivers for topical solutions. Also, most require pharmacokinetic studies if there are safety concerns relating to systemic exposure. However, it is refreshing to see that the regulatory authorities are giving credence to alternative science-based methods for demonstration of bioequivalence, rather than insistence on clinical endpoint studies.

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