This is a list of known sex-hormonal crystalline aqueous suspension formulations. Brand names and developmental code names are in parentheses.
Testosterone buciclate is applied intramuscularly as a microcrystalline aqueous suspension. [...] After air milling [...] of crystalline testosterone buciclate to a particle size of at least 75% in the range of 10 - 50 μm, the drug was [...] suspended in sterile, aqueous suspension vehicle [...].
The following dosages for estradiol in the form of aqueous suspension injected intramuscularly, or pellets implanted subcutaneously, are recommended by a leading maunfacturer: Menopausal syndrome.—In average cases, 1 mg. intramuscularly 2 or 3 times weekly for 2 or 3 weeks; in more severe cases, 1 to 1.5 mg. Thereafter dosage is reduced to the minimum requirement, usually within the range of 0.5 to 1 mg. of estradiol twice weekly.
Estradiol, U.S.P. (AQUADiOL, PROGYNON, others), is available in aqueous suspension containing 0.5 or 1 mg/ml for intramuscular injection and as 25-mg pellets for subcutaneous implantation. Various esters of estradiol (benzoate, cypionate, enanthate, propionate, undecylate, and valerate) are prepared in aqueous suspensions or oily solutions for slow release after intramuscular injection. These preparations contain 0.5 to 40 mg/ml and are sold under various trade names (DELESTROGEN, DEPO-ESTRADIOL, OVOCYLIN, many others). Polyestradiol phosphate (ESTRADURIN) is also available for intramuscular use in prostatic carcinoma. Various sulfate esters of Estrone, U.S.P., are available in tablets containing 0.75 to 6 mg (OGEN, others). These esters and estrone are also supplied under various trade names in aqueous suspension and oily solution containing 1 to 5 mg/ml for intramuscular injection.
The exact formulation and the size of the microcrystals is most important for duration of action. The smaller particles are more rapidly dissolved than larger ones and, hence, MPA appears more rapidly in the circulation, with more rapid elimination from the body. This is also true for the once-a-month formulation, Cyclofem. From our laboratory's data, the distribution of particle size of Cyclofem is showed in Table 2. [...] TABLE 2. Distribution of particle size of crystalline steroids in Cyclofem (aqueous suspension). Size of particle (μm): ≤4: 0.3%. 5–6: 7.3%. 6–8: 16.7%. 8–10: 29.0%. 10–13: 29.7%. 13–16: 9.9%. 16–20: 0.5%. >20: 0.1%. [...] Mego-E, containing megestrol acetate 25 mg in combination with 3.5 mg 17B-estradiol in 1 ml of aqueous microcrystalline suspension with a defined particle size range, [...]
C. Dysfunktionelle Uterusblutungen. [...] 1. Depotinjektionen. 1. Originalmethode nach KAUFMANN und OBER. Es wird 1 Amp. mit 200 mg Progesteron und 10 mg Oestradiol-Monobenzoat als Kristallsuspension (Sistocyclin) injiziert [676, 678, 679, 295, 482, 365, 434, 563, 400]. [...] Beispiele. KAUFMANN et al. [485]: 400 mg Progesteron + 20 mg Oestradiolmonobenzoat Kristallsuspension. ELERT [224] U. HERRMANN [363]: 200 mg Progesteron + 10 mg Oestradiolmono benzoat Kristallsuspension.
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In addition, testosterone isobutyrate in FOLIVIRIN, Biotika, an injection containing 25 mg testosterone isobutyrate and 2.5 mg estradiol benzoate is available. It is applied every 4-6 weeks depending on the effect.
This is a list of known sex-hormonal crystalline aqueous suspension formulations. Brand names and developmental code names are in parentheses.
Testosterone buciclate is applied intramuscularly as a microcrystalline aqueous suspension. [...] After air milling [...] of crystalline testosterone buciclate to a particle size of at least 75% in the range of 10 - 50 μm, the drug was [...] suspended in sterile, aqueous suspension vehicle [...].
The following dosages for estradiol in the form of aqueous suspension injected intramuscularly, or pellets implanted subcutaneously, are recommended by a leading maunfacturer: Menopausal syndrome.—In average cases, 1 mg. intramuscularly 2 or 3 times weekly for 2 or 3 weeks; in more severe cases, 1 to 1.5 mg. Thereafter dosage is reduced to the minimum requirement, usually within the range of 0.5 to 1 mg. of estradiol twice weekly.
Estradiol, U.S.P. (AQUADiOL, PROGYNON, others), is available in aqueous suspension containing 0.5 or 1 mg/ml for intramuscular injection and as 25-mg pellets for subcutaneous implantation. Various esters of estradiol (benzoate, cypionate, enanthate, propionate, undecylate, and valerate) are prepared in aqueous suspensions or oily solutions for slow release after intramuscular injection. These preparations contain 0.5 to 40 mg/ml and are sold under various trade names (DELESTROGEN, DEPO-ESTRADIOL, OVOCYLIN, many others). Polyestradiol phosphate (ESTRADURIN) is also available for intramuscular use in prostatic carcinoma. Various sulfate esters of Estrone, U.S.P., are available in tablets containing 0.75 to 6 mg (OGEN, others). These esters and estrone are also supplied under various trade names in aqueous suspension and oily solution containing 1 to 5 mg/ml for intramuscular injection.
The exact formulation and the size of the microcrystals is most important for duration of action. The smaller particles are more rapidly dissolved than larger ones and, hence, MPA appears more rapidly in the circulation, with more rapid elimination from the body. This is also true for the once-a-month formulation, Cyclofem. From our laboratory's data, the distribution of particle size of Cyclofem is showed in Table 2. [...] TABLE 2. Distribution of particle size of crystalline steroids in Cyclofem (aqueous suspension). Size of particle (μm): ≤4: 0.3%. 5–6: 7.3%. 6–8: 16.7%. 8–10: 29.0%. 10–13: 29.7%. 13–16: 9.9%. 16–20: 0.5%. >20: 0.1%. [...] Mego-E, containing megestrol acetate 25 mg in combination with 3.5 mg 17B-estradiol in 1 ml of aqueous microcrystalline suspension with a defined particle size range, [...]
C. Dysfunktionelle Uterusblutungen. [...] 1. Depotinjektionen. 1. Originalmethode nach KAUFMANN und OBER. Es wird 1 Amp. mit 200 mg Progesteron und 10 mg Oestradiol-Monobenzoat als Kristallsuspension (Sistocyclin) injiziert [676, 678, 679, 295, 482, 365, 434, 563, 400]. [...] Beispiele. KAUFMANN et al. [485]: 400 mg Progesteron + 20 mg Oestradiolmonobenzoat Kristallsuspension. ELERT [224] U. HERRMANN [363]: 200 mg Progesteron + 10 mg Oestradiolmono benzoat Kristallsuspension.
{{
cite web}}
: CS1 maint: archived copy as title (
link)
In addition, testosterone isobutyrate in FOLIVIRIN, Biotika, an injection containing 25 mg testosterone isobutyrate and 2.5 mg estradiol benzoate is available. It is applied every 4-6 weeks depending on the effect.