List of sex-hormonal aqueous suspensions

This is a list of known sex-hormonal crystalline aqueous suspension formulations. Brand names and developmental code names are in parentheses.

Single-drug formulations

Androstanolone[1]
Dienestrol diacetate (Farmacyrol KS)[2][3]
Diethylstilbestrol dipropionate (Cyren B)[2]
Estradiol benzoate (Agofollin Depot, Ovocyclin M)[2]
Estrone (Kestrone, Theelin)[4]
Medroxyprogesterone acetate (Depo-Provera)[5][6][7][8]
Methandriol (Notandron, Protandren)[2][9]
Progesterone (Agolutin Depot, Flavolutan, Luteosan, Lutocyclin M, Lutren)[2][10]
Testosterone (Andronaq, Sterotate, Virosterone)[11]
Testosterone buciclate (20 Aet-1, CDB-1781; never marketed)[12]
Testosterone isobutyrate (Agovirin Depot, Perandren M, Testocryst, Virex-Cryst)[13][10][3][9]
Testosterone ketolaurate (Testosid)
Testosterone nicotinate (Bolfortan, Linobol)
Testosterone phenylacetate (Perandren, Androject)
Testosterone propionate (Anertan)[2]

Multi-drug formulations

Estradiol/megestrol acetate (Mego-E, Chinese injectable No. 2)[14][5][15]
Estradiol benzoate/progesterone (Sistocyclin)[3][16]
Estradiol benzoate/testosterone isobutyrate (Femandren M, Folivirin)[17][18][19][10]
Estradiol cypionate/medroxyprogesterone acetate (Cyclofem, Lunelle)[5]
Estrone/progesterone/testosterone (Tristeron, Tristerone)[20]

References

Alan C. Sartorelli; David G. Johns (27 November 2013). Antineoplastic and Immunosuppressive Agents. Springer Science & Business Media. pp. 181–. ISBN 978-3-642-65806-8.
Heinrich Kahr (8 March 2013). Konservative Therapie der Frauenkrankheiten: Anzeigen, Grenzen und Methoden Einschliesslich der Rezeptur. Springer-Verlag. pp. 20–22. ISBN 978-3-7091-5694-0.
Willibald Pschyrembel (15 June 2011). Praktische Gynäkologie: für Studierende und Ärzte. Walter de Gruyter. pp. 598, 600, 601. ISBN 978-3-11-150424-7.
https://www.accessdata.fda.gov/drugsatfda_docs/anda/pre96/85239_Estrone%20Suspension_Medr.pdf
Sang GW (April 1994). "Pharmacodynamic effects of once-a-month combined injectable contraceptives". Contraception. 49 (4): 361–85. doi:10.1016/0010-7824(94)90033-7. PMID 8013220. 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, [...]
Garza-Flores J, Hall PE, Perez-Palacios G (1991). "Long-acting hormonal contraceptives for women". J. Steroid Biochem. Mol. Biol. 40 (4–6): 697–704. doi:10.1016/0960-0760(91)90293-e. PMID 1958567.
Gabelnick, Henry L.; Hall, Peter E. (1987). "Long-acting methods for fertility regulation". Journal of Controlled Release. 6 (1): 387–394. doi:10.1016/0168-3659(87)90092-7. ISSN 0168-3659.
Antal, E; Dick, C; Wrightiii, C; Welshman, I; Block, E (1989). "Comparative bioavailability of two medroxyprogesterone acetate suspensions". International Journal of Pharmaceutics. 54 (1): 33–39. doi:10.1016/0378-5173(89)90162-2. ISSN 0378-5173.
Hans Schuermann; Rudolf Doepfmer (13 March 2013). Fertilitätsstörungen beim Manne. Springer-Verlag. pp. 260–. ISBN 978-3-642-94784-1.
Hans Hermann Julius Hager; Walther Kern; Paul Heinz List; Hermann Josef Roth (29 July 2013). Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL). Springer-Verlag. pp. 109, 141, 178. ISBN 978-3-662-25655-8.
William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 385–394. ISBN 978-0-9828280-1-4.
Hermann M. Behre; Gerhard F. Weinbauer; Eberhard Nieschlag (13 February 1996). "Testosterone Buciclate". In Shalender Bhasin; Henry L. Gabelnick; Jeffrey M. Spieler (eds.). Pharmacology, Biology, and Clinical Applications of Androgens: Current Status and Future Prospects. John Wiley & Sons. pp. 471–480. ISBN 978-0-471-13320-9. 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 [...].
William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 314–322. ISBN 978-0-9828280-1-4.
Garza-Flores J (April 1994). "Pharmacokinetics of once-a-month injectable contraceptives". Contraception. 49 (4): 347–59. doi:10.1016/0010-7824(94)90032-9. PMID 8013219.
Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S (2014). "Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control" (PDF). World J Pharm Pharm Sci. 3 (10): 364–392. ISSN 2278-4357.
Ufer, Joachim (1968). "Die therapeutische Anwendung der Gestagene beim Menschen" [Therapeutic Use of Progestagens in Humans]. Die Gestagene [Progestogens]. Springer-Verlag. pp. 1026–1124. doi:10.1007/978-3-642-99941-3_7. ISBN 978-3-642-99941-3. 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.
Kubíková, Drahomíra (2014). "Menopauzální symptomy a hormonální substituční terapie" [Menopausal symptoms and hormone replacement therapy]. Praktické Lékárenství (in Czech). 10 (2): 68–73. ISSN 1801-2434.
Marek Josef; a kolektiv (14 May 2010). Farmakoterapie vnitřních nemocí: 4., zcela přepracované a doplněné vydání. Grada Publishing a.s. pp. 380–. ISBN 978-80-247-9524-9. 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.
Georg Arends; Heinrich Zörnig; Hermann Hager; Georg Frerichs, Walther Kern (14 December 2013). Hagers Handbuch der pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Drogisten, Ärzte u. Medizinalbeamte. Springer-Verlag. pp. 1163–. ISBN 978-3-662-36329-4.
Hormone und Psyche die Endokrinologie des Alternden Menschen: Fünftes Symposion der Deutschen Gesellschaft für Endokrinologie Freiburg (Breisgau), den 7. bis 9. März 1957. Springer-Verlag. 9 March 2013. pp. 55–. ISBN 978-3-642-87014-9.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[SartorelliJohns2013-1] Alan C. Sartorelli; David G. Johns (27 November 2013). Antineoplastic and Immunosuppressive Agents. Springer Science & Business Media. pp. 181–. ISBN 978-3-642-65806-8.

[Kahr2013-2] Heinrich Kahr (8 March 2013). Konservative Therapie der Frauenkrankheiten: Anzeigen, Grenzen und Methoden Einschliesslich der Rezeptur. Springer-Verlag. pp. 20–22. ISBN 978-3-7091-5694-0.

[Pschyrembel2011-3] Willibald Pschyrembel (15 June 2011). Praktische Gynäkologie: für Studierende und Ärzte. Walter de Gruyter. pp. 598, 600, 601. ISBN 978-3-11-150424-7.

[Estrone-FDA-Review-1979-4] ttps://www.accessdata.fda.gov/drugsatfda_docs/anda/pre96/85239_Estrone%20Suspension_Medr.pdf

[pmid8013220-5] Sang GW (April 1994). "Pharmacodynamic effects of once-a-month combined injectable contraceptives". Contraception. 49 (4): 361–85. doi:10.1016/0010-7824(94)90033-7. PMID 8013220. 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, [...]

[pmid1958567-6] Garza-Flores J, Hall PE, Perez-Palacios G (1991). "Long-acting hormonal contraceptives for women". J. Steroid Biochem. Mol. Biol. 40 (4–6): 697–704. doi:10.1016/0960-0760(91)90293-e. PMID 1958567.

[GabelnickHall1987-7] Gabelnick, Henry L.; Hall, Peter E. (1987). "Long-acting methods for fertility regulation". Journal of Controlled Release. 6 (1): 387–394. doi:10.1016/0168-3659(87)90092-7. ISSN 0168-3659.

[AntalDick1989-8] Antal, E; Dick, C; Wrightiii, C; Welshman, I; Block, E (1989). "Comparative bioavailability of two medroxyprogesterone acetate suspensions". International Journal of Pharmaceutics. 54 (1): 33–39. doi:10.1016/0378-5173(89)90162-2. ISSN 0378-5173.

[SchuermannDoepfmer2013-9] Hans Schuermann; Rudolf Doepfmer (13 March 2013). Fertilitätsstörungen beim Manne. Springer-Verlag. pp. 260–. ISBN 978-3-642-94784-1.

[HagerKern2013-10] Hans Hermann Julius Hager; Walther Kern; Paul Heinz List; Hermann Josef Roth (29 July 2013). Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL). Springer-Verlag. pp. 109, 141, 178. ISBN 978-3-662-25655-8.

[Llewellyn2011a-11] William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 385–394. ISBN 978-0-9828280-1-4.

[BhasinGabelnick1996-12] Hermann M. Behre; Gerhard F. Weinbauer; Eberhard Nieschlag (13 February 1996). "Testosterone Buciclate". In Shalender Bhasin; Henry L. Gabelnick; Jeffrey M. Spieler (eds.). Pharmacology, Biology, and Clinical Applications of Androgens: Current Status and Future Prospects. John Wiley & Sons. pp. 471–480. ISBN 978-0-471-13320-9. 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 [...].

[Llewellyn2011b-13] William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 314–322. ISBN 978-0-9828280-1-4.

[pmid8013219-14] Garza-Flores J (April 1994). "Pharmacokinetics of once-a-month injectable contraceptives". Contraception. 49 (4): 347–59. doi:10.1016/0010-7824(94)90032-9. PMID 8013219.

[BagadePawar2014-15] Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S (2014). "Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control" (PDF). World J Pharm Pharm Sci. 3 (10): 364–392. ISSN 2278-4357.

[Ufer1968-16] Ufer, Joachim (1968). "Die therapeutische Anwendung der Gestagene beim Menschen" [Therapeutic Use of Progestagens in Humans]. Die Gestagene [Progestogens]. Springer-Verlag. pp. 1026–1124. doi:10.1007/978-3-642-99941-3_7. ISBN 978-3-642-99941-3. 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.

[Kubíková2014-17] Kubíková, Drahomíra (2014). "Menopauzální symptomy a hormonální substituční terapie" [Menopausal symptoms and hormone replacement therapy]. Praktické Lékárenství (in Czech). 10 (2): 68–73. ISSN 1801-2434.

[Josefkolektiv2010-18] Marek Josef; a kolektiv (14 May 2010). Farmakoterapie vnitřních nemocí: 4., zcela přepracované a doplněné vydání. Grada Publishing a.s. pp. 380–. ISBN 978-80-247-9524-9. 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.

[ArendsZörnig2013-19] Georg Arends; Heinrich Zörnig; Hermann Hager; Georg Frerichs, Walther Kern (14 December 2013). Hagers Handbuch der pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Drogisten, Ärzte u. Medizinalbeamte. Springer-Verlag. pp. 1163–. ISBN 978-3-662-36329-4.

[Springer2013-20] Hormone und Psyche die Endokrinologie des Alternden Menschen: Fünftes Symposion der Deutschen Gesellschaft für Endokrinologie Freiburg (Breisgau), den 7. bis 9. März 1957. Springer-Verlag. 9 March 2013. pp. 55–. ISBN 978-3-642-87014-9.

List of sex-hormonal aqueous suspensions

Single-drug formulations

Multi-drug formulations

See also

References