Chemistry:List of sex-hormonal aqueous suspensions

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


Single-drug formulations

Androgens

Estrogens

Progestogens

Others

Multi-drug formulations

Estrogens and progestogens

  • Estradiol/megestrol acetate (Mego-E, Chinese injectable No. 2)[23][18][24]
  • Estradiol benzoate/progesterone (Sistocyclin)[8][25]
  • Estradiol benzoate/progesterone/lidocaine (Clinomin Forte)[26]
  • Estradiol cypionate/medroxyprogesterone acetate (Cyclofem, Lunelle)[18]

Estrogens and androgens

  • Estradiol benzoate/testosterone isobutyrate (Femandren M, Folivirin)[27][28][29][7]

Estrogens, progestogens, and androgens

  • Estrone/progesterone/testosterone (Tristeron, Tristerone)[30]

Non-sex-hormonal aqueous suspensions

Corticosteroids

Antipsychotics

See also

References

  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. https://books.google.com/books?id=aU_oCAAAQBAJ&pg=PA181. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 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. https://books.google.com/books?id=Hte1BgAAQBAJ&pg=PA20. 
  3. ↑ 3.0 3.1 Hans Schuermann; Rudolf Doepfmer (13 March 2013). Fertilitätsstörungen beim Manne. Springer-Verlag. pp. 260–. ISBN 978-3-642-94784-1. https://books.google.com/books?id=m1iqBgAAQBAJ&pg=PA260. 
  4. ↑ William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 385–394. ISBN 978-0-9828280-1-4. https://books.google.com/books?id=afKLA-6wW0oC&pg=PT385. 
  5. ↑ Hermann M. Behre; Gerhard F. Weinbauer; Eberhard Nieschlag (13 February 1996). "Testosterone Buciclate". Pharmacology, Biology, and Clinical Applications of Androgens: Current Status and Future Prospects. John Wiley & Sons. pp. 471–480. ISBN 978-0-471-13320-9. https://books.google.com/books?id=hurRyWje4DMC&pg=PA471. "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 [...]." 
  6. ↑ William Llewellyn (2011). Anabolics. Molecular Nutrition Llc. pp. 314–322. ISBN 978-0-9828280-1-4. https://books.google.com/books?id=afKLA-6wW0oC&pg=PT314. 
  7. ↑ 7.0 7.1 7.2 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. https://books.google.com/books?id=a2a0BgAAQBAJ&pg=PA141. 
  8. ↑ 8.0 8.1 8.2 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://books.google.com/books?id=vVaTnHDFzZ0C&pg=PA598. 
  9. ↑ AMA Drug Evaluations. Americal Medical Association. 1971. p. 318. https://archive.org/details/amadrugevaluatio00coun. 
  10. ↑ Drug Topics Redbook. Topics Publishing Company. 1976. p. 580. https://books.google.com/books?id=MUIeAQAAMAAJ. 
  11. ↑ John Christian Krantz; Charles Jelleff Carr; Domingo M. Aviado (1972). Krantz and Carr's Pharmacologic principles of medical practice: a textbook on pharmacology and therapeutics for students and practitioners of medicine, pharmacy, and dentistry. Williams & Wilkins. p. 1258. ISBN 9780683002928. https://books.google.com/books?id=C-tsAAAAMAAJ. 
  12. ↑ Marion E. Howard (1949). Modern Drug Encyclopedia and Therapeutic Index. Drug Publications. p. 697. https://books.google.com/books?id=ltlLAQAAMAAJ. 
  13. ↑ Vademecum International. J. Morgan Jones Publications.. 1959. p. 147. https://books.google.com/books?id=uMkrAQAAMAAJ. 
  14. ↑ Frederick H. Meyers; Ernest Jawetz; Alan Goldfien (1978). Review of Medical Pharmacology. Lange Medical Pub.. p. 400. ISBN 978-0-87041-151-9. https://books.google.com/books?id=Yg1tAAAAMAAJ. 
  15. ↑ Arthur Osol; Robertson Pratt (1973). The United States dispensatory. Lippincott. p. 498. ISBN 978-0-397-55901-5. https://books.google.com/books?id=jQy0AAAAIAAJ. "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." 
  16. ↑ Louis Sanford Goodman (1980). Goodman and Gilman's The Pharmacological Basis of Therapeutics. Macmillan. p. 1428. ISBN 978-0-02-344720-4. https://archive.org/details/goodmangilmansphe6good. "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." 
  17. ↑ https://www.accessdata.fda.gov/drugsatfda_docs/anda/pre96/85239_Estrone%20Suspension_Medr.pdf [bare URL PDF]
  18. ↑ 18.0 18.1 18.2 "Pharmacodynamic effects of once-a-month combined injectable contraceptives". Contraception 49 (4): 361–85. April 1994. 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, [...]". 
  19. ↑ "Long-acting hormonal contraceptives for women". J. Steroid Biochem. Mol. Biol. 40 (4–6): 697–704. 1991. doi:10.1016/0960-0760(91)90293-e. PMID 1958567. 
  20. ↑ 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. 
  21. ↑ 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. 
  22. ↑ Pharmacy International. McGraw-Hill International Corporation. 1950. p. 34. https://books.google.com/books?id=PNkrAQAAMAAJ. 
  23. ↑ "Pharmacokinetics of once-a-month injectable contraceptives". Contraception 49 (4): 347–59. April 1994. doi:10.1016/0010-7824(94)90032-9. PMID 8013219. 
  24. ↑ "Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control". World J Pharm Pharm Sci 3 (10): 364–392. 2014. ISSN 2278-4357. http://www.wjpps.com/download/article/1412071798.pdf. Retrieved 2019-06-09. 
  25. ↑ Ufer, Joachim (1968). "Die therapeutische Anwendung der Gestagene beim Menschen". Die Gestagene. Springer-Verlag. pp. 1026–1124. doi:10.1007/978-3-642-99941-3_7. ISBN 978-3-642-99941-3. https://books.google.com/books?id=t8GpBgAAQBAJ&pg=PA1058. "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." 
  26. ↑ "Archived copy". http://www.indufar.com.py/files/shares/prospectos/400000154.pdf. 
  27. ↑ Kubíková, Drahomíra (2014). "Menopauzální symptomy a hormonální substituční terapie" (in cs). Praktické Lékárenství 10 (2): 68–73. ISSN 1801-2434. http://www.medvik.cz/link/bmc14059249. 
  28. ↑ 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. https://books.google.com/books?id=bUqECwAAQBAJ&pg=PA380. "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." 
  29. ↑ 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. https://books.google.com/books?id=8bLwBgAAQBAJ&pg=PA1163. 
  30. ↑ 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. https://books.google.com/books?id=4NKEBwAAQBAJ&pg=PA55. 

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| group1 = Androgens
(incl. AAS)

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AR agonists
Progonadotropins
5α-Reductase
Others
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  | group4 = Others
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See also
Androgen receptor modulators
Estrogens and antiestrogens
Progestogens and antiprogestogens
List of androgens/anabolic steroids

}}



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