Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
  • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07J—STEROIDS
  • C07J19/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 by a lactone ring
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07J—STEROIDS
  • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07J—STEROIDS
  • C07J75/00—Processes for the preparation of steroids in general

Definitions

• the invention concerns water-soluble corticoid compounds that decompose instantaneously in plasma or tissue fluid with liberation of corticoid in free form. Furthermore the invention concerns a method of producing said compounds. The compounds in question are especially effective for treating shock and shock-like conditions.
• corticoids effective against said conditions such as hydrocortisone and cognate substances in the form of an alcoholic suspension of a free corticoid mixed with aqueous infusion liquids
• corticoids effective against said conditions
• hydrocortisone and cognate substances in the form of an alcoholic suspension of a free corticoid mixed with aqueous infusion liquids
• the administration of medicines in the form of infusions has the drawback that special equipment is necessary for carrying out the infusion, which ordinarily necessitates that the patient be hospitalized.
• carrying out the preparatory measurements for the infusion is time consuming and the infusion process itself takes a long time, in most cases at least a couple of hours.
• such water-soluble corticoid compounds which in plasma or tissue fluid are split up instantaneously while giving off free corticoid are produced by contacting an aqueous solution of mono-alkalimetal salt of di-corticoidphosphate or a corresponding ammonium salt with a solution of corticoid in a solvent which is at least partly miscible with water.
• the desired product is obtained which when injected is found to have an instaneous effect corresponding to the amount of free corticoid used for the preparation.
• the amount of corticoid used as phosphate is liberated gradually in the organism. Consequently the preparation is very well suited for use in the treatment of shock or shock-like conditions.
• the reaction mixture is transformed into a homogeneous solid state in which it is stable which is shown by the fact that it dissolves to form clear solutions at the abovementioned high and in some cases even higher concentrations, which solutions when used for injections show the abovementioned effect.
• the transformation of the reaction mixture into a homogeneous solid state takes place by freeze-drying, so-called, i.e., a drying process at such low temperature that the reaction mixture stays solid. It has been found that the mixture stands the freezing very well and that the product obtained when adding thereto the amount of water necessary to form a concentrated solution dissolves spontaneously to form a clear liquid which may be injected intravenously.
• the 21-phosphates of corticoids may be used for the di-steroid-phosphate, and in connection herewith the same or another corticoid in free form may be used, subject to the condition that it has a hydroxyl group in the 11- or the 21-position. Exactly these corticoids are generally well suited for the treatment of shock or shock-like conditions.
• solvent for the steroid component any solvent or mixture of solvents which is suitable for dissolving the corticosteroid in question can be used, provided that it is partly or completely miscible with water.
• solvents may be mentioned ethanol, methanol, dioxane, pyridine, mixtures of pyridine and benzene, dimethylformamide and many others. Care must be taken that during the conversion of the reaction mixture into solid state no separation of solid steroid takes place. Such separation can inany case be easily avoided when said sensitive enough for registering it after 60 minutes.
• the analytic method used is: J. van der Vies, Acta Endocrinologica 38, 399 (1961).
• Time after injection 'y/100-30 sec., 136; 5 min., 80; FOREIGN T E 0 min., 2 5; i 0. Great Bl'ltaln.

Landscapes

• Chemical & Material Sciences (AREA)
• Health & Medical Sciences (AREA)
• Organic Chemistry (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Epidemiology (AREA)
• Pharmacology & Pharmacy (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Chemistry (AREA)
• Steroid Compounds (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=26066136

Family Applications (1)

Country Status (2)

Citations (2)

• 1956
  • 1956-05-15 FR FR57112A patent/FR5434M/fr not_active Expired
• 1966
  • 1966-04-06 US US540528A patent/US3513177A/en not_active Expired - Lifetime

Patent Citations (2)

Also Published As

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