IL38375A - Anaesthetic compositions comprising a solution of 3alpha-hydroxy-5alpha-pregnane-11,20-dione in organic solvent - Google Patents

Anaesthetic compositions comprising a solution of 3alpha-hydroxy-5alpha-pregnane-11,20-dione in organic solvent

Info

Publication number
IL38375A
IL38375A IL38375A IL3837571A IL38375A IL 38375 A IL38375 A IL 38375A IL 38375 A IL38375 A IL 38375A IL 3837571 A IL3837571 A IL 3837571A IL 38375 A IL38375 A IL 38375A
Authority
IL
Israel
Prior art keywords
composition
present
water
weight
oil
Prior art date
Application number
IL38375A
Other versions
IL38375A0 (en
Original Assignee
Glaxo Lab Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxo Lab Ltd filed Critical Glaxo Lab Ltd
Publication of IL38375A0 publication Critical patent/IL38375A0/en
Publication of IL38375A publication Critical patent/IL38375A/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

1379730 Steroid anaesthetic compositions GLAXO LABORATORIES Ltd 16 Dec 1971 [17 Dec 1970] 60067/70 Heading ASB An anaesthetic composition suitable for use by injection comprises 3a-hydroxy-5a-pregnane-11, 20-dione in solution in an inert organic liquid injection medium. Water-soluble organic liquids may be employed, in which case water may be present in the solution. Specified watersoluble organic liquids are C 1 -C 6 diof polyhydric alcohols, glycerol formal, water-soluble amides (e.g. nicotinamide or N-#-hydroxyethyl lactomide) and water-soluble esters, e.g. ethyl lactate. Alternatively, water-insoluble organic liquids may be employed, especially oils such as fatty alcohols and their esters, fatty acid esters (including alkyl esters of fatty acids and vegetable oils) and hydrocarbons (including liquid paraffin, squalane, n-dodecane, n-hexadecane). Such oil solutions of steroid may be employed in the form of an aqueous emulsion wherein the oil is the continuous of the disperse phase. Such emulsions may contain a surface active component, e.g. a polyoxyethylated derivative of a fatty glyceride oil, a polyoxyethylene ether of a fatty alcohol, or polyoxyethylenepolyoxypropylene ether, a polyoxyethylated fatty acid ester of sorbiton or mannitan, a polyethylene glycol ester of a fatty acid or a phospholified. Additional ingredients which may be present are emulsion stabilising agents, surface disordering agents and additional steroids. Water-soluble substances such as dextrose, glycerol and sodium chloride, serving to render the compositions approximately isotonic with blood, may also be present. The composition may be made up in unit dosage form. (From GB1379730 A) [FR2118120A1]

Claims (1)

1. What we claim is:- 1. A composition adapted for use in medicine by injection as an anaesthetic comprising 3a-hydrox.y-5a-pregnane-ll , 20-dione in solutio in an inert organic liquid medium, as herein defined.1 2. A composition as claimed in claim 1 in the form of a solution also containing water. 3. A composition as claimed in either of claims 1 or 2. wherein the inert organic liquid medium comprises a polyhydric alcohol, a water soluble ester, or a water-soluble amide. 4. A composition as claimed in any of the. preceding claims wherein the inert organic liquid medium comprises propylene glycol, glycerol, ethyl lactate, N-^-hydroxyethyl)lactamide, glycerol formal or nicotinamide . 5. A composition as claimed in any one of claims 2 to 4 wherein 3cc~hydroxy- Sa-pregnane- 11 , 20-dione is present in an amount of 0.1-4% by weight. 6. A composition as claimed in claim 1 in the form of a non-aqueous solution. 7. A composition as claimed in claim o wherein the inert organic liquid, medium is an oil. 8. A composition as claimed in claim 7 wherein the inert organic liquid medium is an aliphatic alcohol having 10-15 carbon atoms or an ester thereof with an aliphatic carboxylic acid having 1-6 carbon atoms, an ester of a fatty acid having 12-18 carbon atoms, a hydrocarbon oil, or a vegetable oil . 9. A composition as claimed in claim 8 wherein the inert organic liquid medium is tridecyl or isopropyl myristate, isopropyl palmitate, ethyl or n-octyl oleate, liquid paraffin, n-dodecane, n-hexadecane, squalane, coconut oil, castor oil, corn 011, arachis oil, soyabean oil, or cottonseed oil. 10. A composition as claimed in any one of claims 6 to 9 wherein the 3a--hydroxy-5a-pregnane-ll , 20-dione is present in an amount of 0.1 to 3% by weight. llt, A composition as claimed in claim 1 in the form of an emulsion or micro-emulsion comprising a continuous phase comprising a water-immiscible inert organic liquid solution as claimed in any one of claims 7 to 9 and additional Av ter. 12. A composition as claimed in claim 1 in the form o an emulsio wherein the disperse phase comprises a water-immiscible inert organic liquid medium as defined in any one of claim 7 to 9 and the continuous phase comprises water. 13. A composition as claimed in claim 12 wherein a parenterally acceptable surface active component having an HLB value of Q.JtL.1 - at least 9, optionally 9-15, is present.' 14. A composition as claimed in claim 13 wherein the surface active component comprises a polyoxy-ethylated derivative of a fatty glyceride oil (having 12-20 carbon atoms) and containing 35-45 oxyethylene groups per mole of fatty oil; a polyoxyeth lene ether of an alcohol having 12-1.8 carbon atoms and containing 10-30 oxyethylene groups; a polyoxyethylene-polyoxypropylene ether containing 15-150 oxyethylene groups and 15-50 oxypropylene groups; a polyoxyethylated fatty acid (having 12-18 carbon atoms) ester of sorbitan or mannitan containing 15-30 oxyethylene groups; a polyethylene glycol ester of a fatty acid (having 12-18 carbon atotas) and containing 6-40 oxyethylene groups: or a phospholipid. 15. A composition as claimed in any one of claims 12 -33- 14 wherein a parenterally acceptable surface active component having an HLB value of 3 to '8 is additionally present as an emulsion stabilising agent. 1 16. A composition as claimed in any one of claims 12 to 15 wherein the inert organic liquid medium is present in an amount of 5 to 50% by weight. 17. A composition as claimed in any one of claims 12 to 16 wherein the surface active component is present in an amount 0.1 to 5%. by weight. 18. A composition as claimed in any one of claims 12 to 17 wherein the droplet size of the emulsion is less than 5 μπι. 19. A composition as claimed in any one of claims 12 to 18. wherein the 3a-hydroxy-5a-pregnane-ll , 20-dione is present in an amount of 0.1 to 2.5% by weight. 20. A composition as claimed in claim 1 in the form of a micro-emulsion wherein the dispersed phase comprises a water-immiscible inert organic, liquid medium as defined in any one of claims 7 to and the continuous phase comprises water. 21. A composition as claimed in claim 20 wherein a surface active component as defined in claim 13 or claim 14 is present. 22 . A composition as claimed in claim 20 or claim 21 wherein an aliphatic alcohol having at least 12 carbon atoms or a polyethylene glycol having a molecular weight of at least 4000 is present as a surface disordering agent. 23. A composition as claimed in an}' one of claims 20 to 22 wherein the surface active component and the surface disordering agent content is from 5 to 60% by weight. 24 . A composition as claimed in any one of claims 20 to 23 wherein the inert organic liquid medium is present in an amount of 5 to 30% by weight. 25 . A composition as claimed in any one of claims 20 to 24 wherein the 3a-hydroxy- 5a-pregnane- 11 , 20-dione is present in an amount of 0. 1 to 0. 6% by weight. 26 . A composition as claimed in any one of claims 1 to A , 6 to 9 , 1 1 to 18 , or 20 to 24 wherein a second of formula II, herein defined, steroid of the 5oc - regnane series ,/ having a 3a -hydroxy group, an oxo group at the 11 and 20 positions, j>5 1 and a group of the formula OR at the 21 position (where R is alkanoyl group having a straight or branched chain which may substituted or unsubstituted by a j^up_r_i^^l-iia_ ^erLL. carbooyl group or a benzoyl group, is also present. 27. A. composition as claimed in claim 26 wherein R is an acetyl group. 28. A composition as claimed in claim 26 or claim 27 wherein the weight ratio of said second steroid to the 3a-hydroxy-5<'i-pregnane-ll , 20-dione is from 1:20 to 1:1. 29. A composition as claimed in any one of claims 26 to 28 when dependent on any one of claims 2 to , wherein the 3a-hydroxy-5a-pregnane- 11 , 20-dione is present in an amount of 0.5 to 10% by weight. 30. A composition as claimed in any one of claims 26 to 28 when dependent on any one of claims & to 9. wherein the 3 31. A composition as claimed in any one of claims 26 to 2.8 when dependent on any one of claims 12 to 18, wherein the 3a-hydroxy- 5a -pregnane- 11 , 20-dione is present in an amount of 0.3 to 12% by weight. - 36
IL38375A 1970-12-17 1971-12-16 Anaesthetic compositions comprising a solution of 3alpha-hydroxy-5alpha-pregnane-11,20-dione in organic solvent IL38375A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB6006770A GB1379730A (en) 1970-12-17 1970-12-17 Pharmaceutical compositions

Publications (2)

Publication Number Publication Date
IL38375A0 IL38375A0 (en) 1972-02-29
IL38375A true IL38375A (en) 1976-07-30

Family

ID=10484946

Family Applications (1)

Application Number Title Priority Date Filing Date
IL38375A IL38375A (en) 1970-12-17 1971-12-16 Anaesthetic compositions comprising a solution of 3alpha-hydroxy-5alpha-pregnane-11,20-dione in organic solvent

Country Status (11)

Country Link
AT (1) AT333963B (en)
AU (1) AU471022B2 (en)
BE (1) BE776788A (en)
CA (1) CA970281A (en)
DE (1) DE2162593A1 (en)
FR (1) FR2118120B1 (en)
GB (1) GB1379730A (en)
IE (1) IE36705B1 (en)
IL (1) IL38375A (en)
NL (1) NL7117255A (en)
ZA (1) ZA718463B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5581735A (en) * 1978-12-14 1980-06-20 Kao Corp Emulsifier composition
JP2655190B2 (en) * 1989-06-21 1997-09-17 エスエス製薬 株式会社 Ointment containing corticosteroid
SE9302295D0 (en) * 1993-07-02 1993-07-02 Kabi Pharmacia Ab NEW PHARMACEUTICAL COMPOSITION
US6787530B1 (en) 1996-08-23 2004-09-07 Monash University Use of pregnane-diones as analgesic agents
AU2019396217A1 (en) * 2018-12-10 2021-07-08 Halo Science LLC Stable formulations of anesthetics and associated dosage forms

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL91070C (en) * 1900-01-01
DE1262509B (en) * 1962-04-19 1968-03-07 Hoechst Ag Process for the production of aqueous solutions of steroid hormones
FR6555M (en) * 1967-05-03 1968-12-23

Also Published As

Publication number Publication date
IL38375A0 (en) 1972-02-29
ATA1082571A (en) 1976-04-15
FR2118120B1 (en) 1976-04-16
AU471022B2 (en) 1976-04-08
GB1379730A (en) 1975-01-08
ZA718463B (en) 1973-08-29
BE776788A (en) 1972-06-16
CA970281A (en) 1975-07-01
IE36705B1 (en) 1977-02-02
AT333963B (en) 1976-12-27
DE2162593A1 (en) 1972-07-06
FR2118120A1 (en) 1972-07-28
AU3695971A (en) 1973-06-21
NL7117255A (en) 1972-06-20
IE36705L (en) 1972-06-17

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