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
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/47—Quinolines; Isoquinolines
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0048—Eye, e.g. artificial tears

Definitions

• the present invention relates to topical opthalmic compositions useful in the treatment of glaucoma. More particularly, this invention relates to anti-glaucoma agents which effectively lower intraocular pressure and to methods for the preparation and administration of such compositions.
• a further object is to topically administer such compositions to the eye in a dosage form that will significantly lower intraocular pressure while achieving the pupillary goals of a submaximally dilated and mobile pupil, retaining sensitivity to stimulation by light.
• compositions of this invention contain one of the following compounds as novel intraocular hypotensive agents:
• compositions of this invention wherein the novel hypotensive agents form the only active ingredient effectively lower intraoclar tension for some purposes it may be desirable to combine treatment with exogenous sympathomirnetic amines.
• the sympathomimetic amine can be administered with the intraocular hypotensive agent of this invention in a single vehicle in dosages which effectively lower intraocular pressure.
• exemplary of such sympathomimetic amines are epinephrine, norepinephrine and isoproterenol.
• the sympathomimetic amine can be administered following instillation of the novel hypotensive agent of this invention.
• compositions of this invention are administered topically to the eye, either in the form of opthalmic solutions, or as opthalmic ointments.
• Formulations are herein expressed as percent weight by volume and generally the dosages for the intraocular hypotensive agent fall within the range of 0.01 to 0.02 percent. Higher dosages, as for example, up to about 0.2 percent, or lower dosages can be employed, provided the dose is effective in lowering intraocular pressure, is non-irritating and achieves the desired pupillary goals previously set forth.
• compositions of this invention are incorporated into a sterile opthalmic vehicle.
• sterile opthalmic vehicles are Well known in the art and are fully described in such standard reference works as Remingtons Pharmaceutical Sciences, Martin and Cook, Mack Publishing Co., Easton, 13th 3 edition (1965). The following is a suitable example. (The percentages in the following examples refer to a percent weight by volume.)
• the 8-hydroxyquinolone and the sodium bisulfite act as anti-oxidants and can vary tenfold (the former up to about 0.1% and the latter down to about 0.03%.)
• any opthalmic anti-oxidant can be employed. These are more fully described in Remington (supra).
• Phenyl mercuric acetate is employed as a preservative. Any preservative suitable for opthalmic formulation such as those described in Remington (supra) can be employed.
• pH of the foregoing sterile vehicle is adjusted using base or acid it should be recognized that standard buffering agents such as those described in Remington (supra) or in the Merck Index, volume 7 (1960), so long as these buffering agents are suitable for opthalmic formulation, can be utilized. Thus a pH range from about 3.5-8 can be employed, although pH within the physiological range is preferred. When employing a buffered system it is preferred to utilize a pH of about 6.0 to about 8. With a buffered system pH is conventionally adjusted by adjusting the concentration and at the time altering the ratio of the buffered tonicity so as to maintain an isotonic solution.
• buffers can be used at varying pH, when pH is less than 6.0, sodium hydroxide or hydrochloric acid can conveniently be employed to adjust the pH. When using a buffered system it is preferred to adjust the range to that of the physiological pH range of about 6 to 7.5 or 8. US. Patent 3,149,035 sets forth suitable sterile vehicles for use, especially when a catechol amine, such as epinephrine, is employed in the compositions of this invention.
• compositions of this invention can also be administered as opthalmic ointments. These are compounded, for example, by mixing finely milled powdered ingredients with a small amount of white petrolatum and levigating or otherwise mixing until a uniform distribution is achieved. The balance of white petrolatum is added by geometric addition until the desired dosage form is made.
• An anti-glaucoma topical opthalmic composition comprising a topical opthalmic vehicle and 0.01 to 0.2% of a member selected from the group consisting of 10,11- dihydro 5 (3-dimethylaminopropyl)-5,10-epoxy-5H-dibenzo[a,d]cycloheptene-1l-hydroxy-imino, trans 10,1 1-dihydro 5-(3-methylaminopropyl)-5,10-epoxy-1l-hydroxy- 5H-dibenzo[a,d]cycloheptene and a non-toxic acid addition salt thereof.
• a method for lowering intraocular pressure which comprises applying topically to the eye an effective amount of a composition comprising a topical opthalmic vehicle and 0.01 to 0.2% of a member selected from the group consisting of 10,11 dihydro-5-(3-dimethylaminopropyl)- 5,10 epoxy 5H-dibenzo[a,d]cycloheptene-ll-hydroxyimino, trans 10,11 dihydro-5-(3-methylaminopropyl)-5, 10 epoxy-11-hydroxy-5H-dibenzo[a,d]cycloheptene and a non-toxic acid addition salt thereof.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Ophthalmology & Optometry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (1)

Publications (1)

Family

ID=24498471

Family Applications (1)

Country Status (8)

Cited By (4)

Citations (2)

• 1967
  • 1967-03-16 US US623540A patent/US3467756A/en not_active Expired - Lifetime
• 1968
  • 1968-02-28 NL NL6802823A patent/NL6802823A/xx unknown
  • 1968-03-04 IL IL29570A patent/IL29570A/en unknown
  • 1968-03-04 IE IE249/68A patent/IE31971B1/xx unknown
  • 1968-03-12 GB GB01980/68A patent/GB1174882A/en not_active Expired
  • 1968-03-15 BE BE712259D patent/BE712259A/xx unknown
  • 1968-03-15 FR FR144115A patent/FR7841M/fr not_active Expired
  • 1968-03-15 DE DE19681667898 patent/DE1667898A1/de active Pending

Patent Citations (2)

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