Classifications

• • 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
  • A61K9/007—Pulmonary tract; Aromatherapy
  • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
  • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• • 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
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
• • 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
  • A61K9/0043—Nose
• • 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
  • A61K9/10—Dispersions; Emulsions
  • A61K9/12—Aerosols; Foams
• • C—CHEMISTRY; METALLURGY
  • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
  • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
  • C09K3/00—Materials not provided for elsewhere
  • C09K3/30—Materials not provided for elsewhere for aerosols

Definitions

• This invention relates to aerosol preparations for the topical application of a medicament and particularly to a selfpropelling composition containing phenylephrine as the active therapeutic agent.
• compositions of the Thiele et al. patent are open to the objection that the surfactant is irritating to sensitive body surfaces and tissues. This is true even though this patent utilizes a small relative amount of the surfactant.
• the US. Pat. No. 2,868,691 to Porush et al. teaches the use of ethanol as a solvent or suspending agent for the medicament but as large relative amounts of this alcohol are necessary to accomplish its intended purpose these compositions have also proved to be irritating.
• vasoconstrictor The problem of preparing an aerosol composition in which the medicament is a vasoconstrictor has been particularly troublesome. These vasoconstrictors are usually to be applied to the nasal orifice in instances of head colds and allergies, at which time the mucosa is already in an inflamed, irritated state. This calls for an aerosol composition which is especially nonirritative.
• dipropylene glycol not only is nonirritating but that it serves as an excellent cosolvent with the conventional aerosol propellents to keep the vasoconstrictor in solution.
• This function of serving to codissolve the drug with the volatile propellant results in a single liquid phase composition under the pressure conditions in the container. Accurate metering is thereby obtained so that from the first to the last spray dose there is uniformity in the spray content, varying only by the proportion of liquid propellent evaporating into the headspace.
• composition is a true solution throughout and consequently it is exceptionally uniform in its entirety and there are no localized zones within the container where the concentration is higher or lower. if it is put in a pressure-sustaining glass container it will be found to be water clear and this accounts for -its uniformity and free passage through the discharge nozzle.
• a further advantage of this composition is that the spray is an exceptionally fine mist which penetrates well and is nonirritating.
• the propellant may be any of the ones described in the above mentioned patent and these propellants are incorporated herein by reference. They are halogenated hydrocarbons and although a single entity may be used, it has been found that mixtures of the halogenated hydrocarbons are especially effective as they provide a better solvent action and give lower, more desirable pressures. These mixtures are described in the above patents and also in US. Pat. Nos. 3,320,125 and 3,282,791.
• he dipropylene glycol preferably should constitute about 60 percent by weight of the total composition but it may be from 50 to 70 percent. The remainder will be tee propellant except for the vasoconstrictor which will constitute 1 percent of the composition at most.
• composition is made by the conventional methods wellknown in the art.
• EXAMPLE 3 Penylepherine HCL 0.60% by wt. Dipropylene glycol (approximately) 70.00% by wt. Pmpellant (Same) 30.00% by wt.
• EXAMPLE 4 Phenylepherine HCL 0.60% by wt. Dipropylene glycol 59.40% by wt. Propellant 40.00% by wt. Dichlorofluoromethane 40.00% by wt. Dichlorotetrafluoro ethane 60.00% by wt.
• the propellant is a mixture of specific halohydrocarbons but although this is a preferred propellant, the composition of the invention is not limited to it.
• the various halohydrocarbon propellants are known in the art as is represented for instance by the patents mentioned above; these propellants are incorporated herein by this reference.
• the essential feature of this invention is the combination of dipropylene glycol and phenylephrin in an aerosol propellant as this particular glycol acts as a cosolvent for this particular vasoconstrictor.
• the aerosol propellant may be of the nontoxic kind described in lines 15 to 51 of column 4 of the above-mentioned U.S. Pat. No. 3, 14,8
• the invention also contemplates the inclusion in the composition of other active therapeutic agents which are completely soluble therein.
• an aerosol composition for confining in a valved sealed container and comprising up to 1 percent phenylephrine as an active ingredient and a nontoxic halohydrocarbon volatile propellant, the feature involving the inclusion therein of dipropylene glycol as a cosolvent to solubilize the phenylephrine.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Engineering & Computer Science (AREA)
• Dispersion Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Otolaryngology (AREA)
• Pulmonology (AREA)
• Materials Engineering (AREA)
• Organic Chemistry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (1)

Publications (1)

Family

ID=25325514

Family Applications (1)

Country Status (2)

Cited By (4)

• 1969
  • 1969-09-11 US US857229A patent/US3608065A/en not_active Expired - Lifetime
• 1971
  • 1971-03-25 BE BE764848A patent/BE764848A/fr unknown

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