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
  • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
  • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• • H—ELECTRICITY
  • H01—ELECTRIC ELEMENTS
  • H01C—RESISTORS
  • H01C3/00—Non-adjustable metal resistors made of wire or ribbon, e.g. coiled, woven or formed as grids
  • H01C3/04—Iron-filament ballast resistors; Other resistors having variable temperature coefficient

Definitions

• This invention relates to an improved medicinal composition adapted for use on the gingival and lip surfaces as well as on the mucosa of the buccal and oral cavity in general, said surfaces and mucosa being referred to herein as the oral mucosa, in order to achieve relief of pain.
• Deciduous teeth are twenty in number and first appear at six to eight months of age. up to approximately 30 months of age and it appears that many infants are in need of some comfort of irritating symptomatology resulting from this physiologic process for approximately the first two and one-half years of their life.
• Painful conditions peculiar to the gingivae and mucosal membranes in and about the oral cavity are well known. Relief of pain associated with these conditions has been an especially diflicult problem.
• the commonly practiced dental, surgical procedure of multiple extraction of diseased teeth has'created problems of effective pain control during the post-operative period.
• a wide area of gingival tissue becomes painful and generally exhibits a local inflammatory response to the surgical trauma.
• the practice of suturing the wound in order to prevent excessive bleeding gives rise to prolonged pain during the postoperative period.
• This practice is further complicated by other advances in dental science which now permit the immediate insertion of new dentures after surgery. It is an extremely difficult process to achieve pain relief in these conditions.
• Local anesthetic agents are generally not utilized because of their transient period of activity as well as the great danger of allergic reactions arising from their multiple use.
• Relief of pain may be achieved through four fundamental methods. These are: (a) removing the underlying cause of the pain; (b) blocking the pathway of the painful impulses; (c) raising the pain threshold; or (d) suppressing the pain reaction by depressing the cortical area of the brain.
• the removal of the cause of the pain is the most desirable method of pain relief, but this is not always possible.
• pain, after surgery arises from the trauma to the tissues and will disappear when this injury has been resolved. During the period of healing, however, pain will be present as a natural consequence to surgery. On the other hand, in certain infectious states, the pain may be relieved to a very great degree 'and about the buccal cavity.
• the raising of the pain threshold will generally involve a central nervous system effect, this may also be achieved by modifying or altering the response at the peripheral or cellular level.
• topical local anesthetic renders the area insensitive to pain by blocking the perception of these painful stimuli. While this may be considered to be a special form of nerve blockade, it is generally recognized that the essential physiology of nerve transmission remains intact although the response of the nerve endings in their sensitivity to painful stimuli, has been altered.
• a particular advantage of the use of the product of this invention is that it will provide effective pain relief to these common and distressing painful symptoms without subjecting the patient to the noxious effects of large quantities of systemically 'acting analgesic agents, nor does this product influence the functioning of the cardiovascular system, the renal system and central nervous system as would be observed after the use of narcotic, sedative and tranqualizing medications.
• This new material may be used for infants. No allergic side reactions have been reported.
• Any water soluble salicylate as for example, choline salicylate, potassium salicylate, sodium salicylate, calcium salicylate and morpholine salicylate may be used to achieve this effect.
• choline salicylate is a preferred compound.
• an optimal concentration will be approximately 7.5 percent with an effective range of from 2 to. 10 percent.
• the preferred pH for the preparation containing choline salicylate is between pH 5.5 and pH 6.5, although a pH range of 4 to 7 may be employed.
• the preferred dosage form is a hydroalcoholic gel although an aqueous gel may be used.
• aqueous gel or hydroalcoholic gel to be used as a vehicle for the salicylate ion
• gelling agents as methyl cellulose, methylethyl cellulose, polyoxyethylene glycol, polyvinyl pyrrolidone, dextran, gum guar, algin gum, gum acacia and gum tragacanth.
• a preferred gelling agent is methyl cellulose.
• Methocel-4000 a proprietary form of methyl cellulose, has been found particularly useful. This form has a viscosity of 4000 centipoises when a 2 percent aqueous solution is maintained at 20 C.
• concentration of the gelling agent ranges from 0.1 to 4 percent, depending upon the desired viscosity of the finished gel as well as the physical properties of the particular gelling agent selected.
• the gel is prepared by dispersing the gelling compound in the selected menstrum which may be water or hydroalcoholic solutions containing from to 60 percent of alcohol, containing the appropriate quantity of the selected water soluble salicylate and the pH adjusted, if necessary, to the desired range.
• the finished gel may be flavored with appropriate aromatic substances.
• An antiseptic may be incorporated into the gel and compounds such as .cetyldimethylbenzylammonium chloride, in concentrations of from 0.005 to 0.05 percent; penicillin and penicillin salts, from 100,000 to 1 million units per gram; tyrothrycin from 2 to 5 mg. per gram; tetracyline, from 5 to mg. per gram and neomycin, 5 mg. per gram, may be utilized.
• compounds such as .cetyldimethylbenzylammonium chloride, in concentrations of from 0.005 to 0.05 percent; penicillin and penicillin salts, from 100,000 to 1 million units per gram; tyrothrycin from 2 to 5 mg. per gram; tetracyline, from 5 to mg. per gram and neomycin, 5 mg. per gram, may be utilized.
• the alcoholic solution is then mixed with the aqueous solution while stirring and the whole gently warmed to about 50 C. and filtered.
• the solution is brought to proper volume with additional quantities of water. On cooling, a clear viscous gel forms which is suitable for application to the painful area.
• the aqueous dispersion of the gelling agent is added slowly, with constant stirring, to the warmed (to 4050 C.) alcohol solution prepared earlier.
• the mixture is filtered and the pH of the solution determined.
• the pH is then adjusted to ph 6 with choline base, or with salicylic acid, depending on whether the original pH of the mixture is greater or lesser than pH 6.
• the dispersion is then brought to proper volume, gm., with distilled water, and allowed to cool. On cooling the mixture forms a semisolid g'el, suitable for application to the oral mucosa.
• the antiseptic may be omitted.
• Example 2 In place of the choline salicylate used there may be substituted any water soluble salicylate, as for example, sodium salicylate, potassium salicylate, calcium salicylate and morpholine salicylate, in a concentration of from 2 to 10 percent by weight of salicylate ion of the quantity of gel prepared. If necessary, the pH of the gel should then be adjusted to approximately pH 5-7 by the addition of the required amount of non-toxic acid or base.
• any water soluble salicylate as for example, sodium salicylate, potassium salicylate, calcium salicylate and morpholine salicylate, in a concentration of from 2 to 10 percent by weight of salicylate ion of the quantity of gel prepared. If necessary, the pH of the gel should then be adjusted to approximately pH 5-7 by the addition of the required amount of non-toxic acid or base.
• Example 3 In place of cetyldimethylbenzylammonium chloride used in Example 1 there may be substituted, in respective amounts, such germicidal substances as: penicillin and penicillin salts in concentration of from 100,000 to 1 million units per gram of preparation; tyrothricin, from 2 to 5 mgm. per gram of preparation; tetracycline, from 5 to 15 mg. per gram of preparation; and neomycin, 5 mg.
• germicidal substances as: penicillin and penicillin salts in concentration of from 100,000 to 1 million units per gram of preparation; tyrothricin, from 2 to 5 mgm. per gram of preparation; tetracycline, from 5 to 15 mg. per gram of preparation; and neomycin, 5 mg.
• Example 2 When it is desired to obtain relief of pain arising from the gingival mucosa or the oral mucosa, a small amount of gel containing the water soluble salicylate is applied to the affected area, from one to six times daily, depending upon the severity of the pain. Gentle massage is used to assure penetration, and an even distribution. A prompt relief of pain results after application.
• a small amount of the gel In applying the gel to relieve the pain resulting from new dentures, a small amount of the gel. is applied directly to the gingival surface and an additional quantity may be distributed over the surface of the denture, coming in contact with the gingival tissue.
• the applications may be repeated as often as is necessary although from 1 to 6 times daily is the preferred regimen.
• a small amount of the gel is applied directly to the affected area. Pain relief will be prompt without a numbing sensation and the applications of the agent may be repeated from 1 to 4 times daily.
• An analgesic preparation for the application to the oral mucosa comprising a gel selected from the group consisting of aqueous and hydroalcoholic gels and a water soluble salicylate compound dissolved in said gel, said preparation having a pH of from pH 4 through pH 7 and the salicylate ion content of said compound being from 2 percent to percent by weight of said preparation.
• An analgesic preparation for application to the oral mucosa comprising a gel selected from the group consisting of aqueous and hydroalcoholic gels and choline salicylate dissolved in said gel, the salicylate ion content of said choline Salicylate being from 2 percent to 10' percent by weight of said preparation and the pH of said preparation being from pH 4 through pH 7.
• An analgesic preparation for application to the oral mucosa comprising a gel selected from the group consisting of aqueous and hydroalcoholic gels and morpholine. salicylate dissolved in said gel, the salicylate ion con, tent of said morpholine salicylate being from 2 percent to 10 percent by weight of said preparation and the pH of said preparation being from pH 4 through pH 7.
• An analgesic preparation for application to the oral mucosa comprising a gel selected from the group consisting of aqueous and hydroalcoholic gels and sodium sa- 8 licylate dissolved in-said gel, the salicylateion content of. said sodium salicylate being from 2 to 10' percent by weight of said preparation and the pH of said preparation being from pH 4 through pH 7.
• FRANK CACCIAPAGLIA, JR;, EUGENE FRANK,

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• Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Nutrition Science (AREA)
• Physiology (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Microelectronics & Electronic Packaging (AREA)
• Engineering & Computer Science (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

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Cited By (13)

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Citations (1)

• 0
  • BE BE626627D patent/BE626627A/xx unknown
  • NL NL287272D patent/NL287272A/xx unknown
  • NL NL31756D patent/NL31756C/xx active
• 1962
  • 1962-04-26 US US190235A patent/US3257276A/en not_active Expired - Lifetime
  • 1962-12-31 GB GB49070/62A patent/GB979909A/en not_active Expired

Patent Citations (1)

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