US3257276A - Oral analgesic preparation - Google Patents

Oral analgesic preparation Download PDF

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Publication number
US3257276A
US3257276A US190235A US19023562A US3257276A US 3257276 A US3257276 A US 3257276A US 190235 A US190235 A US 190235A US 19023562 A US19023562 A US 19023562A US 3257276 A US3257276 A US 3257276A
Authority
US
United States
Prior art keywords
salicylate
preparation
gel
pain
gum
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
US190235A
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English (en)
Inventor
Robert H Broh-Kahn
Ernest J Sasmor
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LAB FOR PHARMACEUTICAL DEV Inc
LABORATORIES FOR PHARMACEUTICAL DEVELOPMENT Inc
Original Assignee
LAB FOR PHARMACEUTICAL DEV Inc
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
Priority to NL287272D priority Critical patent/NL287272A/xx
Priority to NL31756D priority patent/NL31756C/xx
Priority to BE626627D priority patent/BE626627A/xx
Application filed by LAB FOR PHARMACEUTICAL DEV Inc filed Critical LAB FOR PHARMACEUTICAL DEV Inc
Priority to US190235A priority patent/US3257276A/en
Priority to GB49070/62A priority patent/GB979909A/en
Application granted granted Critical
Publication of US3257276A publication Critical patent/US3257276A/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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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)
  • General Health & Medical Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Microelectronics & Electronic Packaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
US190235A 1962-04-26 1962-04-26 Oral analgesic preparation Expired - Lifetime US3257276A (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
NL287272D NL287272A (en, 2012) 1962-04-26
NL31756D NL31756C (en, 2012) 1962-04-26
BE626627D BE626627A (en, 2012) 1962-04-26
US190235A US3257276A (en) 1962-04-26 1962-04-26 Oral analgesic preparation
GB49070/62A GB979909A (en) 1962-04-26 1962-12-31 Novel oral analgesic preparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US190235A US3257276A (en) 1962-04-26 1962-04-26 Oral analgesic preparation

Publications (1)

Publication Number Publication Date
US3257276A true US3257276A (en) 1966-06-21

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Family Applications (1)

Application Number Title Priority Date Filing Date
US190235A Expired - Lifetime US3257276A (en) 1962-04-26 1962-04-26 Oral analgesic preparation

Country Status (4)

Country Link
US (1) US3257276A (en, 2012)
BE (1) BE626627A (en, 2012)
GB (1) GB979909A (en, 2012)
NL (2) NL287272A (en, 2012)

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0026332A3 (en) * 1979-10-01 1982-02-17 Richardson-Vicks, Inc. Non-adhesive gel composition for stabilizing dentures
US4590065A (en) * 1985-04-18 1986-05-20 Colgate-Palmolive Company Stable flavor-containing dentifrice
US5192802A (en) * 1991-09-25 1993-03-09 Mcneil-Ppc, Inc. Bioadhesive pharmaceutical carrier
US5955097A (en) * 1996-10-18 1999-09-21 Virotex Corporation Pharmaceutical preparation applicable to mucosal surfaces and body tissues
US6103266A (en) * 1998-04-22 2000-08-15 Tapolsky; Gilles H. Pharmaceutical gel preparation applicable to mucosal surfaces and body tissues
US20040102429A1 (en) * 2002-02-07 2004-05-27 Modak Shanta M. Zinc salt compositions for the prevention of dermal and mucosal irritation
US20040219227A1 (en) * 2001-10-23 2004-11-04 Shanta Modak Gentle-acting skin-disinfectants and hydroalcoholic gel formulations
US20050019431A1 (en) * 2003-07-17 2005-01-27 Modak Shanta M. Antimicrobial compositions containing synergistic combinations of quaternary ammonium compounds and essential oils and/or constituents thereof
US20050048139A1 (en) * 2002-02-07 2005-03-03 Modak Shanta M. Zinc salt compositions for the prevention of dermal and mucosal irritation
US20070020342A1 (en) * 2002-02-07 2007-01-25 Modak Shanta M Non-irritating compositions containing zinc salts
US20090035390A1 (en) * 2006-01-06 2009-02-05 Modak Shanta M Compositions containing zinc salts for coating medical articles
US20090047357A1 (en) * 2005-12-22 2009-02-19 Otsuka Pharmaceutical Co., Ltd. Method of producing drug-containing wax matrix particles, extruder to be used in the method and sustained-release preparation containing cilostazol
US20150335549A1 (en) * 2012-12-20 2015-11-26 Colgate-Palmolive Company Oral Care Composition Containing Ionic Liquids

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH655656B (en, 2012) * 1982-10-07 1986-05-15
DE3243546A1 (de) * 1982-11-25 1984-05-30 Bayer Ag, 5090 Leverkusen Antimykotische mittel in gelform zur behandlung von pilzinfektionen der mundhoehle
WO1989010745A1 (en) * 1988-05-02 1989-11-16 Pomerantz, Edwin Compositions and in situ methods for forming films on body tissue

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA545560A (en) * 1957-08-27 D. Waters Richard Analgesic composition

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA545560A (en) * 1957-08-27 D. Waters Richard Analgesic composition

Cited By (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0026332A3 (en) * 1979-10-01 1982-02-17 Richardson-Vicks, Inc. Non-adhesive gel composition for stabilizing dentures
DK155866B (da) * 1979-10-01 1989-05-29 Richardson Vicks Inc Klaebefrit gelpraeparat til stabilisering af tandproteser
US4590065A (en) * 1985-04-18 1986-05-20 Colgate-Palmolive Company Stable flavor-containing dentifrice
US5192802A (en) * 1991-09-25 1993-03-09 Mcneil-Ppc, Inc. Bioadhesive pharmaceutical carrier
US5314915A (en) * 1991-09-25 1994-05-24 Mcneil-Ppc, Inc. Bioadhesive pharmaceutical carrier
US5462749A (en) * 1991-09-25 1995-10-31 Mcnell-Ppc, Inc. Bioadhesive pharmaceutical carrier
US5955097A (en) * 1996-10-18 1999-09-21 Virotex Corporation Pharmaceutical preparation applicable to mucosal surfaces and body tissues
US6290984B1 (en) 1996-10-18 2001-09-18 Virotex Corporation Pharmaceutical preparation applicable to mucosal surfaces and body tissues
US6103266A (en) * 1998-04-22 2000-08-15 Tapolsky; Gilles H. Pharmaceutical gel preparation applicable to mucosal surfaces and body tissues
US8436050B2 (en) * 2001-10-23 2013-05-07 The Trustees Of Columbia University In The City Of New York Gentle-acting skin-disinfectants and hydroalcoholic gel formulations
US20040219227A1 (en) * 2001-10-23 2004-11-04 Shanta Modak Gentle-acting skin-disinfectants and hydroalcoholic gel formulations
US20040247685A1 (en) * 2001-10-23 2004-12-09 Shanta Modak Gentle-acting skin-disinfectants and hydroalcoholic gel formulations
US8293802B2 (en) 2001-10-23 2012-10-23 The Trustees Of Columbia University Gentle-acting skin-disinfectants and hydroalcoholic gel formulations
US20100305211A1 (en) * 2001-10-23 2010-12-02 Shanta Modak Gentle-Acting Skin-Disinfectants and Hydroalcoholic Gel Formulations
US20070020342A1 (en) * 2002-02-07 2007-01-25 Modak Shanta M Non-irritating compositions containing zinc salts
US7951840B2 (en) 2002-02-07 2011-05-31 Modak Shanta M Zinc salt compositions for the prevention of dermal and mucosal irritation
USRE45435E1 (en) 2002-02-07 2015-03-24 The Trustees Of Columbia University In The City Of New York Zinc salt compositions for the prevention of dermal and mucosal irritation
US7745425B2 (en) 2002-02-07 2010-06-29 The Trustees Of Columbia University In The City Of New York Non-irritating compositions containing zinc salts
US20040102429A1 (en) * 2002-02-07 2004-05-27 Modak Shanta M. Zinc salt compositions for the prevention of dermal and mucosal irritation
US20050048139A1 (en) * 2002-02-07 2005-03-03 Modak Shanta M. Zinc salt compositions for the prevention of dermal and mucosal irritation
US20110117140A1 (en) * 2002-02-07 2011-05-19 Modak Shanta M Zinc Salt Compositions for the Prevention of Dermal and Mucosal Irritation
US20110070316A1 (en) * 2003-07-17 2011-03-24 Modak Shanta M Antimicrobial Compositions Containing Synergistic Combinations of Quaternary Ammonium Compounds and Essential Oils and/or Constituents Thereof
US7871649B2 (en) 2003-07-17 2011-01-18 The Trustees Of Columbia University In The City Of New York Antimicrobial compositions containing synergistic combinations of quaternary ammonium compounds and essential oils and/or constituents thereof
US20050019431A1 (en) * 2003-07-17 2005-01-27 Modak Shanta M. Antimicrobial compositions containing synergistic combinations of quaternary ammonium compounds and essential oils and/or constituents thereof
US9421263B2 (en) 2003-07-17 2016-08-23 The Trustees Of Columbia University In The City Of New York Antimicrobial compositions containing synergistic combinations of quaternary ammonium compounds and essential oils and/or constituents thereof
US20090047357A1 (en) * 2005-12-22 2009-02-19 Otsuka Pharmaceutical Co., Ltd. Method of producing drug-containing wax matrix particles, extruder to be used in the method and sustained-release preparation containing cilostazol
US20090035390A1 (en) * 2006-01-06 2009-02-05 Modak Shanta M Compositions containing zinc salts for coating medical articles
US8207148B2 (en) 2006-01-06 2012-06-26 The Trustees Of Columbia University In The City Of New York Compositions containing zinc salts for coating medical articles
US7759327B2 (en) 2006-01-06 2010-07-20 The Trustees Of Columbia University In The City Of New York Compositions containing zinc salts for coating medical articles
US20150335549A1 (en) * 2012-12-20 2015-11-26 Colgate-Palmolive Company Oral Care Composition Containing Ionic Liquids
US9717667B2 (en) * 2012-12-20 2017-08-01 Colgate-Palmolive Company Oral care composition containing ionic liquids

Also Published As

Publication number Publication date
NL31756C (en, 2012)
BE626627A (en, 2012)
GB979909A (en) 1965-01-06
NL287272A (en, 2012)

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