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
  • A61K31/395—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
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/12—Antivirals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/12—Antivirals
  • A61P31/20—Antivirals for DNA viruses
  • A61P31/22—Antivirals for DNA viruses for herpes viruses

Definitions

• Herpes Simplex Herpesvirus Hominis
• Herpes Simplex occurs in two antigenic tyes. Herpes febrilis and Herpes genitalis, referred as Type 1 and Type 2. Infection is usually manifested by the appearance of vesicular eruptions, oral herpetic lesions, commonly referred to as fever blisters, or cold sores about the lips in the instance of Herpes Simplex Type 1, and vesicular lesions on and about the male or female genitalia in the instance of Herpes Simplex Type 2.
• Persons with Herpes Simplex infections are likely to have recurrent periods of lesion development spaced by periods of remission. Management of the condition involves easing the itching sensation which accompanies the lesion periods, and speeding remission.
• (p-hydroxyphenyl) phthalide in amounts up to 100 milligrams, preferably 15 to 30 milligrams initially and repetitively at predetermined intervals. Because 3,3-bis (p-hydroxyphenyl) phthalide is a cathartic, there is an unpleasant side effect to its use which suggests reduced usage concentrations, but the patentee does not suggest any lower dosage will be effective in Herpes Simplex management. Summary of the Invention
• Still other objects include provision of products comprising phenol, 4,4'- (2-pyridinyl methylene) bis diacetate (ester), carriers and therapeutic agents for coapplication with phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester).
• the method includes administering such dosage orally, administering a dosage of from about 0.1 to about 9.5 milligrams of phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester), suspending the phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) in a carrier for administration, combining the phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) with a second therapeutic agent in an effective dosage for administration therewith, e.g.
• the invention further contemplates provision of a product comprising a dosage of phenol, 4,4'- (2-pyridinyl methylene) bis,- diacetate (ester) effective upon oral ingestion for management of Herpes Simplex, and less than is effective for catharsis of the person receiving the dosage and combined with an ingestible carrier.
• the product comprises a dosage between 0.1 and 9.5 milligrams, and may further comprise one or more vitamins in effective dosage, preferably free of an enteric coating.
• Phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester), commonly referred to as Bisacodyl is a diphenyl trimethane suitably prepared from 2-pyridine- carboxaldehyde condensed with phenol in the presence of sulfuric acid or other dehydrant, followed by esterification with acetic anhydride and anhydrous sodium acetate, as described in U.S.P. 2,764,590. It is a white to off-white crystalline powder slightly soluble in water but fairly soluble in common organic solvents. It is known to be used as a contact laxative, acting to increase peristalsis throughout the large intestine.
• a typical dose as a laxative is oral or rectal not less than 10 milligrams and up to 30 milligrams and is administered in an enteric coating to ensure passage to the larage intestine. It is known to inhibit glucose absorption and intestinal Na-K-ATPase activity.
• the phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) may be combined with other therapeutic agents each for its own purpose e.g. to relieve stress, or to enhance the effectiveness of the phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) when administered.
• agents as vitamins A, D, E, C, Folic acid, B-l, B-2, Niacin, B-6, and B-12, among others can be combined with the phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester).
• agents for combining with phenol, 4,4'- ⁇ 2-pyridinyl methylene) bis diacetate (ester) include amino acids, such as lysine and leucine; proteins such as gelatin and gliadin; or carbohydrates, e.g. starch, lactose and the like.
• the phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) may be suitably dispersed in a carrier, e.g. tablet or capsule carriers and components such as excipients, bulking agents, lubricants, disintegrants, dyes and the like as are known in tablet making technology for the purpose of easing the administration of the phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester).
• carrier further embraces vehicles used or useful in preparing injection form of the phenol, 4,4 ⁇ -(2-pyridinyl methylene) bis,- diacetate (ester) products of the invention, such as sesame oil and the like.
• OMPI capsule 3.35 milligrams of phenol, 4,4'-(2-pyridinyl methylene) bis,- diacetate (ester) with 490 milligrams of an aliquot of a mixture of vitamins comprising:
• Vitamin A 2500 units Vitamin D 400 units Vitamin E 15 units Vitamin C 60 mg. Folic acid 0.3 mg. Vitamin B-l 1.0 mg. Vitamin B-2 1.2 mg. Niacin 13.5 mg. Vitamin B-6 1.0 mg. Vitamin B-12 4.5 mg. blended with 2 parts of cornstarch per part of vitamin mix.
• the effective dosage rate for the CONTROL I and II treatments was 30 milligrams per 8 hours for the first day, and a like amount at 12 hour intervals
• the EXAMPLE I dosage rate was one capsule (3.35 mg. per dosage) every six to eight hours on the first day and thereafter at 8 to 12 hour intervals.
• vitamins in the EXAMPLE I formulation adds stress relief factors to the formulation to ameliorate the stress which often accompanies onset of a Herpes condition.
• a second capsule formula of the invention composition was prepared from: phenol, 4,4*-(2-pyridinyl methylene) bis diacetate (ester) 3 . 5 mg . phenacetin 350. mg . chloropheniramine maleate 3. mg . caffein 38. mg . phenylpropanolamine HCL 9. mg . by blending the ingredients eutectically.
• a tablet form of the invention dosage is prepared by blending phenol, 4,4 • -(2-pyridinyl methylene) bis diacetate (ester), 3.5 mg. , 100 mg. lactose, 100 mg. starch, and 10 mg. talc as a lubricant. It will be noted that this formulation can be packaged in capsule form with the omission of the talc and adjusting the lactose and starch concentration accordingly.
• a protein containing capsule is prepared by blending eutectically phenol, 4,4'-(2- ⁇ yridinyl methylene) bis diacetate (ester), 3.5 mg. , 200 mg. lactose, 100 mg. gliadin or gelatin protein, and about 100 mg. of the amino acid lysine.
• An intramuscular injectable formulation is prepared by blending, per dosage, 5 cc. sesame oil, 250 units of Vitamin E, and 5 mg. of phenol, 4,4'-(2-pyridinyl methylene) bis diacetate (ester).

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• 1984
  • 1984-06-11 EP EP19840902564 patent/EP0183694A4/de not_active Withdrawn
  • 1984-06-11 WO PCT/US1984/000920 patent/WO1986000016A1/en not_active Application Discontinuation
  • 1984-06-11 JP JP59502497A patent/JPS61502395A/ja active Pending

Non-Patent Citations (2)

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