WO1998017297A1

WO1998017297A1 - Method for topical treatment of nonviral epithelial disorders

Info

Publication number: WO1998017297A1
Application number: PCT/US1997/019192
Authority: WO
Inventors: Frank L. Greenway
Original assignee: Chiralt Corporation
Priority date: 1996-10-24
Filing date: 1997-10-23
Publication date: 1998-04-30
Also published as: AU4916197A

Abstract

It has been discovered that geranium oil, preferably geranium oil bourbon, can treat several nonviral epithelial disorders characterized by inflammation or lesions. For example, the geranium oil treatment can relieve the itching and limit the inflammatory response of insect bites. Geranium oil treatment can be effective in decreasing the pain, swelling, and blistering associated with skin burns. The healing time for canker sores can be decreased with geranium oil treatment. A geranium oil-water gargle is effective in relieving pain from a sore throat for an extended period of time.

Description

METHOD FOR TOPICAL TREATMENT OF NONVIRAL EPITHELIAL DISORDERS

TECHNICAL FIELD

This invention pertains to a topical treatment for several nonviral epithelial disorders characterized by inflammation or lesions.

BACKGROUND ART Pruritus or itching is a common problem, frequently associated with insect or arachnid bites or stings, e.g., those of the imported fire ants, Solenopsis richderi, found in the southern United States. Fire ant bites or stings usually cause immediate pain, then within forty-five minutes develop a lesion that gives rise to a pustule that lasts thirty to seventy hours. The lesion can also become infected by scratching and remain many days. Although topical treatments are available with an antihistamine such as calamine lotion, current topical treatments are not always effective. Topical benzocaine may not only be ineffective but also cause temporary numbness. Topical corticosteroids take hours to be effective.

Acute skin burns cause great pain, swelling, and blistering. Current topical treatments only prevent bacterial infections and do not decrease the pain, swelling, or blistering. Canker sores, recurrent aphthous stomatitis, are acute, painful ulcers on the mouth mucosa. Minor ulcers of less than one cm can persist for ten to fourteen days. Larger ulcers can last weeks or months. The cause of canker sores is unknown, but is thought to be a localized immune response that can be precipitated by stress or local trauma. Current treatments include several topical ointments, e.g., a topical anesthetic lidocaine for short term pain relief, a dental paste of triancinoline acetonide to decrease pain and promote healing, and an oral suspension of tetracycline to promote healing. In severe cases, both oral and topical corticosteroids may be prescribed.

Pharyngitis, or sore throat, is a common malady that causes considerable discomfort. This condition can be caused by a bacterial infection. People experiencing this pain often use aspirin or topical anesthetics such as lozenges that have limited, short-term effectiveness.

Geranium oil has been used in perfumes and as a food additive since the 1800's. It is on the GRAS (Generally Regarded As Safe) list of the United States Food and Drug Administration. Geranium oil is extracted from plants of the family Geraniaceae, frequently by steam distillation of fresh plants. A variety of species of geranium plants exist throughout the world. The oils extracted from most geranium plants have approximately the same chemical constituents. "Geranium oil bourbon," however, derived from Pelargonium graveolens Ait. from Reunion Island off the east African coast, has a unique composition, including a higher level of the semi-volatile alcohol citronellol than do geranium oils derived from other species and varieties.

U.S. Pat. No. 5,260,342, U.S. Pat. No. 5,126,376, U.S. Pat. No. 5,086,076, and

U.S. Pat. No. 4,983,637 describe a method of treating viral infections with terpenes that have been oxidized with ozone to produce "ozonides of terpenes. " Examples include oxidation products of limonene, citronellol, alpha-carotene, beta-carotene, vitamin A, linalool, linalyl acetate, squalene, and geraniol.

U.S. Pat. No. 5,260,313 describes a method to treat neuropathic pain syndromes resulting from Postherpetic Neuralgia or Reflex Sympathetic Dystrophy with topical application of geranium oil bourbon.

U.S. Pat. No. 4,923,685 describes antimicrobial, flavored compositions for use as mouthwashes, and includes geranium oil in a list of possible aromatic, flavoring oils. U.S. Pat. No. 4,832,947 descπoes a process to incorporate essential oils, such as geranium oil, into hair fibers of freshly permanent waved hair to remove bad odors and to change the consistency of the hair.

Polyphenols isolated from Geranium macrorrhizum L. and G. sanguineum L. have been reported to inhibit the in vitro growth of certain bacteria and fungi. See Ivancheva et al., "Polyphenols from Bulgarian Medicinal Plants with Anti-infectious Activity," in Polyphenols: Synthesis, Properties, Significance, pp. 717-28 (R.W. Hemingway & P.E. Laks eds., 1992). A polyphenolic complex isolated from G. sanguineum L. in combination with rimantadine has been reported to protect mice from infection by influenza virus. See Gegova et al. , "Combined Effect of Selected Antiviral Substances of Natural and Synthetic Origin. II.

Anti-influenza Activity of a Combination of a Polyphenolic Complex Isolated from Geranium sanguineum L. and rimantadine in vivo," Acta Microbiologica Bulgarica, Vol. 30, pp. 37-40 (1993).

It has not previously been suggested that geranium oil might be used as topical treatment for nonviral epithelial disorders.

DISCLOSURE OF INVENTION

It has been discovered that geranium oil, preferably geranium oil bourbon, can reduce the pain or inflammation associated with several nonviral epithelial disorders. The novel geranium oil treatment can relieve the itching of, and limit the inflammatory response to, insect or arachnid bites or stings. Treatment with geranium oil can decrease the pain, swelling, and blistering associated with skin burns. The healing time for canker sores can be decreased with a geranium oil treatment. A geranium oil-water gargle is effective in relieving pain from a sore throat for an extended period of time.

Topically applied geranium oil is effective in reducing the pain and inflammation associated with nonviral epithelial inflammation and lesions generally. Commercially-available, substantially pure geranium oil bourbon applied topically to insect bites or stings has relieved itching within minutes and limited the inflammatory response. Geranium oil acted quickly, without causing numbness.

Topical application of geranium oil to acute skin burns relieved the pain associated with such burns, and prevented inflammation and blistering from developing. Geranium oil was most effective when applied immediately following the burn. Attempts to treat burns after swelling and blisters had already developed were unsuccessful.

Topical application of geranium oil to canker sores decreased the healing time.

A geranium oil-water^" gargle relieved the pain from a sore throat foi an extended period of time.

The novel treatment with geranium oil bourbon has several advantages over prior methods for treating these skin disorders. It is non-toxic, provides long-term relief, and decreases the inflammation response.

In the specification and claims, a concentration or amount of geranium oil or citronellol is considered to be "therapeutically effective" if it relieves the pain or inflammation associated with epithelial inflammation or lesions.

METHODS FOR CARRYING OUT THE INVENTION

Treatment of Insect Bites A patient stepped in a fire ant hill and was stung many times on the foot. The stings became inflamed and were associated with intense itching that interrupted sleep. The itching and inflammation took ten days to resolve.

Two weeks later the patient stepped on another fire ant hill and again was stung many times on the foot. Geranium oil was applied immediately, relieving the initial burning associated with the ant stings, and totally relieving the itching for a period of four hours.

After four hours, the itching began to return but did not become severe until twelve hours after the first application of geranium oil. At that time, geranium oil was reapplied and the itching was again relieved. Then geranium oil treatment was stopped. Thirty-six hours after the first application, inflammation began to occur. At that point, the geranium oil applications were resumed on a twelve-hour schedule. The itching and inflammation resolved in five days.

At a later date, the patient again was stung by fire ants. Geranium oil bourbon was immediately applied and reapplied on a twelve-hour schedule. Both itching and inflammation were prevented by this twelve-hour schedule of geranium oil application.

Regular applications of geranium oil can prevent the onset of inflammation and severe itching. Even with sporadic applications of geranium oil, the itching and inflammation resolved in five days, compared to ten days without geranium oil.

Treatment of Skin Burns

Geranium oil bourbon was applied topically to skin burns of three patients. The first patient burned a finger while reaching into the oven to remove a Thanksgiving turkey. Geranium oil bourbon was topically applied, and the pain disappeared almost immediately. The swelling and blistering that would have normally been expected never developed. The skin in the area of the burn became hard, dark-brown, and leathery before finally shedding to reveal normal skin after seven to ten days.

A second patient was working in a laundry business when a steam pipe broke, spraying an arm below the elbow, including the hand, with pressurized steam. The area was red and very painful. Geranium oil bourbon was topically applied and the pain disappeared almost immediately. The pain did not return, and blistering with edema did not develop as would normally be expected.

A third patient was suffering from a three-day-old sunburn, which had already caused swelling and blistering. Attempts to treat this area with geranium oil were unsuccessful. When applied soon after a burn, geranium oil is effective in decreasing the pain, swelling, and blistering associated with skin burns. Treatment of Canker Sores

A patient who suffered from frequently recurring canker sores was the subject of a single-patient trial. During the one-month period prior to initiating treatment with geranium oil bourbon, the patient had five canker sores that healed in three to five days, with an average of four days. When the next canker sore appeared, one drop of geranium oil bourbon, 0.025 cc, was topically applied twice a day. The sore healed in two days.

Because a drop is hard to apply inside the mouth, one drop of geranium oil was mixed with one ounce of water to apply to two new canker sores that developed later. The patient rinsed his mouth with this solution for one minute twice a day. Each sore healed within two days.

Geranium oil substantially decreases the healing time for canker sores.

Miscellaneous

Although the preferred geranium oil for practicing this invention is commercially- available geranium oil bourbon, other geranium oils will work also. Geranium oils, especially oils of the genus Pelargonium, comprise chiefly two alcohols, geraniol and citronellol. The quantities and ratios of these two alcohols vary with variety and place of origin. Oil of geranium Reunion (geranium oil bourbon), the most commercially-available oil, has a high citronellol content, 44 to 52%. See Guenther, "VI. Essential Oils of the Plant Family Geraniaceae," in The Essential Oils, Vol. IV, 1950.

Without wishing to be bound by this theory, it is believed that citronellol is the active ingredient in geranium oil. Because it has been discovered that diluted geranium oil bourbon can be therapeutically effective, other geranium oils of lower citronellol content will also be effective. While not limiting the scope of the invention, examples of other geranium oils that may prove especially effective include geranium oil Madagascar (less than 45% citronellol), geranium oil Algerian (26 to 40% citronellol), geranium oil Moroccan (45% citronellol), geranium oil French (37 to 40% citronellol), geranium oil Spanish (32.9% citronellol), geranium oil Italian (26 to 40% citronellol), geranium oil Egyptian (50% citronellol), geranium oil Congo (34-48% citronellol), and geranium oil Russian (64% citronellol).

The complete disclosures of all references cited in this specification are hereby incorporated by reference. In the event of an otherwise irreconcilable conflict, however, the present specification shall control.

Claims

What is claimed: 1. A method for treating a nonviral epithelial inflammation or lesion in a human, comprising applying topically a therapeutically effective amount of geranium oil to the affected area.

2. The method of claim 1, wherein the inflammation or lesion is caused by an insect or arachnid bite or sting.

3. The method of claim 2, wherein the insect bite or sting is from an ant.

4. The method of claim 2, wherein the topical application is applied promptly after the sting or bite and at intervals thereafter.

5. The method of claim 4, wherein the interval between topical applications is about twelve hours.

6. The method of claim 1, wherein the inflammation or lesion is caused by a burn.

7. The method of claim 6, wherein the topical application is applied promptly after the burn.

8. The method of claim 1 , wherein the inflammation or lesion is a canker sore.

9. The method of claim 8, wherein said topical application of geranium oil comprises gargling with a mixture of geranium oil and water.

10. The method of claim 9, wherein the mixture of geranium oil and water comprises about one drop of geranium oil in about one ounce of water.

11. The method of claim 1, wherein the inflammation or lesion is associated with pharyngitis.

12. The method of claim 11 , wherein said topical application of geranium oil comprises gargling with a mixture of geranium oil and water.

13. The method of claim 1, wherein the geranium oil comprises geranium oil bourbon.

14. The method of claim 1, wherein the geranium oil is in combination with a pharmaceutically acceptable carrier.

15. A method for treating a nonviral epithelial inflammation or lesion in a human, comprising applying topically a therapeutically effective amount of citronellol to the affected area.

16. The method of claim 15, wherein the inflammation or lesion is caused by an insect or arachnid bite or sting.

17. The method of claim 16, wherein the insect bite or sting is from an ant.

18. The method of claim 16, wherein the topical application is applied promptly after the sting or bite and at intervals thereafter.

19. The method of claim 18, wherein the interval between topical applications is about twelve hours.

20. The method of claim 15, wherein the inflammation or lesion is caused by a burn.

21. The method of claim 20, wherein the topical application is applied promptly after the burn.

22. The method of claim 15, wherein the inflammation or lesion is a canker sore.

23. The method of claim 22, wherein said topical application of citronellol comprises gargling with a mixture of citronellol and water.

24. The method of claim 23, wherein the mixture of citronellol and water comprises about one drop of citronellol in about one ounce of water.

25. The method of claim 15, wherein the inflammation or lesion is associated with pharyngitis.

26. The method of claim 25, wherein said topical application of citronellol comprises gargling with a mixture of citronellol and water.

27. The method of claim 15, wherein the citronellol is in combination with a pharmaceutically acceptable carrier.