CA1189794A - Composition for treating pruritis - Google Patents
Composition for treating pruritisInfo
- Publication number
- CA1189794A CA1189794A CA000423216A CA423216A CA1189794A CA 1189794 A CA1189794 A CA 1189794A CA 000423216 A CA000423216 A CA 000423216A CA 423216 A CA423216 A CA 423216A CA 1189794 A CA1189794 A CA 1189794A
- Authority
- CA
- Canada
- Prior art keywords
- naloxone
- composition
- pharmaceutically acceptable
- pruritis
- itching
- 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
Links
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
ABSTRACT
A topical treatment for relieving pruritis wherein Naloxone, a pharmaceutically acceptable salt of a pharmaceutically acceptable chemical derivative is topically applied in a lotion, solution, cream or ointment.
A topical treatment for relieving pruritis wherein Naloxone, a pharmaceutically acceptable salt of a pharmaceutically acceptable chemical derivative is topically applied in a lotion, solution, cream or ointment.
Description
3~
The present invention relates to a composition for relieving pruritis.
Itching or pruritis is a common dermatologic symptom. The causes of pruritis are complex and poorly 5 understood. The best understood mechanism of itching is the release of histamine in the skin leading to urticarial wheals and intense itching. Such itching has -traditionally been relieved by antihistamines. While antihistamine therapy is often effective, the sedation and drowsiness 10 produced by antihistaminic agents limits their ef~ectiveness.
Many kinds of itching are not however easily re-lieved by antihistamines. For example, conditions such as Hodgkinls Disease, mycosis fungoides (cutaneous malig~
nacy) and severe jaundice produce intense itching unrelieved 15 by antihistamines. Therefore, there is a need for improved treatment to relieve severe itching which can not only be an alternative to antihlstaminic treatment of itching due to such causes as mos~uitoe bites which responds to such treatm~nt, but which further provides relief in intractable 20 cases of pruritis which heretofore have been virtually im-possible to treat except as disclosed in U. S. Patent No.
4,181,~26 which relates to a method based on the systemic effects on the central nervous system.
The object of the present invention is to provide 25 ~or treating pruritis which acts independent of systemic effects on the central nervous system.
.
. ..
The presen-t invention provides a composi-tion for re]ieveing pruritls comprising a therapeutically ef-fective amount of Naloxone*or a pharmaceutically acceptable salt thereof of Naltrexone*in a solution, lotion, cream 5 or ointment.
Naloxone is a narcotic antagonist which is not known to cause physical or psychological dependence and which exhibits essentially no pharmacological activity in non-addicts. Naloxone is normally given by injection 10 to addicts to assist them in narcotic withdrawal and some-times is administered to post operative patients for partial reversal of narcotic depression following the use of nar-cotics during surgery.
It has been ~ound surprisingly that topical ap-15 plications of Naloxone are useful in alleviating sevexeitching in various conditions.
Naloxone hydrochloride is commercially available from Endo Laboratories, Inc., a subsidiary of the DuPont Company, 1000 Stewart Avenue, Garden City, New York 11530.
20 The preparation of Naloxone is disclosed in U. S. Patent ~o. 3,254,088.
The term pharmaceutically acceptable salts, as - used herein, re~ers to the physiologically acceptable acid addition salts of Naloxone such as the hydrochloride, 25 hydrobxomide! hydroiodide, ace-tate, valerate, oleate, etc.
Liquid dosage forms for topical administration includes acceptable emulsions, solutions and suspensions containiny volatile diluents commonly used in the art, such as alcohol, glycol and the liXe. Besides such 30 diluents, topically applied compositions may also include wetting agents, emulsifying and suspending agents.
In the practice o~ this invention Naloxone ln *Trade ~lark ' .,~
-the form of a pharmaceutically acceptable sal-t such as the hydrochloride and pharmaceutically acceptable chem-ical derivatives thereo~ such as naltrexone which is the n-methyl cyclopropyl derivative are incorporated into solutions, lotions, creams, and ointments for topical application in concentrations of from 0.01 to about 5 percent by weight. These topical products are applied to the skin 1 to 8 times daily. The relief experienced by those receiving the topical application was prompt although temporary.
EXAMPLE l 1 percent by weight Naloxone hydrochloride was incorporated into a solution eomposed of 70 percent by volume ethyl aleohol and 30 percent by volume propylene glyeol and applied 6 times daily to 2 mosquito bites of less than 24 hours duration on an 11 year-old male. This child noted relief from his itching within lO minutes of eaeh applieation and the relief lasted ~-4 hours.
~o A 0.05% by weight Naloxone hydroehloride was incorporated into Eucerin (R.T.M.) eream and applied 4 times daily to the body of a 60 year-old male with in-tractable itehing due to mycosis fungoides. Eueerin (R.T.M.) cream is a synthetie lanolin containing cream produced by Beiersdorf, Inc. of South Norwalk, Conneetieut 06854. This was the first topical product the patient used that provided him with any signifieant relief from his itching.
An ointment composed chiefly of petrolatum and containing 0.01% by weight Naloxone hydrochloride was applied 4 times daily to the body of a 60 year-old male with mycosis fungoides. Itching was diminished, although not as much as with the higher eoncentration of Naloxone in Example 2.
. 4 _ EXAMPI,E 4 0.1% by we:ight Naloxone hydrochloride was incorporated into a zinc shake lotion and applied to the mosquitoe bites of a 6 year-old girl durlng a 5 one month five interval in the summer. This lotion provided excellent relief from the itching.
5~ by weight Maloxone hydrochloride was incor-porated into an ointment and applied 4 times daily for 10 two days to a small ec2ematous patch on the left hand of a 38 year-old male. Itching was dramatically re-duced by each application of the -test ointmentO
The present invention relates to a composition for relieving pruritis.
Itching or pruritis is a common dermatologic symptom. The causes of pruritis are complex and poorly 5 understood. The best understood mechanism of itching is the release of histamine in the skin leading to urticarial wheals and intense itching. Such itching has -traditionally been relieved by antihistamines. While antihistamine therapy is often effective, the sedation and drowsiness 10 produced by antihistaminic agents limits their ef~ectiveness.
Many kinds of itching are not however easily re-lieved by antihistamines. For example, conditions such as Hodgkinls Disease, mycosis fungoides (cutaneous malig~
nacy) and severe jaundice produce intense itching unrelieved 15 by antihistamines. Therefore, there is a need for improved treatment to relieve severe itching which can not only be an alternative to antihlstaminic treatment of itching due to such causes as mos~uitoe bites which responds to such treatm~nt, but which further provides relief in intractable 20 cases of pruritis which heretofore have been virtually im-possible to treat except as disclosed in U. S. Patent No.
4,181,~26 which relates to a method based on the systemic effects on the central nervous system.
The object of the present invention is to provide 25 ~or treating pruritis which acts independent of systemic effects on the central nervous system.
.
. ..
The presen-t invention provides a composi-tion for re]ieveing pruritls comprising a therapeutically ef-fective amount of Naloxone*or a pharmaceutically acceptable salt thereof of Naltrexone*in a solution, lotion, cream 5 or ointment.
Naloxone is a narcotic antagonist which is not known to cause physical or psychological dependence and which exhibits essentially no pharmacological activity in non-addicts. Naloxone is normally given by injection 10 to addicts to assist them in narcotic withdrawal and some-times is administered to post operative patients for partial reversal of narcotic depression following the use of nar-cotics during surgery.
It has been ~ound surprisingly that topical ap-15 plications of Naloxone are useful in alleviating sevexeitching in various conditions.
Naloxone hydrochloride is commercially available from Endo Laboratories, Inc., a subsidiary of the DuPont Company, 1000 Stewart Avenue, Garden City, New York 11530.
20 The preparation of Naloxone is disclosed in U. S. Patent ~o. 3,254,088.
The term pharmaceutically acceptable salts, as - used herein, re~ers to the physiologically acceptable acid addition salts of Naloxone such as the hydrochloride, 25 hydrobxomide! hydroiodide, ace-tate, valerate, oleate, etc.
Liquid dosage forms for topical administration includes acceptable emulsions, solutions and suspensions containiny volatile diluents commonly used in the art, such as alcohol, glycol and the liXe. Besides such 30 diluents, topically applied compositions may also include wetting agents, emulsifying and suspending agents.
In the practice o~ this invention Naloxone ln *Trade ~lark ' .,~
-the form of a pharmaceutically acceptable sal-t such as the hydrochloride and pharmaceutically acceptable chem-ical derivatives thereo~ such as naltrexone which is the n-methyl cyclopropyl derivative are incorporated into solutions, lotions, creams, and ointments for topical application in concentrations of from 0.01 to about 5 percent by weight. These topical products are applied to the skin 1 to 8 times daily. The relief experienced by those receiving the topical application was prompt although temporary.
EXAMPLE l 1 percent by weight Naloxone hydrochloride was incorporated into a solution eomposed of 70 percent by volume ethyl aleohol and 30 percent by volume propylene glyeol and applied 6 times daily to 2 mosquito bites of less than 24 hours duration on an 11 year-old male. This child noted relief from his itching within lO minutes of eaeh applieation and the relief lasted ~-4 hours.
~o A 0.05% by weight Naloxone hydroehloride was incorporated into Eucerin (R.T.M.) eream and applied 4 times daily to the body of a 60 year-old male with in-tractable itehing due to mycosis fungoides. Eueerin (R.T.M.) cream is a synthetie lanolin containing cream produced by Beiersdorf, Inc. of South Norwalk, Conneetieut 06854. This was the first topical product the patient used that provided him with any signifieant relief from his itching.
An ointment composed chiefly of petrolatum and containing 0.01% by weight Naloxone hydrochloride was applied 4 times daily to the body of a 60 year-old male with mycosis fungoides. Itching was diminished, although not as much as with the higher eoncentration of Naloxone in Example 2.
. 4 _ EXAMPI,E 4 0.1% by we:ight Naloxone hydrochloride was incorporated into a zinc shake lotion and applied to the mosquitoe bites of a 6 year-old girl durlng a 5 one month five interval in the summer. This lotion provided excellent relief from the itching.
5~ by weight Maloxone hydrochloride was incor-porated into an ointment and applied 4 times daily for 10 two days to a small ec2ematous patch on the left hand of a 38 year-old male. Itching was dramatically re-duced by each application of the -test ointmentO
Claims (4)
1. A composition for relieving pruritis compri-sing a therapeutically effective amount of Naloxone or a pharmaceutically acceptable salt thereof of Naltrexone in a solution, lotion, cream or ointment.
2. The composition of claim 1, wherein Naloxone or a pharmaceutically acceptable salt thereof or Naltre-xone is present in the solution, lotion, cream or ointment in the range of between about 0.01 percent by weight to about 5 percent by weight.
3. The composition of claim 1, wherein the pharmaceutically acceptable salt of Naloxone is a physio-logically acceptable acid addition salt.
4. The composition of claim 1, wherein said salt is Naloxone hydrochloride.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000423216A CA1189794A (en) | 1983-03-09 | 1983-03-09 | Composition for treating pruritis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000423216A CA1189794A (en) | 1983-03-09 | 1983-03-09 | Composition for treating pruritis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1189794A true CA1189794A (en) | 1985-07-02 |
Family
ID=4124743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000423216A Expired CA1189794A (en) | 1983-03-09 | 1983-03-09 | Composition for treating pruritis |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA1189794A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115397419A (en) * | 2020-02-14 | 2022-11-25 | 帝国制药美国公司 | Topical naloxone compositions and methods of use thereof |
-
1983
- 1983-03-09 CA CA000423216A patent/CA1189794A/en not_active Expired
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115397419A (en) * | 2020-02-14 | 2022-11-25 | 帝国制药美国公司 | Topical naloxone compositions and methods of use thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEC | Expiry (correction) | ||
| MKEX | Expiry |