CA1214393A - Composition useful in the treatment of diarrhea - Google Patents
Composition useful in the treatment of diarrheaInfo
- Publication number
- CA1214393A CA1214393A CA000457392A CA457392A CA1214393A CA 1214393 A CA1214393 A CA 1214393A CA 000457392 A CA000457392 A CA 000457392A CA 457392 A CA457392 A CA 457392A CA 1214393 A CA1214393 A CA 1214393A
- Authority
- CA
- Canada
- Prior art keywords
- composition
- pharmaceutically acceptable
- antidiarrheal
- diarrhea
- ingredient
- 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
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
COMPOSITION USEFUL IN THE TREATMENT OF DIARRHEA
ABSTRACT OF THE DISCLOSURE
A composition useful for the symptomatic treatment of diarrhea in humans, and especially diarrhea associated with gastrointestinal hypermotility and associated distress by administering to a human having diarrhea an effective antidiarrheal amount of dextrome-thorphan, preferably as the hydrobromide.
ABSTRACT OF THE DISCLOSURE
A composition useful for the symptomatic treatment of diarrhea in humans, and especially diarrhea associated with gastrointestinal hypermotility and associated distress by administering to a human having diarrhea an effective antidiarrheal amount of dextrome-thorphan, preferably as the hydrobromide.
Description
3~.33 COMPOSITION USEFUL IN THE TREATMENT OF DIARRHEA
BACKGROUND OF THE INVENTION
1. Field of the Invention The invention relates to a composition useful for the symptomatic treatment for diarrhea. More particularly the invention relates to a composition useful for temporarily reducing the signs and symptoms of diarrhea.
BACKGROUND OF THE INVENTION
1. Field of the Invention The invention relates to a composition useful for the symptomatic treatment for diarrhea. More particularly the invention relates to a composition useful for temporarily reducing the signs and symptoms of diarrhea.
2 Background of the Prior Art .
Diarrhea is present when movements of the bowels occur with abnormal frequency and the total daily bulk is abnormally large, the movements watery, foamy, mucoid or blood-tinged. These derangements of colonic function may be due to trivial or serious disorders; and are frequent occurrences in people of all ages. Discomfort in the abdomen often precedes, and painful anal spasm may follow, the diarrheal movement. The causes of diarrhea include improper diet, drugs, bacterial or parasitic infection or infestation, organic disease, systemic disease or disturbances of the personality and emotions.
Dextromethorphan is an old compound used here-tofore as an antitussive. It is marketed in a wide variety of "over-the-counter" (OTC) and prescription (Rx) products for relief of cough, typically as the hydrobromide.
U.S. Patent No. 4,316,493 (Applicant's parent application S.N. 140,493) discloses that dextromethorphan is useful in the temporary reduction of pain. The scientific basis of the discovery, while not fully understood, is believed to be that dextromethorphan is active on enkephalin receptors which have been associated with pain.
~47~
i~L~ 3~3 SU~A~Y OF THE INVENTION
An aspect of the present invention provides a composition useful for temporarily reducing the signs and symptoms of diarrhea in humans comprising an effective, antidiarrheal amount of dextromethorphan or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Another aspect of the invention provides a process for producing a composition as defined above, which comprises admixing an antidiarrheal effective amount of dextromorphan or a pharmaceutically acceptable acid addition salt thereof with a pharmaceutically acceptable carrier.
DETAILED DESCRIPTION OF THE_INVENTION
Dextromethorphan (d-3-methoxy-N-methylmorphinan) is well known in the art as a cough suppressant (antitussive) and is commercially available; e~g., U.S. Patent No. 2,676,177 and Hafliger et al., Helv. Chim. Acta 39, 2053 (1956). The hydrobromide salt of dextromethorphan is widely commerically used as an "over-the-counter" (OTC) orally administered anti-tussive. It is also used as an antitussive in combination with antihistamines and decongestants in prescription (Rx) products for cold remedies.
Dextromethorphan may be used in the present invention in daily dosage amounts between about 5 mg and 1,000 mg and preferably between about 10 mg and about 500 mg
Diarrhea is present when movements of the bowels occur with abnormal frequency and the total daily bulk is abnormally large, the movements watery, foamy, mucoid or blood-tinged. These derangements of colonic function may be due to trivial or serious disorders; and are frequent occurrences in people of all ages. Discomfort in the abdomen often precedes, and painful anal spasm may follow, the diarrheal movement. The causes of diarrhea include improper diet, drugs, bacterial or parasitic infection or infestation, organic disease, systemic disease or disturbances of the personality and emotions.
Dextromethorphan is an old compound used here-tofore as an antitussive. It is marketed in a wide variety of "over-the-counter" (OTC) and prescription (Rx) products for relief of cough, typically as the hydrobromide.
U.S. Patent No. 4,316,493 (Applicant's parent application S.N. 140,493) discloses that dextromethorphan is useful in the temporary reduction of pain. The scientific basis of the discovery, while not fully understood, is believed to be that dextromethorphan is active on enkephalin receptors which have been associated with pain.
~47~
i~L~ 3~3 SU~A~Y OF THE INVENTION
An aspect of the present invention provides a composition useful for temporarily reducing the signs and symptoms of diarrhea in humans comprising an effective, antidiarrheal amount of dextromethorphan or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Another aspect of the invention provides a process for producing a composition as defined above, which comprises admixing an antidiarrheal effective amount of dextromorphan or a pharmaceutically acceptable acid addition salt thereof with a pharmaceutically acceptable carrier.
DETAILED DESCRIPTION OF THE_INVENTION
Dextromethorphan (d-3-methoxy-N-methylmorphinan) is well known in the art as a cough suppressant (antitussive) and is commercially available; e~g., U.S. Patent No. 2,676,177 and Hafliger et al., Helv. Chim. Acta 39, 2053 (1956). The hydrobromide salt of dextromethorphan is widely commerically used as an "over-the-counter" (OTC) orally administered anti-tussive. It is also used as an antitussive in combination with antihistamines and decongestants in prescription (Rx) products for cold remedies.
Dextromethorphan may be used in the present invention in daily dosage amounts between about 5 mg and 1,000 mg and preferably between about 10 mg and about 500 mg
3~3~
- 2a -depending on the age and weight o the person and the severity of diarrhea to be treated. A typical daily dosage amount suitable or a human varies between about 10 mg and about 300 mg and preferably between about 20 mg and 200 mg. For example, a typical dosage amount of dextromethorphan hydrobromide effective in temporarily L~3{33 reducing the signs and symptoms associated with diarrhea in an adult human would be about 20 mg to about 50 mg administered in equal doses 1 to 4 times per day.
For therapeutic use, dextromethorphan will normally be administered as a pharmaceutical composition in the basic form or in the form of an addition salt with a pharmaceutically acceptable acid and in association with a pharmaceutical carrier therefor. Such addition salts include those with hydrochloric, hydrobromic, hydriodic, sulphuric and maleic acids and preferably hydrobromide.
Other pharmacologically active compounds known to be useful in the treatment of diarrhea may, in certain cases, be included in the composition including, for example, kaolin, pectin, bacterial cultures such as Lactobacillus acidophilus and L. bulgaricus, bismuth subsalicylate, bismuth subnitrate and calcium hydroxide and attapulgite. Advantageously, the composition will be made up in a dosage unit form appropriate to the desired mode of administration, for example, as a tablet, capsule, sustained release type, oral suspension, or in a suitable formulation for conventional or sustained release topical administration.
The pharmaceutical compositions may be in a form suitable for oral use, for example, as tablets, lozenges, aqueous or oily suspensions, dispersible powders or granules, emulsions, hard or soft capsules, or syrups or elixirs. Compositions intended for oral use may be prepared according to any method known to the art for the manufacture of pharmaceutical compositions and such compositions may contain one or more agents selected from the group consisting of sweetening agents, flavoring agents, coloring agents and preserving agents in order to provide a pharmaceutically elegant and palatable 3~3 preparation. Tablets contain the active ingredient in admixture with nontoxic pharmaceutically acceptable excipients which are suitable for manufacture of tablets.
These excipients may be inert diluents, for example calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate; granulating and disintegra-ting agents, for example, maize starch, or alginic acid;
binding agents for example, starch, gelatine or acacia, and lubricating agents, for example, magnesium stearate or stearic acid. The tablets may be uncoated or they may be coated by known techniques to delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period.
Formulations for oral use may also be presented as hard gelatine capsules wherein the active ingredient is mixed with an inert solid diluent, for example, calcium carbonate~ calcium phosphate or kaolin, or as soft gelatine capsules wherein the active ingredient is mixed with an oil medium, for example, arachis oil, liquid paraffin or olive oil.
Aqueous suspensions contain the active ingredients in admixture with excipients suitable for the manufacture of aqueous suspensions. Such excipients are suspending agents, for example, sodium carboxymethyl cellulose, methylcellulose, hydroxypropylmethylcellulose, sodium alginate, polyvinylpyrrolidone, gum tragacanth and gum acacia; dispersing or wetting agents may be a naturally occurring phosphatide, for example, lecithin, or conden-sation products of an alkylene oxide with fatty acids, for example, polyoxyethylene stearatet or condensation products of ethylene oxide with long chain aliphatic alcohols, for example heptadecaethyleneoxycetanol, or condensation products of ethylene oxide with partial esters derived from fatty acids and a hexitol, for ~z~393 example, polyoxyethylene sorbitol monooleate, or condensa-tion product of ethylene oxide with partial esters derived from fatty acids and hexitol anhydrides, for example, polyoxyethylene sorbitan monooleate. The said aqueous suspensions may also contain one or more preserva-tives, for example ethyl- or n-propyl- p-hydroxy benzoate, one or more coloring agents, one or more flavoring agents and one or more sweetening agents, such as sucrose, saccharin, or sodium or calcium cyclamate.
Dispersible powders and granules suitable for preparation of an aqueous suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent, suspending agent and one or ~.ore preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified by those already mentioned above. Additional excipients, for example, sweetening, flavoring and coloring agents, may `
also be present.
Syrups and elixirs may be formulated with sweetening agents, for example glycerol, sorbitol or sucrose. Such formulations may also contain a demulcent7 a preservative and flavoring and coloring agents.
The pharmaceutical compositions may be tableted or otherwise formulated so that for every 100 parts by weight of the composition there are present between 5 and 95 parts by weight of the active ingredient and preferably between 25 and 85 parts by weight of the active ingredient.
The dosage unit form will generally contain between about 10 mg and about 500 mg of the active ingredient of the formula stated above.
From the foregoing formulation discussion, it is apparent that the composition of this invention is preferably administered orally.
~Z,~ 3t33 The scientific basis of the discovery set forth herein is not fully understood; however, it is believed that dextromethorphan is able to exert its antidiarrheal activity by acting upon specific enkephalin receptors in the body, in particularly in the gastrointestinal area.
Enkephalin receptors are believed to be associated with hypermotility and associated distress of the gastrointes-~inal tract, a causative factor in diarrhea.
- 2a -depending on the age and weight o the person and the severity of diarrhea to be treated. A typical daily dosage amount suitable or a human varies between about 10 mg and about 300 mg and preferably between about 20 mg and 200 mg. For example, a typical dosage amount of dextromethorphan hydrobromide effective in temporarily L~3{33 reducing the signs and symptoms associated with diarrhea in an adult human would be about 20 mg to about 50 mg administered in equal doses 1 to 4 times per day.
For therapeutic use, dextromethorphan will normally be administered as a pharmaceutical composition in the basic form or in the form of an addition salt with a pharmaceutically acceptable acid and in association with a pharmaceutical carrier therefor. Such addition salts include those with hydrochloric, hydrobromic, hydriodic, sulphuric and maleic acids and preferably hydrobromide.
Other pharmacologically active compounds known to be useful in the treatment of diarrhea may, in certain cases, be included in the composition including, for example, kaolin, pectin, bacterial cultures such as Lactobacillus acidophilus and L. bulgaricus, bismuth subsalicylate, bismuth subnitrate and calcium hydroxide and attapulgite. Advantageously, the composition will be made up in a dosage unit form appropriate to the desired mode of administration, for example, as a tablet, capsule, sustained release type, oral suspension, or in a suitable formulation for conventional or sustained release topical administration.
The pharmaceutical compositions may be in a form suitable for oral use, for example, as tablets, lozenges, aqueous or oily suspensions, dispersible powders or granules, emulsions, hard or soft capsules, or syrups or elixirs. Compositions intended for oral use may be prepared according to any method known to the art for the manufacture of pharmaceutical compositions and such compositions may contain one or more agents selected from the group consisting of sweetening agents, flavoring agents, coloring agents and preserving agents in order to provide a pharmaceutically elegant and palatable 3~3 preparation. Tablets contain the active ingredient in admixture with nontoxic pharmaceutically acceptable excipients which are suitable for manufacture of tablets.
These excipients may be inert diluents, for example calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate; granulating and disintegra-ting agents, for example, maize starch, or alginic acid;
binding agents for example, starch, gelatine or acacia, and lubricating agents, for example, magnesium stearate or stearic acid. The tablets may be uncoated or they may be coated by known techniques to delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period.
Formulations for oral use may also be presented as hard gelatine capsules wherein the active ingredient is mixed with an inert solid diluent, for example, calcium carbonate~ calcium phosphate or kaolin, or as soft gelatine capsules wherein the active ingredient is mixed with an oil medium, for example, arachis oil, liquid paraffin or olive oil.
Aqueous suspensions contain the active ingredients in admixture with excipients suitable for the manufacture of aqueous suspensions. Such excipients are suspending agents, for example, sodium carboxymethyl cellulose, methylcellulose, hydroxypropylmethylcellulose, sodium alginate, polyvinylpyrrolidone, gum tragacanth and gum acacia; dispersing or wetting agents may be a naturally occurring phosphatide, for example, lecithin, or conden-sation products of an alkylene oxide with fatty acids, for example, polyoxyethylene stearatet or condensation products of ethylene oxide with long chain aliphatic alcohols, for example heptadecaethyleneoxycetanol, or condensation products of ethylene oxide with partial esters derived from fatty acids and a hexitol, for ~z~393 example, polyoxyethylene sorbitol monooleate, or condensa-tion product of ethylene oxide with partial esters derived from fatty acids and hexitol anhydrides, for example, polyoxyethylene sorbitan monooleate. The said aqueous suspensions may also contain one or more preserva-tives, for example ethyl- or n-propyl- p-hydroxy benzoate, one or more coloring agents, one or more flavoring agents and one or more sweetening agents, such as sucrose, saccharin, or sodium or calcium cyclamate.
Dispersible powders and granules suitable for preparation of an aqueous suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent, suspending agent and one or ~.ore preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified by those already mentioned above. Additional excipients, for example, sweetening, flavoring and coloring agents, may `
also be present.
Syrups and elixirs may be formulated with sweetening agents, for example glycerol, sorbitol or sucrose. Such formulations may also contain a demulcent7 a preservative and flavoring and coloring agents.
The pharmaceutical compositions may be tableted or otherwise formulated so that for every 100 parts by weight of the composition there are present between 5 and 95 parts by weight of the active ingredient and preferably between 25 and 85 parts by weight of the active ingredient.
The dosage unit form will generally contain between about 10 mg and about 500 mg of the active ingredient of the formula stated above.
From the foregoing formulation discussion, it is apparent that the composition of this invention is preferably administered orally.
~Z,~ 3t33 The scientific basis of the discovery set forth herein is not fully understood; however, it is believed that dextromethorphan is able to exert its antidiarrheal activity by acting upon specific enkephalin receptors in the body, in particularly in the gastrointestinal area.
Enkephalin receptors are believed to be associated with hypermotility and associated distress of the gastrointes-~inal tract, a causative factor in diarrhea.
Claims (8)
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. A composition useful for temporarily reducing the signs and symptoms of diarrhea in humans comprising an effective antidiarrheal amount of dextromethorphan or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
2. The composition of claim 1, including at least one other pharmacologically active antidiarrheal ingredient.
3. The composition of claim 2, wherein said at least one other pharmacologically active antidiarrheal ingredient is selected from kaolin, pectin, a bacterial culture of Lactobacillus acidophilus, a bacterial culture of Lactobacillus bulgaricus, bismuth subsalicylate, bismuth subnitrate, calcium hydroxide or attapulgite.
4. The composition of claim 4, wherein dertromethorphan is in the hydrobromide form.
5. The composition of claim 2, 3 or 4, which is in the dosage unit form.
6. The composition of claim 2, 3 or 4, which is in the tablet, capsule, sustained release type or oral suspention form.
7. A process for producing a composition as defined in claim 1, which comprises admixing an antidiarrheal effective amount of dextromorphan or a pharmaceutically acceptable acid addition salt thereof with a pharmaceutically acceptable carrier.
8. A process for producing a composition as defined in claim 2 or 3, which comprises admixing antidiarrheal effective amount of dextromorphan or a pharmaceutically acceptable acid addition salt thereof and at least one other pharmacologically active antidiarrheal ingredient with a pharmaceutically acceptable carrier.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000457392A CA1214393A (en) | 1984-06-26 | 1984-06-26 | Composition useful in the treatment of diarrhea |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000457392A CA1214393A (en) | 1984-06-26 | 1984-06-26 | Composition useful in the treatment of diarrhea |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1214393A true CA1214393A (en) | 1986-11-25 |
Family
ID=4128171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000457392A Expired CA1214393A (en) | 1984-06-26 | 1984-06-26 | Composition useful in the treatment of diarrhea |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA1214393A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4950655A (en) * | 1985-10-14 | 1990-08-21 | Poul Bachmann | Composition for treating and preventing diarrhoea in humans and animals and a method of preparing same |
| EP1986620A1 (en) * | 2006-02-24 | 2008-11-05 | Blue Blood Biotech Corp | Methods and compositions for bactericide, bacteriostatic and anti-inflammation |
-
1984
- 1984-06-26 CA CA000457392A patent/CA1214393A/en not_active Expired
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4950655A (en) * | 1985-10-14 | 1990-08-21 | Poul Bachmann | Composition for treating and preventing diarrhoea in humans and animals and a method of preparing same |
| EP1986620A1 (en) * | 2006-02-24 | 2008-11-05 | Blue Blood Biotech Corp | Methods and compositions for bactericide, bacteriostatic and anti-inflammation |
| EP1986620B1 (en) * | 2006-02-24 | 2012-01-04 | Blue Blood Biotech Corp. | Dextromethorphan for the treatment of acne |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |