CN1146150A - Low dosage ranitidine compositions - Google Patents
Low dosage ranitidine compositions Download PDFInfo
- Publication number
- CN1146150A CN1146150A CN95192537A CN95192537A CN1146150A CN 1146150 A CN1146150 A CN 1146150A CN 95192537 A CN95192537 A CN 95192537A CN 95192537 A CN95192537 A CN 95192537A CN 1146150 A CN1146150 A CN 1146150A
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- China
- Prior art keywords
- ranitidine
- dosage
- combination
- oral medication
- treatment
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The present invention relates to low dosage formulations containing the histamine H2-receptor antagonist ranitidine and their use in the treatment of gastric disorders such as episodic heartburn.
Description
The present invention relates to contain histamine H
2The low dose of preparation of-receptor antagonist ranitidine and be used for the treatment of the purposes of gastropathy (as the acute attack heartburn).
In No. 1565966, british patent specification, describe and asked for protection ranitidine-N-[2-[[[5-(dimethylamino) methyl-2-furyl] methyl] sulfenyl] ethyl]-N '-methyl-2-nitro-1; the 1-ethylenediamine; and physiologically acceptable salt, and in No. 2084580, british patent specification, describe and asked for protection the special crystal formation of ranitidine hydrochloride.In two parts of explanations, all mention the preparation that is used for oral administration, can adopt for example dosage forms such as tablet, capsule, granule, powder, solution, syrup, suspendible liquor, perhaps adopt tablet or lozenge to be used for the buccal administration.Oral administration is an optimization approach of using ranitidine.
Described in the United States Patent (USP) 5229137 ranitidine and the pyrotic purposes of antacid combined treatment acute attack.According to United States Patent (USP) 5229137, when using H separately
2When-antagonist such as ranitidine,, can feel just that acute attack is pyrotic to alleviate up to taking medicine after after a while.Particularly when two are suffered from the pyrotic patient of acute attack and use the 150mg ranitidine, take medicine the back in the time of 45 and 60 minutes heartburn just alleviate.Therefore, according to US5229137, need to adopt antacid and H
2-antagonist is together used so that alleviate heartburn rapidly.Work as H
2When-antagonist is ranitidine, its dosage that in mixture, is adopted 100 to 150mg.
Described among EP0193400 and the WO93/12779 and contained the H that lowers dosage
2The compositions of-antagonist.The H that is used for the treatment of gastritis or gastroduodenal ulcer has been described among the EP0193400
2The mixture of-antagonist (thunderous Buddhist nun is for Buddhist nun's fourth) and sodium polyacrylate.According to EP0193400, H
2The synergism of-antagonist and polyacrylate makes and adopts low dose of H
2-antagonist becomes possibility.
Described H among the WO93/12779
2The mixture of-antagonist (comprising ranitidine) and antacid is used for the treatment of gastropathy, and wherein mixture is buffered to pH value and H
2The pKa value of-antagonist is equal substantially, and H in wherein every unit dosage form
2The dosage of-antagonist is less than 25mg.Low dose is thought effectively, because the mixture of active ingredient has improved H
2-antagonist is in the bioavailability of local coat of the stomach receptor site.
The H that lowers dosage that has that is used for treatments such as heartburn has also been described among the EP0492247
2The compositions of-antagonist.That said composition adopts herein is water solublity H
2-antagonist and effervescent delivery system (as alkali metal hydrogencarbonate and citric acid) combine.Adopt this effervescent delivery system to think and to shorten H
2The time that-antagonist works, and can increase its effectiveness, so said preparation need be used for the treatment of the H of the duodenal ulcer of outbreak at present
2About 25% of-antagonist prescribed dose.For ranitidine, this effervescent delivery system can reduce to its dosage and be lower than 37.5mg from 150mg.
When ranitidine is used separately, it is generally acknowledged that its dosage level is medicable at 50-600mg (as 150-300mg).
Find at present that surprisingly using very low dose of ranitidine separately is effectively in the treatment slight gastrointestinal disease (for example acute attack heartburn) relevant with the excess stomach acid secretion, and after using in 30-45 minute symptom begin to alleviate.And dosage of the present invention also helps controlling the persistent period of gastric acid secretion simultaneously.
The invention provides a kind of combination of oral medication (as tablet), wherein contain ranitidine or its physiologically acceptable salt as unique active ingredient, said composition is characterised in that and contains the ranitidine that dosage is 10-30mg (as 25mg) (in the weight of its free alkali) in every dosage form units.
Another aspect of the present invention provides a kind of ranitidine or its physiologically acceptable salt of containing as the tablet of swallowing of unique active component, it is characterized in that containing in every dosage form units the ranitidine that dosage is 10-30mg (as 25mg) (in the weight of its free alkali).
Another aspect of the present invention provides the method for a kind of treatment slight gastrointestinal disease relevant with the excess stomach acid secretion, use comprising the patient to the described treatment of needs and mainly to contain ranitidine or its physiologically acceptable salt combination of oral medication as unique active component, said composition is characterised in that and contains the ranitidine that dosage is 10-30mg (as 25mg) (in the weight of its free alkali) in every dosage form units.
Compositions of the present invention be should understand and antacid, polyacrylate or effervescent delivery system do not contained substantially.
The form that is used for the ranitidine of tablet of the present invention can be its free alkali or its physiologically acceptable salt.These salt comprise inorganic acid salt or acylate example hydrochloric acid salt, hydrobromate, sulfate, acetate, maleate, succinate, citrate, tartrate, fumarate and Ascorbate.The particularly preferred salt of ranitidine is hydrochlorate.
The ranitidine that is used for tablet of the present invention can be conventionally form, perhaps also can adopt coating or encapsulation form.At for example EP538034, EP523847, WO92/21328, EP473431, EP459695, EP349103 has described the coating or the encapsulation form that are suitable among CA2068636 and the US5084278.In UK2218333, describe ranitidine resin absorption thing and also can be used for tablet of the present invention.
Preferred ranitidine and the salt thereof that adopts conventionally form.
The amount preferably every dosage device (for example every slice) of ranitidine (the preferably hydrochlorate of the form of its physiologically acceptable salt, particularly ranitidine) in the present composition contains 10-30mg, for example 25mg (in its free alkali weight).
According to required sanatory character and the order of severity and patient's age and body weight, but maximum 12 times of administration unit dosage every day (the contained dosage of tablet for example of the present invention).Like this, for treating slight gastrointestinal disease relevant such as hyperchlorhydria dyspepsia, crapulence (for example inebriant) gluttony, acid stomach with the excess stomach acid secretion, sour stomach, when the heartburn that waterbrash/ regurgitation, heartburn such as acute attack heartburn, night, the property sent out heartburn and food brought out, gastritis and dyspepsia, use for example maximum 12 times of the ranitidine of 25mg dosage (in free alkali weight) of 10-30mg as required every day, for example every day 6 times.
Also can contain other this area excipient such as filler, binding agent, disintegrating agent, lubricant and desiccant commonly used in the pharmaceutical composition of the present invention.The excipient that is suitable for all is well-known to those skilled in the art.
The binding agent that is suitable for comprises methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, alginic acid, ethyl cellulose, arabic gum, gelatin, pregelatinized Starch, sucrose slurry, polyvinylpyrrolidone and guar gum.
The lubricant that is suitable for comprises magnesium stearate, zinc stearate, calcium stearate, stearic acid, stearyl fumaric acid sodium, hydrogenated vegetable oil, palmitoleostearin, behenic acid glyceride, sodium benzoate, sodium lauryl sulfate, lauryl magnesium sulfate, mineral oil, Pulvis Talci and composition thereof.
Preferred lubricant is a magnesium stearate.
The desiccant that is suitable for comprises silica gel.
The filler that is suitable for comprises microcrystalline Cellulose.The disintegrating agent that is suitable for comprises cross-linking sodium carboxymethyl cellulose.
In our common unsettled PCT application PCT/EP93/02763, the chewable tablet that is suitable for has been described.Disclosed especially chewable tablet is not included in the scope of the present invention in this common pending application.
These contain the chewable tablet of ranitidine or its physiologically acceptable salt, and its chew base is selected from sucrose, glucose, lactose, maltose or its mixture, flavoring agent, and can randomly contain strong sweetener.
This chewable tablet can prepare by conventional steps, comprises miscible granulation, drying, mixing, tabletting and packing.
The label of swallowing that is suitable for can prepare by conventional method, for example available with incorporate the same procedure described in this paper british patent specification 2084580 as a reference into.Therefore the ranitidine that can for example aequum or the physiologically acceptable disintegrating agent (as cross-linking sodium carboxymethyl cellulose) of its salt, lubricant (as magnesium stearate) and randomly adding mix mutually and are pressed into label.
The sheet of swallowing is that to carry out routine by conventional steps (method of water or organic solvent) film-coated.Incorporate in this paper british patent specification 2218336 as a reference and described preferred film coating.
Below be also the illustrating of indefiniteness embodiment of pharmaceutical composition of the present invention.Opaspray white K-1-7000 is titanium dioxide and the suspension of hydroxypropyl cellulose in industrial methylated spirit.Opadry Yellow Y S-1-12606 is the mixture of hydroxypropyl methylcellulose 2910, titanium dioxide, glycerol triacetate and iron sesquioxide Huang.Opaspray and Opadry are Colorcon Inc., (West Point, Philadelphia, trade name USA).Reference example 1 chewable tablet
Composition mg/ sheet
Ranitidine hydrochloride 28.0
Sucrose 2268.0
Aspartame 37.5
Polyvinylpyrrolidone 50.0
Mentha piperita essence 41.5
Silica gel 50.0
Magnesium stearate 25.0
Isopropyl alcohol+an amount of+in end product, do not exist embodiment 2 sheet of swallowing
Label mg/ sheet
Ranitidine hydrochloride 28.0
Microcrystalline Cellulose 263.75
A type cross-linking sodium carboxymethyl cellulose 6.00
Magnesium stearate 2.25
The heavy 300mg of purpose sheet
Film coating % weight cell amount (mg/ sheet)
*
Methylhydroxypropylcellulose 4.0 11.3
Opaspray?White?K-1-7000 3.3 4.7
Isopropyl alcohol
*26.3 it is an amount of
Dichloromethane
*66.4 it is an amount of
*According to the efficient of method, every film coating that is adopted can be less than described amount.
*In end product, there is not embodiment 3 sheet of swallowing
Label quantity of units (mg/ sheet)
Ranitidine hydrochloride 28.000
Microcrystalline Cellulose 120.875
Magnesium stearate 1.125
Total sheet weighs 150.00
Film coating
Opadry?Yellow?YS-1-12606 6.75
Pure water
*42.34
*In step, remove clinical research
In the double blinding placebo-controlled trial of the pyrotic effectiveness of acute attack of measuring 25mg ranitidine (with the hydrochloride form administration) treatment general population, the sheet of swallowing of the chewable tablet of embodiment 1 and embodiment 2 all can onset in administration 30-45 minute.
Claims (7)
1. an oral pharmaceutical composition wherein contains ranitidine or its physiologically acceptable salt as unique active ingredient, and said composition is characterised in that the dosage that every unit dosage form contains in free alkali weight is the ranitidine of 10-30mg.
2. the combination of oral medication of claim 1, the dosage that wherein every dosage device contains in free alkali weight is the ranitidine of 25mg.
3. claim 1 or 2 combination of oral medication, wherein ranitidine is the form of its hydrochlorate.
4. the combination of oral medication of arbitrary claim among the claim 1-3, it is the form of tablet.
5. the combination of oral medication of claim 4, it is the form of swallowing tablet.
6. the method for a treatment slight gastrointestinal disease relevant with the excess stomach acid secretion, this method comprises combination of oral medication from arbitrary claim among the claim 1-5 to the patient of the described treatment of needs that use.
7. the combination of oral medication of arbitrary claim is used for the treatment of application in the medicine of the slight gastrointestinal disease relevant with excess stomach acid secretion in preparation among the claim 1-5.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9407235A GB9407235D0 (en) | 1994-04-12 | 1994-04-12 | Pharmaceutical compositions |
| GB9407235.2 | 1994-04-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1146150A true CN1146150A (en) | 1997-03-26 |
Family
ID=10753423
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN95192537A Pending CN1146150A (en) | 1994-04-12 | 1995-04-10 | Low dosage ranitidine compositions |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP0755251A1 (en) |
| JP (1) | JPH10502331A (en) |
| KR (1) | KR970702034A (en) |
| CN (1) | CN1146150A (en) |
| AU (1) | AU690664B2 (en) |
| BR (1) | BR9507312A (en) |
| CA (1) | CA2187651A1 (en) |
| GB (1) | GB9407235D0 (en) |
| NZ (1) | NZ283354A (en) |
| WO (1) | WO1995027486A1 (en) |
| ZA (1) | ZA952931B (en) |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9025710D0 (en) * | 1990-11-27 | 1991-01-09 | Beecham Group Plc | Novel treatment |
| CA2055661A1 (en) * | 1990-12-21 | 1992-06-22 | Manley A. Paulos | Treatment of upset stomach associated with heartburn, sour stomach or acid indigestion with an effervescent h2 blocker formulation |
| GB9127150D0 (en) * | 1991-12-20 | 1992-02-19 | Smithkline Beecham Plc | Novel treatment |
-
1994
- 1994-04-12 GB GB9407235A patent/GB9407235D0/en active Pending
-
1995
- 1995-04-10 CN CN95192537A patent/CN1146150A/en active Pending
- 1995-04-10 ZA ZA952931A patent/ZA952931B/en unknown
- 1995-04-10 WO PCT/EP1995/001271 patent/WO1995027486A1/en not_active Application Discontinuation
- 1995-04-10 BR BR9507312A patent/BR9507312A/en unknown
- 1995-04-10 CA CA002187651A patent/CA2187651A1/en not_active Abandoned
- 1995-04-10 EP EP95914346A patent/EP0755251A1/en not_active Withdrawn
- 1995-04-10 NZ NZ283354A patent/NZ283354A/en unknown
- 1995-04-10 AU AU21380/95A patent/AU690664B2/en not_active Ceased
- 1995-04-10 JP JP7526068A patent/JPH10502331A/en active Pending
-
1996
- 1996-10-11 KR KR1019960705716A patent/KR970702034A/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| GB9407235D0 (en) | 1994-06-08 |
| MX9604553A (en) | 1997-11-29 |
| JPH10502331A (en) | 1998-03-03 |
| BR9507312A (en) | 1997-10-07 |
| EP0755251A1 (en) | 1997-01-29 |
| ZA952931B (en) | 1996-01-05 |
| AU690664B2 (en) | 1998-04-30 |
| AU2138095A (en) | 1995-10-30 |
| WO1995027486A1 (en) | 1995-10-19 |
| KR970702034A (en) | 1997-05-13 |
| CA2187651A1 (en) | 1995-10-19 |
| NZ283354A (en) | 1998-08-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |