CN1068519C - Medicinal composition for curing ulcer of upper digestive tract and effectively inhibiting recurrance thereof - Google Patents

Medicinal composition for curing ulcer of upper digestive tract and effectively inhibiting recurrance thereof Download PDF

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CN1068519C
CN1068519C CN95101386A CN95101386A CN1068519C CN 1068519 C CN1068519 C CN 1068519C CN 95101386 A CN95101386 A CN 95101386A CN 95101386 A CN95101386 A CN 95101386A CN 1068519 C CN1068519 C CN 1068519C
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treatment
ulcer
furazolidone
digestive tract
oxytetracycline
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CN1129107A (en
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袁凤兰
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Cancer Hospital and Institute of CAMS and PUMC
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Cancer Hospital and Institute of CAMS and PUMC
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Abstract

The present invention relates to a medical composition which can treat upper gastrointestinal tract ulcers and particularly and effectively inhibit the recrudescence of the upper gastrointestinal tract ulcers. The composition contains oxytetracycline and furazolidone of which the weight ratio is from 2.5 to 4:1, and can also contain methoxy chlorobenzene amide. The weight ratio of the methoxy chlorobenzene amide and the furazolidone is from 1:0 to 0.08.

Description

A kind of pharmaceutical composition for the treatment of ulcer of upper digestive tract and effectively suppressing its recurrence
The present invention relates to a kind of pharmaceutical composition and application thereof, particularly relate to a kind of pharmaceutical composition and application thereof that has the treatment ulcer of upper digestive tract and can effectively suppress its recurrence effect.
Ulcer of upper digestive tract, especially gastric ulcer and duodenal bulbar ulcer are a kind of commonly encountered diseases, and its cause of disease and pathogeny are fuzzy so far.
Before the seventies, the treatment peptic ulcer never has effective way.Arrived early seventies, histamine H 2Receptor antagonist has occurred, this H 2Receptor antagonist is secreted by gastric acid inhibitory, reaches the effect of curing gastric ulcer.As cimetidine (Cimetidine), ranitidine (Ranitidine), famotidine (Famotidine) etc." safe stomach U.S. " (effective ingredient is a cimetidine) that the mid-80 occurs made peptic ulcer healing clinically obtain breakthrough progress.
The eighties, people are again to pumping into acid the H of gastral cavity +K +-ATP enzyme is studied, and from H +K +Found omeprazole (that is: losec) in-atpase inhibitor, had the report patient only to need to take every day 20 milligrams, it almost is 100% that 4 all healing rates reach 90%, 8 all healing rates.
The mid-80, owing to isolated helicobacter pylori from gastric mucosa, this bacterium mainly is present in gastric mucosa surface, and the recall rate of duodenal ulcer is 90-100%, the recall rate of gastric ulcer is more than 70%, so assert that this bacterium is relevant with most digestive tract ulcer morbidity.Existing report adopts the effect of mixing the antibiotic therapy gastric ulcer to be better than antacid.
Though said medicine can reach the purpose of curing peptic ulcer, can not guarantee to cure the back Peptic Ulcers and no longer recur.Someone thinks that the healing of peptic ulcer does not have problems, and key is recurrence, and the nearly half of the recurrence of peptic ulcer at present, this is not still had the way of solution again.The inventor finds in nearly 3 years medical practice, with at present commercially available " safe stomach U.S. " (effective ingredient is a cimetidine) is example, statistics half a year, 1 year, 2 years, 3 years treatment example is totally 36 examples, and its stomach and duodenal bulbar ulcer relapse rate have reached 19.4%.
How suppressing the recurrence of ulcer of upper digestive tract, is that people thirst for to solve for a long time always, but the difficult problem that solves of always failing.
The objective of the invention is to provide a kind of pharmaceutical composition that can effectively suppress the ulcer of upper digestive tract recurrence.
Another object of the present invention is to provide a kind of and can treat the pharmaceutical composition that ulcer of upper digestive tract can effectively suppress its recurrence again.
A further object of the present invention is that the application of aforementioned pharmaceutical compositions in pharmacy will be provided.
To achieve the above object of the invention, pharmaceutical composition of the present invention contains oxytetracycline and furazolidone, and both weight ratios are 2.5-4: 1.
Pharmaceutical composition of the present invention also can contain the emesis composition of effective dose, and as the methoxychlor benzamide, the weight ratio of itself and described furazolidone is 1: 0-0.08.
The weight ratio of the oxytetracycline described in the pharmaceutical composition of the present invention, furazolidone can be 5: 2; Or be preferably, the weight ratio of described oxytetracycline, furazolidone and methoxychlor benzamide is 4: 1: 0.08; Or, also containing vitamin B6, the weight ratio of wherein said oxytetracycline, furazolidone, methoxychlor benzamide and vitamin B6 is 2.5: 1: 0.04: 0.1.
Pharmaceutical composition of the present invention can be applicable to prepare the treatment ulcer of upper digestive tract, especially is applied to prepare and has the medicine that suppresses ulcer of upper digestive tract recurrence effect.
Furazolidone (Furazolidonum as one of composition of the present composition, Furazolidone), have another name called " furazolidone ", be extensive pedigree antibiotic, Gram-positive and gram negative bacteria all there is effect, all effective to escherichia coli, Crewe Bai Shi pneumobacillus, Salmonella, dysentery bacterium, staphylococcus, enterococcus, its antibacterial principle it be unclear that.Furazolidone is the medicine of a kind of treatment enteritis commonly used, dysentery, typhoid fever, paratyphoid fever, and effective to treatment stomach, duodenal ulcer.This medical instrument has antibiotic wide, stable performance, convenient oral, synthetic easy, cheap and be difficult for developing immunity to drugs, and do not have advantages such as the drug resistance of intersection shape with other antibacterials, but certain toxic and side effects is arranged, and oral absorption is poor, so can only make the enteritis curative.
Just contain furazolidone among " Si Damoke (Film coated tablets) (the Tabellae Stomachi) " in the market (Harbin pharmacy four factories product)." Si Damoke " is applicable to treatment stomach, duodenal ulcer disease, chronic gastritis etc.But do not see that it has the effect that suppresses the digestive tract ulcer recurrence after healing, and its side effect is bigger.
Another main component of the present composition is oxytetracycline (Oxytetracycline), it is all effective to coccus, Gram-positive bacillus, spirillum, actinomycetes, but not as good as penicillin, effective to gram negative bacteria, responsive inadequately to typhoid fever, Salmonella paratyphi, not good to the bacillus pyocyaneus clinical effectiveness, stronger to rickettsia, chlamydia, mycoplasma effect.Its antibacterial mechanisms is that Profilin matter is synthetic.Though the report that utilizes the antibiotic therapy digestive tract ulcer is arranged, clinical middle oxytetracycline is applied to various infectious disease always, and Shang Weijian is applied to treat ulcer of upper digestive tract, does not see that also it has the report to the effect of digestive tract ulcer recurrence.
Above-mentioned oxytetracycline and furazolidone are by 2.5-4: 1 compositions of making after mixing promptly has the treatment ulcer of upper digestive tract and suppresses the effect of its recurrence, as illustrated in fig. 1 and 2, partly is clearly better with above-mentioned medicine composite for curing front and back gastric ulcer.But side reaction is bigger, as feel sick, vomiting etc., so in said composition a certain proportion of Bendectin of adding, be preferably the methoxychlor benzamide, its medicine be called paspertin metoclopramide (Paspertinum, Paspertin), have another name called metoclopramide (Primperan), perhaps add vitamin B6 etc. again.
The methoxychlor benzamide is antiemetic commonly used, and it can promote gastric peristalsis, quickens the gastric content emptying, improve the stomach function; Owing to can promote gastric emptying, prevent that duodenal juice from backflowing into stomach, destroy gastric mucosal barrier, can prevent the generation of stress ulcer, peptic ulcer there is certain curative effect.But this class Bendectin is seen at the end report that suppresses the digestive tract ulcer recurrence is arranged.
So pharmaceutical composition of the present invention can contain above-mentioned composition more than three kinds or three kinds, and wherein the weight ratio of oxytetracycline, furazolidone and methoxychlor benzamide is 2.5-4: 1: 0-0.08, the weight ratio that is preferably oxytetracycline, furazolidone and methoxychlor benzamide is 4: 1: 0.08, or the weight ratio of oxytetracycline, furazolidone, methoxychlor benzamide and vitamin B6 is 2.5: 1: 0.04: 0.1.
Compositions of the present invention is applied to preparation and has the treatment ulcer of upper digestive tract, when especially suppressing the medicine of ulcer of upper digestive tract recurrence, can be directly with after above-mentioned three kinds or the four kinds of compound, during metering incapsulates, or, make the oral agents of tablet or other types with after a certain amount of pharmaceutically acceptable carrier mixes.Above-mentioned preparation method is familiar with to those skilled in the art.
The oral conventional amount used of said medicine is respectively: oxytetracycline 0.5 gram, 3-4 time/day; Furazolidone 0.2 gram, 3 times/day; 8 milligrams of methoxychlor benzamides, 3 times/day.
Pharmaceutical composition of the present invention is when being used for the treatment of ulcer of upper digestive tract and suppress the ulcer of upper digestive tract recurrence, 8 days courses of treatment, 12 to 28 restrain altogether, every day 1-4 time, each 0.7-1.4 gram, but the conventional amount used when controlling various composition consumptions every day and being no more than it and using is separately preferably taken number of times and is per diem successively decreased.
Perhaps, get commercially available hydroxytetracycline tablet, furaxone and metoclopramide sheet respectively and place dry mortar to grind in proportion, sieve (as using 80 mesh sieves), make that mixed medicine grain is even and have certain particulate, be sub-packed in capsule or be pressed in the tablet, promptly made above-mentioned medicine.
Medicine composite for curing stomach of the present invention and duodenal bulbar ulcer, behind the 0.5-8, its average cure rate is 98.9%, average relapse rate is 1.1%; And with as " safe stomach U.S. " treatment stomach and duodenal bulbar ulcer, behind the 3-6, its average cure rate is 80.4%, average relapse rate is 19.4%.Concrete comparative example is seen below.As seen, the medicine of the treatment digestive tract ulcer that relates to prior art is compared, pharmaceutical composition of the present invention not only improves the cure rate of ulcer of upper digestive tract significantly, and has controlled the recurrence of ulcer of upper digestive tract especially effectively, has promptly suppressed to cure back ulcer palindromia.
Among the present invention, the inventor uses oxytetracycline, furazolidone and the present composition to do contrast respectively separately, and the result shows that oxytetracycline is invalid to ulcer of upper digestive tract, and furazolidone has certain effect to ulcer of upper digestive tract, but almost can not control the recurrence of ulcer.
Brief Description Of Drawings is as follows:
Figure 1A and B are and treatment back patient's preceding with medicine composite for curing of the present invention abrasive net-balloon for stomach portion gastroscope photo;
Fig. 2 A and B are and treatment back patient's preceding with medicine composite for curing of the present invention stomach bight gastroscope photo.
Below in conjunction with embodiment and treatment and reference examples pharmaceutical composition of the present invention is described, but be not used in restriction the present invention.Used tablet oxytetracycline, furazolidone and metoclopramide and used raw material oxytetracycline, furan are sat ketone, methoxybenzene amide and VB6 and are commercially available among the following embodiment.
Embodiment 1
Respectively get 80 of the furazolidones of 80 of the oxytetracyclines of 0.25 gram/sheet and 0.1 gram/sheet, after the pulverizing, be pressed into tablet A, totally 40, every contains oxytetracycline 0.5 gram, furazolidone 0.2 gram.
Embodiment 2
Respectively get 100 of the furazolidones of 160 of oxytetracyclines, the 0.1 gram/sheet of 0.25 gram/sheet, and after 200 pulverizing of the metoclopramide of 4 milligrams/sheet, the capsule of packing into No. 0 after sieving with 80 is made capsule B100 ball altogether.Every contains oxytetracycline 0.4 gram, furazolidone 0.1 gram, 8 milligrams of methoxybenzene amide.
Embodiment 3
Respectively get 100 of the furazolidones of 160 of oxytetracyclines, the 0.1 gram/sheet of 0.25 gram/sheet, and after 200 pulverizing of the metoclopramide of 4 milligrams/sheet, the capsule of packing into No. 1 after sieving with 80 is made capsule C300 ball altogether.Every contains oxytetracycline 0.13 gram, furazolidone 0.3 gram, 2.7 milligrams of methoxybenzene amide.
Embodiment 4
Respectively fetch earth mycin 400 gram, furazolidone 100 grams, and methoxybenzene amide 8 grams, and an amount of carrier are made tablet D behind the mix homogeneously, wherein every contains oxytetracycline 0.4 gram, furazolidone 0.1 gram, and 8 milligrams of methoxychlor benzamides.
Embodiment 5
Respectively fetching earth, mycin 250 restrains, furazolidone 100 grams, methoxybenzene amide 4 grams, vitamin B6 10 grams, and dress is made capsule E as No. 0 capsule behind an amount of carrier mix homogeneously, and wherein every ball contains oxytetracycline 0.25 gram, furazolidone 0.1 gram, 4 milligrams of methoxychlor benzamides, VB610 milligram.
Below used gastroscope is P10 type (an OLYMPUS product) in the treatment example, and GI produces for Tianjin, island.
Treatment example 1
1985, gastric and duodenal ulcers patient 5 examples, with the capsules A that embodiment 1 makes, 8 days courses of treatment, first and second day, 4 times/day, each 2, third and fourth day, 3 times/day, each 2, the 5th, six day, 2 times/day, each 2, the 7th, eight day, 1 time/day, each 2.Reaction is for nauseating, dizzy and weak during the treatment, and treatment back pain disappears, and dietary amount significantly increases, healing example 5 examples, and cure rate is 100%, (8 years) do not have recurrence so far.
Figure 1A, B and Fig. 2 A, B reflect abrasive net-balloon for stomach portion and the stomach bight ulcer healing situation before and after its typical treatment.
Treatment example 2
1986, gastric and duodenal ulcers patient 7 examples, with the capsule B that embodiment 2 makes, 8 days courses of treatment, medicining mode is with treatment example 1.Reaction is for nauseating, dizzy and weak during the treatment, and treatment back pain disappears, and dietary amount significantly increases, healing example 7 examples, and cure rate is 100%, (7 years) do not have recurrence so far.
Treatment example 3
1987, gastric and duodenal ulcers patient 24 examples, with the tablet D that embodiment 4 makes, 8 days courses of treatment, medicining mode is with treatment example 1.Reaction is nauseating, dizziness and weak during the treatment, and treatment back pain disappears, and dietary amount significantly increases, healing example 23 examples, and cure rate is 95.8%, (6 years) recur 1 example, relapse rate 4.2% so far.
Treatment example 4
1988, gastric and duodenal ulcers patient 133 examples, with the tablet D that embodiment 4 makes, 8 days courses of treatment, medicining mode is with treatment example 1.Reaction is nauseating, dizziness and weak during the treatment, and treatment back pain disappears, and dietary amount significantly increases, healing example 132 examples, and cure rate is 99.2%, (5 years) recur 1 example, relapse rate 0.8% so far.
Treatment example 5
Nineteen ninety, gastric and duodenal ulcers patient 116 examples, with the capsule B that embodiment 2 makes, 8 days courses of treatment, medicining mode is with treatment example 1.Reaction is nauseating, dizziness and weak during the treatment, and treatment back pain disappears, and dietary amount significantly increases, healing example 115 examples, and cure rate is 99.1%, (4 years) recur 1 example, relapse rate 0.9% so far.
Treatment example 6
1991, gastric and duodenal ulcers patient 77 examples, with the capsule B that embodiment 2 makes, 8 days courses of treatment, first to fourth day, 3 times/day, each 2, the 5th, six day, 2 times/day, each 2, the 7th, eight day, 1 time/day, each 2.Reaction is for slightly weak and dizzy during the treatment, and treatment back pain disappears, and dietary amount significantly increases, and cures example 75 examples, and cure rate is 97.4%, and (3 years) recur 2 examples, relapse rate 2.6% so far.
Treatment example 7
1992, gastric and duodenal ulcers patient 17 examples, with the capsule C that embodiment 3 makes, 8 days courses of treatment, medicining mode is with treatment example 6.Reaction is for slight weak and dizzy during the treatment, and treatment back pain disappears, and dietary amount significantly increases, and cures example 17 examples, and cure rate is 100%, and (2 years) do not have recurrence so far.
Treatment example 8
1993, gastric and duodenal ulcers patient 28 examples, with the capsule E that embodiment 5 makes, 8 days courses of treatment, medicining mode is with treatment example 6.Reaction is for slight weak and dizzy during the treatment, and treatment back pain disappears, and dietary amount significantly increases, and cures example 28 examples, and cure rate is 100%, and (1 year) does not have recurrence so far.
Treatment example 9
1994, gastric and duodenal ulcers patient 146 examples, with the capsule E that embodiment 5 makes, 8 days courses of treatment, medicining mode is treatment example 6 together, or increases a course of treatment according to the state of an illness.Reaction is for slightly weak and dizzy during the treatment, and treatment back pain disappears, and dietary amount significantly increases, and cures example 144 examples, and cure rate is 98.6%, and (6 to December) recurs 2 examples, relapse rate 1.4% so far.
Comprehensive above-mentioned treatment example 1-9, total case 637 people cure 630 examples, recur 7 examples, and total cure rate is 98.9%, and relapse rate is 1.1%.
Comparative Examples
0.5-3 behind " safe stomach U.S. " treatment stomach of producing with Xi'an Janssen Pharmaceutica factory and the duodenal bulbar ulcer, totally 36 examples are cured 29 examples, recur 7 examples, and total cure rate is 80.4%, and relapse rate is 19.4%.Concrete treatment and clinical observation are as shown in table 1.
Table 1
Time (year) 0.5 123 add up to
The example number 12 11 8 5 36
Diagnosis Gastric and duodenal ulcers
Method Gastroscope+GI
Dosage 800mg/ day
The course of treatment (month number) 6 6-10 6-12 12-18
Cure routine number 10 9 6 4 29
Recur routine number 2 2 2 1 7
Cure rate (%) 83.3 82 75 80 80.4
Relapse rate (%) 16.7 18 25 20 19.4

Claims (8)

1, a kind of pharmaceutical composition, this pharmaceutical composition contains oxytetracycline and furazolidone, and both weight ratios are 2.5-4: 1.
2, pharmaceutical composition as claimed in claim 1 is characterized in that it also contains the emesis composition of effective dose.
3, pharmaceutical composition as claimed in claim 2 is characterized in that described emesis composition is the methoxychlor benzamide, and the weight ratio of itself and furazolidone is 0-0.08: 1.
4, pharmaceutical composition as claimed in claim 1, the weight ratio that it is characterized in that oxytetracycline, furazolidone is 5: 2.
5, as claim 2 or 3 described pharmaceutical compositions, the weight ratio that it is characterized in that oxytetracycline, furazolidone and methoxychlor benzamide is 4: 1: 0.08.
6, as claim 2 or 3 described pharmaceutical compositions, it is characterized in that wherein also containing vitamin B6, and the weight ratio of oxytetracycline, furazolidone, methoxychlor benzamide and vitamin B6 is 2.5: 1: 0.04: 0.1.
7, a kind of have the treatment ulcer of upper digestive tract and can suppress the medicine of its recurrence effect, wherein contains the pharmaceutical composition as claimed in claim 1 or 2 and the carrier of effective dose.
8, have the treatment ulcer of upper digestive tract and suppress application in the medicine of its recurrence effect in preparation as the pharmaceutical composition of claim 1 or 2.
CN95101386A 1995-02-14 1995-02-14 Medicinal composition for curing ulcer of upper digestive tract and effectively inhibiting recurrance thereof Expired - Fee Related CN1068519C (en)

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Publication number Priority date Publication date Assignee Title
CN1086944C (en) * 1999-04-22 2002-07-03 山东农业大学动物保健品厂 Composition for treating and preventing coccidiosis of chicken
CN100420447C (en) * 2006-06-23 2008-09-24 吕维江 Medicine for treating gastropathy and duodenal ulcer
CN103550390A (en) * 2013-10-26 2014-02-05 武文栋 Pharmaceutical composition for treating gastric ulcer
CN104983748A (en) * 2015-06-12 2015-10-21 梁美赠 Medicine for treating stomach illness

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989003219A1 (en) * 1987-10-12 1989-04-20 Borody Thomas J Improved method for treatment of gastrointestinal disorders

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989003219A1 (en) * 1987-10-12 1989-04-20 Borody Thomas J Improved method for treatment of gastrointestinal disorders

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
《中国医院药学杂志》老药治疗消化性溃疡八则 1991.11.2 张瑜等 *

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