CN1683013A - Oral administration gastric slow release preparation for treating chronic gastritis, peptic ulcer and intestinal infection - Google Patents
Oral administration gastric slow release preparation for treating chronic gastritis, peptic ulcer and intestinal infection Download PDFInfo
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- CN1683013A CN1683013A CN 200510009758 CN200510009758A CN1683013A CN 1683013 A CN1683013 A CN 1683013A CN 200510009758 CN200510009758 CN 200510009758 CN 200510009758 A CN200510009758 A CN 200510009758A CN 1683013 A CN1683013 A CN 1683013A
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- slow releasing
- peptic ulcer
- chronic gastritis
- intestinal infection
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Abstract
The present invention discloses a kind of orally taken gastric slow releasing preparation for treating chronic gastritis, peptic ulcer and intestinal infection. The preparation includes bactericidal medicine component, slow releasing agent, float assistant and adhesive in the weight ratio of 1 to 1.5-8 to 0.5-2.5 to 0.5-2.5. The bactericidal medicine component may be Clarithromycin, gentamicin sulfate, Metronidazole or Tinidazole for treating digestive tract infection caused by pyloric spirobacterium infection.
Description
Technical field:
The present invention relates to a kind of gastric slow releasing preparation for oral use for the treatment of chronic gastritis, peptic ulcer and intestinal infection that Helicobacter pylori infection causes.
Background technology:
Continuous expansion along with the chronic disease crowd, extensive patients is being perplexed in chronic gastritis that is caused by helicobacter pylori and peptic ulcer and responsive microbial intestinal infection, helicobacter pylori (HP) is a chronic gastritis, the pathogen of gastric and duodenal ulcers, multiple antibiotics is to the HP sensitivity, as xacin-series, cephalo-type etc., said medicine can absorb, thereby body worked the mischief cause liver, renal damage and anaphylaxis, slow release by comparison, controlled release preparation has overcome above shortcoming, seek the new slow releasing agent and the kind and the weight proportion thereof of adjuvant,, simplify medication to reduce the human body infringement, be that the medical research personnel endeavour the problem that solves always.
Summary of the invention:
The gastric slow releasing preparation for oral use that the purpose of this invention is to provide chronic gastritis, peptic ulcer and intestinal infection that the long treatment helicobacter pylori of a kind of taking convenience, holdup time causes.
Above-mentioned purpose realizes by following technical scheme:
The oral gastric slow releasing preparation of treatment chronic gastritis peptic ulcer and intestinal infection, its composition comprises: bactericidal properties crude drug, slow releasing agent, bleach activator and binding agent, ratio of weight and number is between described bactericidal properties crude drug, slow releasing agent, bleach activator and the binding agent: bactericidal properties crude drug 1, slow releasing agent 1.5-8, bleach activator 0.5-2.5, binding agent 0.5-2.5, described bactericidal properties crude drug comprises clarithromycin, gentamycin sulfate, metronidazole, tinidazole.
The oral gastric slow releasing preparation of above-mentioned treatment chronic gastritis peptic ulcer and intestinal infection, described slow releasing agent can be one or more mixture in stearyl alcohol, monostearate, glyceride, carbomer, the Rikemal B 200.
The oral gastric slow releasing preparation of above-mentioned treatment chronic gastritis peptic ulcer and intestinal infection, described binding agent can be one or more mixture in dextrin, microcrystalline Cellulose, starch slurry or the Polyethylene Glycol.
The oral gastric slow releasing preparation of above-mentioned treatment chronic gastritis peptic ulcer and intestinal infection, described bleach activator can be one or more mixture in sodium bicarbonate, stearic acid or the glyceryl monostearate.
The oral gastric slow releasing preparation of above-mentioned treatment chronic gastritis peptic ulcer and intestinal infection, described bleach activator can be one or more mixture in sodium bicarbonate, stearic acid or the glyceryl monostearate.
This technical scheme has following beneficial effect:
1. proportioning of the present invention can reduce patient's medicining times and medication dose, improves the compliance that the patient takes medicine, and taking convenience.
2. this law is bright is slow releasing preparation, and medicine is dissolved in the skeleton, discharges with constant rate of speed, thereby makes stomach keep for a long time (6-12 hour) constant active drug concentration, thereby overcome the oral antibiotic gastric valid density short shortcoming of holding time.
3. the present invention can the long period be stranded in the gastric juice, and prolong drug is improved drug absorption in digestive tract release time, has reduced the toxic and side effects of medicine, has also guaranteed the safety and the effectiveness of medicine simultaneously.
4. product of the present invention can improve the compliance that patient takes medicine greatly, easy to use, medicining times is few, can reduce simultaneously the toxic and side effects of medicine, both remedied the weak point of ordinary preparation, made things convenient for vast chronic gastritis, peptic ulcer and intestinal infection patient, give again slow release, controlled release preparation interpolation new blood.
5. the slow releasing agent Rikemal B 200 of the present invention and the acidic drug compatibility are good, and the release of disintegration time and medicine is not had influence, reduce ejection force, and improve the compressibility in the tablet manufacturing, have adhesion characteristic, and be responsive to the long nothing of incorporation time.Pharmaceutical compositions is scattered in its skeleton, and when meeting with physiological liquid, it just discharges lentamente by flooding mechanism or erosion mechanism.It can be used in wet granulation, direct compression, hot melt coating, melt granulation, extrude spheronization etc., amplifies easily and produces.Have flavor, chemoproection and the anti-oxidation or anti-hydrolysis of screening.
6. the used slow releasing agent of the present invention has inherent unique cross-linked structure, and viscosity that it is good and hydrophilic make it have good control slow releasing function.Carbomer has the good compatibility chemically very stable with various active medicines, with other adjuvants good mixing is arranged.The preparation that adopts carbomer to make shows zero level or near the release dynamics of zero level.These polymer have extremely rapid and effective gelation characteristics, and they also have good control slow releasing function under very low concentration.Compare with the slow releasing agent that existing medicine is used: as slow-release material, can obtain the preparation of approximate zero level medicine-releasing system with carbomer; More less than other slow-release material consumptions, can increase the choice of prescription; And have fabulous compressibility, fine with other adjuvant compatibility.
7. the present invention is the preparation that contains bleach activator, and when contacting with gastric juice, chemical reaction generation carbon dioxide at first takes place for bleach activator and gastric juice makes slice, thin piece begin to float.After treating that carbon dioxide is released ease, hydrophilic gel begins to form the fluid-tight colloid barrier film of one deck in tablet surface through hydration swelling, and the density of keeping slice, thin piece is less than 1 and control drug release.Because the sheet sub-volumes after expanding increases, be difficult to by pylorus, simultaneously so can be stranded in gastric for a long time.Smaller volume just finally is drained after carrying medicament discharges complete or gel layer corrosion.The release in vitro of floating tablets medicine can be described with multiple dynamics formula, and wherein most Higuchi equation (square root that is burst size and time is linear) and Korsemeyer-Peppas empirical equation (are M
t/ M
∞=kt
n, most of intra-gastric floating tablet spread in dispose procedure and corrosion is carried out simultaneously, so its n is between 0.5 and 1.0, meet non-Fickian diffusion law).In addition, the release in vitro of minority medicine meets zero level or first order kinetics.
Solubility curve after solubility curve 8. of the present invention and the accelerated aging test (external, USP method, pH=6.8)
Solubility curve
Solubility curve after the accelerated aging test (external, USP method, pH=6.8)
By above solubility curve, whole as can be seen prescription has good stable, and the change of any physical behavior does not take place at duration of storage.
The specific embodiment of the present invention:
Embodiment 1:
Get 1 part of gentamycin sulfate, add 1.5 parts of carbomers, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of dextrin, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of sodium bicarbonate, cross 60 or 80 or 100 or 120 mesh sieves respectively, fully mix, tabletting promptly gets the present invention; Or the medical alcohol with 70%～95% is granulated after the mixing of sieving, granulate, and tabletting promptly gets product of the present invention.Described umber is parts by weight.
The adding scheme of adjuvant:
A. add 1.5 parts of carbomers and change----3 parts of carbomers of adding and 2.5 parts of glyceride into
B.0.5 or 1 part or 1.5 parts or 2.5 parts of starch slurries change-----0.5 part of dextrin and 1 part of microcrystalline Cellulose and 0.5 part of starch slurry into;
C.0.5 part or 1 part or 1.5 parts or 2 parts or 2.5 parts of mono stearate glyceryl esters change----0.5 part of sodium bicarbonate and 0.5 part of hard ester acid into;
D.1.5 part glyceride changes the pure and mild 4.5 parts of Rikemal B 200s of-----0.5 part of hard ester into.
Embodiment 2:
Get 1 part of metronidazole, add 1.5 parts of wych-elm acid glycerides, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of starch slurries, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of stearic acid, cross 60 or 80 or 100 or 120 mesh sieves respectively, fully mix, tabletting promptly gets the present invention; Or the medical alcohol with 70%～95% is granulated after the mixing of sieving, granulate, and tabletting promptly gets the present invention.Described umber is parts by weight.The adjustment scheme of adjuvant is seen upward example.
Embodiment 3:
Get 1 part of clarithromycin, add 1.5 portions of glyceride, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of microcrystalline Cellulose, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of glyceryl monostearate, cross 60 or 80 or 100 or 120 mesh sieves respectively, fully mix, tabletting promptly gets the present invention; Or the medical alcohol with 70%～95% is granulated after the mixing of sieving, granulate, and tabletting promptly gets the present invention.Described umber is parts by weight.The adjustment scheme of adjuvant is seen above each example.
Embodiment 4:
Get 1 part of tinidazole, add 1.5 portions of glyceride, 0.5 or 1 part or 1.5 parts or 2 parts or 2.5 parts of Polyethylene Glycol, 0.5-2.5 part stearic acid, cross 60 or 80 or 100 or 120 mesh sieves respectively, fully mix, tabletting promptly gets the present invention; Or the medical alcohol with 70%～95% is granulated after the mixing of sieving, granulate, and tabletting promptly gets the present invention.Described umber is parts by weight.The adjustment scheme of adjuvant is seen above each example.
This product is used for the treatment of light-duty acute enteritis, 2 times on the one, one time 2, be 3-5 days the course of treatment.
This product is used for the treatment of stomach and duodenum Helicobacter pylori infection, 2 times on the one, one time 2,3-4 week is a course of treatment, takes in 1 hour after the meal.
Claims (5)
1. oral gastric slow releasing preparation for the treatment of chronic gastritis peptic ulcer and intestinal infection, its composition comprises: bactericidal properties crude drug, slow releasing agent, bleach activator and binding agent, it is characterized in that: ratio of weight and number is between described bactericidal properties crude drug, slow releasing agent, bleach activator and the binding agent: bactericidal properties crude drug 1, slow releasing agent 1.5-8, bleach activator 0.5-2.5, binding agent 0.5-2.5, described bactericidal properties crude drug comprises clarithromycin, gentamycin sulfate, metronidazole, tinidazole.
2. the oral gastric slow releasing preparation of treatment chronic gastritis peptic ulcer according to claim 1 and intestinal infection is characterized in that: described slow releasing agent can be one or more mixture in stearyl alcohol, monostearate, glyceride, carbomer, the Rikemal B 200.
3. the oral gastric slow releasing preparation of treatment chronic gastritis peptic ulcer according to claim 1 and 2 and intestinal infection is characterized in that: described binding agent can be one or more mixture in dextrin, microcrystalline Cellulose, starch slurry or the Polyethylene Glycol.
4. the oral gastric slow releasing preparation of treatment chronic gastritis peptic ulcer according to claim 1 and 2 and intestinal infection is characterized in that: described bleach activator can be one or more mixture in sodium bicarbonate, stearic acid or the glyceryl monostearate.
5. the oral gastric slow releasing preparation of treatment chronic gastritis peptic ulcer according to claim 3 and intestinal infection is characterized in that: described bleach activator can be one or more mixture in sodium bicarbonate, stearic acid or the glyceryl monostearate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510009758 CN1683013A (en) | 2005-02-21 | 2005-02-21 | Oral administration gastric slow release preparation for treating chronic gastritis, peptic ulcer and intestinal infection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510009758 CN1683013A (en) | 2005-02-21 | 2005-02-21 | Oral administration gastric slow release preparation for treating chronic gastritis, peptic ulcer and intestinal infection |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1683013A true CN1683013A (en) | 2005-10-19 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510009758 Pending CN1683013A (en) | 2005-02-21 | 2005-02-21 | Oral administration gastric slow release preparation for treating chronic gastritis, peptic ulcer and intestinal infection |
Country Status (1)
| Country | Link |
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| CN (1) | CN1683013A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265708A (en) * | 2016-07-20 | 2017-01-04 | 南京正宽医药科技有限公司 | A kind of clarithromycin tablet and preparation method thereof |
| CN113367247A (en) * | 2021-01-05 | 2021-09-10 | 安徽科技学院 | Feed additive for preventing broiler chicken myogastric and glandular gastritis |
-
2005
- 2005-02-21 CN CN 200510009758 patent/CN1683013A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265708A (en) * | 2016-07-20 | 2017-01-04 | 南京正宽医药科技有限公司 | A kind of clarithromycin tablet and preparation method thereof |
| CN113367247A (en) * | 2021-01-05 | 2021-09-10 | 安徽科技学院 | Feed additive for preventing broiler chicken myogastric and glandular gastritis |
| CN113367247B (en) * | 2021-01-05 | 2023-11-14 | 安徽科技学院 | Feed additive for preventing stomach proventriculitis of broiler chickens |
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