CN1039195C - Gastric slow-released preparation of curing gastrosia by killing pyloric spirillum - Google Patents

Gastric slow-released preparation of curing gastrosia by killing pyloric spirillum Download PDF

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Publication number
CN1039195C
CN1039195C CN95100772A CN95100772A CN1039195C CN 1039195 C CN1039195 C CN 1039195C CN 95100772 A CN95100772 A CN 95100772A CN 95100772 A CN95100772 A CN 95100772A CN 1039195 C CN1039195 C CN 1039195C
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China
Prior art keywords
preparation
weight
entogastric
helicobacter pylori
acrylic resin
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Expired - Fee Related
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CN95100772A
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Chinese (zh)
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CN1111131A (en
Inventor
刘理
刘智
钱进
廖敢
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JIANGXI PHARMACEUTICAL CO Ltd
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JIANGXI PHARMACEUTICAL CO Ltd
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Priority to CN95100772A priority Critical patent/CN1039195C/en
Publication of CN1111131A publication Critical patent/CN1111131A/en
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Publication of CN1039195C publication Critical patent/CN1039195C/en
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Expired - Fee Related legal-status Critical Current

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Abstract

The present invention relates to an entogastric sustained release preparation for treating gastritis and peptic ulcer, which is composed of the following raw materials by the weight rate: 1 portion of aminocyclitol antibiotic, 2 to 7.5 portions of hydrophilic polymer material, 1 to 5 portions of acrylic resin and 2 to 7.5 portions of high fat alcohol, wherein the aminocyclitol antibiotic is used as raw medicinal materials, and the hydrophilic polymer material, the acrylic resin and the high fat alcohol are used as auxiliary materials. The preparation can reach the needed medicinal bactericidal concentration and prolongs the entogastric detention time of the medicinal preparation by controlling the entogastric detention time of medicines and the slow release of the medicines; thus, pyloric spirillum is effectively killed, and gastritis, peptic ulcer and enteritis caused by the infection with intestinal bacteria are cured.

Description

Kill the Entogastric lingering slow releasing preparation of treatment of helicobacter pylori gastropathy
The present invention relates to a kind of preparation for the treatment of gastritis and peptic ulcer, especially a kind of gastric retention type slow releasing preparation.
Development along with the medical science technology, the expert has done a large amount of work to the reason that causes chronic gastropathy both at home and abroad, especially from 1993 isolate helicobacter pylori (being called for short HP) first from people's gastric mucosa since, they have carried out a large amount of research to this bacterium, and tentative confirmation HP is the main diseases therefore of chronic gastritis.Gastritis is a kind of commonly encountered diseases, frequently-occurring disease, and it can slowly develop into atrophic gastritis, and the latter is closely related with gastric cancer, eradicates chronic indigestion or the intravital helicobacter pylori of peptic ulcer patient and seems more and more important.
Helicobacter pylori (HP) is a kind of gram negative bacilli, and this bacterium is positioned at gastric mucus deep layer mucomembranous surface, is grown in little aerobic environment, so can exempt from the injury of acidic gastric juice.This bacterium can infect normal gastric mucosa, causes acute or chronic gastritis.Yet aminocyclitol antibiotic is extremely sensitive to the HP bacterium.MIC to isolating 50 strain HP bacterium is 0.16mg/ml.
The object of the present invention is to provide a kind of may command medicine in the holdup time of gastric and the slow release of medicine, reach required medicine bacteriocidal concentration in the body, thereby kill helicobacter pylori effectively, cure the gastric retention type slow releasing preparation of gastritis and peptic ulcer.
Task of the present invention realizes in the following manner: this Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy is as raw material with aminocyclitol antibiotic, with hydrophilic high molecular material, acrylic resin and high fat alcohol as adjuvant, in per 1 part of (weight) aminocyclitol antibiotic, allocate 2~7.5 parts of (weight) hydrophilic high molecular materials into, 1~5 part of (weight) acrylic resin and 2~7.5 parts of (weight) high fat alcohols.
Used aminocyclitol antibiotic is gentamycin sulfate, Micronomicin Sulfate, tobramycin sulfate or streptomycin sulfate etc. among the present invention.
Used in the present invention hydrophilic high molecular material is hydroxypropyl methylcellulose (HPMC), carboxymethyl cellulose (CMC) and sodium carboxymethyl cellulose (CMC-Na).
Used in the present invention high fat alcohol comprises 14~20 alkanols.
The manufacture method of slow releasing preparation of the present invention is as follows: at first crude drug and adjuvant are crossed the mixing of 20~80 mesh sieves, use dry method then, former, the adjuvant that mixes directly pushed granule.The supplementary material concentration that also available wet-mixed is good is the alcohol granulation drying of 10~90% (weight).With the granule that the makes punch die tabletting with 8~12mm/mm, pressure is 3~7kg/cm at last 2
The present invention can reach required medicine bacteriocidal concentration in the body by the control medicine in the holdup time of gastric and the slow release of medicine.The gastric retention type slow releasing tablet that the present invention designs according to fluid dynamic equilibrium control system principle can significant prolongation pharmaceutical preparation in the time of Entogastric lingering, play the effect of drug depot.Said preparation has adopted hydrophilic high molecular material, and when with after gastric juice contacts, its dosage surface aquation forms gel, and makes volumetric expansion, and at this moment the proportion of tablet makes slice, thin piece can float in the stomach Dissolve things inside less than gastric juice proportion.This preparation adds an amount of acrylic resin, as the basic framework of said preparation, makes medicine slowly to discharge from skeleton.In order to increase the flotation property of preparation, added an amount of high fat alcohol in this preparation.The adjuvant of this preparation can not only make preparation proportion reduce, and floats in the stomach, and can discharge by blocking medicine.Prove that through test of many times said preparation can discharge certain drug level by certain speed in the regular hour.Medicine in the preparation discharged 40~60%, 4 hours in 2 hours and discharges release in 60~80%, 6 hours more than 70%; The said preparation sheet is 5~6 hours in the holdup time of gastric; This slow releasing preparation not only can be treated the gastritis and the peptic ulcer of Helicobacter pylori infection, can also treat the enteritis of enterobacterial infection.
Below in conjunction with embodiment the present invention is described in more detail.
Embodiment 1:
This Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy with Micronomicin Sulfate as crude drug, with carboxymethyl cellulose (CMC), acrylic resin and tetradecanol as adjuvant, in the Micronomicin Sulfate of 1 part (weight), allocate 3 parts of (weight) carboxymethyl celluloses into, 2 parts of (weight) acrylic resins and 5 parts of (weight) tetradecanols.
At first above-mentioned supplementary material is crossed 40 mesh sieve mix homogeneously, with dry method the supplementary material that mixes directly is squeezed into granule then, the punch die tabletting of reuse 8mm/mm, pressure are 4kg/cm 2
Embodiment 2:(commodity are called Swibec TAB)
This Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy with gentamycin sulfate as crude drug, with hydroxypropyl methylcellulose (HPMC), acrylic resin and octadecanol are as adjuvant, in the gentamycin sulfate of 1 part (weight), allocate 7 parts of (weight) hydroxypropyl methylcellulose into, 4 parts of (weight) acrylic resins and 3 parts of (weight) octadecanols.
At first above-mentioned supplementary material is crossed 80 mesh sieve mix homogeneously, with dry method the supplementary material that mixes directly is pressed into granule then, the punch die tabletting of 10mm/mm is arranged again, pressure is 5kg/cm 2
Embodiment 3:
This Entogastric lingering slow releasing agent system of killing treatment of helicobacter pylori gastropathy with tobramycin sulfate as crude drug, with sodium carboxymethyl cellulose (CMC-Na), acrylic resin and hexadecanol as adjuvant, in the tobramycin sulfate of 1 part (weight), allocate 5 parts of (weight) sodium carboxymethyl cellulose into, 3 parts of (weight) acrylic resins and 6 parts of (weight) hexadecanols.
At first above-mentioned supplementary material being crossed 60 mesh sieve mix homogeneously, used wet method then, is 75% alcohol granulation drying with the supplementary material concentration that mixes.At last the granule that makes is used the punch die tabletting of 12mm/mm, pressure is 5kg/cm 2
Embodiment 4:
This Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy with streptomycin sulfate as crude drug, with carboxymethyl cellulose (CMC), acrylic resin and EICOSANOL as adjuvant, in the streptomycin sulfate of 1 part (weight), allocate 4 parts of (weight) carboxymethyl celluloses into, 4.5 parts of (weight) acrylic resins and 4 parts of (weight) EICOSANOL.
At first above-mentioned supplementary material being crossed 80 mesh sieve mix homogeneously, used wet method then, is 90% alcohol granulation drying with the supplementary material concentration that mixes, and at last the granule that makes is had the punch die tabletting of 10mm/mm, and pressure is 4kg/cm 2

Claims (4)

1, a kind of Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy, it is characterized in that: with aminocyclitol antibiotic as crude drug, with hydrophilic high molecular material, acrylic resin and high fat alcohol are as adjuvant, in per 1 part of (weight) aminocyclitol antibiotic, allocate 2-7.5 part (weight) hydrophilic high molecular material into, 1-5 part (weight) acrylic resin and 2-7.5 part (weight) high fat alcohol.
2, the Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy according to claim 1, it is characterized in that: aminocyclitol antibiotic is gentamycin sulfate, Micronomicin Sulfate, tobramycin sulfate or streptomycin sulfate.
3. the Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy according to claim 1 is characterized in that: hydrophilic high molecular material is hydroxypropyl methylcellulose, carboxymethyl cellulose and sodium carboxymethyl cellulose.
4, the Entogastric lingering slow releasing preparation of killing treatment of helicobacter pylori gastropathy according to claim 1, it is characterized in that: high fat alcohol is the 14-20 alkanol.
CN95100772A 1995-02-22 1995-02-22 Gastric slow-released preparation of curing gastrosia by killing pyloric spirillum Expired - Fee Related CN1039195C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN95100772A CN1039195C (en) 1995-02-22 1995-02-22 Gastric slow-released preparation of curing gastrosia by killing pyloric spirillum

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN95100772A CN1039195C (en) 1995-02-22 1995-02-22 Gastric slow-released preparation of curing gastrosia by killing pyloric spirillum

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CN1111131A CN1111131A (en) 1995-11-08
CN1039195C true CN1039195C (en) 1998-07-22

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1049451A (en) * 1989-08-16 1991-02-27 三乐株式会社 Antibiotic composite
CN1015975B (en) * 1987-01-21 1992-03-25 意凯合股公司 Packaging machine operating under vacuum or controlled atmosphere with bells and covers always integral to different ring-shaped conveyers

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1015975B (en) * 1987-01-21 1992-03-25 意凯合股公司 Packaging machine operating under vacuum or controlled atmosphere with bells and covers always integral to different ring-shaped conveyers
CN1049451A (en) * 1989-08-16 1991-02-27 三乐株式会社 Antibiotic composite

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
《同济医科大学学报》86年,15(13) *
《同济医科大学学报》86年,15(13);《药学通报》21(6)86年;《医药工业》86年17(3);《中华骨科杂志》86年6(6) *
《药学通报》21(6)86年;《医药工业》86年17(3);《中华骨科杂志》86年6(6) *

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