CN1765360A - Long acting(sustained-release) amoxilin capsule and preparation method thereof - Google Patents
Long acting(sustained-release) amoxilin capsule and preparation method thereof Download PDFInfo
- Publication number
- CN1765360A CN1765360A CN 200410051963 CN200410051963A CN1765360A CN 1765360 A CN1765360 A CN 1765360A CN 200410051963 CN200410051963 CN 200410051963 CN 200410051963 A CN200410051963 A CN 200410051963A CN 1765360 A CN1765360 A CN 1765360A
- Authority
- CN
- China
- Prior art keywords
- amoxicillin
- micropill
- enteric
- granule
- capsules
- 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.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
Disclosed is a long acting (sustained-release) amoxilin capsule and preparation method, which comprises making amoxicillin particles or micro-pellets through conventional methods, then dressing the obtained particles or micro-pellets to make stomach- or intestine-dissolvable amoxicillin particles or micro-pellets.
Description
Technical field:
The present invention relates to the preparation of a kind of chemicals amoxicillin (Amoxillin), specifically long-acting (slow release) Amoxicillin Capsules and preparation method and medical usage.
Background technology:
The amoxicillin is a penicillins antibiotics.To streptococcus pneumoniae, Hemolytic streptococcus belongs to.
Do not produce the penicillin staphylococcus, aerobic gram positive coccus such as enterococcus faecalis, escherichia coli.Proteus mirabilis, the Salmonella hemophilus influenza, the strain of not beta-lactamase-producing and the helicobacter pylori of aerobic gram positive bacteria such as Diplococcus gonorrhoeae have good antibacterial action.The bacterial cell wall is synthetic brings into play bactericidal action by suppressing in the amoxicillin, can make the rapid englobement thing of antibacterial and dissolves, and breaks.
At present, the common oral preparation of amoxicillin has: amoxicillin sheet, Amoxicillin Capsules, amoxicillin granule, amoxicillin chewable tablet, amoxicillin dispersible tablet, the amoxicillin buccal tablet, above dosage form need be taken 3～4 times every day, brings to patient and takes inconvenience.Domestic have bibliographical information amoxicillin slow release sheet, oral 2 times an of every day.EP0222914 reports amoxicillin composite particles agent, wherein contain the amoxicillin gastric solubleness micropill and the amoxicillin enteric micropill of low content, but amoxicillin content is low, the volume of composite particles is big, can't make capsule, can only make the granule (electuary) of every bag 5 gram, usage is oral 2 times of every day.Because of consumption is big, patient takes inconvenience.
Simultaneously, the oral post-absorption in amoxicillin is rapid, and about 75～90% can be in gastrointestinal absorption.Food is not remarkable to the inhalation effects of amoxicillin.The protein binding rate of amoxicillin is 17～20%.It is short that the half-life is eliminated in the amoxicillin, only is about 60 minutes.Therefore, need take once (being to take every day 3～4 times) in per 6～8 hours.This shows that the amoxicillin ordinary preparation exists takes inconvenience, misses the phenomenon of forgetting to obey easily.And long-acting (slow release) Amoxicillin Capsules only need be taken 2 times every day, promptly sooner or later each 1 time.Be taking convenience, curative effect is reliable simultaneously.
Summary of the invention:
The invention provides a kind of long-acting (slow release) capsule preparations and medical usage and preparation method of amoxicillin.Mixture gastric solubleness and amoxicillin granules enteric or micropill is housed in long-acting (slow release) Amoxicillin Capsules, and amoxicillin granules that is equipped with in perhaps long-acting (slow release) Amoxicillin Capsules or micropill wherein contain existing amoxicillin that can gastric solubleness and contain the amoxicillin of enteric again.
The medical function of above-mentioned long-acting (slow release) provided by the present invention Amoxicillin Capsules is consistent with the ordinary preparation of amoxicillin.
The preparation method of above-mentioned long-acting (slow release) provided by the present invention Amoxicillin Capsules, comprising as follows:
The content of a. long-acting (slow release) Amoxicillin Capsules is the amoxicillin granules or the micropill its preparation method of gastric solubleness and enteric; be to use coating machine or high speed granulator or fluid bed or the preparation of conventional manual operation craft; with the water-insoluble high-molecular resin solution granule or micropill are directly made in the amoxicillin, more obtained granule or micropill are carried out coating with the coating solution that contains the water-insoluble macromolecule resin.
The content of b. long-acting (slow release) Amoxicillin Capsules is the amoxicillin granules or the micropill preparation of gastric solubleness and enteric; it is a conventionally pharmaceutical worker skill of using coating machine or high speed granulation or fluid bed or conventional manual operation craft application celphere; with the water-insoluble high-molecular resin solution amoxicillin is adhered to celphere and make granule or micropill, the coating solution of the water-insoluble macromolecule resin of more obtained granule or micropill being had a meal carries out coating.
The content of c. long-acting (slow release) Amoxicillin Capsules is the amoxicillin granules or the micropill its preparation method of gastric solubleness and enteric; be with above-mentioned a; amoxicillin granules that the b item is made or micropill; get wherein and 70～90% use above-mentioned a; the coating solution coating of b item, again will be coating and the amoxicillin granules or the micropill of coating do not mix by a certain percentage.
The content of d. long-acting (slow release) Amoxicillin Capsules is the amoxicillin granules or the micropill preparation of gastric solubleness and enteric; be to use coating machine or high speed granulation or fluid bed or conventional manual operation craft, gastric solubleness and enteric coated particles or micropill directly made in the amoxicillin with water-insoluble high-molecular resin solution repeatable operation
The content of e. long-acting (slow release) Amoxicillin Capsules is the amoxicillin granules or the micropill its preparation method of gastric solubleness and enteric; it is the conventionally pharmaceutical worker skill of using coating machine or high speed granulator or fluid bed or conventional manual operation craft application celphere; with the water-insoluble high-molecular resin solution amoxicillin is repeatedly adhered on the celphere repeatedly, directly make gastric solubleness and enteric coated particles or micropill.
Long-acting (slow release) Amoxicillin Capsules that invention provides, the tolerant 40～500mg of every intragranular, and the amoxicillin is 30～400mg.
The mensuration of release: change the basket method, rotating speed is that per minute 100 changes.With 0.1mol/lHcl solution 900ml is dissolution medium, measures after 2 hours, dissolution medium is changed among phosphate buffer (PH6.0) 900ml measures 2 hours.The dissolution result: release must not must not be greater than 55% greater than 35%, the 2 hour release the 1st hour the time in 0.1mol/l Hcl solution.2 hours release must not be less than 70% in phosphate buffer (PH6.0).
Technological merit of the present invention is that made long-acting (slow release) Amoxicillin Capsules content is the amoxicillin granules or the micropill of stomach appearance and enteric, and wherein contained pharmaceutical excipient is few, and amoxicillin content height, cumulative volume is little, in therefore incapsulating.
The specific embodiment
Enumerate 4 embodiment below, the present invention is further specified.
Embodiment 1
Amoxicillin 1kg is placed high speed granulator, and technology is started granulating cutter routinely, slowly drip 10% No. 2 alcoholic solution of polyacrylic resin, granulate, the particle of screening between 24～20 orders, unclassified stores repeats above-mentioned granulation again.Drying is put the particle between 24～20 orders in the coating pan into, and the ethanol coating solution that No. 2, the polyacrylic resin with 5% carries out coating, makes particle weightening finish 0.5～1.0%, drying, and encapsulated, every capsules includes amoxicillin 250mg.
By the aforementioned drug release determination that carries out, the result is as follows with the above-mentioned capsule that makes:
The dissolution medium time (hour) accumulative total dissolution rate (%)
0.1mol/l Hcl solution 1 28.5
2 43.2
Phosphate buffer (PH6.0) 2 76.5
Embodiment 2
1kg places fluid bed with the amoxicillin, and technology is slowly sprayed the alcoholic solution of No. 2,10% polyacrylic resin routinely, granulate, and the particle between screening 24～20 orders, unclassified stores repeats above-mentioned granulation again.Drying is put the particle between 24～20 orders in the coating pan into, and the ethanol coating solution that No. 2, the polyacrylic resin with 5% carries out coating, particle weightening finish 0.5～1.0%, and drying, encapsulated, every capsules includes amoxicillin 250mg.
By the aforementioned drug release determination that carries out, the result is as follows with the above-mentioned capsule that makes:
The dissolution medium time (hour) accumulative total dissolution rate (%)
0.1mol/l Hcl solution 1 30.6
2 46.3
Phosphate buffer (PH6.0) 2 81.0
Embodiment 3
1kg places coating pan with the amoxicillin, slowly drips 10% polyacrylic resin alcoholic solution, and technology is granulated repeatedly routinely, the particle between screening 24～20 orders, and unclassified stores repeats above-mentioned granulation again.Drying, encapsulated, every capsules includes amoxicillin 250mg.
By the aforementioned drug release determination that carries out, the result is as follows with the above-mentioned capsule that makes:
The dissolution medium time (hour) accumulative total dissolution rate (%)
0.1mol/l Hcl solution 1 26.9
2 41.7
Phosphate buffer (PH6.0) 2 77.1
Embodiment 4
Get embodiment 1 or embodiment 2 obtained amoxicillin particles, dry, get the particle 1000g between 24～20 orders, divide 800g wherein to put in the coating pan, the ethanol coating solution that No. 2, the polyacrylic resin with 5% carries out coating, particle weightening finish 0.8～1.2%, dry, the coating amoxicillin mix particles that is is uneven, encapsulated with 200g, and every capsules includes amoxicillin 250mg.
By the aforementioned drug release determination that carries out, the result is as follows with the above-mentioned capsule that makes:
The dissolution medium time (hour) accumulative total dissolution rate (%)
0.1mol/l Hcl solution 1 31.6
2 47.9
Phosphate buffer (PH6.0) 2 80.1
Claims (9)
1. the content of long-acting (slow release) Amoxicillin Capsules is made up of the granule of the amoxicillin of gastric solubleness and enteric or the amoxicillin micropill of gastric solubleness and enteric, wherein includes the amoxicillin for the treatment of effective dose and can control the pharmaceutical excipient that the amoxicillin discharges in gastrointestinal tract;
2. as described in claims 1, pharmaceutical composition is the amoxicillin, and every intragranular contains amoxicillin 20mg～400mg, contains 50mg～280mg and optimised quantity is every intragranular;
3. as described in claims 1, in the compositions of the amoxicillin of gastric solubleness and enteric, the amoxicillin part of gastric solubleness is 15～50%, and the best is 20～40%, and the amoxicillin part of enteric is 30～90%, and the best is 40～80%.
4. as described in claims 1, available pharmaceutical excipient is the water-insoluble macromolecular material as No. 2, polyacrylic resin, No. 3, polyacrylic resin, No. 4, polyacrylic resin, and the coating material of various gastric solubleness or enteric, ethyl cellulose, cellulose acetate, celluloid;
5. as described in claims 1, oral 2 times of long-acting (slow release) Amoxicillin Capsules every day;
6. as described in claims 1, the content of long-acting (slow release) Amoxicillin Capsules is that the granule or the micropill of gastric solubleness and enteric can directly be made granule or micropill with the amoxicillin raw material with as claims 4 described alcoholic solution that contain the water-insoluble macromolecular material, all granules or micropill coating, or only part (30～80%) granule or micropill coating;
7. as described in claims 1, the content of long-acting (slow release) Amoxicillin Capsules is gastric solubleness and enteric amoxicillin, capsular content can be added medicine on celphere with the amoxicillin raw material, or be that binding agent is made granule or micropill as the alcoholic solution of claims 4 described water-insoluble macromolecular materials, and with granule or micropill coating, or with part (30～80%) granule or micropill coating;
8. as described in claims 1, the content of long-acting (slow release) Amoxicillin Capsules is the mixture of gastric solubleness and enteric coated particles or micropill, can directly make granule or micropill with the alcoholic solution repeatable operation of amoxicillin raw material and claims 4 described water-insoluble macromolecular materials;
9. as described in claims 1; the content of long-acting (slow release) Amoxicillin Capsules is the content of gastric solubleness and enteric Amoxicillin Capsules; available amoxicillin raw material is added medicine on celphere, and is that the binding agent repeatable operation is made granule or micropill with the alcoholic solution that claims 4 described water contain insoluble macromolecular material.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410051963 CN1765360A (en) | 2004-10-28 | 2004-10-28 | Long acting(sustained-release) amoxilin capsule and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410051963 CN1765360A (en) | 2004-10-28 | 2004-10-28 | Long acting(sustained-release) amoxilin capsule and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1765360A true CN1765360A (en) | 2006-05-03 |
Family
ID=36741610
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410051963 Pending CN1765360A (en) | 2004-10-28 | 2004-10-28 | Long acting(sustained-release) amoxilin capsule and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1765360A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103168923A (en) * | 2012-01-16 | 2013-06-26 | 北京伟嘉人生物技术有限公司 | Enteric microencapsulated compound amino acid additive for animal feed and preparation method thereof |
| CN107115316A (en) * | 2017-05-18 | 2017-09-01 | 海口市制药厂有限公司 | Amoxicillin granule composition, the preparation method and the usage of a kind of stabilization |
| CN113116860A (en) * | 2021-04-22 | 2021-07-16 | 海南通用三洋药业有限公司 | Amoxicillin capsule and preparation method thereof |
-
2004
- 2004-10-28 CN CN 200410051963 patent/CN1765360A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103168923A (en) * | 2012-01-16 | 2013-06-26 | 北京伟嘉人生物技术有限公司 | Enteric microencapsulated compound amino acid additive for animal feed and preparation method thereof |
| CN107115316A (en) * | 2017-05-18 | 2017-09-01 | 海口市制药厂有限公司 | Amoxicillin granule composition, the preparation method and the usage of a kind of stabilization |
| CN113116860A (en) * | 2021-04-22 | 2021-07-16 | 海南通用三洋药业有限公司 | Amoxicillin capsule and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US7122204B2 (en) | Antibiotic composition with inhibitor | |
| CA2494015C (en) | Antibiotic product, use and formulation thereof | |
| HRP960032A2 (en) | New oral pharmaceutical dosage form | |
| IL134079A (en) | Process for the preparation of pellets with a content of up to 90 wt.% of a pharmaceutical active ingredient | |
| CN1708307A (en) | Water-soluble meloxicam granules | |
| CN106074543B (en) | A kind of water-soluble synergistic composition and its application containing Amoxicillin | |
| US20070134327A1 (en) | Compositions and methods for improved efficacy of penicillin-type antibiotics | |
| EP2601938A1 (en) | Pharmaceutical compositions for the treatment of Helicobacter pylori associated diseases | |
| CS208196B2 (en) | Method of making the perorally applicable preparation with the retarded liberation of the cefalexine as the active component | |
| CN1765360A (en) | Long acting(sustained-release) amoxilin capsule and preparation method thereof | |
| CN101601657A (en) | A kind of amoxicillin soluble powder and preparation method thereof | |
| CN1084188C (en) | Pharmaceutical formulations of ciprofloxacin | |
| CA2516327A1 (en) | Therapeutic system comprising amoxicillin and clavulanic acid | |
| CN102240285A (en) | Amoxicillin and potassium clavulanate tablet for dogs and cats, and its preparation method and application | |
| CA2399856C (en) | Antibiotic composition with inhibitor | |
| CN102526007A (en) | Florfenicol taste masking preparation and preparation method for same | |
| CN1813722A (en) | Composition containing amoxicillin and dicloxacillin sodium | |
| CN1319533C (en) | Cefetamet pivoxil hydrochloride dispersion dispersion tablets and preparation method | |
| CA2533292A1 (en) | Antibiotic product, use and formulation thereof | |
| AU2001239869A1 (en) | Antibiotic composition with inhibitor | |
| CA2533178A1 (en) | Antibiotic product, use and formulation thereof | |
| CZ407298A3 (en) | Process for preparing potassium clavulanate | |
| CN112206217A (en) | Cefradine pharmaceutical composition and preparation method thereof | |
| CN112263569B (en) | Amoxicillin capsule and preparation method thereof | |
| CA2533358A1 (en) | Antibiotic product, use and formulation thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |