CN100574759C - A kind of preparation method of Lansoprazole intestine micropill - Google Patents
A kind of preparation method of Lansoprazole intestine micropill Download PDFInfo
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- CN100574759C CN100574759C CN200610029942A CN200610029942A CN100574759C CN 100574759 C CN100574759 C CN 100574759C CN 200610029942 A CN200610029942 A CN 200610029942A CN 200610029942 A CN200610029942 A CN 200610029942A CN 100574759 C CN100574759 C CN 100574759C
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Abstract
The present invention relates to a kind of preparation method of Lansoprazole intestine micropill, step comprises that lansoprazole raw material 20-30g and microcrystalline Cellulose 80-150g, sodium hydrogen phosphate 1-5g, anhydrous sodium sulfite 1-5g, sodium lauryl sulphate 1-5g, the L-arginine 3-12g mix homogeneously of getting the 0-100 micron make active ball core, bag contagion gown layer and enteric-coating layer.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to a kind of preparation method of Lansoprazole intestine micropill.
Technical background
Lansoprazole Lansoprazole has another name called: Takepron, TAKEPRON, the listing of O-GAST Japanese military field in 1992 drug company; Its chemical name is: (±)-2[[[3-methyl-4-(2,2, the 2-trifluoro ethoxy)-2-pyridine radicals] methyl] sulfinyl] benzimidazole.
Its structural formula is:
Molecular formula: C16H14F3N3O2S, molecular weight: 369.37, its character is brownish white crystalline powder.166 ℃ of fusing points; Be soluble in dimethyl formamide, dissolve in methanol, be insoluble in dehydrated alcohol, ether, water-soluble hardly.Lansoprazole is a novel proton pump inhibitor, is the benzimidazole substituent of exploitation after omeprazole, is proton pump inhibitor, the activity of the specific inhibition of lansoprazole H+-K+-ATP enzyme, and this enzyme is the key enzyme that gastric acid generates.To basic gastric acid with by the irritability gastric acid secretion that stimulation causes inhibitory action is arranged.Lansoprazole is applicable to gastric ulcer, duodenal ulcer, erosive stomach-esophageal reflux disease, helicobacter pylori, Zollimger-ellison syndrome.What show clinical practice is lansoprazole tablet and lansoprazole intestine dissolving capsule.
Lansoprazole is unstable under acidic condition, and is destroyed easily in gastric acid, makes capsule oral and absorbs the raising of artifact availability.
Summary of the invention
The objective of the invention is to overcome above-mentioned deficiency, a kind of preparation method of Lansoprazole intestine micropill is provided, can obviously improve bioavailability.
Lansoprazole intestine micropill of the present invention contains:
1) the active ball core of forming by lansoprazole active ingredient and one or more pharmaceutically acceptable excipient, table 1:
Table 1
1) wherein, the lansoprazole material fineness is the 0-100 micron.
2) contain the isolation coat layer of stomach dissolution type Opadry, wherein preferred stomach dissolution type Opadry 80-120g
3) contain the enteric coat layer of enteric solubility Opadry, wherein preferred enteric solubility Opadry 80-120g
4) cosolvent is sodium lauryl sulphate and L-arginine
The invention provides a kind of preparation method of Lansoprazole intestine micropill, comprise the following steps:
1) preparation of active ball core:
Get lansoprazole raw material 20-30g, microcrystalline Cellulose 80-150g, sodium hydrogen phosphate 1-5g, anhydrous sodium sulfite 1-5g, sodium lauryl sulphate 1-5g, the L-arginine 3-12g mix homogeneously of 0-100 micron; Make wetting agent with 10% polyvidone, uniform powder is made active ball core.
2) bag contagion gown layer
The contagion gown layer is to adopt 80% alcoholic solution of 10% stomach dissolution type Opadry to carry out coating to obtain its weightening finish 10%;
3) enteric-coating layer
Enteric coating layer is to adopt 80% alcoholic solution of 10% enteric solubility Opadry to carry out coating to obtain its weightening finish 20%.
The coating parameter is the fluidized coating drying, is preheated to about 38 ℃, and micropill moisture is sprayed less than 2.5%, temperature 30-38 ℃, and pressure 0.35-0.45, seal-air pressure 0.11-0.15, flow parameter 30-60 (125g/s)
Because lansoprazole is an insoluble drug, the present invention adds an amount of cosolvent, makes medicine can reach rapid release, improves the purpose of bioavailability., as cosolvent both different amounts are investigated with sodium lauryl sulphate and L-arginine, it the results are shown in Table the comparison (mg) of 2 cosolvents:
Table 2
As can be seen from Table 2, the cosolvent that adopts prescription 6 to form, this product can obtain satisfied release.
Coating material is the Opadry of the happy Kanggong of card department production.This coating material has good film property, plasticity, and made film-coat is colourless, tasteless, flexible good, has good crack resistance, and is very stable under heat, light, air and certain humidity.This coating material has the viscosity height, and consumption is few, can adapt to quick coating, the color and luster favorable reproducibility, and it is available to have multiple models such as gastric solubleness and enteric, so we have selected the film-coat material of this model.
Lansoprazole intestine micropill of the present invention is made capsule, quantity-produced three batch samples, its assay such as table 3.
Table 3
Quality standard
Study on the stability
Get lansoprazole intestine dissolving capsule and placed 10 days under each influence factor's condition, and placed 6 months down in room temperature condition after the simulation listing packing, regularly carry out study on the stability respectively, each is investigated and the results are shown in Table 4, table 5:
Lansoprazole intestine dissolving capsule influence factor stability test result (050401)
The specific embodiment
Embodiment 1
Get fully mix homogeneously of the lansoprazole raw material (20-30g) of 0-100 micron and microcrystalline Cellulose (80-150g), sodium hydrogen phosphate (1-5g), anhydrous sodium sulfite (1-5g), sodium lauryl sulphate (1-5g), L-arginine (3-12g); Make wetting agent with 10% polyvidone, the powder art of abundant mix homogeneously is made the active ball core that contains the principal agent lansoprazole; The bag contagion gown: contagion gown adopts 80% alcoholic solution of 10% stomach dissolution type Opadry, weightening finish 10%.Enteric coated: enteric coating adopts 80% alcoholic solution of 10% enteric solubility Opadry, and weightening finish 20% makes the lansoprazole micropill.
Claims (3)
1. the preparation method of a Lansoprazole intestine micropill is characterized in that:
1) preparation of active ball core
Get lansoprazole raw material 20-30g, microcrystalline Cellulose 80-150g, sodium hydrogen phosphate 1-5g, anhydrous sodium sulfite 1-5g, cosolvent sodium lauryl sulphate 1-5g, the cosolvent L-arginine 3-12g mix homogeneously of 0-100 micron; Make wetting agent with 10% polyvidone, uniform powder is made active ball core;
2) bag contagion gown layer;
3) enteric-coating layer.
2. a kind of Lansoprazole intestine microsphere and its preparation as claimed in claim 1 is characterized in that: the contagion gown layer is to adopt 80% alcoholic solution of 10% stomach dissolution type Opadry to carry out coating to obtain its weightening finish 10%.
3. a kind of Lansoprazole intestine microsphere and its preparation as claimed in claim 1 is characterized in that: enteric coating layer is to adopt 80% alcoholic solution of 10% enteric solubility Opadry to carry out coating to obtain its weightening finish 20%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610029942A CN100574759C (en) | 2006-08-11 | 2006-08-11 | A kind of preparation method of Lansoprazole intestine micropill |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610029942A CN100574759C (en) | 2006-08-11 | 2006-08-11 | A kind of preparation method of Lansoprazole intestine micropill |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1907281A CN1907281A (en) | 2007-02-07 |
| CN100574759C true CN100574759C (en) | 2009-12-30 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN200610029942A Active CN100574759C (en) | 2006-08-11 | 2006-08-11 | A kind of preparation method of Lansoprazole intestine micropill |
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Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100522165C (en) * | 2007-09-15 | 2009-08-05 | 潮州市强基制药厂 | Lansoprazole enteric liquid capsule and preparation method thereof |
| CN101288654B (en) * | 2008-05-16 | 2012-05-02 | 北京正大绿洲医药科技有限公司 | Lansoprazole sustained-release drop pills and preparation method thereof |
| CN101991542A (en) * | 2009-08-10 | 2011-03-30 | 杭州赛利药物研究所有限公司 | Lansoprazole enteric dry suspension and preparation method thereof |
| CN101773502A (en) * | 2010-03-12 | 2010-07-14 | 山东鲁抗辰欣药业有限公司 | Lansoprazole medicine composition and preparation method thereof |
| CN102342916A (en) * | 2010-08-01 | 2012-02-08 | 海南中化联合制药工业股份有限公司 | Lansoprazole enteric-coated capsule prescription and preparation method thereof |
| CN101953802B (en) * | 2010-09-14 | 2012-05-09 | 陈敏伟 | Lansoprazole enteric preparation and preparation method thereof |
| CN102008449B (en) * | 2010-11-15 | 2012-11-21 | 扬子江药业集团有限公司 | Lansoprazole enteric pellet and preparation method thereof |
| CN103202820B (en) * | 2012-01-11 | 2016-03-30 | 浙江亚太药业股份有限公司 | A kind of stable lansoprazole intestine dissolving capsule and preparation method thereof |
| CN106491557A (en) * | 2016-11-03 | 2017-03-15 | 中国科学院西北高原生物研究所 | A kind of antineoplastic Swertiridoid A enteric capsules and its preparation technology |
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| CN1907281A (en) | 2007-02-07 |
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Owner name: SHANGHAI MEIYOU PHARMACEUTICAL CO., LTD. |
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Effective date of registration: 20100727 Address after: 200233 room 1806, North Building, 443 Dapu Road, Shanghai, Luwan District Co-patentee after: Shanghai Meiu Pharmaceutical Co., Ltd. Patentee after: Shanghai Micro-Pellets Pharmaceutical Development Co., Ltd. Address before: 200233 room 1806, North Building, 443 Dapu Road, Shanghai, Luwan District Patentee before: Shanghai Micro-Pellets Pharmaceutical Development Co., Ltd. |
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Address after: 200233 room 1806, North Building, 443 Dapu Road, Shanghai, Luwan District Co-patentee after: Shanghai Meiu Pharmaceutical Co., Ltd. Patentee after: Shanghai Micro-Pellets Pharmaceutical Development Co., Ltd. Address before: 200233 room 1806, North Building, 443 Dapu Road, Shanghai, Luwan District Co-patentee before: Shanghai Meiu Pharmaceutical Co., Ltd. Patentee before: Shanghai Micro-Pellets Pharmaceutical Development Co., Ltd. |