CN103462912A - Preparation method of ethionamide tablet - Google Patents
Preparation method of ethionamide tablet Download PDFInfo
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- CN103462912A CN103462912A CN2012101848714A CN201210184871A CN103462912A CN 103462912 A CN103462912 A CN 103462912A CN 2012101848714 A CN2012101848714 A CN 2012101848714A CN 201210184871 A CN201210184871 A CN 201210184871A CN 103462912 A CN103462912 A CN 103462912A
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Abstract
The invention discloses a preparation method of an ethionamide tablet, and the preparation method comprises the following steps: (1) weighing the following raw materials by weight: 250 parts of ethionamide; 40-55 parts of a filler; 15-25 parts of a disintegrating agent; 10-15 parts of a binder; 6.25 parts of a flow aid and 1 part of a lubricant; and (2) mixing the ethionamide and the flow aid, crushing, sieving by a 100 mesh standard sieve, adding the filler, the disintegrating agent and the binder for mixing, adding an auxiliary solvent with an amount being 6% of the total amount of the formula for wet granulation, baking at the temperature of 60DEG C for 20min, trimming granules by a 16-20 mesh standard sieve, adding the lubricant, and tabletting to obtain the ethionamide tablet. By using the preparation method of the invention, crushing and sieving of ethionamide raw material drug is convenient, the prepared tablet is small in tablet weight difference, and the quality of the drug is well controlled.
Description
Technical field
The invention belongs to field of medicaments, particularly relate to a kind of preparation method of antimycobacterial drug.
Background technology
Pulmonary tuberculosis (Tuberculosis, TB) is a global problem, and its sickness rate is high, and infectiousness is strong, especially wayward by the special route of transmission of respiratory tract droplet transmission, very big to social danger.Because it is by respiratory infectious, as long as breathe, remain, just can't fundamentally keep off infection.Because of antibiotic use, the sickness rate of TB once once reduced, but the eighties in last century, tuberculosis was revivable once again, and especially in developing country, incidence rate lungy and mortality rate are always high.Announced the global pulmonary tuberculosis state of emergency from the World Health Organization (WHO) in 1993, the data of announcing according to another WHO: the whole world has 800～1,000 ten thousand to infect the tubercule bacillus person every year, and annual approximately 3,000,000 people die from tuberculosis.China belongs to one of 22, the world high popular country of tuberculosis, the statistics demonstration that health ministry is announced in 2010, and within 2009, there are 1,070,000 tuberculosis cases in China, and nowadays phthisical preventing and controlling have been listed in the great brainstorm project of country " 12 ".
In recent years, the continuous rise of tuberculosis epidemic situation in global range, the generation of drug resistance and multiple drug-resistance pulmonary tuberculosis (Multi-drug resistant TB, MDR-TB) case is one of them major reason with rolling up.At present, China's anti-multi-drug resistance pulmonary tuberculosis patient number accounts for 1/4 of the whole world, and tulase resistant rate and anti-multiple medicines rate are generally in higher level, and the anti-multiple medicines rate of new patient reaches 4.5%～10%, higher than global average level.Simultaneously, the 4th the national tuberculosis epidemiology investigation report demonstration in the whole nation, China's primary drug resistance tuberculosis ratio is 18.6%, to rifampicin and isoniazid (isoniazid) drug resistance ratio, is wherein 7.6%; The acquired drug-resistance rate is 46.5%, to rifampicin and isoniazid resistant rate, is wherein 17.1%.MDR-TB refers to expectorant bacterium lasting masculin, and pathogenic tulase is anti-isoniazid and rifampicin at least simultaneously.MDR-TB is because the patient of anti-multiple medicines produces drug resistance to the first-line treatment medicine, and carriagable time and treatment time long, potential propagation number can be more, so its treatment should be selected the two wires antituberculotics.
At present, the phthisical Second line Drug of state's internal therapy mainly comprises: prothionamide, para-aminosalicylic acid, fluoroquinolones, macrolide antibiotics etc.Bibliographical information is arranged, and except anti-first-line drug, the most common anti-Second line Drug is levofloxacin, amikacin, prothionamide, sodium aminosalicylate isoniazid etc.Because there is some un-reasonable phenomenon in some therapeutic scheme, patient treatment is lacked to management or mismanagement, antituberculotics is under-supply, and kind is incomplete or quality is not good and the factors such as the financial difficulties patient have caused the phthisical generation of multiple drug-resistance.Therefore, anti-multiple medicines patient often the course for the treatment of long, focus is extensive, expense is high, case fatality rate is high, need to select suitable medicine, formulates rationally, chemotherapy regimen efficiently.Unique affirming effectively adopts from original medicine, coordinates appropriate and enough courses for the treatment of more than at least 3 kinds, carries out combined chemotherapy.Because above-mentioned present situation is introduced at home the Antitubercular Second line Drug and selected for enriching clinical application, strengthen the phthisical therapeutic effect important role of multiple drug-resistance.
The character of ethionamide crude drug is acicular crystal, and mobility is poor, is difficult for pulverizing and sieving, and therefore its tablet weight variation of tablet of preparation is large according to a conventional method, is difficult to control the quality of medicine.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, a kind of preparation method of ethionamide sheet is provided.
Technical scheme of the present invention is summarized as follows:
A kind of preparation method of ethionamide sheet, is characterized in that comprising the steps:
(1) take by weight following raw material: 250 parts of ethionamides; 40～55 parts of filleies; 15～25 parts of disintegrating agents; 10～15 parts of binding agents; 6.25 parts of fluidizer; 1 part of lubricant;
(2) ethionamide is mixed with fluidizer, pulverize, cross 100 mesh standard sieves, add filler, disintegrating agent and binding agent to mix, the secondary solvent that adds total recipe quantity 6%, wet granulation, dry 20min, 20 mesh standard sieve granulate for 60 ℃, add lubricant, tabletting, obtain.
Described filler is microcrystalline Cellulose, starch, lactose, pregelatinized Starch and mannitol at least one.
Described binding agent is polyvidone, methylcellulose, ethyl cellulose, gelatin or alginic acid.
Described lubricant is magnesium stearate, Pulvis Talci or calcium stearate.
Described disintegrating agent is cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose or starch.
Described fluidizer is silicon dioxide or Pulvis Talci.
Described secondary solvent is ethanol, propanol, butanols and amylalcohol at least one.
Utilize method of the present invention, can make to facilitate pulverizing and sieving of ethionamide crude drug, its tablet weight variation of the tablet of preparation is less, has controlled well the quality of medicine.
The specific embodiment
Below in conjunction with specific embodiment, the present invention is further illustrated.
Embodiment 1
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Microcrystalline Cellulose (filler) 25g; Lactose (filler) 30g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 15g; Polyvidone (binding agent) 10g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add microcrystalline Cellulose, lactose, cross-linking sodium carboxymethyl cellulose and polyvidone, mix 3min, add the dehydrated alcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 2%
Embodiment 2
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Microcrystalline Cellulose (filler) 30g; Lactose (filler) 20g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 20g; Polyvidone (binding agent) 10g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add microcrystalline Cellulose, lactose, cross-linking sodium carboxymethyl cellulose and polyvidone, mix 3min, add the dehydrated alcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 4%
Embodiment 3
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Pregelatinized Starch (filler) 15g; Lactose (filler) 25g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 25g; Polyvidone (binding agent) 15g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add pregelatinized Starch, lactose, cross-linking sodium carboxymethyl cellulose and polyvidone, mix 3min, add the dehydrated alcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 3.5%
Embodiment 4
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Mannitol (filler) 30g; Lactose (filler) 20g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 20g; Polyvidone (binding agent) 10g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add mannitol, lactose, cross-linking sodium carboxymethyl cellulose and polyvidone, mix 3min, add the dehydrated alcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 5%
Embodiment 5
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Starch (filler) 30g; Lactose (filler) 20g; Microcrystalline Cellulose (disintegrating agent) 20g; Methylcellulose (binding agent) 10g; Silicon dioxide (fluidizer) 6.25g; Calcium stearate (lubricant) 1g;
(2) by ethionamide crude drug and silicon dioxide mixing 2min, cross 100 mesh standard sieves after pulverizing, add starch, lactose, microcrystalline Cellulose and methylcellulose, mix 3min, add the anhydrous propanol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 4.3%
Embodiment 6
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Mannitol (filler) 30g; Lactose (filler) 20g; Starch (disintegrating agent) 20g; Ethyl cellulose (binding agent) 10g; Silicon dioxide (fluidizer) 6.25g; Pulvis Talci (lubricant) 1g;
(2) by ethionamide crude drug and silicon dioxide mixing 2min, cross 100 mesh standard sieves after pulverizing, add mannitol, lactose, starch and ethyl cellulose, mix 3min, add the anhydrous butanols of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 2.5%
Embodiment 7
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Mannitol (filler) 30g; Lactose (filler) 20g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 20g; Gelatin (binding agent) 10g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add mannitol, lactose, cross-linking sodium carboxymethyl cellulose and gelatin, mix 3min, add the anhydrous amylalcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 4%
Embodiment 8
A kind of preparation method of ethionamide sheet, comprise the steps: (preparing 1000 ethionamide sheets)
(1) take: ethionamide crude drug 250g; Mannitol (filler) 30g; Lactose (filler) 20g; Cross-linking sodium carboxymethyl cellulose (disintegrating agent) 20g; Alginic acid (binding agent) 10g; Pulvis Talci (fluidizer) 6.25g; Magnesium stearate (lubricant) 1g;
(2) by ethionamide crude drug and Pulvis Talci mixing 2min, cross 100 mesh standard sieves after pulverizing, add mannitol, lactose, cross-linking sodium carboxymethyl cellulose and alginic acid, mix 3min, add the anhydrous amylalcohol of total recipe quantity 6%, above-mentioned material is carried out to wet mixing, carry out pelletize with 14 mesh standard sieves, dry 20min, 16 mesh standard sieve granulate for 60 ℃, dry granule is pulverized, cross 80 mesh standard sieves, add magnesium stearate, mix, tabletting, obtain.
Tablet weight variation: ± 3.5%
Embodiment 9
To the ethionamide tablet of the embodiment of the present invention 1 preparation, " second appendix X C first method of Chinese pharmacopoeia carries out dissolution in vitro comparative study according to 2010 editions, the hydrochloric acid solution that dissolution medium is 0.1M (PH is 1.2), and determine dissolution by the stripping quantity that the HPLC method is measured each time point ethionamide, the prepared ethionamide tablet of the present invention has the stripping that surpasses 90% under this leaching condition in 30min.
The quality standard of the ethionamide tablet of embodiment 4 preparations comprises:
Tablet specification: 250mg;
Tablet content:>95%;
Dissolution of Tablet: in 30 minutes >=75%.
Claims (7)
1. the preparation method of an ethionamide sheet, is characterized in that comprising the steps:
(1) take by weight following raw material: 250 parts of ethionamides; 40～55 parts of filleies; 15～25 parts of disintegrating agents; 10～15 parts of binding agents; 6.25 parts of fluidizer; 1 part of lubricant;
(2) ethionamide is mixed with fluidizer, pulverize, cross 100 mesh standard sieves, add filler, disintegrating agent and binding agent to mix, the secondary solvent that adds total recipe quantity 6%, wet granulation, dry 20min, 16-20 mesh standard sieve granulate for 60 ℃, add lubricant, tabletting, obtain.
2. the preparation method of a kind of ethionamide sheet according to claim 1, described filler is microcrystalline Cellulose, starch, lactose, pregelatinized Starch and mannitol at least one.
3. the preparation method of a kind of ethionamide sheet according to claim 1, is characterized in that described binding agent is polyvidone, methylcellulose, ethyl cellulose, gelatin or alginic acid.
4. the preparation method of a kind of ethionamide sheet according to claim 1, is characterized in that described lubricant is magnesium stearate, Pulvis Talci or calcium stearate.
5. the preparation method of a kind of ethionamide sheet according to claim 1, is characterized in that described disintegrating agent is cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose or starch.
6. the preparation method of a kind of ethionamide sheet according to claim 1, is characterized in that described fluidizer is silicon dioxide or Pulvis Talci.
7. the preparation method of a kind of ethionamide sheet according to claim 1, is characterized in that described secondary solvent is ethanol, propanol, butanols and amylalcohol at least one.
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| CN2012101848714A CN103462912A (en) | 2012-06-06 | 2012-06-06 | Preparation method of ethionamide tablet |
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| CN2012101848714A CN103462912A (en) | 2012-06-06 | 2012-06-06 | Preparation method of ethionamide tablet |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473897A (en) * | 2014-11-27 | 2015-04-01 | 天津坤健生物制药有限公司 | Preparation method of ethionamide tablet |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006045006A1 (en) * | 2004-10-20 | 2006-04-27 | Wyeth | Antibiotic product formulation |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006045006A1 (en) * | 2004-10-20 | 2006-04-27 | Wyeth | Antibiotic product formulation |
Non-Patent Citations (1)
| Title |
|---|
| 无: "微粉硅胶内加的问题", 《HTTP://WWW.DXY.CN/BBS/THREAD/24419907》, 27 December 2010 (2010-12-27), pages 1 - 2 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473897A (en) * | 2014-11-27 | 2015-04-01 | 天津坤健生物制药有限公司 | Preparation method of ethionamide tablet |
| CN104473897B (en) * | 2014-11-27 | 2017-09-26 | 天津坤健生物制药有限公司 | A kind of preparation method of 2-ethylisonicotinthionamide tablet |
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Application publication date: 20131225 |