CN1394604A - Indapamide slowly-releasing tablet - Google Patents
Indapamide slowly-releasing tablet Download PDFInfo
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- CN1394604A CN1394604A CN 02123999 CN02123999A CN1394604A CN 1394604 A CN1394604 A CN 1394604A CN 02123999 CN02123999 CN 02123999 CN 02123999 A CN02123999 A CN 02123999A CN 1394604 A CN1394604 A CN 1394604A
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- indapamide
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- releasing tablet
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Abstract
The indapamide slow-released tablet includes tablet core and coating, in which the tablet core is formed from indapamide, slow-releasing material, pore-forming agent, filling agent and lubricating agent in the ratio of 1.5g:40-150g:20-100g:10-100g:1-10g, and the coating is formed from film-forming amterial, antisticking agent, masking agent, polyethylene glycol 400, distrilled water and ethyl alcohol. The above-mentioned film-forming material, antisticking agent, masking agent, polyethylene glycol 400 and distilled water according to the ratio of 3-20g:2-15g:1-15g:5ml:140ml are added into the ethyl alcohol, and diluted with ethyl alcohol to 500ml to obtain the coating solution, then the outer layer of the tablet can be coated with said coating solution and dried so as to obtain the invented indapamide slow-release tablet.
Description
Technical field
The present invention relates to a kind of medicine, particularly relate to a kind of indapamide slowly-releasing tablet for the treatment of hypertension and edema.
Background technology
Hypertension is a kind of commonly encountered diseases, frequently-occurring disease, and sickness rate is very high, if malpractice or untimely treatment just might cause severe complications and the physical and mental health that endangers the patient, even life danger occur.Indopamide is an a kind of line antihypertensive drug, clinical various hypertension and the edema of being used for the treatment of, have safety, effectively, convenient, oral absorption rapidly and safety, the reliable advantage of curative effect.The indopamide of present clinical use mostly is the ordinary tablet of 2.5mg/ sheet, because the dosage that the patient takes every day is bigger, thereby the untoward reaction that causes thus increases.And the research of following antihypertensive drug is to develop towards long-actingization direction, promptly should make the patient still can reach treatment concentration when taking the low dosage medicine, and keeps the therapeutic effect of long period.United States Patent (USP) 5,334, disclose a kind of like this slow releasing tablet for No. 392, the main component of this medicine is an indopamide, though this slow releasing tablet can reduce many untoward reaction such as blood medicine peak value, Water-Electrolyte, metabolism disorder and the irregular variation of plasma concentration than common quick release sheet, but its used adjuvant comprises the polyvidone that price is more expensive, thereby the cost of product is raise, and is unsuitable for promoting the use of at home; In addition, need use aqueous alcohol during this method system soft material, pelletization is complicated, thus need carry out explosion-proof processing in the preparation process, very dangerous.And present domestic this quasi drugs appearance of still not having.
Summary of the invention
In order to address the above problem, the object of the present invention is to provide that a kind of taking dose is little, the indapamide slowly-releasing tablet of lasting medicine and stable performance.
In order to achieve the above object, indapamide slowly-releasing tablet provided by the invention comprises label and coating; Label is made up of with the ratio of 1.5g: 40-150g: 20-100g: 10-100g: 1-10g indopamide, slow-release material, porogen, filler and lubricant; Coating is made up of filmogen, antiplastering aid, screening agent, PEG400, distilled water and ethanol, and it is to join in the ethanol with the ratio of 3-20g: 2-15g: 1-15g: 5ml: 140ml and the coating solution of finally making to 500ml with ethanol dilution is coated on the outer drying of label and forms by filmogen, antiplastering aid, screening agent, PEG400 and distilled water.
Described slow-release material is carboxymethyl cellulose, ethyl cellulose, hydroxypropyl emthylcellulose, methylcellulose, hydroxypropyl cellulose, hydroxyethyl-cellulose, pectin, sodium alginate, chitin, glycerol mountain heal any one or two kinds in acid esters and the acrylic resin; Porogen is any one or two kinds in lactose, carboxymethyl starch sodium, Polyethylene Glycol and the microcrystalline Cellulose; Filler is any one or two kinds in sorbitol, mannitol, starch, modified starch and the sucrose; Lubricant is any in magnesium stearate and the Pulvis Talci.
Described filmogen is any one in hydroxypropyl cellulose, methylcellulose, hydroxyethyl-cellulose and the hydroxypropyl emthylcellulose; Antiplastering aid is any in Pulvis Talci and the calcium carbonate; Screening agent is a titanium dioxide.
Indapamide slowly-releasing tablet provided by the invention proves through effect experiment, have that ordinary tablet taking dose than 2.5mg/ sheet is little, advantage such as lasting medicine, oral absorption are rapid, particularly the external stripping curve of this medicine reaches zero level release substantially, the release in vitro degree 8 hours was 40%-60%, thereby slow release effect is obvious, can further reduce the side effect that produces after the patient takes medicine like this, and safety is good, and cost is low, is easy to the patient and accepts.
The specific embodiment
Embodiment 1:
With 1000 indapamide slowly-releasing tablets is benchmark, get the indopamide that 1.5g pulverizes the back and screens through 200 mesh sieves, take by weighing 100g hydroxypropyl emthylcellulose, 30g microcrystalline Cellulose, 10g carboxymethyl starch sodium and 60g sucrose respectively through the screening of 100 mesh sieves, these raw materials are placed the mixer mix homogeneously, and water makes soft material, makes few fine powder and neatly do not have rectangular granule with 30 order nylon wires then.This granule placed under 60 ± 2 ℃ the temperature and carry out drying, granulate sieve after the drying to remove oversized particles, add magnesium stearate and the mix homogeneously of 10g subsequently, make 1000 labels that contain the 1.5mg indopamide through carrying out tabletting after the assay was approved through the screening of 100 mesh sieves.Take by weighing the 3g methylcellulose simultaneously, the distilled water 70ml that under stirring condition, adds, and use ultrasonic Treatment, and add 70ml distilled water to solution then and clarify, add 15g Pulvis Talci and 8g titanium dioxide again and use ultrasonic Treatment, make solution A; Other gets 250ml ethanol, adds the 5ml PEG400, and uses ultrasonic Treatment, makes solution B; Solution A and solution B are mixed, mixed liquor is diluted to the 500ml coating solution with ethanol.Under 40 ℃ inlet temperature, the coating solution for preparing is carried out Cotton seeds with the hydrojet speed of 15ml/min to label, and with the product behind the coating in 40 ℃ dry 12 hours down, promptly can be made into indapamide slowly-releasing tablet of the present invention.
Embodiment 2:
With 1000 indapamide slowly-releasing tablets is benchmark, makes label according to the addition of 1.5g indopamide, 10g methylcellulose, 30g hydroxypropyl cellulose, 5g lactose, 15g mannitol, 40g modified starch and 1g magnesium stearate with embodiment 1 identical technology.Simultaneously make coating solution with the technology identical with embodiment 1 according to 20g hydroxyethyl-cellulose, 8g Pulvis Talci, 1g titanium dioxide, 5ml PEG400,140ml distilled water and the amount of alcohol added that adds to the 500ml coating solution at last.The method of Cotton seeds is also identical with embodiment 1.
Embodiment 3:
With 1000 indapamide slowly-releasing tablets is benchmark, makes label according to the addition of 1.5g indopamide, 60g methyl fiber system, 30g sodium alginate, 70g lactose, 30g modified starch and 8g magnesium stearate with embodiment 1 identical technology.Simultaneously make coating solution with the technology identical with embodiment 1 according to 8g hydroxypropyl cellulose, 2g Pulvis Talci, 15g titanium dioxide, 5ml PEG400,140ml distilled water and the amount of alcohol added that adds to the 500ml coating solution at last.The method of Cotton seeds is also identical with embodiment 1.
Indapamide slowly-releasing tablet provided by the invention is a kind of low dosage type resisting hypertension slow releasing pharmaceutical that contains 1.5mg indopamide effective ingredient, and outward appearance is the white film coated tablet, and the patient only need take a slice every day can reach treatment concentration.The indapamide slow release of low dosage (SR) sheet (1.5mg) compares with indapamide common (IR) sheet (2.5mg), with patient's decreased number 50% that patient's number ratio of indapamide (SR) treatment hypertensive patient serum potassium concentration＜3.4mmol/L is treated with indapamide (IR), indapamide (SR) also demonstrates and can reduce left ventricle index (LVMI) in the hypertension people in 1 year of indapamide treatment.
The illumination that will place 4500LX according to the indapamide slowly-releasing tablet that the present invention makes down irradiation 10 days and detects once every sampling in 5 days carrying out the strong illumination stability test, and testing result sees Table 1.
The stability test of table 1 strong illumination as a result blanking time outward appearance, color and luster release (%) catabolite content (my god) 2 hours 8 hours 16 hours (%) (%) 0 white film coating tablet, 18.5 57.9 86.2 0.27 99.85 white film coating tablets, 17.6 55.6 85.3 0.37 98.710 white film coating tablets 17.8 58.5 84.5 0.48 97.9
To place 60 ℃ calorstat to handle according to the indapamide slowly-releasing tablet that the present invention makes 10 days, and detect once every sampling in 5 days, testing result sees Table 2.
60 ℃ of thimble tests of table 2 as a result blanking time outward appearance, color and luster release (%) catabolite content (my god) 2 hours 8 hours 16 hours (%) (%) 0 white film coating tablet, 18.5 57.9 86.2 0.27 99.85 white film coating tablets, 18.2 59.2 84.9 0.46 100.110 white film dressings 17.4 58.2 85.2 0.76 98.9
To place relative humidity to be respectively 75% and 92.5% calorstat according to the indapamide slowly-releasing tablet that the present invention makes and handle 10 days, and detect once every sampling in 5 days, testing result sees Table 3, table 4.
Table 3 75% high humidity stability test is the interval outward appearance as a result, color and luster draw moist draw before and after moist release (%) the catabolite content time (%) 2 hours 8 hours 16 hours (%) (%) (my god) (g) (g) 0 white film coating tablet 18.5 57.9 86.2 0.27 99.85 white film coating tablets 3.3395 3.5509 6.33 17.3 56.6 85.5 0.33 98.910 white film coating tablets 3.1467 3.3527 6.55 18.5 56.1 84.3 0.32 99.4
Table 4 92.5% high humidity stability test is the interval outward appearance as a result, color and luster draw moist draw before and after moist release (%) the catabolite content time (%) 2 hours 8 hours 16 hours (%) (%) (my god) (g) (g) 0 white film coating tablet 18.5 57.9 86.2 0.27 99.85 white film coating tablets 3.1612 3.7152 17.5 17.1 55.1 85.5 0.38 99.210 white film coating tablets 3.1305 3.7330 19.2 17.0 55.1 85.0 0.36 98.6
According to dissolution method (two appendix XC of Chinese Pharmacopoeia version in 2000 three therapeutic methods of traditional Chinese medicine), be solvent with water, rotating speed is that per minute 75 changes, volume is 150ml, operation in accordance with the law, respectively 2,8,16, hour to get solution an amount of, filter.Other gets indapamide reference substance (105 ℃ are dried to constant weight) 25mg, the accurate title, decide, and puts in the 50ml measuring bottle, and it is an amount of to add ethanol, made its dissolving in ultrasonic 10 minutes,, filter to scale with ethanol dilution, get subsequent filtrate 2ml and put in the 100ml measuring bottle, thin up is to scale, measure trap at 242nm wavelength place according to spectrophotography (Chinese Pharmacopoeia two appendix IVA in 2000), will refund the stripping cylinder after each solution that takes out has been surveyed trap, calculate every release at different time.Operation repeats six times in accordance with the law, the results are shown in Table 5.
Table 5 release testing result (n=6)
| Time (hour) | ????2 | ????8 | ????16 | ????24 |
| Product of the present invention | ?17.6 | ??53.7 | ??88.3 | ??100.7 |
As can be seen from Table 5, indapamide slowly-releasing tablet of the present invention has good release.
By above-mentioned experimental result as seen, indapamide slowly-releasing tablet of the present invention release, catabolite and content under illumination, high temperature and super-humid conditions have no significant change, thereby can stablize preservation.
Claims (3)
1, a kind of indapamide slowly-releasing tablet is characterized in that: described indapamide slowly-releasing tablet comprises label and coating; Label is made up of with the ratio of 1.5g: 40-150g: 20-100g: 10-100g: 1-10g indopamide, slow-release material, porogen, filler and lubricant; Coating is made up of filmogen, antiplastering aid, screening agent, PEG400, distilled water and ethanol, and it is to join in the ethanol with the ratio of 3-20g: 2-15g: 1-15g: 5ml: 140ml and the coating solution of finally making to 500ml with ethanol dilution is coated on the outer drying of label and forms by filmogen, antiplastering aid, screening agent, PEG400 and distilled water.
2, indapamide slowly-releasing tablet according to claim 1 is characterized in that: described slow-release material is carboxymethyl cellulose, ethyl cellulose, hydroxypropyl emthylcellulose, methylcellulose, hydroxypropyl cellulose, hydroxyethyl-cellulose, pectin, sodium alginate, chitin, glycerol mountain heal any one or two kinds in acid esters and the acrylic resin; Porogen is any one or two kinds in lactose, Sodium Hydroxymethyl Stalcs, the Polyethylene Glycol; Filler is any one or two kinds in sorbitol, mannitol, starch, modified starch and the sucrose; Lubricant is any one in magnesium stearate and the Pulvis Talci.
3, indapamide slowly-releasing tablet according to claim 1 is characterized in that: described filmogen is any one in hydroxypropyl cellulose, methylcellulose, hydroxyethyl-cellulose and the hydroxypropyl emthylcellulose; Antiplastering aid is any in Pulvis Talci and the calcium carbonate; Screening agent is a titanium dioxide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02123999 CN1394604A (en) | 2002-07-12 | 2002-07-12 | Indapamide slowly-releasing tablet |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02123999 CN1394604A (en) | 2002-07-12 | 2002-07-12 | Indapamide slowly-releasing tablet |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579382A (en) * | 2012-03-30 | 2012-07-18 | 重庆科瑞制药(集团)有限公司 | Preparation method for slow-release tablet of indapamide-containing medicament |
| CN101756927B (en) * | 2008-12-23 | 2013-04-10 | 北京科信必成医药科技发展有限公司 | Indapamide sustained release tablet and preparation method thereof |
| CN103142529A (en) * | 2013-03-07 | 2013-06-12 | 宁夏康亚药业有限公司 | Indapamide sustained-release drug composite and preparation method thereof |
| CN108653219A (en) * | 2018-05-22 | 2018-10-16 | 远大医药（中国）有限公司 | A kind of indapamide tablets and preparation method thereof |
-
2002
- 2002-07-12 CN CN 02123999 patent/CN1394604A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101756927B (en) * | 2008-12-23 | 2013-04-10 | 北京科信必成医药科技发展有限公司 | Indapamide sustained release tablet and preparation method thereof |
| CN102579382A (en) * | 2012-03-30 | 2012-07-18 | 重庆科瑞制药(集团)有限公司 | Preparation method for slow-release tablet of indapamide-containing medicament |
| CN103142529A (en) * | 2013-03-07 | 2013-06-12 | 宁夏康亚药业有限公司 | Indapamide sustained-release drug composite and preparation method thereof |
| CN108653219A (en) * | 2018-05-22 | 2018-10-16 | 远大医药（中国）有限公司 | A kind of indapamide tablets and preparation method thereof |
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