CN101485634A - Nitroglycerin tablets and preparation method thereof - Google Patents
Nitroglycerin tablets and preparation method thereof Download PDFInfo
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- CN101485634A CN101485634A CNA2008100007880A CN200810000788A CN101485634A CN 101485634 A CN101485634 A CN 101485634A CN A2008100007880 A CNA2008100007880 A CN A2008100007880A CN 200810000788 A CN200810000788 A CN 200810000788A CN 101485634 A CN101485634 A CN 101485634A
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Abstract
The invention relates to a glonoin tablet which is a drug for treating angina and a method for preparing the same. The glonoin tablet contains 0.5 milligram of glonoin and a proper amount of pharmaceutic adjuvants which are selected from a bulking agent, a stabilizing agent, a bonding agent, a disintegrating agent and a lubricating agent. In the prescription, the valuing ranges of all components for preparing one thousand tablets are that: 5.0 milliliter of 10 percent glonoin solution, 1 to 15 grams of microcrystalline cellulose, 0.1 to 1.0 gram of polyvinyl pyrrolidon, 10 to 30 grams of lactose, 1.0 to 4.0 grams of cross-linking polyvidone, 0.1 to 0.4 gram of magnesium stearate, and 10 to 20 gram of 65 percent ethanol; and the raw materials and the pharmaceutic adjuvants are screened, mixed, granulated and tableted to prepare the glonoin tablet. In the glonoin tablet, the stabilizing agent is added in the prescription, thereby lowering the vapor pressure for volatilizing the glonoin, shortening disintegration time, improving stabilization and prolonging period of validity.
Description
Technical field
The present invention relates to the anginal medicine nitroglycerin of a kind of treatment tablet and preparation method thereof.
Background technology
Angina pectoris is the common sympton of coronary atherosclerotic heart disease (abbreviating coronary heart disease as), is coronary insufficiency, rapid, temporary transient ischemia of cardiac muscle and the caused clinical syndrome of anoxia.Paroxysmal colic or vexed pain appear in breastbone rear portion and pareordia during outbreak, and can be radiated to left upper extremity, and pain is that the institutes such as many skins class material by ischemia, anoxybiotic metabolite lactic acid, acetone acid or similar sharp skin cause.
Nitroglycerin is the anginal medicine of finding the earliest of treatment, it is the representative medicine of nitrate esters, be used for the treatment of the history in existing more than 100 year of angina pectoris, because that it has is rapid-action, curative effect is sure, easy to use, economic dispatch advantage, is still one of anginal choice drug of domestic and international control so far.The action principle of nitroglycerin: can coronary artery dilator and vein blood vessel, alleviate the anginal cause of disease, reduce the oxygen consumption of cardiac muscle, increase the blood supply of cardiac muscle, thereby reach the analgesic effect.Nitroglycerin can be prevented anginal outbreak effectively fast, is that blood drug level reaches peak value very soon because of its fat-soluble high sublingual administration is very easily absorbed by euangiotic oral mucosa, can avoid the first influence of crossing elimination of liver.The bioavailability of sublingual administration is 80%, and oral only be 8%, onset in 1-2 minutes behind the buccal, drug effect continues 20-30 minutes.
As a kind of first aid medicine, nitroglycerin must possess the content height, discharges soon the characteristics that storage period is long.But because nitroglycerin has higher vapour pressure, have stronger volatility, very easily be subjected to the influence of factors such as temperature, humidity, packing, so volatilization easily in put procedure is the nitroglycerine tablets rather unstable.According to clinical statistics, the nitroglycerine tablets curative effect of different manufacturers production both at home and abroad has certain difference, and disintegration time is long, and storage period is also different in size, greatly reduces clinical application safety.
Nitroglycerine tablets of the present invention add stabilizing agent in prescription, reduced the evaporable vapour pressure of nitroglycerin, shorten disintegration time, improve stability, extend the expiration date.
Summary of the invention
The objective of the invention is to shorten disintegration time, improve stability, extend the expiration date, a kind of nitroglycerine tablets and preparation method thereof are provided in order to solve the volatile problem of nitroglycerine tablets.
Nitroglycerine tablets of the present invention, every contains 0.5 milligram of nitroglycerin and proper quantity of medicinal auxiliary material.Pharmaceutic adjuvant is selected from filler, stabilizing agent, binding agent, disintegrating agent and lubricant.Wherein pharmaceutic adjuvant comprises: microcrystalline Cellulose, polyvinylpyrrolidone, lactose, polyvinylpolypyrrolidone, magnesium stearate, 65% ethanol.
Each component is made the span of thousand tablets of tablets and is in prescription: 5.0 milliliters of 10% nitroglycerin solutions, microcrystalline Cellulose 1～15 gram, polyvinylpyrrolidone 0.1～1.0 gram, lactose 10～30 grams, polyvinylpolypyrrolidone 1.0～4.0 grams, magnesium stearate 0.1～0.4 gram, 65% ethanol, 10～20 grams.Aborning, to make thousand tablets of tablets is example, the preferable prescription span of each component is: 5.0 milliliters of 10% nitroglycerin solutions, microcrystalline Cellulose 1～10 gram, polyvinylpyrrolidone 0.1～0.5 gram, lactose 15～25 grams, polyvinylpolypyrrolidone 1.0～2.5 grams, magnesium stearate 0.1～0.3 gram, 65% ethanol, 10～15 grams.
Design a kind of preparation method of nitroglycerine tablets according to above-mentioned purpose, it is characterized in that this method may further comprise the steps:
1, get the raw materials ready: (1) crosses 100 mesh sieves respectively to microcrystalline Cellulose, lactose, polyvinylpolypyrrolidone, and magnesium stearate is crossed 120 mesh sieves.Take by weighing adjuvant respectively by the prescription specified volume, standby.(2) preparation nitroglycerin～polyvinylpyrrolidone mixed solution: 10% nitroglycerin solution and the polyvinylpyrrolidone of recipe quantity are put in the appropriate vessel altogether, and it is molten entirely to be stirred to polyvinylpyrrolidone, sealing, stand for standby use.
2, mix: the microcrystalline Cellulose of the recipe quantity after will sieving, lactose are done and are mixed, and the time is 1 hour, adds nitroglycerin～polyvinylpyrrolidone mixed solution then, fully stir, and mix 3 hours with supplementary material.
3, granulate: (1) makes qualified soft material with mixed supplementary material; With the wet grain of 18 order nylon sieve series.(2) grain that will wet divides pot to carry out drying, and temperature＜50 ℃ are about 1～3 hour drying time.(3) dried granule is crossed 16 mesh sieves and carry out granulate.
4, tabletting: with polyvinylpolypyrrolidone, the magnesium stearate mix homogeneously of dried granule and recipe quantity, punch die tabletting.This product is white compressed tablet.
Polyvinylpyrrolidone is one of medicinal synthetic new adjuvant, can be used as tablet, particulate binding agent, also can be used as the stabilizing agent of temperature-sensitive medicine, can be water-soluble, can be dissolved in most of organic solvent again, have good complexing power and colloidal nature and physiological compatibility.Polyvinylpyrrolidone of the present invention not only is used as binding agent, and is even more important as stabilizing agent.Polyvinylpyrrolidone is dissolved in the nitroglycerin alcoholic solution, utilizes its absorption nitroglycerin, has reduced vapour pressure, has reduced evaporation rate, has improved stability, has prolonged effect duration.
Adjuvant of the present invention is all selected novel import adjuvant for use, and lactose is main filler, is a kind of economical adjuvant, has the formedness price ratio, no hygroscopicity, stable in properties, with most drug chemically reactive not, add microcrystalline Cellulose simultaneously and improve particulate flowability, compressibility; Polyvinylpolypyrrolidone is as disintegrating agent, is the powder of white, good fluidity, but in water swelling but full-bodied gel layer can not occur rapidly, thereby its disintegrating property is very superior, and adopts outer addition, the disintegrate better effects if has shortened disintegration time greatly.
The specific embodiment
, the present invention prepares as stated above, its detailed component is provided by the following example, but protection model circle of the present invention is not limited to this.
Preparation method:
1, get the raw materials ready: (1) crosses 100 mesh sieves respectively to microcrystalline Cellulose, lactose, polyvinylpolypyrrolidone, and magnesium stearate is crossed 120 mesh sieves.Take by weighing adjuvant respectively by the prescription specified volume, standby.(2) preparation nitroglycerin～polyvinylpyrrolidone mixed solution: 10% nitroglycerin solution and the polyvinylpyrrolidone of recipe quantity are put in the appropriate vessel altogether, and it is molten entirely to be stirred to polyvinylpyrrolidone, sealing, stand for standby use.
2, mix: the microcrystalline Cellulose of the recipe quantity after will sieving, lactose are done and are mixed, and the time is 1 hour, adds nitroglycerin～polyvinylpyrrolidone mixed solution then, fully stir, and mix 3 hours with supplementary material.
3, granulate: (1) makes qualified soft material with mixed supplementary material; With the wet grain of 18 order nylon sieve series.(2) grain that will wet divides pot to carry out drying, and temperature＜50 ℃ are about 1～3 hour drying time.(3) dried granule is crossed 16 mesh sieves and carry out granulate.
4, tabletting: with polyvinylpolypyrrolidone, the magnesium stearate mix homogeneously of dried granule and recipe quantity, punch die tabletting.This product is white compressed tablet.
Two, nitroglycerine tablets and the commercially available nitroglycerine tablets that the present invention added stabilizing agent carry out stability test relatively:
1, for the test agent interrelated data: make the commercially available nitroglycerine tablets of nitroglycerine tablets (2) by oneself for test agent (1) the present invention
2, investigation project: the situation of change that this tests main investigation project is disintegration, content.Main investigation test is influence factor's test and long term test.
3, preparation packing condition: listing packing
4, investigate time point:
(1) influence factor's test: 0, sampling in 5,10 days, measure the disintegration of nitroglycerine tablets, the situation of change of content.
(2) long term test: 0, sampling in 3,6 months, measure the disintegration of nitroglycerine tablets, the situation of change of content.
5, influence factor's test and result
Self-control sample and commercially available sample opening are put in the suitable clean container, 40 ℃ of temperature, relative humidity (R.H.) 75%, place under illumination 4500 ± 500LX condition, in sampling in the 0th, 5,10 day, by " regulation under 2005 editions two nitroglycerine tablets normal terms of Chinese pharmacopoeia is measured the disintegration of nitroglycerine tablets, the situation of change of content.The results are shown in following table:
6, long term test and result
To make sample by oneself and the intact packing of commercially available sample is put under the room temperature condition, in sampling in 0,3,6 month, by " regulation 2005 editions two nitroglycerine tablets normal terms of Chinese pharmacopoeia under, the disintegration of mensuration nitroglycerine tablets, the situation of change of content.The results are shown in following table:
Claims (6)
1, the anginal medicine nitroglycerin of a kind of treatment tablet and preparation method thereof is characterized in that every in this tablet contains 0.5 milligram of nitroglycerin and proper quantity of medicinal auxiliary material.
2, tablet according to claim 1 is characterized in that above-mentioned pharmaceutic adjuvant is selected from filler, stabilizing agent, binding agent, disintegrating agent and lubricant.
3, tablet according to claim 2. it is characterized in that pharmaceutic adjuvant comprises: microcrystalline Cellulose, polyvinylpyrrolidone, lactose, polyvinylpolypyrrolidone, magnesium stearate, 65% ethanol.。
4, tablet according to claim 1, it is characterized in that described prescription is an example to make thousand tablets of tablets, the prescription span of each component is: 5.0 milliliters of 10% nitroglycerin solutions, microcrystalline Cellulose 1～15 gram, polyvinylpyrrolidone 0.1～1.0 gram, lactose 10～30 grams, polyvinylpolypyrrolidone 1.0～4.0 grams, magnesium stearate 0.1～0.4 gram, 65% ethanol, 10～20 grams.
5, tablet according to claim 4, it is characterized in that described prescription is an example to make thousand tablets of tablets, the preferable prescription span of each component is: 5.0 milliliters of 10% nitroglycerin solutions, microcrystalline Cellulose 1～10 gram, polyvinylpyrrolidone 0.1～0.5 gram, lactose 15～25 grams, polyvinylpolypyrrolidone 1.0～2.5 grams, magnesium stearate 0.1～0.3 gram, 65% ethanol, 10～15 grams.
6, a kind of method for preparing tablet as claimed in claim 1 is characterized in that this method may further comprise the steps:
(1) gets the raw materials ready: 1) microcrystalline Cellulose, lactose, polyvinylpolypyrrolidone are crossed 100 mesh sieves respectively, magnesium stearate is crossed 120 mesh sieves.Take by weighing adjuvant respectively by the prescription specified volume, standby.2) preparation nitroglycerin～polyvinylpyrrolidone mixed solution: 10% nitroglycerin solution and the polyvinylpyrrolidone of recipe quantity are put in the appropriate vessel altogether, and it is molten entirely to be stirred to polyvinylpyrrolidone, sealing, stand for standby use.
(2) mix: the microcrystalline Cellulose of the recipe quantity after will sieving, lactose are done and are mixed, and the time is 1 hour, adds nitroglycerin～polyvinylpyrrolidone mixed solution then, fully stir, and mix 3 hours with supplementary material.
(3) granulate: 1) mixed supplementary material is made qualified soft material; With the wet grain of 18 order nylon sieve series.2) grain that will wet divides pot to carry out drying, and temperature＜50 ℃ are about 1～3 hour drying time.3) dried granule is crossed 16 mesh sieves and carry out granulate.
(4) tabletting: with polyvinylpolypyrrolidone, the magnesium stearate mix homogeneously of dried granule and recipe quantity, punch die tabletting.This product is white compressed tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100007880A CN101485634A (en) | 2008-01-17 | 2008-01-17 | Nitroglycerin tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100007880A CN101485634A (en) | 2008-01-17 | 2008-01-17 | Nitroglycerin tablets and preparation method thereof |
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| CN101485634A true CN101485634A (en) | 2009-07-22 |
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| CNA2008100007880A Pending CN101485634A (en) | 2008-01-17 | 2008-01-17 | Nitroglycerin tablets and preparation method thereof |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150272919A1 (en) * | 2012-10-03 | 2015-10-01 | Dipharma Francis S.R.L. | Pharmaceutical composition |
| CN111517960A (en) * | 2020-05-19 | 2020-08-11 | 启东市新晨企业管理咨询有限公司 | Continuous production nitroglycerin tablet |
| CN111559964A (en) * | 2020-05-19 | 2020-08-21 | 启东市新晨企业管理咨询有限公司 | Green preparation method of nitroglycerin |
| CN111568859A (en) * | 2020-05-19 | 2020-08-25 | 启东市新晨企业管理咨询有限公司 | External preparation of nitroglycerin |
| CN112315920A (en) * | 2020-09-29 | 2021-02-05 | 南京斯泰尔医药科技有限公司 | Nitroglycerin sublingual tablet and preparation method thereof |
| CN114404374A (en) * | 2022-01-20 | 2022-04-29 | 北京微智瑞医药科技有限公司 | Nitroglycerin micro-tablet and preparation method and preparation thereof |
| CN114469881A (en) * | 2022-03-14 | 2022-05-13 | 河北坤安药业有限公司 | Nitroglycerin tablet and preparation method thereof |
| WO2024105695A1 (en) * | 2022-11-16 | 2024-05-23 | Modi-Mundipharma Pvt. Ltd. | Stabilized nitroglycerin fast dissolving tablet preparation and process for preparation thereof |
-
2008
- 2008-01-17 CN CNA2008100007880A patent/CN101485634A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150272919A1 (en) * | 2012-10-03 | 2015-10-01 | Dipharma Francis S.R.L. | Pharmaceutical composition |
| CN111517960A (en) * | 2020-05-19 | 2020-08-11 | 启东市新晨企业管理咨询有限公司 | Continuous production nitroglycerin tablet |
| CN111559964A (en) * | 2020-05-19 | 2020-08-21 | 启东市新晨企业管理咨询有限公司 | Green preparation method of nitroglycerin |
| CN111568859A (en) * | 2020-05-19 | 2020-08-25 | 启东市新晨企业管理咨询有限公司 | External preparation of nitroglycerin |
| CN111568859B (en) * | 2020-05-19 | 2022-07-19 | 启东市新晨企业管理咨询有限公司 | External preparation of nitroglycerin |
| CN112315920A (en) * | 2020-09-29 | 2021-02-05 | 南京斯泰尔医药科技有限公司 | Nitroglycerin sublingual tablet and preparation method thereof |
| CN114404374A (en) * | 2022-01-20 | 2022-04-29 | 北京微智瑞医药科技有限公司 | Nitroglycerin micro-tablet and preparation method and preparation thereof |
| CN114469881A (en) * | 2022-03-14 | 2022-05-13 | 河北坤安药业有限公司 | Nitroglycerin tablet and preparation method thereof |
| WO2024105695A1 (en) * | 2022-11-16 | 2024-05-23 | Modi-Mundipharma Pvt. Ltd. | Stabilized nitroglycerin fast dissolving tablet preparation and process for preparation thereof |
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Open date: 20090722 |