CN100421662C - Disperese torasemide tablet and its prepn and application - Google Patents
Disperese torasemide tablet and its prepn and application Download PDFInfo
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- CN100421662C CN100421662C CNB2005101176492A CN200510117649A CN100421662C CN 100421662 C CN100421662 C CN 100421662C CN B2005101176492 A CNB2005101176492 A CN B2005101176492A CN 200510117649 A CN200510117649 A CN 200510117649A CN 100421662 C CN100421662 C CN 100421662C
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- torasemide
- disperese
- tablet
- microcrystalline cellulose
- hyprolose
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Abstract
The present invention relates to torasemide dispersive tablets which contain torasemide, disintegrating agents and diluting agents. The present invention is characterized in that the disintegrating agents are sodium carboxymethyl starch and hydroxypropyl cellulose, and the diluting agents are microcrystalline cellulose. The dispersive tablets have the advantages of rapid disintegration, good dispersion uniformity, high dissolution and stable product. The present invention can be used for treating diseases such as edema or cerebral edema or high blood pressure, etc., caused by congestive heart failure or kidney diseases or hepatosis.
Description
Technical field:
The present invention relates to a kind of Disperese torasemide tablet and preparation method thereof and medical usage, belong to medical technical field.
Background technology:
Torasemide (torasemide) is a pyridine sulfonylurea loop diuretic, and its chemical name is: the amino N-[[(1-Methylethyl)] carbonyl]-the 4-[(3-aminomethyl phenyl) amino]-the 3-pyridine sulfonamide.Structural formula is as follows:
Molecular formula: C
16H
20N
4O
3S
Molecular weight: 348.43
The loop diuretic is widely used in treating all kinds of edema, and its common adverse reactions is a hypokalemia.Not only diuresis is strong and the potassium loss is few in torasemide, and this is relevant with its competitive inhibition aldosterone.
Torasemide can be used for the treatment of keeping of edema therapeutic that congestive heart failure, nephropathy or hepatopathy cause and cerebral edema, also can be used for treating hypertension.Oral or the quiet notes of this product 10mg, once-a-day.Do not control as the state of an illness, dosage is multiplicable, and maximum dose level is no more than 40mg, and intravenously administrable should not surpass 40mg, and intravenously administrable should not surpass for 1 week.Predose when emergency such as pulmonary edema is 20mg, subsequently can be every 30 minutes repeat administration according to the state of an illness, but daily dose should not surpass 200mg; To the general predose of chronic renal failure patient is 20mg, doubles as need, and daily dose should not surpass 200mg; One day on the general one 5mg of hyperpietic, if in 4～6 weeks the miss the mark blood pressure, can increase dosage and arrive 10mg once-a-day.
Torasemide went on the market in Europe, the U.S. and Japan and other countries and area in 1993, was mainly used in the treatment edema disease, as heart failure, liver cirrhosis and kidney disease, also can treat hypertension.The list marketing of torasemide of domestic Zhejiang Cheng Yi Pharmaceutical Co., Ltd capsule.
Disclosed polymorphic or impalpable structure that torasemide exists among Chinese patent application open CN1520403A, CN1452613A, the CN1378448A, the open CN1623987A of Chinese patent application discloses the preparation method of torasemide.Research about torasemide's dosage form is less, finds no the research and the report that close the Disperese torasemide tablet preparation.The Demadex of using clinically only has capsule at present.Capsule exists usually that disintegration rate is slow, dissolution is little, drug absorption is had the shortcoming of certain influence, and simultaneously for the patient who is not easy to swallow, also there is the shortcoming of the inconvenience of taking medicine in capsule.
Summary of the invention:
Defective at Demadex in the prior art, the present invention improves by dosage form, through prescription design and preferred, be surprised to find, torasemide and specific pharmaceutic adjuvant are mixed and made into Disperese torasemide tablet, specifically, with carboxymethyl starch sodium and hyprolose is disintegrating agent, microcrystalline Cellulose is a diluent, makes Disperese torasemide tablet, and not only prepared dispersible tablet has good stability, and the medicine disintegrate is fast, the dissolution height, dispersing uniformity is good, thereby will obviously improve bioavailability of medicament.
Technical scheme of the present invention is as follows:
Disperese torasemide tablet of the present invention comprises torasemide, disintegrating agent and diluent, it is characterized in that described disintegrating agent is carboxymethyl starch sodium and hyprolose, and described diluent is a microcrystalline Cellulose.
According to above-mentioned described Disperese torasemide tablet, wherein, to calculate with weight percentage, torasemide 5%～20% is preferably 5%, 10% or 20%; Carboxymethyl starch sodium 5%～10% is preferably 6%; Hyprolose 10%～20% is preferably 15%; Microcrystalline Cellulose 30%～70%, preferred 50%～65%, more preferably 50%, 60% or 65%.
According to above-mentioned described Disperese torasemide tablet, it can also contain lubricant or correctives.Wherein, described lubricant is selected from one or more in Pulvis Talci, stearic acid, magnesium stearate, Polyethylene Glycol or the micropowder silica gel; Described correctives is selected from one or more in steviosin, aspartame or the saccharin sodium.
According to above-mentioned described Disperese torasemide tablet, wherein, carboxymethyl starch sodium adds.
According to above-mentioned described Disperese torasemide tablet, wherein, contain the 5～20mg of torasemide, microcrystalline Cellulose 50～65mg, carboxymethyl starch sodium 6mg, hyprolose 15mg, steviosin 6mg, Pulvis Talci 3mg in every; Wherein preferred:
The 5mg of torasemide, microcrystalline Cellulose 65mg, carboxymethyl starch sodium 6mg, hyprolose 15mg, steviosin 6mg, Pulvis Talci 3mg;
The 10mg of torasemide, microcrystalline Cellulose 60mg, carboxymethyl starch sodium 6mg, hyprolose 15mg, steviosin 6mg, Pulvis Talci 3mg;
The 20mg of torasemide, microcrystalline Cellulose 50mg, carboxymethyl starch sodium 6mg, hyprolose 15mg, steviosin 6mg, Pulvis Talci 3mg.
A kind of method for preparing above-mentioned described Disperese torasemide tablet of the present invention, it comprises the steps:
(1) 100 mesh sieves is crossed by torasemide and adjuvant pulverize separately;
(2) accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin mix homogeneously, again with torasemide's mix homogeneously, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
(3) survey granule content, it is heavy to calculate sheet, tabletting.
The application of above-mentioned described Disperese torasemide tablet is characterized in that can be used for preparing diuretic.Wherein, preferred agents is used for the treatment of the diseases such as edema, cerebral edema or hypertension because of congestive heart failure, nephropathy or hepatopathy cause.
The specific embodiment:
Further specify the present invention by the following examples, but the claim protection domain is not limited to the scope of embodiment.
Embodiment 1:
(1) prescription is formed:
The 20g of torasemide
Microcrystalline Cellulose 50g
Carboxymethylstach sodium 6g
Hyprolose 15g
Steviosin 6g
Pulvis Talci 3g
70% ethanol is an amount of
Make 1000
(2) preparation technology
1. 100 mesh sieves are crossed by torasemide and adjuvant pulverize separately, standby;
2. accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin adjuvant mix homogeneously, again with the principal agent mixing, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
3. the survey granule content calculates sheet and weighs;
4. tabletting, promptly.
Embodiment 2:
(1) prescription is formed:
The 10g of torasemide
Microcrystalline Cellulose 60g
Carboxymethylstach sodium 6g
Hyprolose 15g
Steviosin 6g
Pulvis Talci 3g
70% ethanol is an amount of
Make 1000
(2) preparation technology
1. 100 mesh sieves are crossed by torasemide and adjuvant pulverize separately, standby;
2. accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin adjuvant mix homogeneously, again with the principal agent mixing, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
3. the survey granule content calculates sheet and weighs;
4. tabletting, promptly.
Embodiment 3:
(1) prescription is formed:
The 5g of torasemide
Microcrystalline Cellulose 65g
Carboxymethylstach sodium 6g
Hyprolose 15g
Steviosin 6g
Pulvis Talci 3g
70% ethanol is an amount of
Make 1000
(2) preparation technology
1. 100 mesh sieves are crossed by torasemide and adjuvant pulverize separately, standby;
2. accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin adjuvant mix homogeneously, again with the principal agent mixing, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
3. the survey granule content calculates sheet and weighs;
4. tabletting, promptly.
Embodiment 4:
(1) prescription is formed:
The 2.0g of torasemide
Microcrystalline Cellulose 4.6g
Carboxymethylstach sodium 0.5g
Hyprolose 2.0g
Steviosin 0.6g
Pulvis Talci 0.3g
70% ethanol is an amount of
Make 100
(2) preparation technology
1. 100 mesh sieves are crossed by torasemide and adjuvant pulverize separately, standby;
2. accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin adjuvant mix homogeneously, again with the principal agent mixing, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
3. the survey granule content calculates sheet and weighs;
4. tabletting, promptly.
Embodiment 5:
(1) prescription is formed:
The 1.5g of torasemide
Microcrystalline Cellulose 5.6g
Carboxymethylstach sodium 0.6g
Hyprolose 1.5g
Saccharin sodium 0.5g
Pulvis Talci 0.3g
70% ethanol is an amount of
Make 100
(2) preparation technology
1. 100 mesh sieves are crossed by torasemide and adjuvant pulverize separately, standby;
2. accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, saccharin sodium adjuvant mix homogeneously, again with the principal agent mixing, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
3. the survey granule content calculates sheet and weighs;
4. tabletting, promptly.
Embodiment 6 (contrast test):
Prescription and technology: the prescription of pressing table 1 design, take by weighing torasemide and each adjuvant respectively with 100 recipe quantities, cross 100 mesh sieves respectively, earlier with auxiliary materials and mixing such as microcrystalline Cellulose, lactose, hyprolose or steviosin, again with the principal agent mixing, add 70% ethanol system soft material, 20 mesh sieves are granulated, 55 ℃ of dryings 1 hour, 60 mesh sieve granulate, again with auxiliary materials and mixing such as carboxymethylstach sodium or Pulvis Talci, tabletting.
Get the Disperese torasemide tablet of embodiment 1～4, the dispersible tablet that makes with table 1 prescription 1-3 carries out disintegration and dispersing uniformity investigation test.Investigation the results are shown in Table 2.
Table 1 prescription is formed
Table 2 is investigated the result disintegration
Annotate: disintegration and dispersing uniformity are all measured by Chinese Pharmacopoeia two appendix IA in 2000.
The result of above-mentioned test shows, is disintegrating agent with carboxymethyl starch sodium and hyprolose, and microcrystalline Cellulose is a diluent, and the Disperese torasemide tablet disintegrate that makes is fast, and good dispersion reaches the feature request of dispersible tablet.
Embodiment 7: stability test
Get the Disperese torasemide tablet that embodiment 1 makes, press the stability test principle in two appendix of Chinese Pharmacopoeia version in 2000, sample put respectively under high light (4700Lx), high temperature (60 ℃), high humidity (RH92.5%) condition investigate 5 days and 10 days, and, the results are shown in Table 3 to every investigation index and comparison in 0 day.
Table 3 stability test result
By the stability test result as can be known, this product outward appearance, content, disintegration, dispersing uniformity under high light, high temperature (60 ℃) condition do not have significant change; Under super-humid conditions, all there is not content, dispersing uniformity and disintegration obvious change.This product has moisture absorption phenomenon under super-humid conditions, can carry out airtight package.
Claims (6)
1. Disperese torasemide tablet, comprise torasemide, disintegrating agent and diluent, it is characterized in that described disintegrating agent is carboxymethyl starch sodium and hyprolose, described diluent is a microcrystalline Cellulose, wherein, calculates with weight percentage, torasemide 5%～20%, carboxymethyl starch sodium 5%～10%, hyprolose 10%～20%, microcrystalline Cellulose 50%～70%.
2. Disperese torasemide tablet according to claim 1 is characterized in that described dispersible tablet also contains lubricant or correctives.
3. Disperese torasemide tablet according to claim 2 is characterized in that described lubricant is one or more in Pulvis Talci, stearic acid, magnesium stearate, Polyethylene Glycol or the micropowder silica gel; Described correctives is one or more in steviosin, aspartame or the saccharin sodium.
4. according to each described Disperese torasemide tablet of claim 1-3, it is characterized in that carboxymethyl starch sodium adds.
5. Disperese torasemide tablet according to claim 1 contains the 5～20mg of torasemide, microcrystalline Cellulose 50～65mg, carboxymethyl starch sodium 6mg, hyprolose 15mg, steviosin 6mg, Pulvis Talci 3mg in it is characterized in that every.
6. method for preparing Disperese torasemide tablet according to claim 5, it comprises the steps:
(1) 100 mesh sieves is crossed by torasemide and adjuvant pulverize separately;
(2) accurately take by weighing supplementary material by recipe quantity, earlier with microcrystalline Cellulose, hyprolose, steviosin mix homogeneously, again with torasemide's mix homogeneously, add 70% ethanol and make soft material in right amount, 20 mesh sieves are granulated, 55 ℃ of dryings, 60 mesh sieve granulate add carboxymethylstach sodium, Pulvis Talci mixing again;
(3) survey granule content, it is heavy to calculate sheet, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005101176492A CN100421662C (en) | 2005-11-08 | 2005-11-08 | Disperese torasemide tablet and its prepn and application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005101176492A CN100421662C (en) | 2005-11-08 | 2005-11-08 | Disperese torasemide tablet and its prepn and application |
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| Publication Number | Publication Date |
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| CN1771945A CN1771945A (en) | 2006-05-17 |
| CN100421662C true CN100421662C (en) | 2008-10-01 |
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| CNB2005101176492A Expired - Fee Related CN100421662C (en) | 2005-11-08 | 2005-11-08 | Disperese torasemide tablet and its prepn and application |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101632665B (en) * | 2009-09-01 | 2011-08-17 | 严洁 | Novel torasemide oral medicine composition |
| CN106038500A (en) * | 2016-05-26 | 2016-10-26 | 南京正科医药股份有限公司 | Torasemide tablet |
| CN107157994A (en) * | 2017-06-09 | 2017-09-15 | 董鹏 | A kind of sublingual oral formulations of Torasemide |
| CN115778912A (en) * | 2021-09-09 | 2023-03-14 | 苏中药业集团股份有限公司 | Torasemide-containing tablet and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1452613A (en) * | 2000-03-20 | 2003-10-29 | 普利瓦股份公司 | Amorphous torasemide modification |
| CN1505512A (en) * | 2000-02-17 | 2004-06-16 | ������ҩ��ҵ����˾ | A stable pharmaceutical formulation comprising torsemide modification II |
| CN1520403A (en) * | 2000-05-19 | 2004-08-11 | ������ҩ�﹤ҵ��˾ | Novel polymorph v of torasemide |
-
2005
- 2005-11-08 CN CNB2005101176492A patent/CN100421662C/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1505512A (en) * | 2000-02-17 | 2004-06-16 | ������ҩ��ҵ����˾ | A stable pharmaceutical formulation comprising torsemide modification II |
| CN1452613A (en) * | 2000-03-20 | 2003-10-29 | 普利瓦股份公司 | Amorphous torasemide modification |
| CN1520403A (en) * | 2000-05-19 | 2004-08-11 | ������ҩ�﹤ҵ��˾ | Novel polymorph v of torasemide |
Non-Patent Citations (4)
| Title |
|---|
| 托拉塞米片多次给药药动学研究. 况扶华等.中国药学杂志，第40卷第9期. 2005 |
| 托拉塞米片多次给药药动学研究. 况扶华等.中国药学杂志，第40卷第9期. 2005 * |
| 新编药物学. 陈新谦，金有豫，372，人民卫生出版社. 1998 |
| 新编药物学. 陈新谦，金有豫，372，人民卫生出版社. 1998 * |
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| CN1771945A (en) | 2006-05-17 |
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Assignee: Guangdong Aimin Pharmaceutical Co., Ltd. Assignor: Zhou Zhuohe Contract fulfillment period: 2008.10.20 to 2014.10.20 contract change Contract record no.: 2009440001747 Denomination of invention: Disperese torasemide tablet and its prepn and application Granted publication date: 20081001 License type: Exclusive license Record date: 20091026 |
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Free format text: EXCLUSIVE LICENSE; TIME LIMIT OF IMPLEMENTING CONTACT: 2008.10.20 TO 2014.10.20; CHANGE OF CONTRACT Name of requester: GUANGDONG AIMIN MEDICINE CO., LTD. Effective date: 20091026 |
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Assignee: Guangdong Aimin Pharmaceutical Co., Ltd. Assignor: Zhou Zhuohe Contract record no.: 2009440001747 Date of cancellation: 20100416 |
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Assignee: Guangdong Aimin Pharmaceutical Co., Ltd. Assignor: Zhou Zhuohe Contract record no.: 2011440001032 Denomination of invention: Disperese torasemide tablet and its prepn and application Granted publication date: 20081001 License type: Exclusive License Open date: 20060517 Record date: 20111116 |
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