CN1507861A - Trimebutine maleate tablet and preparing method thereof - Google Patents
Trimebutine maleate tablet and preparing method thereof Download PDFInfo
- Publication number
- CN1507861A CN1507861A CNA021485763A CN02148576A CN1507861A CN 1507861 A CN1507861 A CN 1507861A CN A021485763 A CNA021485763 A CN A021485763A CN 02148576 A CN02148576 A CN 02148576A CN 1507861 A CN1507861 A CN 1507861A
- Authority
- CN
- China
- Prior art keywords
- tablet
- trimebutine maleate
- accounts
- trimebutine
- agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of oral trimebutine tablet and its preparation method. Said invention is characterized by that the trimebutine raw material can be coated with water soluble film-forming agent and plasticizer. The tablet made up by said method can hide the taste of trimebutine, at the same time it does not affect disintegration and does not affect resolution of its main component.
Description
Technical field
The present invention relates to a kind of kind of oral trimebutine tablet and preparation method thereof that is used for.
Background technology
Because of Trimebutine Maleate has lasting insufferable astringent taste, oral conventional tablet promptly produces strong fiber crops flavor between medicine and a very short time that tongue contacts, makes the people can't continue to take.
The technology of previously known only is related to the lasting bitterness that overcomes Trimebutine Maleate or guarantees stability at preparation Trimebutine Maleate when preserving medicine, but equal imperfections.
In disclosed FR2468364 on May 8th, 1981, a kind of preparation method of microcapsule has been described, this microcapsule is equipped with pharmaceutical active compounds, its wall is an ethyl cellulose, implements in thiacyclohexane, and this method is used the derivant that is separated, the preferred phospholipid derivant that is separated, as an example, preparation Trimebutine Maleate microcapsule, one of them standard of estimating their quality is not have bitterness.
Having described its wall in nineteen eighty-two December disclosed FR2506613 on the 3rd is by ethyl cellulose and a kind of water insoluble but be dissolved in the microcapsule that the polymer of acid medium constitutes, and its objective is rapid release product in the stomach medium.
April 13 nineteen eighty-three, disclosed EP0076515 also related to the microcapsule of rapid release in the stomach medium, its wall be by ethyl cellulose and a kind of in water and/or in acid medium polymer soluble constitute.
April 13 nineteen eighty-three, disclosed EP0076428 was identical with the purpose of above-mentioned patent, their wall be by ethyl cellulose and a kind of in water " expandable " polymer constitute.
Obviously, the purpose of above-mentioned each patent is covers bitterness, but effect is not satisfactory, and the preparation method complexity, and production cost is higher, and uses flammable solvent, and residual solvent is difficult to remove, and Determination of Residual Organic Solvents does not meet standard; On the other hand, by the preparation of method for preparing, the principal agent component content is low, and the dosage of patient every day is the 300-600mg Trimebutine Maleate, but the amount of excipient is through high several times of the amount of active component.
About being used for the kind of oral trimebutine tablet agent, disclosed patent FR2640876 has described a kind of nonencapsulated tablet medicine compositions June 29 nineteen ninety, said composition contains the Trimebutine Maleate as active component, it is characterized in that this active component weight content is 35-45%, it is evenly dispersed in the hydrophilic porous matrix of hypromellose, and the amount of hypromellose is 15-20% (weight ratio), and other contains 20-25% (weight) water-soluble diluent and 10-20% (weight) tartaric acid.
On August 18th, 1999, disclosed CN1226162A described a kind of new oral trimebutine maleate table agent that has improved, a kind of nuclear of the main content of its feature, and it contains the 30-60% Trimebutine Maleate; Also contain a kind of water solublity peplos, in the medium of oral cavity, it has of short duration and enough effect to the disintegrate that keeps nuclear with the too early active component that discharges.
Summary of the invention
Purpose of the present invention mainly provides the trimebutine maleate table agent of no bad mouthfeel, and the higher dissolution of this product tool dissolves quick acting rapidly in gastric juice simultaneously.
The foregoing invention purpose is achieved by the following technical solution: a kind of preparation method of trimebutine maleate table, may further comprise the steps: (1) is sieved the Trimebutine Maleate raw material and is put at the bottom of the fluid bed in the spray apparatus, carry out coating with water-soluble film forming agent and plasticizer as coating material, obtain the feed particles of coating; (2) diluent, binding agent and acidulant are mixed, and drying and granulating; (3) above-mentioned two step gained granules are added disintegrating agent, lubricant and flowable, and mix homogeneously, tabletting is made.
Described water-soluble film forming agent is selected from acrylate copolymer or cellulosic polymer, as: low viscous hypromellose, methylcellulose, ethyl cellulose, hyprolose, polyacrylic resin E100.Described plasticizer is selected from Polyethylene Glycol, propylene glycol, glycerol or Oleum Ricini that mean molecule quantity is 3000-6000; Described diluent is selected from crystallite or powdery cellulose, mannitol, starch, more specifically, lactose, special Lactose hydrate, the weight ratio that diluent accounts for tablet is 20-40%; Binding agent is selected from microcrystalline Cellulose, gelatin, methylcellulose, pregelatinized Starch, polyvidone, hypromellose, preferred especially low viscous hypromellose, and the weight ratio of binder constitutes tablet is 2.5-25%; Acidulant is selected from the pharmacology and goes up acceptable organic acid, is selected from lactic acid or tartaric acid, tartaric acid preferably, and the weight ratio that accounts for tablet is 0.5-2%; Flowable is selected from the silicon dioxide of anhydrous or hydration, and the weight ratio that accounts for tablet is 0.7-2.5%; Lubricant is selected from Metallic stearates, preferred calcium stearate or magnesium, and magnesium stearate concentration preferably accounts for the weight 0.5-1.5% of tablet, more preferably accounts for the weight 1% of tablet; Disintegrating agent is selected from low-substituted hydroxypropyl fiber system, cross-linked carboxymethyl fiber is sodium, polyvidone, carboxymethyl starch sodium, crospovidone and their mixture, is preferably cross-linking sodium carboxymethyl cellulose, accounts for the weight 1-15% of tablet, is preferably 5-10%.
The trimebutine maleate table of preceding method preparation comprises the feed particles 40%-70% that the Trimebutine Maleate raw material obtains as coating material with water-soluble film forming agent and plasticizer; Other adjuvants 30%-60%.
Described adjuvant comprises the diluent of 20-40%, the binding agent of 2.5-25%, the acidulant of 0.5-2%, the disintegrating agent of 1-15%, the lubricant of 0.5-1.5% and the flowable of 0.7-2.5%.
This tablet is the raw material coating, and for having covered the Trimebutine Maleate capsule-core tablet of bitterness, this tablet does not influence disintegrate, does not influence the stripping of principal agent composition yet, but has covered the bitterness of Trimebutine Maleate effectively.In the oral cavity, when tablet contacts with saliva, do not produce the fiber crops flavor, make the glad this product of taking of people; And this product is not a coated tablet, has avoided the slower shortcoming of conventional coated tablet stripping
For further setting forth technical scheme of the present invention, illustrated below in conjunction with embodiment and effect thereof
The specific embodiment
Embodiment 1
Trimebutine maleate table (100mg)
Table 1: the trimebutine maleate table prescription is formed
| Component | Every content | Percentage composition |
| Coating Malaysia love song U.S. spit of fland | 110mg | ?49.91 |
| Lactose | 47mg | ?21.32 |
| Starch | 22mg | ?9.98 |
| Microcrystalline Cellulose | 22mg | ?9.98 |
| Hypromellose (6cp.s) | 0.05mg | ?0.05 |
| Cross-linked carboxymethyl cellulose sodium | 11mg | ?4.99 |
| Tartaric acid | 4.4mg | ?2.0 |
| Silicon dioxide | 2mg | ?0.91 |
| Magnesium stearate | 2mg | ?0.91 |
| Add up to | 220.4mg | ?100.00 |
The Trimebutine Maleate raw material sieved put at the bottom of the fluid bed in the spray apparatus, carry out the raw material coating, obtain the feed particles of coating with polyacrylic resin E100, polyacrylic resin NE30D and the dispersion liquid of colloid silicon in ethanol.
With lactose, starch, microcrystalline Cellulose, granulate drying, secondary grain with being dissolved with tartaric hypromellose.
Get Trimebutine Maleate raw material, the granules of accessories of coating, add crosslinked dimension acid, Herba Menthae essence and silicon dioxide, mix homogeneously, tabletting, packing.
Table 2: Trimebutine Maleate raw material coating prescription
| Component | Every content | Percentage composition |
| Malaysia love song Mei Dingting | ?100mg | ?80.91 |
| Polyacrylic resin E100 | ?5mg | ?8.29 |
| Polyacrylic resin NE30D | ?3mg | ?0.83 |
| Tartaric acid | ?2mg | ?2.48 |
| Add up to | 110mg | ?100.00 |
According to said method Zhi Bei tablet does not have bitterness in mouthful;
Embodiment 2
Trimebutine maleate table (100mg)
Table 3: the trimebutine maleate table prescription is formed
| Component | Every content | Percentage composition |
| Coating Malaysia love song U.S. spit of fland | 110mg | ?49.91 |
| Lactose | 47mg | ?21.32 |
| Starch | 22mg | ?9.98 |
| Microcrystalline Cellulose | 22mg | ?9.98 |
| Hypromellose (6cp.s) | 0.05mg | ?0.05 |
| Cross-linked carboxymethyl cellulose sodium | 11mg | ?4.99 |
| Tartaric acid | 4.4mg | ?2.0 |
| Silicon dioxide | 2mg | ?0.91 |
| Magnesium stearate | 2mg | ?0.91 |
| Add up to | 220.4mg | ?100.00 |
The Trimebutine Maleate raw material sieved put at the bottom of the fluid bed in the spray apparatus, the dispersion liquid in ethanol carries out the raw material coating with HPMC and colloid silicon, obtains the feed particles of coating.
With lactose, starch, microcrystalline Cellulose, granulate drying, secondary grain with being dissolved with tartaric hypromellose.
Get Trimebutine Maleate raw material, the granules of accessories of coating, add crosslinked dimension acid, Herba Menthae essence and silicon dioxide, mix homogeneously, tabletting, packing.
Table 4: Trimebutine Maleate raw material coating prescription
| Component | Every content | Percentage composition |
| Malaysia love song Mei Dingting | ?100mg | ?90.91 |
| HPMC | ?5mg | ?4.55 |
| Silicon dioxide | ?3mg | ?2.73 |
| Tartaric acid | ?2mg | ?1.82 |
| Add up to | ?110mg | ?100.00 |
According to said method Zhi Bei tablet does not have bitterness.
Claims (5)
1, a kind of preparation method of trimebutine maleate table, it is characterized in that may further comprise the steps: (1) is sieved the Trimebutine Maleate raw material and is put at the bottom of the fluid bed in the spray apparatus, carry out coating with water-soluble film forming agent and plasticizer as coating material, obtain the feed particles of coating; (2) diluent, binding agent and acidulant are mixed, and drying and granulating; (3) above-mentioned two step gained granules are added disintegrating agent, lubricant and flowable, and mix homogeneously, tabletting is made.
2, the preparation method of trimebutine maleate table as claimed in claim 1, it is characterized in that described water-soluble film forming agent is selected from acrylate copolymer or cellulosic polymer, as: low viscous hypromellose, methylcellulose, ethyl cellulose, hyprolose, polyacrylic resin E100.
3, the preparation method of trimebutine maleate table as claimed in claim 1 or 2 is characterized in that described plasticizer, is selected from Polyethylene Glycol, propylene glycol, glycerol or Oleum Ricini that mean molecule quantity is 3000-6000; Described diluent is selected from crystallite or powdery cellulose, mannitol, starch, more specifically, lactose, special Lactose hydrate, the weight ratio that diluent accounts for tablet is 20-40%; Binding agent is selected from microcrystalline Cellulose, gelatin, methylcellulose, pregelatinized Starch, polyvidone, hypromellose, preferred especially low viscous hypromellose, and the weight ratio of binder constitutes tablet is 2.5-25%; Acidulant is selected from the pharmacology and goes up acceptable organic acid, is selected from lactic acid or tartaric acid, tartaric acid preferably, and the weight ratio that accounts for tablet is 0.5-2%; Flowable is selected from the silicon dioxide of anhydrous or hydration, and the weight ratio that accounts for tablet is 0.7-2.5%; Lubricant is selected from Metallic stearates, preferred calcium stearate or magnesium, and magnesium stearate concentration preferably accounts for the weight 0.5-1.5% of tablet, more preferably accounts for the weight 1% of tablet; Disintegrating agent is selected from low-substituted hydroxypropyl fiber system, cross-linked carboxymethyl fiber is sodium, polyvidone, carboxymethyl starch sodium, crospovidone and their mixture, is preferably cross-linking sodium carboxymethyl cellulose, accounts for the weight 1-15% of tablet, is preferably 5-10%.
4, a kind of trimebutine maleate table is characterized in that the feed particles 40%-70% that comprises that the Trimebutine Maleate raw material obtains as coating material with water-soluble film forming agent and plasticizer; Other adjuvants 30%-60%.
5, trimebutine maleate table as claimed in claim 4 is characterized in that described adjuvant comprises the diluent of 20-40%, the binding agent of 2.5-25%, the acidulant of 0.5-2%, the disintegrating agent of 1-15%, the lubricant of 0.5-1.5% and the flowable of 0.7-2.5%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02148576 CN1289077C (en) | 2002-12-19 | 2002-12-19 | Trimebutine maleate tablet and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02148576 CN1289077C (en) | 2002-12-19 | 2002-12-19 | Trimebutine maleate tablet and preparing method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1507861A true CN1507861A (en) | 2004-06-30 |
| CN1289077C CN1289077C (en) | 2006-12-13 |
Family
ID=34233211
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02148576 Expired - Lifetime CN1289077C (en) | 2002-12-19 | 2002-12-19 | Trimebutine maleate tablet and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1289077C (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100393311C (en) * | 2006-01-26 | 2008-06-11 | 孙伟丰 | Trimebutine maleate dispersion tablet |
| CN1927185B (en) * | 2006-10-19 | 2010-05-19 | 开开援生制药股份有限公司 | Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof |
| CN108078936A (en) * | 2018-01-03 | 2018-05-29 | 浙江昂利康制药股份有限公司 | Trimebutine maleate dispersion tablet and preparation method thereof |
| CN113171353A (en) * | 2021-04-25 | 2021-07-27 | 海南普利制药股份有限公司 | Trimebutine maleate tablet |
-
2002
- 2002-12-19 CN CN 02148576 patent/CN1289077C/en not_active Expired - Lifetime
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100393311C (en) * | 2006-01-26 | 2008-06-11 | 孙伟丰 | Trimebutine maleate dispersion tablet |
| CN1927185B (en) * | 2006-10-19 | 2010-05-19 | 开开援生制药股份有限公司 | Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof |
| CN108078936A (en) * | 2018-01-03 | 2018-05-29 | 浙江昂利康制药股份有限公司 | Trimebutine maleate dispersion tablet and preparation method thereof |
| CN113171353A (en) * | 2021-04-25 | 2021-07-27 | 海南普利制药股份有限公司 | Trimebutine maleate tablet |
| CN113171353B (en) * | 2021-04-25 | 2022-10-21 | 海南普利制药股份有限公司 | Trimebutine maleate tablet |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1289077C (en) | 2006-12-13 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2424001C (en) | Oral preparations with favorable disintegration characteristics | |
| EP1557179B2 (en) | Analgesic dosage forms that are unable to be inhaled or injected | |
| US20060093668A1 (en) | Melt granulated composition and modified release dosage form prepared from said composition | |
| EP2554169B1 (en) | Pharmaceutical preparation comprising phenylalanine derivative | |
| EP2674149B1 (en) | Method of preparing composite granule comprising low-substituted hydroxypropyl cellulose and rapid release preparation | |
| US11413295B2 (en) | Oral preparation of obeticholic acid | |
| RU2669351C1 (en) | Film coated tablet containing choline alfoscerate and process for preparing same | |
| US20110136883A1 (en) | Granulation of active pharmaceutical ingredients | |
| WO2009102172A2 (en) | Pharmaceutical formulation containing choline alfoscerate | |
| KR20130030261A (en) | Manufacturing of active-free granules and tablets comprising the same | |
| JP2014224079A (en) | Granules for tableting and method for producing the same, orally disintegrating tablet using the granules for tableting | |
| SK7162001A3 (en) | Compositions comprising cefuroxime axetil | |
| JPH0587488B2 (en) | ||
| EP2804588B1 (en) | Method for producing cinacalcet compositions for direct tableting | |
| JP4280074B2 (en) | Multiple unit type sustained release tablets | |
| CN1289077C (en) | Trimebutine maleate tablet and preparing method thereof | |
| AU2005215221B9 (en) | Compression-coated tablets and manufacture thereof | |
| JP2019524683A (en) | Oral pharmaceutical formulation comprising tamsulosin hydrochloride-containing sustained release pellets with improved content uniformity | |
| JP4370050B2 (en) | Clarithromycin tablets and method for producing the same | |
| EP2153822A1 (en) | Granulation of active pharmaceutical ingredients | |
| KR20120060983A (en) | Sustained release dosage form and manufacturing procedure of Sarpogrelate HCl | |
| AU2019254487B2 (en) | Sustained release pyridostigmine compositions | |
| JPH10182448A (en) | Production of composition for compressed preparation | |
| EP4279075A1 (en) | A pharmaceutical composition comprising elagolix | |
| JP2011126857A (en) | Paroxetine hydrochloride-containing tablet for oral use |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C56 | Change in the name or address of the patentee |
Owner name: HAINAN PLOY PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME: HAINAN PULIN PHARMACEUTICAL CO., LTD. |
|
| CP01 | Change in the name or title of a patent holder |
Address after: Hangzhou City, Zhejiang province 310009 Qingchun Road No. 11 Triumphal Arch commercial center 18 floor, room D C Patentee after: HAINAN POLY PHARM. Co.,Ltd. Patentee after: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Address before: Hangzhou City, Zhejiang province 310009 Qingchun Road No. 11 Triumphal Arch commercial center 18 floor, room D C Patentee before: Hainan Poly Pharm Co.,Ltd. Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. |
|
| CX01 | Expiry of patent term |
Granted publication date: 20061213 |
|
| CX01 | Expiry of patent term |