CN1742726A - Piperazine ferulate oral cavity disintegrating tablet and preparing method - Google Patents
Piperazine ferulate oral cavity disintegrating tablet and preparing method Download PDFInfo
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- CN1742726A CN1742726A CNA2005101053416A CN200510105341A CN1742726A CN 1742726 A CN1742726 A CN 1742726A CN A2005101053416 A CNA2005101053416 A CN A2005101053416A CN 200510105341 A CN200510105341 A CN 200510105341A CN 1742726 A CN1742726 A CN 1742726A
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- oral cavity
- piperazine ferulate
- sodium
- disintegration tablet
- cavity disintegration
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Abstract
The present invention relates to a ferulic acid piperazine oral disintegrant tablet for curing nephritis, chronic nephritis, nephrotic synhrome and early uremia and auxiliary therapy of coronary heart disease, cerebral infarction and angitis, etc. and its preparation method. It is made up by using ferulic acid piperazine as main raw material and adding a certain auxiliary material through a certain preparation process.
Description
Technical field
The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically piperazine ferulate oral cavity disintegrating tablet and preparation method thereof.
Background technology
The chemical name of piperazine ferulate is 3-methoxyl group-4-Hydroxycinnamic Acid piperazine, and molecular formula is C
4H
10N
2.C
10H
10O
4, structural formula is
Piperazine ferulate has anticoagulant, antiplatelet aggregation, expansion blood capillary, increases coronary flow, vasospasmolytic effect.
Piperazine ferulate oral absorption blood medicine peak time is 29 minutes, and the distribution phase half-life, ((t1/2 β) was 27 minutes, and eliminating the phase half-life ((t1/2)) is 5.5 hours.Piperazine ferulate is distributed more widely in vivo, in liver, kidney blood, distribute more, it is also more to distribute in stomach, small intestinal fat, mainly discharges from urine, feces.Can see through placental barrier.List marketing at present have only ferulic acid croak throat sheet, dosage form is single.The clinical renal glomerular disease that is used for all kinds of with microscopic hematuria and hypercoagulability is as the auxiliary treatment of nephritis, chronic nephritis, nephrotic syndrome early stage uremia and coronary heart disease, cerebral infarction, vasculitis etc.
Oral cavity disintegration tablet is a kind of new pharmaceutical dosage forms, English " Orally disintegrating tables " by name.U.S. FDA has been ratified this dosage form listing, and reason is: make things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment.
Oral cavity disintegration tablet definition: be that a kind of water that do not need in the oral cavity can disintegrate or dissolved tablet.Specification requirement: 1. should be in the oral cavity rapidly disintegrate, no grittiness, good mouthfeel, swallow easily, to the oral mucosa nonirritant.Should stipulate under the character item in the quality standard: disintegrate rapidly, no grittiness, good mouthfeel in the oral cavity; 2. set up suitable disintegration time mensuration method and limit, and be incorporated into standard; 3. to insoluble medicine, should set up suitable dissolution determination method and limit; 4. other should meet general rule requirement under the tablet item.
The characteristics of oral cavity disintegration tablet: 1. absorption is fast, bioavailability is high; 2. instructions of taking does not need water 3. intestinal is residual few, few side effects; 4. avoid the first pass effect of liver sausage.
By retrieval, do not see the relevant patent report and the document of relevant piperazine ferulate oral cavity disintegrating tablet.
Summary of the invention
The purpose of this invention is to provide a kind of disintegrate fast, absorb rapidly, can effectively improve the bioavailability of piperazine ferulate and blood drug level, taking convenience, few side effects, be fit to special population, as the piperazine ferulate oral cavity disintegrating tablet of the patient's medication under old man, child, dysphagia or the special environment and preparation method thereof.
Piperazine ferulate oral cavity disintegrating tablet of the present invention also contains adjuvant except principal agent, by weight percentage, contain piperazine ferulate 5-900%, and the percentage by weight of adjuvant is 10-95%.Adjuvant is any available adjuvant that is fit to make oral cavity disintegration tablet, and they can comprise filler, disintegrating agent, effervescent, correctives, binding agent, lubricant etc.In each oral formulations unit, contain piperazine ferulate 12.5-100mg, preferred dose is 25-75mg.
Because oral cavity disintegration tablet requires disintegrate rapidly in the oral cavity, good mouthfeel, to the oral mucosa nonirritant.Therefore the selection to supplementary product kind and performance thereof is the key of preparation oral cavity disintegration tablet.
The present invention is through selecting, found the pharmaceutic adjuvant of suitable piperazine ferulate oral cavity disintegrating tablet, wherein filler selects to be used for increasing the weight and volume of oral cavity disintegration tablet, so that the molding of preparation and divided dose, filler preferably is selected from one or more the mixture in lactose, microcrystalline Cellulose, sucrose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc. among the present invention.
The kind of disintegrating agent and the selection of consumption are for can this preparation disintegrate be most important fully at the appointed time.Disintegrating agent of the present invention one of is selected to comprise in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium or wherein several mixture.
In oral cavity disintegration tablet, can add an amount of effervescent, help the disintegrate of tablet, and an amount of acid can also be regulated taste.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the effervescent that the present invention selects, or alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.
The correctives that the present invention uses one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, the stevioside or wherein several mixture.
The adding of binding agent and lubricant is for the ease of the preparation of preparation and molding.Binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, the povidone solution.Lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, the Pulvis Talci.
Oral cavity disintegration tablet of the present invention can be by freeze-drying or direct powder compression or granulating tabletting process preparation.
Adopt freeze-drying to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, correctives, piperazine ferulate can be mixed with various adjuvants, add the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization, being shaped to the material lyophilizing gets final product.
Adopt direct powder compression to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, lubricant, correctives, and behind piperazine ferulate and various adjuvant mix homogeneously, direct powder compression gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, binding agent, lubricant, correctives.With piperazine ferulate and partial supplementary material mix homogeneously, add binding agent system soft material, granulate, dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, binding agent, lubricant, correctives, the main method step is: acid source in the effervescent and alkali source can be separated granulation, or acid source mixed with alkali source, employing contains the dehydrated alcohol binding agent granulates, dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting gets final product.
The specific embodiment
Come piperazine ferulate oral cavity disintegrating tablet of the present invention done further specifying by following example, but be not limited in following example.
Embodiment 1
Prescription:
Piperazine ferulate 50g
Polyvinylpolypyrrolidone 60g
Microcrystalline Cellulose 90g
Lactose 25g
Sucrose 25g
Saccharin sodium 2.5g
Flavoring orange essence 2.5g
Make 1000 altogether
Preparation method:
Piperazine ferulate is added suitable quantity of water, after stirring, add polyvinylpolypyrrolidone, microcrystalline Cellulose, lactose, sucrose, saccharin sodium, flavoring orange essence, the limit edged stirs, become suspension after, in perfusion and the suitable mould, lyophilization, press seal, packing.
Embodiment 2
Prescription:
Piperazine ferulate 25g
Xylitol 45g
Microcrystalline Cellulose 40g
Aspartame 1.5g
Crosslinked carboxymethyl fecula sodium 7.0g
Honey peach essence 1.5g
Make 1000 altogether
Preparation method:
Piperazine ferulate is added in the entry, after stirring, add xylitol, microcrystalline Cellulose, aspartame, crosslinked carboxymethyl fecula sodium, honey peach essence, the limit edged stirs, become suspension after, in perfusion and the suitable mould, lyophilization, press seal, packing.
Embodiment 3
Prescription:
Piperazine ferulate 50g
Mannitol 140g
Microcrystalline Cellulose 120g
Lactose 45g
Crospolyvinylpyrrolidone 32g
Sodium bicarbonate 12g
Citric acid 16g
Pulvis Talci 4g
Aspartame 6g
Make 1000 altogether
Preparation method:
Piperazine ferulate, microcrystalline Cellulose, mannitol, lactose, sodium bicarbonate, the citric acid mix homogeneously of 80 mesh sieves will all be crossed, other gets crospolyvinylpyrrolidone, aspartame adopts the equivalent method of progressively increasing to mix with above mixture, add the Pulvis Talci mix homogeneously, direct powder compression gets final product.
Embodiment 4
Prescription:
Piperazine ferulate 50g
Xylitol 160g
Microcrystalline Cellulose 80g
Sucrose 60g
Citric acid 14g
Sodium bicarbonate 18g
Herba Menthae essence 3g
PVP-K30 (dehydrated alcohol) 8g
CMS-Na 4g
Pulvis Talci 3g
Make 1000 altogether
Preparation method:
With all crossing piperazine ferulate, sucrose, microcrystalline Cellulose, citric acid, the sodium bicarbonate mix homogeneously of 80 mesh sieves, with PVP-K30 anhydrous alcohol solution system soft material, to granulate, dry, granulate add CMS-Na, Pulvis Talci, mix homogeneously, tabletting gets final product.
Embodiment 5
Prescription:
Piperazine ferulate 50g
Microcrystalline Cellulose 50g
Xylitol 90g
Sucrose 50g
Starch 70.5g
Stevioside 4.5g
Crosslinked carboxymethyl fecula sodium 10.5g
Flavoring orange essence 3.0g
Polyvinylpolypyrrolidone (50% alcoholic solution) 6.0g
Magnesium stearate 4.5g
Make 1000 altogether
Preparation method:
Piperazine ferulate, xylitol, sucrose, starch, aspartame, flavoring orange essence, the part microcrystalline Cellulose mix homogeneously of 80 mesh sieves will all be crossed, with polyvinylpolypyrrolidone alcohol liquid system soft material, granulate, dry, granulate, the microcrystalline Cellulose, CMS-Na, the magnesium stearate that add surplus, mix homogeneously, tabletting gets final product.
Claims (10)
1 one kinds of piperazine ferulate oral cavity disintegrating tablets contain piperazine ferulate active component and the excipient substance that is fit to make oral cavity disintegration tablet, contain pharmaceutically suitable carrier and the about 100mg piperazine ferulate of about 12.5mg-.
The compositions of 2 claim 1, the content of wherein said piperazine ferulate is about 25-75mg.
The compositions of 3 claim 1 by weight percentage, contains piperazine ferulate 5-90%, and the percentage by weight of adjuvant is 10-95%.The described excipient substance that is fit to make oral cavity disintegration tablet comprises or is selected from filler, disintegrating agent, effervescent, correctives, binding agent or lubricant.
The described oral cavity disintegration tablet of 4 claim 3 is characterized in that described filler is selected from one or more the mixture in microcrystalline Cellulose, sucrose, lactose, mannitol, pregelatinized Starch, sorbitol, the xylitol; Described disintegrating agent is selected from a kind of or wherein several mixture in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium; Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the described effervescent, and alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate; Described binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, the povidone solution; Described lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, the Pulvis Talci; Described correctives one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, the stevioside or wherein several mixture.
5, the described oral cavity disintegration tablet of claim 3 is characterized in that, (1000) composed as follows fill a prescription:
Piperazine ferulate 50g
Polyvinylpolypyrrolidone 60g
Microcrystalline Cellulose 90g
Lactose 25g
Sucrose 25g
Saccharin sodium 2.5g
Flavoring orange essence 2.5g
6, the described oral cavity disintegration tablet of claim 3 is characterized in that, (1000) composed as follows fill a prescription:
Piperazine ferulate 50g
Mannitol 140g
Microcrystalline Cellulose 120g
Lactose 45g
Crospolyvinylpyrrolidone 32g
Sodium bicarbonate 12g
Citric acid 16g
Pulvis Talci 4g
Aspartame 6g
7, the described oral cavity disintegration tablet of claim 3 is characterized in that, (1000) composed as follows fill a prescription:
Piperazine ferulate 50g
Xylitol 160g
Microcrystalline Cellulose 80g
Sucrose 60g
Citric acid 14g
Sodium bicarbonate 18g
Herba Menthae essence 3g
PVP-K30 (dehydrated alcohol) 8g
CMS-Na 4g
Pulvis Talci 3g
8, the described oral cavity disintegration tablet of claim 3 is characterized in that, (1000) composed as follows fill a prescription:
Piperazine ferulate 50g
Microcrystalline Cellulose 50g
Xylitol 90g
Sucrose 50g
Starch 70.5g
Stevioside 4.5g
Crosslinked carboxymethyl fecula sodium 10.5g
Flavoring orange essence 3.0g
Polyvinylpolypyrrolidone (50% alcoholic solution) 6.0g
Magnesium stearate 4.5g
9, the preparation method of the oral cavity disintegration tablet of claim 1, it is characterized in that, adopt the preparation of freeze-drying or direct powder compression or granulating tabletting process, wherein the preparation process of freeze-drying is: piperazine ferulate and filler, disintegrating agent, correctives are added the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization is shaped to the material lyophilizing; Wherein the direct powder compression preparation process is: behind piperazine ferulate and filler, disintegrating agent, effervescent, lubricant, correctives mix homogeneously, and direct powder compression; Wherein the granulating tabletting process preparation process is: with piperazine ferulate and partially filled dose, disintegrating agent, correctives, add binding agent system soft material, granulate, and dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting.
10, the described preparation method of claim 9, it is characterized in that, the step that wherein adds effervescent is, acid source in the effervescent and alkali source are separated granulation, or acid source is mixed with alkali source, adopt to contain the granulation of dehydrated alcohol binding agent, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101053416A CN1742726A (en) | 2005-09-23 | 2005-09-23 | Piperazine ferulate oral cavity disintegrating tablet and preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005101053416A CN1742726A (en) | 2005-09-23 | 2005-09-23 | Piperazine ferulate oral cavity disintegrating tablet and preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1742726A true CN1742726A (en) | 2006-03-08 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005101053416A Pending CN1742726A (en) | 2005-09-23 | 2005-09-23 | Piperazine ferulate oral cavity disintegrating tablet and preparing method |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101879167A (en) * | 2010-05-06 | 2010-11-10 | 四川宝盛康药业有限公司 | Antihypertension drug compound preparation |
| CN109692176A (en) * | 2017-10-23 | 2019-04-30 | 康普药业股份有限公司 | A kind of piperazine ferulate pharmaceutical preparation |
| JP2022551239A (en) * | 2019-09-30 | 2022-12-08 | シャンハイ インスティチュート オブ マテリア メディカ，チャイニーズ アカデミー オブ サイエンシーズ | Drugs and their uses for treating artery-related diseases |
-
2005
- 2005-09-23 CN CNA2005101053416A patent/CN1742726A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101879167A (en) * | 2010-05-06 | 2010-11-10 | 四川宝盛康药业有限公司 | Antihypertension drug compound preparation |
| CN101879167B (en) * | 2010-05-06 | 2012-01-25 | 四川宝盛康药业有限公司 | Antihypertension drug compound preparation |
| CN109692176A (en) * | 2017-10-23 | 2019-04-30 | 康普药业股份有限公司 | A kind of piperazine ferulate pharmaceutical preparation |
| JP2022551239A (en) * | 2019-09-30 | 2022-12-08 | シャンハイ インスティチュート オブ マテリア メディカ，チャイニーズ アカデミー オブ サイエンシーズ | Drugs and their uses for treating artery-related diseases |
| JP7500715B2 (en) | 2019-09-30 | 2024-06-17 | シャンハイ インスティチュート オブ マテリア メディカ，チャイニーズ アカデミー オブ サイエンシーズ | Drugs for treating arterial-related diseases and their uses |
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Open date: 20060308 |