CN106420637A - Ketotifen fumarate tablets and preparation method thereof - Google Patents
Ketotifen fumarate tablets and preparation method thereof Download PDFInfo
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- CN106420637A CN106420637A CN201510481286.4A CN201510481286A CN106420637A CN 106420637 A CN106420637 A CN 106420637A CN 201510481286 A CN201510481286 A CN 201510481286A CN 106420637 A CN106420637 A CN 106420637A
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Abstract
The invention provides ketotifen fumarate tablets. The ketotifen fumarate tablets are prepared by adopting superfine grinding technology and tablet process technology and are high in dissolution rate, lasting in action, few in administration times, stable in blood-drug concentration and higher in safety, and treatment effect of the ketotifen fumarate tablets is brought into full play.
Description
Technical field
The present invention relates to a kind of Determination of Ketotifen Fumarate Tablets and preparation method thereof, belong to field of pharmaceutical preparations.
Background technology
Ketotifen (Ketotifen) is that potent allergy mediator sustained-release agent is administered orally, and commonly uses its fumarate, is antiallergic action class medicine.This medicine can not only suppress the slow reacting substance (SRS-A) of antigen induced lung and bronchial tissue's histamine release of mast cell and allergy, and antigen, serum or calcium ion mediator can also be suppressed to induce eosinophilic granulocyte or the slow reacting substance of neutrophilic granulocyte release histamine and allergy.This medical instrument has stronger H1 receptor antagonism, the slow reacting substance of energy antagonism 5-hydroxy tryptamine and allergy.Studies have found that, this medicine can suppress the non-specific airway high response of Bronchial Asthmas, the bronchospasm that antagonism anaphylactogen, histamine, carbon dioxide, acetylcholine etc. cause.Ketotifen blood medicine valid density is 1.4mg/L, mainly through the excretion of liver, kidney and lung, it is used in conjunction 2～3 weeks and can show clinical effectiveness, therapeutical effect is the strongest within 6～12 weeks, and duration of efficacy is longer, and prolonged application does not produce drug resistance, therapy discontinued also no rebound phenomenon, untoward reaction occur less it is seen that drowsiness, weak, xerostomia, gastrointestinal reaction etc., occasionally have abnormal liver function.Ketotifen all obtains the extensive application of clinic in respiratory system, rhinitis, urticaria and allergic disease, and clinic is applied to allergic rhinitises and allergic bronchial asthma.Research recently also finds, ketotifen can suppress the retting conditions of mastocyte in Severe Acute Pancreatitis SAP (SAP) treatment by stablizing mast cell membrane, reduce the release of Mediators of inflammation and cytokine and play suppression pancreas inflammatory and increase the effect with relief of symptoms.
The Determination of Ketotifen Fumarate Tablets sold in the market be administered orally after from gastrointestinal absorption, but disintegrate is long in this world, and onset is slower, medication several weeks side display effect, most of in liver metabolism.Metabolite and a small amount of raw material are by urinating and feces excretion.Bioavailability is relatively low.Acting duration is longer, only needs within 1st to be administered 2 times.
Content of the invention
In order that tablet fater disintegration, rapid absorption, dissolution rate is accelerated, bioavailability provides, we are improved to the production technology of tablet, prepare Determination of Ketotifen Fumarate Tablets using superfine communication technique and tablet Technology, thus overcoming the shortcoming and defect of existing tablet technology, provide a kind of there is high-dissolution, persistent, medicining times are few, blood drug level is steady, safety is higher Determination of Ketotifen Fumarate Tablets, so that the therapeutical effect of Determination of Ketotifen Fumarate Tablets is given full play to.
For achieving the above object, the technical solution used in the present invention is as follows：
A kind of Determination of Ketotifen Fumarate Tablets and preparation method thereof it is characterised in that：From ketotifen fumarate, calcium hydrogen phosphate, filler, binding agent, lubricant, disintegrating agent, 50% appropriate amount of ethanol.By ketotifen fumarate first individually through micronizing, then carry out with adjuvant mixing, pelletize, be dried, granulate, mixed pressuring plate, the treatment for allergic rhinitises and allergic bronchial asthma is it can also be used to the disease such as multiple allergy dermatitis, eczema.
Include the component of following mass percent using the high-dissolution Determination of Ketotifen Fumarate Tablets of superfine communication technique preparation in the present invention：
Used in the present invention, filler is selected from starch, Pregelatinized Starch, Lactose, dextrin, Microcrystalline Cellulose or its mixture.
Described adhesive be selected from starch, polyvidone, hydroxypropyl cellulose, methylcellulose, sodium carboxymethyl cellulose,Gelatin, arabic gum or its mixture.
Described lubricant is selected from magnesium stearate, Pulvis Talci, polyoxyethylene monostearate, Sodium Acetate Trihydrate, sodium stearyl fumarate, sodium benzoate, enuatrol or its mixture.
Described disintegrating agent is selected from Microcrystalline Cellulose, carboxymethyl starch sodium, hydroxypropyl starch, cross-linking sodium carboxymethyl cellulose, Crospovidone or its mixture.
Specific embodiment
The following example is used for being explained further or understands present disclosure, but can not limit the scope of the present invention.
Embodiment 1：
Determination of Ketotifen Fumarate Tablets prescription and preparation method thereof (in terms of 1000)
| Composition | Quality |
| Ketotifen fumarate | 1.38g |
| Pregelatinized Starch | 22.59g |
| Lactose | 35.60g |
| Calcium hydrogen phosphate | 9.82g |
| Hydroxypropyl methyl cellulose | 2.15g |
| Magnesium stearate | 0.83g |
| Microcrystalline Cellulose | 1.56g |
| 50% ethanol | In right amount |
Weigh by above-mentioned prescription and cross the ketotifen fumarate fine powder of 200 mesh sieves, Pregelatinized Starch, Lactose, calcium hydrogen phosphate, Microcrystalline Cellulose through micronizing, be sufficiently mixed 60 minutes, add hydroxypropyl methyl cellulose, appropriate 50% ethanol soft material, granulation of sieving.Then, by wet granular in 65～75 DEG C of dryings, after gained pellet through sieves granulate is dried, add magnesium stearate, tabletting after mixing 30 minutes, obtain final product.
Embodiment 2：
Determination of Ketotifen Fumarate Tablets prescription and preparation method thereof (in terms of 1000)
| Composition | Quality |
| Ketotifen fumarate | 1.38g |
| Starch | 45.50g |
| Dextrin | 18.98g |
| Calcium hydrogen phosphate | 10.25g |
| Hydroxypropyl methyl cellulose | 2.43g |
| Pulvis Talci | 0.89g |
| Microcrystalline Cellulose | 1.50g |
| 50% ethanol | In right amount |
Weigh by above-mentioned prescription and cross the ketotifen fumarate fine powder of 200 mesh sieves, starch, dextrin, calcium hydrogen phosphate, Microcrystalline Cellulose through micronizing, be sufficiently mixed 60 minutes, add hydroxypropyl methyl cellulose fine powder, appropriate 50% ethanol soft material, granulation of sieving.Then, by wet granular in 65～75 DEG C of dryings, after gained pellet through sieves granulate is dried, add Pulvis Talci, tabletting after mixing 30 minutes, obtain final product.
Embodiment 3：
Determination of Ketotifen Fumarate Tablets prescription and preparation method thereof (in terms of 1000)
| Composition | Quality |
| Ketotifen fumarate | 1.38g |
| Starch | 40.88g |
| Lactose | 18.47g |
| Calcium hydrogen phosphate | 10.65g |
| Hydroxypropyl methyl cellulose | 2.50g |
| Magnesium stearate | 1.00g |
| Carboxymethyl starch sodium | 2.86g |
| 50% ethanol | In right amount |
Weigh by above-mentioned prescription and cross the ketotifen fumarate fine powder of 200 mesh sieves, starch, Lactose, calcium hydrogen phosphate, carboxymethyl starch sodium through micronizing, be sufficiently mixed 60 minutes, add hydroxypropyl methyl cellulose, appropriate 50% ethanol soft material, granulation of sieving.Then, by wet granular in 65～75 DEG C of dryings, after gained pellet through sieves granulate is dried, add magnesium stearate, tabletting after mixing 30 minutes, obtain final product.
Embodiment 4
The Determination of Ketotifen Fumarate Tablets of superfine communication technique preparation is compared with commercially available Determination of Ketotifen Fumarate Tablets dissolution in vitro
According to the dissolution determination method of 2010 editions defineds of Chinese Pharmacopoeia, comparing embodiment 1,2,3 tablet and commercially available Determination of Ketotifen Fumarate Tablets dissolution in vitro.When 40 minutes, dissolution determination result is as follows：
| Sample | Dissolution (%) |
| Embodiment 1 tablet | 92.8% |
| Embodiment 2 tablet | 89.7% |
| Embodiment 3 tablet | 90.4% |
| Commercially available Determination of Ketotifen Fumarate Tablets | 83.6% |
In sum, the Determination of Ketotifen Fumarate Tablets of present invention preparation, significantly improves the dissolution in vitro of Determination of Ketotifen Fumarate Tablets, so as to increase the bioavailability of medicine, so that the therapeutical effect of Determination of Ketotifen Fumarate Tablets is given full play to.
Claims (6)
1. a kind of Determination of Ketotifen Fumarate Tablets and preparation method thereof it is characterised in that：From ketotifen fumarate, calcium hydrogen phosphate, filler, binding agent, lubricant, disintegrating agent, 50% appropriate amount of ethanol.By ketotifen fumarate first individually through micronizing, then carry out with adjuvant mixing, pelletize, be dried, granulate, mixed pressuring plate, the treatment for allergic rhinitises and allergic bronchial asthma is it can also be used to the disease such as multiple allergy dermatitis, eczema.
2. method according to claim 1 it is characterised in that include the component of following mass percent using the high-dissolution Determination of Ketotifen Fumarate Tablets of superfine communication technique preparation：
.
3. method according to claim 1 is it is characterised in that the filler using is selected from starch, Pregelatinized Starch, Lactose, dextrin, Microcrystalline Cellulose or its mixture.
4. method according to claim 1 is it is characterised in that described adhesive is selected from starch, polyvidone, hydroxypropyl cellulose, methylcellulose, sodium carboxymethyl cellulose, gelatin, arabic gum or its mixture.
5. method according to claim 1 is it is characterised in that described lubricant is selected from magnesium stearate, Pulvis Talci, polyoxyethylene monostearate, Sodium Acetate Trihydrate, sodium stearyl fumarate, sodium benzoate, enuatrol or its mixture.
6. method according to claim 1 is it is characterised in that described disintegrating agent is selected from Microcrystalline Cellulose, carboxymethyl starch sodium, hydroxypropyl starch, cross-linking sodium carboxymethyl cellulose, Crospovidone or its mixture.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510481286.4A CN106420637B (en) | 2015-08-04 | 2015-08-04 | A kind of Determination of Ketotifen Fumarate Tablets and preparation method thereof |
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|---|---|---|---|
| CN201510481286.4A CN106420637B (en) | 2015-08-04 | 2015-08-04 | A kind of Determination of Ketotifen Fumarate Tablets and preparation method thereof |
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| CN106420637A true CN106420637A (en) | 2017-02-22 |
| CN106420637B CN106420637B (en) | 2019-11-01 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567756A (en) * | 2018-06-25 | 2018-09-25 | 江苏鹏鹞药业有限公司 | Determination of Ketotifen Fumarate Tablets and preparation method thereof |
| CN110638769A (en) * | 2019-10-25 | 2020-01-03 | 仁和堂药业有限公司 | Production method of ketotifen fumarate tablets |
| CN110664767A (en) * | 2019-10-25 | 2020-01-10 | 仁和堂药业有限公司 | Ketotifen fumarate tablet and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1548044A (en) * | 2003-05-11 | 2004-11-24 | 山东绿因药业有限公司 | Fumaric acid-ketotifen dispersion tablet and its prepn process |
| CN1602868A (en) * | 2004-08-23 | 2005-04-06 | 南昌弘益科技有限公司 | Dripping pills of ketotifen fumarate and its preparation method |
-
2015
- 2015-08-04 CN CN201510481286.4A patent/CN106420637B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1548044A (en) * | 2003-05-11 | 2004-11-24 | 山东绿因药业有限公司 | Fumaric acid-ketotifen dispersion tablet and its prepn process |
| CN1602868A (en) * | 2004-08-23 | 2005-04-06 | 南昌弘益科技有限公司 | Dripping pills of ketotifen fumarate and its preparation method |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567756A (en) * | 2018-06-25 | 2018-09-25 | 江苏鹏鹞药业有限公司 | Determination of Ketotifen Fumarate Tablets and preparation method thereof |
| CN110638769A (en) * | 2019-10-25 | 2020-01-03 | 仁和堂药业有限公司 | Production method of ketotifen fumarate tablets |
| CN110664767A (en) * | 2019-10-25 | 2020-01-10 | 仁和堂药业有限公司 | Ketotifen fumarate tablet and application thereof |
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| Publication number | Publication date |
|---|---|
| CN106420637B (en) | 2019-11-01 |
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