CN105326802A - Ebastine dispersible tablet and preparation method thereof - Google Patents
Ebastine dispersible tablet and preparation method thereof Download PDFInfo
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- CN105326802A CN105326802A CN201510549264.7A CN201510549264A CN105326802A CN 105326802 A CN105326802 A CN 105326802A CN 201510549264 A CN201510549264 A CN 201510549264A CN 105326802 A CN105326802 A CN 105326802A
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Abstract
Disclosed are an ebastine dispersible tablet and a preparation method thereof. The ebastine dispersible tablet is prepared by mixing ebastine serving as an active ingredient and pharmaceutical excipients and directly performing powder tableting. The ebastine dispersible tablet is composed of, by weight, 1-20 parts of ebastine, 50-300 parts of filling agent, 10-60 parts of disintegrating agent, 1-10 parts of optional lubricant and 1-10 parts of optional corrective. The preparation method includes following steps: a), taking ebastine for smashing and sieving to obtain fine powder of higher than 100 meshes; b), mixing other components, placing a mixture into a mixer for premixing, smashing and sieving to obtain fine powder of higher than 50 meshes; c), mixing materials of the steps a) and b), placing a mixture into the mixer, and mixing fully; d), weighing the lubricant passing a sieve with more than 50 meshes, and adding the lubricant into the mixer to continue mixing with a material of the step c) to guarantee uniformity; e), directly tabletting obtained ebastine total mixed powder to obtain the ebastine dispersible tablet. The ebastine dispersible tablet has the advantages of stable mass, less proneness to color change, high dissolution rate and good treatment effect.
Description
Technical field
The present invention relates to a kind of antiallergic action medicine tablet and preparation method thereof, particularly relate to a kind of Ebastine dispersible tablet and preparation method thereof.
Background technology
Allergy is a kind of allergic immune reaction, medically be interpreted as body by after antigenic substance sensitization, being again subject to same antigenic substance stimulates the one exception that produces or pathologic immune reaction.According to data report, 10 ~ 20% of world population suffers from anaphylactic disease, and urticaria sickness rate, up to more than 30%, brings great misery to patient, even causes maimed person or death.
Ebastine is the novel allergy preparations developed by Almirall company of Spain, go on the market in Spain first in nineteen ninety, within 1996, go on the market in Japan, continue after respectively in Sweden, Holland, Singapore, Russia, Ukraine, Denmark, listing such as country such as twenties, Finland etc., the Oxypertine class second filial generation belonging to novel non-sedating effect is long-acting, potent, the antihistamine H1 receptor antagonist that quick-acting and selectivity is good, there is H1 receptor antagonism, from pharmacodynamics, pharmacokinetics, toxicological effect, clinical efficacy, dosage, usage, the comprehensive analysis of the aspect such as toleration and clinical comparative study, this product good effect, long half time, clinically there is persistent, the feature of taking convenience.The toleration of ebastine is better than astemizole (breath is thought quick), and the cardiac toxicity produced when the obesity that occurs after astemizole is taken medicine not occurring and uses with other antibiotics.When treating critically ill patient, ebastine (20mg/ days) successful, is better than breath and thinks quick, terfenadine and cetirizine.Clinical research shows: ebastine has good curative effect to treatment urticaria and allergic rhinitis etc., and its side effect is slight, and be the first-selected medicine of clinical practice, clinic is promoted the use of.
But solvellae dissolution is poor hardly in water for ebastine raw material, and bioavailability is lower, and be difficult to abundant absorption in body, curative effect is poor, how effectively improves its dissolution, then improve its bioavailability significant for the development of such medicine.
Current studies in China majority concentrates on ebastine conventional tablet, research for Ebastine dispersible tablet is less, existing patent application comprises: a kind of ebastine solid orally ingestible and preparation method (application number 200710168526.0, Liyi Medicine Science & Tech. Co., Ltd., Hubei), it adopts wet granulation technology to be dissolved in alcoholic solution by ebastine raw material, then after mixing homogeneously with filler, disintegrating agent and other components, pelletizing press sheet obtains; And a kind of Ebastine dispersible tablet of applying for before our company and preparation method thereof (application number 201310051928.8), it adopts hot melt first ebastine raw material and binding agent to be formed hot melt solid-liquid dispersing body, obtain Ebastine dispersible tablet again with after disintegrating agent and filler wet granule compression tablet, its obtained dispersible tablet stripping is fast, dissolution is good, has preferably taste and mouthfeel.
Summary of the invention
The object of the invention is to the deficiency overcoming prior art existence, and provide that a kind of steady quality, dissolution that is not easy to change, tablet are high, good effect, effectively can avoid the impact for product quality in material dissolution or reflow process, Ebastine dispersible tablet that the stability of product and quality thereof can be improved and preparation method thereof.
The object of the invention is to have come by following technical solution, a kind of Ebastine dispersible tablet, it directly adopts pressed powder to make primarily of after active component ebastine and pharmaceutic adjuvant mixing, and described ebastine and the component of pharmaceutic adjuvant and weight are:
Ebastine 1-20 part
Filler 50-300 part
Disintegrating agent 10-60 part
Optional lubricant 1-10 part
Optional correctives 1-10 part;
As preferably: described ebastine and the component of pharmaceutic adjuvant and weight are:
Ebastine 8-12 part
Filler 120-160 part
Disintegrating agent 15-40 part
Optional lubricant 1-3 part
Optional correctives 1-3 part;
As preferably: described filler is any one or more combination in sorbitol, mannitol, Icing Sugar xylitol, sucrose, lactose, maltose alcohol, starch, microcrystalline Cellulose, dextrin, calcium phosphate, calcium hydrogen phosphate, gelatin, amylum pregelatinisatum, calcium sulfate, calcium carbonate;
Described disintegrating agent is any one or more combination in dried starch, sodium carboxymethyl cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethylcellulose calcium, modified starch, microcrystalline Cellulose, ethyl cellulose, hydroxypropyl emthylcellulose, carboxymethyl cellulose;
Described lubricant is one or more combinations in stearic acid, magnesium stearate, calcium stearate, micropowder silica gel, Pulvis Talci, Macrogol 4000, polyethylene glycol 6000, hydrogenated vegetable oil or castor oil hydrogenated.
A preparation method for Ebastine dispersible tablet described above, this preparation method comprises the steps:
A) get ebastine to pulverize and sieve, to obtain the fine powder of more than 100 orders;
B), after other components being mixed, put into mixer premixing, pulverize and sieve, obtain the above fine powder of 50 order;
C) step a) and mixing of materials b) are placed in mixer, fully mix;
D) took 50 orders with the lubricant of top sieve, added in mixer, and continued to mix with the material of step c, to ensure its uniformity;
E) powder is always mixed to the ebastine obtained and carry out direct compression, obtain described Ebastine dispersible tablet.
As preferably: in described step a), ultrafine grinding process is adopted to pulverize and sieve.
Preferred further as one: in described step a), adopt high velocity air comminuting method or ball mill pulverizing method to pulverize and sieve, and after sieving, obtain the micropowder of more than 300 orders.
The present invention is on the basis of prior art research, attempt first adopting the direct mixed pressuring plate legal system of powder for Ebastine dispersible tablet, it is without the need to through material dissolution, soft material processed, granulate and drying and other steps, directly by dry powder sheeting after raw material mixing, the comparatively existing method of its production process is less, action required is simple, avoid the impact for product quality in material dissolution or reflow process, stability and the quality thereof of product are improved, short according to the Ebastine dispersible tablet disintegration time that this method is obtained, dissolution is higher, thus make drug absorption rapid-action, bioavailability obviously increases.
Ebastine tablet steady quality of the present invention, dissolution that is not easy to change, tablet are high, good effect; And owing to adopting direct pressed powder technique, avoid the impact for product quality in material dissolution or reflow process, stability and the quality thereof of product are improved.
Detailed description of the invention
Below in conjunction with embodiment, the invention will be further described.A kind of Ebastine dispersible tablet of the present invention, it directly adopts pressed powder to make primarily of after active component ebastine and pharmaceutic adjuvant mixing, and described ebastine and the component of pharmaceutic adjuvant and weight are:
Ebastine 1-20 part
Filler 50-300 part
Disintegrating agent 10-60 part
Optional lubricant 1-10 part
Optional correctives 1-10 part;
As a kind of preferred version be: described ebastine and the component of pharmaceutic adjuvant and weight are:
Ebastine 8-12 part
Filler 120-160 part
Disintegrating agent 15-40 part
Optional lubricant 1-3 part
Optional correctives 1-3 part;
Filler of the present invention is any one or more combination in sorbitol, mannitol, Icing Sugar xylitol, sucrose, lactose, maltose alcohol, starch, microcrystalline Cellulose, dextrin, calcium phosphate, calcium hydrogen phosphate, gelatin, amylum pregelatinisatum, calcium sulfate, calcium carbonate;
Described disintegrating agent is any one or more combination in dried starch, sodium carboxymethyl cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethylcellulose calcium, modified starch, microcrystalline Cellulose, ethyl cellulose, hydroxypropyl emthylcellulose, carboxymethyl cellulose;
Described lubricant is one or more combinations in stearic acid, magnesium stearate, calcium stearate, micropowder silica gel, Pulvis Talci, Macrogol 4000, polyethylene glycol 6000, hydrogenated vegetable oil or castor oil hydrogenated.
A preparation method for Ebastine dispersible tablet described above, this preparation method comprises the steps:
A) get ebastine to pulverize and sieve, to obtain the fine powder of more than 100 orders;
B), after other components being mixed, put into mixer premixing, pulverize and sieve, obtain the above fine powder of 50 order;
C) step a) and mixing of materials b) are placed in mixer, fully mix;
D) took 50 orders with the lubricant of top sieve, added in mixer, and continued to mix with the material of step c, to ensure its uniformity;
E) powder is always mixed to the ebastine obtained and carry out direct compression, obtain described Ebastine dispersible tablet.
: in described step a) adopt ultrafine grinding process to pulverize and sieve as preferred scheme.
: in described step a) adopt high velocity air comminuting method or ball mill pulverizing method to pulverize and sieve, and after sieving, obtain the micropowder of more than 300 orders as the further preferred version of one.
Adopt the direct mixed pressuring plate legal system of powder for Ebastine dispersible tablet, it is without the need to through material dissolution, soft material processed, granulation and drying and other steps, directly by dry powder sheeting after raw material mixing, the comparatively existing method of its production process is less, action required is simple, avoid the impact for product quality in material dissolution or reflow process, stability and the quality thereof of product are improved.
Embodiment 1: the present invention is by preparing ebastine tablet by following component by following weight proportion:
Ebastine 10 weight portion
Crospolyvinylpyrrolidone (disintegrating agent) 30 weight portion
Microcrystalline Cellulose (filler) 140 weight portion
Stevioside (correctives) 1.5 weight portion
Lubricant (magnesium stearate) 2 weight portion
Described Ebastine dispersible tablet preparation method is as follows:
(1) get ebastine to pulverize through high velocity air, to obtain the micropowder of more than 300 orders;
(2) crospolyvinylpyrrolidone, microcrystalline Cellulose, stevioside are put into CH200 mixer mixing more than 30 minutes by after proportioning mixing, mixture crosses 60 orders with top sieve;
(3) take the component of step (1) and (2) by weight ratio, add CH200 mixer after being mixed and mix more than 20 minutes;
(4) took 60 orders with the magnesium stearate of top sieve, added in mixer, and continued to mix 20 minutes with the material of step (3), to ensure its uniformity;
(5) powder is always mixed to the ebastine of step (4) and carry out direct compression, obtain described Ebastine dispersible tablet;
In above-mentioned preparation process, production cycle or lucifuge production should be shortened, to reduce the time be exposed in light as far as possible; The light-proofness of packaging used must be good, to guarantee the stability of product.
Embodiment 2: plate invention changes the composition weight proportioning in embodiment 1 into following composition weight proportioning, the other the same as in Example 1;
Ebastine 10 weight portion
Carboxymethyl starch sodium (disintegrating agent) 25 weight portion
Lactose (filler) 120 weight portion
Stevioside (correctives) 2 weight portion
Lubricant (magnesium stearate) 2.5 weight portion.
Embodiment 3(comparative example): by following component is prepared ebastine tablet by following weight proportion:
Ebastine 10 weight portion
Crospolyvinylpyrrolidone (disintegrating agent) 20 weight portion
Microcrystalline Cellulose (filler) 140 weight portion
Stevioside (correctives) 1.5 weight portion
Lubricant (magnesium stearate) 2 weight portion
Hydroxypropyl cellulose (binding agent) 5 weight portion
Water (solvent) 100 weight portion
Adopt the wet granulation technology of prior art: take in the water of hydroxypropyl cellulose to 100 weight portion of 5 weight portions, stir to clarify transparence, the ebastine taking 10 weight portions after being heated to 90 DEG C adds wherein makes its hot melt disperse, and jitter time is 20 minutes; Take microcrystalline Cellulose 140 weight portion, add hot melt mixture to granulate, cross 30 order-40 orders to wet granulate, drying 5 hours at 50 DEG C, the magnesium stearate adding the crospolyvinylpyrrolidone of 20 weight portions, the stevioside of 1 weight portion and 2 weight portions after 40 order granulate mixes 20 minutes, and tabletting obtains Ebastine dispersible tablet.
Embodiment 4 (dissolution detection): get each 6 of ebastine tablet sample in embodiment of the present invention 1-3, according to dissolution method (Chinese Pharmacopoeia version in 2000 two annex XC second methods), with hydrochloric acid solution (9--1000) 900ml for solvent, rotating speed is 100 turns per minute, operates in accordance with the law.After 30 minutes, get solution and filter in right amount, getting subsequent filtrate is test liquid.Another precision takes ebastine reference substance and is about 11mg, puts in 20ml measuring bottle, adds appropriate amount of ethanol and dissolves and be diluted to scale, shake up.Precision measures in right amount, and add hydrochloric acid solution (9-1000) and be quantitatively diluted to the solution containing 11ug in every 1ml, shaking up, is contrast solution.According to spectrophotography (Chinese Pharmacopoeia version in 2000 two annex IVA), at 258nm wavelength, place measures trap respectively, calculates the stripping quantity of every sheet, averages.
Dissolution testing result sees the following form:
Claims (6)
1. an Ebastine dispersible tablet, it directly adopts pressed powder to make primarily of after active component ebastine and pharmaceutic adjuvant mixing, it is characterized in that the component of described ebastine and pharmaceutic adjuvant and weight are:
Ebastine 1-20 part
Filler 50-300 part
Disintegrating agent 10-60 part
Optional lubricant 1-10 part
Optional correctives 1-10 part.
2. Ebastine dispersible tablet according to claim 1, is characterized in that the component of described ebastine and pharmaceutic adjuvant and weight are:
Ebastine 8-12 part
Filler 120-160 part
Disintegrating agent 15-40 part
Optional lubricant 1-3 part
Optional correctives 1-3 part.
3. Ebastine dispersible tablet according to claim 1 and 2, is characterized in that described filler is any one or more combination in sorbitol, mannitol, Icing Sugar xylitol, sucrose, lactose, maltose alcohol, starch, microcrystalline Cellulose, dextrin, calcium phosphate, calcium hydrogen phosphate, gelatin, amylum pregelatinisatum, calcium sulfate, calcium carbonate;
Described disintegrating agent is any one or more combination in dried starch, sodium carboxymethyl cellulose, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethylcellulose calcium, modified starch, microcrystalline Cellulose, ethyl cellulose, hydroxypropyl emthylcellulose, carboxymethyl cellulose;
Described lubricant is one or more combinations in stearic acid, magnesium stearate, calcium stearate, micropowder silica gel, Pulvis Talci, Macrogol 4000, polyethylene glycol 6000, hydrogenated vegetable oil or castor oil hydrogenated.
4. the preparation method of Ebastine dispersible tablet according to claim 1 or 2 or 3, is characterized in that this preparation method comprises the steps:
A) get ebastine to pulverize and sieve, to obtain the fine powder of more than 100 orders;
B), after other components being mixed, put into mixer premixing, pulverize and sieve, obtain the above fine powder of 50 order;
C) step a) and mixing of materials b) are placed in mixer, fully mix;
D) took 50 orders with the lubricant of top sieve, added in mixer, and continued to mix with the material of step c, to ensure its uniformity;
E) powder is always mixed to the ebastine obtained and carry out direct compression, obtain described Ebastine dispersible tablet.
5. the preparation method of Ebastine dispersible tablet according to claim 4, is characterized in that:
In described step a), ultrafine grinding process is adopted to pulverize and sieve.
6. the preparation method of Ebastine dispersible tablet according to claim 5, is characterized in that:
In described step a), adopt high velocity air comminuting method or ball mill pulverizing method to pulverize and sieve, and after sieving, obtain the micropowder of more than 300 orders.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510549264.7A CN105326802A (en) | 2015-09-01 | 2015-09-01 | Ebastine dispersible tablet and preparation method thereof |
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| CN201510549264.7A CN105326802A (en) | 2015-09-01 | 2015-09-01 | Ebastine dispersible tablet and preparation method thereof |
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| CN105326802A true CN105326802A (en) | 2016-02-17 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116270472A (en) * | 2023-03-24 | 2023-06-23 | 潍坊医学院 | Ebastine liposome microneedle preparation and preparation method and application thereof |
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| US5460829A (en) * | 1991-12-03 | 1995-10-24 | Rhone-Poulenc Rorer S.A. | Pharmaceutical compositions based on ebastine or analogues thereof |
| CN1868474A (en) * | 2005-05-27 | 2006-11-29 | 杭州澳医保灵药业有限公司 | Ebastine tablet and its prepn. method |
| JP2008120685A (en) * | 2006-10-19 | 2008-05-29 | Yoshindo:Kk | Preparation for oral administration of ebastine and method for producing the same |
| US20090304791A1 (en) * | 2005-11-04 | 2009-12-10 | Simbec Iberica, S.L. | Solid oral forms of ebastine |
| CN102218041A (en) * | 2010-04-15 | 2011-10-19 | 江苏联环药业股份有限公司 | Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same |
| CN103127012A (en) * | 2013-02-17 | 2013-06-05 | 浙江保灵药业有限公司 | Ebastine dispersible tablet and preparation method thereof |
-
2015
- 2015-09-01 CN CN201510549264.7A patent/CN105326802A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5460829A (en) * | 1991-12-03 | 1995-10-24 | Rhone-Poulenc Rorer S.A. | Pharmaceutical compositions based on ebastine or analogues thereof |
| CN1868474A (en) * | 2005-05-27 | 2006-11-29 | 杭州澳医保灵药业有限公司 | Ebastine tablet and its prepn. method |
| US20090304791A1 (en) * | 2005-11-04 | 2009-12-10 | Simbec Iberica, S.L. | Solid oral forms of ebastine |
| JP2008120685A (en) * | 2006-10-19 | 2008-05-29 | Yoshindo:Kk | Preparation for oral administration of ebastine and method for producing the same |
| CN102218041A (en) * | 2010-04-15 | 2011-10-19 | 江苏联环药业股份有限公司 | Ebastine solid dispersion and high-dissolubility ebastine tablet prepared by the same |
| CN103127012A (en) * | 2013-02-17 | 2013-06-05 | 浙江保灵药业有限公司 | Ebastine dispersible tablet and preparation method thereof |
Non-Patent Citations (2)
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| 张汝华，等主编: "《工业药剂学》", 31 July 2001 * |
| 陈优生，等: "依巴斯汀分散片的处方筛选", 《安徽医药》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116270472A (en) * | 2023-03-24 | 2023-06-23 | 潍坊医学院 | Ebastine liposome microneedle preparation and preparation method and application thereof |
| CN116270472B (en) * | 2023-03-24 | 2024-05-31 | 潍坊医学院 | Ebastine liposome microneedle preparation and preparation method and application thereof |
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Application publication date: 20160217 |