CN102805737A - Lansoprazole enteric oral disintegrating tablet and preparation method thereof - Google Patents
Lansoprazole enteric oral disintegrating tablet and preparation method thereof Download PDFInfo
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- CN102805737A CN102805737A CN2012103188418A CN201210318841A CN102805737A CN 102805737 A CN102805737 A CN 102805737A CN 2012103188418 A CN2012103188418 A CN 2012103188418A CN 201210318841 A CN201210318841 A CN 201210318841A CN 102805737 A CN102805737 A CN 102805737A
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- lansoprazole
- nanocapsule
- oral cavity
- disintegration tablet
- cavity disintegration
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Abstract
The invention relates to a nanometer lansoprazole enteric oral disintegrating tablet and a preparation method thereof. The lansoprazole enteric oral disintegrating tablet contains about 10-90 percent by weight of a nanocapsule. The lansoprazole enteric oral disintegrating tablet provided by the invention is not required to be taken with water, and can be used for quickly disintegrating an enteric nanocapsule in an oral cavity; the particle diameter of the nanocapsule is less than 1,000 nanometers, and does not cause sand feel in mouth; and compared with an ordinary enteric tablet or enteric capsule, the nanometer lansoprazole enteric oral disintegrating tablet has the characteristics of good treatment effect, high repeatability, high adaptability and the like, is suitable for patients suffering from mental diseases or dysphagia caused by peptic ulcer, and contributes to bringing greater flexibility to clinical administration.
Description
Technical field
The present invention relates to a kind of oral solid formulation that is used to treat gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome, the oral area ulcer of coincideing, particularly relating to the lansoprazole is the nanorize enteric-coated orally disintegrating tablets preparation of active component.
Background technology
Peptic ulcer mainly refers to betide the duodenal chronic ulcer of harmonization of the stomach, is a frequently-occurring disease, commonly encountered diseases.Ulcer be formed with various factors, wherein acidic gastric juice is the Fundamentals of ulcer to the Digestion of mucosa.Any position of acidic gastric juice contact is like distal esophagus, gastrointestinal anastomosis postoperative anastomotic stoma, jejunum and Meckel diverticulum with ectopic gastric mucosa.Most ulcer betide the duodenum stomach function regulating, therefore claim stomach, duodenal ulcer again.
Lansoprazole is the H by Japan's military field drug company listing exploitation in 1992
+/ K
+-atpase inhibitor is the benzimidazole substituent of exploitation after omeprazole, is proton pump inhibitor.After its mechanism of action is drug absorption, transfer to the sour secretory duct of gastric mucosa parietal cell, under acid condition, change the active body structure into, this kind active matter and proton pump (H
+, K
+-ATP enzyme) SH base combines, thereby suppresses the activity of this enzyme, so the secretion of ability gastric acid inhibitory is mainly used in treatment gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome (Zollinger-Ellison syndrome), the oral area ulcer of coincideing.
Lansoprazole chemistry (+)-2 [[[3-methyl-4-(2,2, the 2-trifluoro ethoxy)-2-pyridine radicals] methyl] sulfinyl] by name benzimidazole, because it introduces fluorine atom at 4 side chains of pyridine ring, substituent group is a trifluoro ethoxy, lipotropy is stronger, can act on H
+/ K
+Three positions of-ATP enzyme, bioavailability improves 30 times than omeprazole.
Lansoprazole, its character is brownish white crystalline powder, is soluble in dimethyl formamide, dissolves in methanol, is insoluble in ethanol, ether, and is water-soluble hardly.It is unstable under acidic condition, and degraded easily in gastric acid environment need be processed enteric coated preparation and absorbed at small intestinal and duodenum.Common enteric coatel tablets can prevent the degraded of medicine, but disintegrate is slower, and bioavailability is lower, are unfavorable for the misery of timely reduction of patient; Part patient swallows and has any problem.The enteric coated orally disintegrating tablet that the present invention relates to; After taking medicine, need not use water delivery service, can in the oral cavity, rapid disintegrate go out the enteric nanocapsule; Compare with common enteric coatel tablets or enteric coated capsule; Have characteristics such as treatment favorable reproducibility, patient compliance height,, be applicable to the gastric ulcer patient who suffers from mental sickness or dysphagia for clinical application brings greater flexibility.
Summary of the invention
In order to solve the deficiency of prior art, the present invention provides a kind of Lansoprazole intestine oral cavity disintegration tablet and preparation method thereof.
The present invention realizes through following technology: a kind of Lansoprazole intestine oral cavity disintegration tablet, it is processed by Lansoprazole intestine nanocapsule and suitable tabletting adjuvant.
A kind of Lansoprazole intestine oral cavity disintegration tablet that the present invention relates to further comprises enteric nanocapsule and Orally disintegrating layer.
A kind of method for preparing of Lansoprazole intestine oral cavity disintegration tablet comprises the steps:
(1) enteric capsule material, lansoprazole, vegetable oil are dissolved in ethanol, process the capsule material solution of mass concentration 1 ~ 10%, stir 0.5 ~ 2h;
(2) with slowly joining 5 ~ 20 times of volumes under the capsule material solution stirring that makes, contain in the aqueous solution of surfactant 0.1 ~ 1% volumetric concentration, stir 1 ~ 3h, cross microporous filter membrane, standing demix;
(3), make the Lansoprazole intestine nanocapsule with drying precipitate;
(4) nanocapsule is mixed with suitable tabletting adjuvant, tabletting promptly gets Lansoprazole intestine nanocapsule oral cavity disintegration tablet.
Above-mentioned lansoprazole raw material is handled through nanorize.
Above-mentioned Lansoprazole intestine oral cavity disintegration tablet contains the Lansoprazole intestine nanocapsule and is about 10% ~ 90% percentage by weight.
Above-mentioned obtained pastille nanocapsule particle diameter is less than 1000nm, no grains of sand sense behind the Orally disintegrating, and the enteric nanocapsule can protect medicine to avoid the external environment influence, reduces GI irritation, absorbs better.
Like the said enteric capsule of step (1) material is acrylic resin.
Like the said vegetable oil of step (1) is in soybean oil, Oleum Arachidis hypogaeae semen, Semen Maydis oil, the Petiolus Trachycarpi oil one or more.
Like the said surfactant of step (2) is poloxamer.
Described Lansoprazole intestine oral cavity disintegration tablet, its Orally disintegrating layer is made up of with adjuvant suitable tabletting, comprises disintegrating agent, lubricant, correctives.
Above-mentioned disintegrating agent can be selected wherein one or more of low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone, microcrystalline Cellulose for use.
Above-mentioned lubricant is one or more in stearic acid and salt thereof, micropowder silica gel, the Pulvis Talci.
Above-mentioned correctives is one or more in fructose, sucrose, malic acid, citric acid, aspartame, the stevioside.
Technical characterstic of the present invention is: Lansoprazole intestine oral cavity disintegration tablet provided by the present invention can go out nanocapsule at Orally disintegrating, and is easy-to-swallow, and the common enteric coated micropill particle diameter of nanocapsule size ratio is little simultaneously; Particle diameter is less than 1000nm, and no grains of sand sense after the disintegrate in the oral cavity is more conducive to absorb; Reducing medicine stimulates gastrointestinal, improves bioavailability, compares with capsule; Have severability, be easier to clinical flexible Application, be applicable to the patient of mental sickness or dysphagia.
The specific embodiment
With by way of example the present invention is described further again below, provides the present invention and get implementation detail, but be not to be intended to limit protection scope of the present invention.
Embodiment 1:
Lansoprazole 20.0g
Soybean oil 20g
Acrylic resin 30g
Poloxamer 10g
Crospolyvinylpyrrolidone 40g
Magnesium stearate 9g
Citric acid 1.2g
Process 1000.
Acrylic resin 30g is made into capsule material solution with ethanol 270g, adds 20g soybean oil, 20g nanorize lansoprazole, stir 0.5h.The stirring of above-mentioned solution limit is slowly joined 5 times of volumes (1500ml) contain in the aqueous solution of 0.1% (1.5ml) poloxamer, stir 1h, cross microporous filter membrane, standing demix; Drying precipitate makes the Lansoprazole intestine nanocapsule; With nanocapsule and recipe quantity PVPP, magnesium stearate, citric acid mixed pressuring plate, every heavily about 0.12g.
Embodiment 2:
Lansoprazole 20.0g
Petiolus Trachycarpi oil 25g
Acrylic resin 30g
Poloxamer 10g
Microcrystalline Cellulose 30g
Magnesium stearate 9g
Aspartame 1.0g
Process 1000.
Acrylic resin 30g is made into capsule material solution with ethanol 270g, adds 35g Petiolus Trachycarpi oil, 20g nanorize lansoprazole, stir 1h.The stirring of above-mentioned solution limit is slowly joined 10 times of volumes (3000ml) contain in the aqueous solution of 0.5% (15ml) poloxamer, stir 2h, cross microporous filter membrane, standing demix; Drying precipitate makes the Lansoprazole intestine nanocapsule; With nanocapsule and recipe quantity microcrystalline Cellulose, magnesium stearate, aspartame mixed pressuring plate, every heavily about 0.12g.
After preparing, above different prescription friabilities and disintegration time are detected, compare concrete outcome such as following table with common enteric coatel tablets:
| Prescription | Hardness (N) | Disintegration time (s) |
| 1 | 42 | 15 |
| 2 | 40 | 16 |
| Lansoprazole enteric-coated tablet | 75 | 720 |
Lansoprazole enteric-coated tablet drug release determination result:
| Sheet number | Oral cavity disintegration tablet burst size (%) | Pu Tuoping burst size (%) |
| 1 | 99.8 | 99.5 |
| 2 | 101.3 | 97.9 |
| 3 | 101.6 | 100.2 |
| 4 | 100.9 | 99.6 |
| 5 | 100.8 | 98.4 |
| 6 | 99.3 | 99.8 |
| Meansigma methods (%) | 100.6 | 99.2 |
| RSD（%） | 0.88 | 0.89 |
The drug release determination result shows that the release degree of Lansoprazole intestine oral cavity disintegration tablet of the present invention is better than the release degree of commercially available article Pu Tuoping.
Claims (10)
1. a Lansoprazole intestine oral cavity disintegration tablet is characterized in that, it processes oral cavity disintegration tablet by Lansoprazole intestine nanocapsule and suitable tabletting adjuvant, is applicable to the digestive tract ulcer patient who suffers from mental sickness or dysphagia.
2. a kind of Lansoprazole intestine oral cavity disintegration tablet that the present invention relates to further comprises enteric nanocapsule, Orally disintegrating layer.
3. the method for preparing of Lansoprazole intestine oral cavity disintegration tablet as claimed in claim 1 is characterized in that, comprises the steps:
(1) enteric capsule material, lansoprazole, vegetable oil are dissolved in ethanol, process the capsule material solution of mass concentration 1 ~ 10%, stir 0.5 ~ 2h;
(2) with slowly joining 5 ~ 20 times of volumes under the capsule material solution stirring that makes, contain in the aqueous solution of surfactant 0.1 ~ 1% volumetric concentration, stir 1 ~ 3h, cross microporous filter membrane, standing demix;
(3), make the Lansoprazole intestine nanocapsule with drying precipitate;
(4) nanocapsule is mixed with suitable tabletting adjuvant, tabletting promptly gets Lansoprazole intestine nanocapsule oral cavity disintegration tablet.
4. handle through nanorize like the said lansoprazole raw material of claim 3.
5. like the prepared Lansoprazole intestine oral cavity disintegration tablet of claim 3, the pastille nanocapsule is characterised in that, contains the Lansoprazole intestine nanocapsule and is about 10% ~ 90% percentage by weight.
6. like the prepared Lansoprazole intestine oral cavity disintegration tablet of claim 3, it is characterized in that obtained pastille nanocapsule particle diameter is less than 1000nm; No grains of sand sense behind the Orally disintegrating; The enteric nanocapsule can protect medicine to avoid the external environment influence, reduces GI irritation, absorbs better.
7. Lansoprazole intestine oral cavity disintegration tablet as claimed in claim 3, said enteric capsule material is an acrylic resin.
8. Lansoprazole intestine oral cavity disintegration tablet as claimed in claim 3, said vegetable oil are one or more in soybean oil, Oleum Arachidis hypogaeae semen, Semen Maydis oil, the Petiolus Trachycarpi oil.
9. Lansoprazole intestine oral cavity disintegration tablet as claimed in claim 3, said surfactant are poloxamer.
10. Lansoprazole intestine oral cavity disintegration tablet as claimed in claim 2, its Orally disintegrating layer are characterised in that it is made up of with adjuvant suitable tabletting, comprises disintegrating agent, lubricant, correctives, the following adjuvant of concrete optional usefulness:
(1) disintegrating agent as claimed in claim 10 can be selected wherein one or more of low-substituted hydroxypropyl cellulose, carboxymethyl starch sodium, crospolyvinylpyrrolidone, microcrystalline Cellulose for use;
(2) lubricant as claimed in claim 10 is one or more in stearic acid and salt thereof, micropowder silica gel, the Pulvis Talci;
(3) correctives as claimed in claim 10 is one or more in fructose, sucrose, malic acid, citric acid, aspartame, the stevioside.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103188418A CN102805737A (en) | 2012-09-03 | 2012-09-03 | Lansoprazole enteric oral disintegrating tablet and preparation method thereof |
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|---|---|---|---|
| CN2012103188418A CN102805737A (en) | 2012-09-03 | 2012-09-03 | Lansoprazole enteric oral disintegrating tablet and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103169683A (en) * | 2013-03-15 | 2013-06-26 | 丽珠集团丽珠制药厂 | Sodium ilaprazole enteric orally disintegrating tablet and preparation method thereof |
| CN103169684A (en) * | 2013-03-15 | 2013-06-26 | 丽珠集团丽珠制药厂 | Ilaprazole enteric orally disintegrating tablet and preparation method thereof |
| US20160256399A1 (en) * | 2013-11-04 | 2016-09-08 | Capsugel Belgium Nv | Methods and systems for improved bioavailability of active pharmaceutical ingredients including esomeprazole |
| US9925148B2 (en) | 2010-10-26 | 2018-03-27 | Capsugel Belgium Nv | Bulk enteric capsule shells |
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| CN1311669A (en) * | 1998-05-18 | 2001-09-05 | 武田药品工业株式会社 | Orally disintegrable tablet |
| CN1883458A (en) * | 2006-07-11 | 2006-12-27 | 锦州九泰药业有限责任公司 | Enteric coated preparation of lansoprazole sodium and preparation method thereof |
| WO2007078271A2 (en) * | 2005-12-20 | 2007-07-12 | Teva Pharmaceutical Industries Ltd. | Lansoprazole orally disintegrating tablets |
| CN101378753A (en) * | 2005-12-20 | 2009-03-04 | 特瓦制药工业有限公司 | Lansoprazole orally disintegrating tablets |
| CN102342916A (en) * | 2010-08-01 | 2012-02-08 | 海南中化联合制药工业股份有限公司 | Lansoprazole enteric-coated capsule prescription and preparation method thereof |
-
2012
- 2012-09-03 CN CN2012103188418A patent/CN102805737A/en active Pending
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| CN1311669A (en) * | 1998-05-18 | 2001-09-05 | 武田药品工业株式会社 | Orally disintegrable tablet |
| WO2007078271A2 (en) * | 2005-12-20 | 2007-07-12 | Teva Pharmaceutical Industries Ltd. | Lansoprazole orally disintegrating tablets |
| CN101378753A (en) * | 2005-12-20 | 2009-03-04 | 特瓦制药工业有限公司 | Lansoprazole orally disintegrating tablets |
| CN1883458A (en) * | 2006-07-11 | 2006-12-27 | 锦州九泰药业有限责任公司 | Enteric coated preparation of lansoprazole sodium and preparation method thereof |
| CN102342916A (en) * | 2010-08-01 | 2012-02-08 | 海南中化联合制药工业股份有限公司 | Lansoprazole enteric-coated capsule prescription and preparation method thereof |
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|---|
| 来小丹: "氟比洛芬口腔崩解片的研究", 《中国优秀硕士学位论文全文数据库 医药卫生科技辑》, 15 March 2009 (2009-03-15), pages 079 - 28 * |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9925148B2 (en) | 2010-10-26 | 2018-03-27 | Capsugel Belgium Nv | Bulk enteric capsule shells |
| CN103169683A (en) * | 2013-03-15 | 2013-06-26 | 丽珠集团丽珠制药厂 | Sodium ilaprazole enteric orally disintegrating tablet and preparation method thereof |
| CN103169684A (en) * | 2013-03-15 | 2013-06-26 | 丽珠集团丽珠制药厂 | Ilaprazole enteric orally disintegrating tablet and preparation method thereof |
| CN103169684B (en) * | 2013-03-15 | 2014-10-22 | 丽珠集团丽珠制药厂 | Ilaprazole enteric orally disintegrating tablet and preparation method thereof |
| US20160256399A1 (en) * | 2013-11-04 | 2016-09-08 | Capsugel Belgium Nv | Methods and systems for improved bioavailability of active pharmaceutical ingredients including esomeprazole |
| US10813886B2 (en) | 2013-11-04 | 2020-10-27 | Capsugel Belgium Nv | Methods and systems for improved bioavailability of active pharmaceutical ingredients including esomeprazole |
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Application publication date: 20121205 |