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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- Prior art keywords
- lansoprazole
- nanocapsule
- oral cavity
- disintegration tablet
- cavity disintegration
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- 229960003174 lansoprazole Drugs 0.000 title claims abstract description 47
- MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 title claims abstract 20
- 238000002360 preparation method Methods 0.000 title abstract description 6
- 239000002088 nanocapsule Substances 0.000 claims abstract description 27
- 210000000214 mouth Anatomy 0.000 claims abstract description 26
- 239000002775 capsule Substances 0.000 claims abstract description 13
- 239000002245 particle Substances 0.000 claims abstract description 5
- 208000019505 Deglutition disease Diseases 0.000 claims abstract description 4
- 239000004576 sand Substances 0.000 claims abstract description 4
- 210000000936 intestine Anatomy 0.000 claims description 28
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- 238000003756 stirring Methods 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 10
- 239000000463 material Substances 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 8
- 239000000243 solution Substances 0.000 claims description 8
- 208000025865 Ulcer Diseases 0.000 claims description 7
- 239000002671 adjuvant Substances 0.000 claims description 7
- 231100000397 ulcer Toxicity 0.000 claims description 7
- 239000004925 Acrylic resin Substances 0.000 claims description 6
- 229920000178 Acrylic resin Polymers 0.000 claims description 6
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 6
- 239000003921 oil Substances 0.000 claims description 6
- 235000019198 oils Nutrition 0.000 claims description 6
- 229960000502 poloxamer Drugs 0.000 claims description 6
- 229920001983 poloxamer Polymers 0.000 claims description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 5
- 230000008569 process Effects 0.000 claims description 5
- 108010011485 Aspartame Proteins 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 4
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 4
- 239000000605 aspartame Substances 0.000 claims description 4
- 229960003438 aspartame Drugs 0.000 claims description 4
- 235000010357 aspartame Nutrition 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 235000015165 citric acid Nutrition 0.000 claims description 4
- 238000001035 drying Methods 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- 239000012528 membrane Substances 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 239000002244 precipitate Substances 0.000 claims description 4
- 210000000582 semen Anatomy 0.000 claims description 4
- 235000012424 soybean oil Nutrition 0.000 claims description 4
- 239000003549 soybean oil Substances 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 235000015112 vegetable and seed oil Nutrition 0.000 claims description 4
- 239000008158 vegetable oil Substances 0.000 claims description 4
- 206010025482 malaise Diseases 0.000 claims description 3
- 230000003340 mental effect Effects 0.000 claims description 3
- 235000010603 pastilles Nutrition 0.000 claims description 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 2
- 229930091371 Fructose Natural products 0.000 claims description 2
- 239000005715 Fructose Substances 0.000 claims description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 2
- 206010070840 Gastrointestinal tract irritation Diseases 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 235000021355 Stearic acid Nutrition 0.000 claims description 2
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- 229930006000 Sucrose Natural products 0.000 claims description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 2
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 2
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 2
- 239000001630 malic acid Substances 0.000 claims description 2
- 235000011090 malic acid Nutrition 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 2
- 239000002994 raw material Substances 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 239000011734 sodium Substances 0.000 claims description 2
- 229910052708 sodium Inorganic materials 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000008117 stearic acid Substances 0.000 claims description 2
- 229940013618 stevioside Drugs 0.000 claims description 2
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 2
- 235000019202 steviosides Nutrition 0.000 claims description 2
- 239000005720 sucrose Substances 0.000 claims description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000008469 Peptic Ulcer Diseases 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 208000011906 peptic ulcer disease Diseases 0.000 abstract description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 2
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- SIXIIKVOZAGHPV-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=C[CH]C2=N1 SIXIIKVOZAGHPV-UHFFFAOYSA-N 0.000 description 27
- 239000003826 tablet Substances 0.000 description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 229940079593 drug Drugs 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
- 208000007107 Stomach Ulcer Diseases 0.000 description 3
- 201000008629 Zollinger-Ellison syndrome Diseases 0.000 description 3
- 230000002378 acidificating effect Effects 0.000 description 3
- 208000000718 duodenal ulcer Diseases 0.000 description 3
- 201000005917 gastric ulcer Diseases 0.000 description 3
- 201000000052 gastrinoma Diseases 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 210000001198 duodenum Anatomy 0.000 description 2
- 239000002662 enteric coated tablet Substances 0.000 description 2
- 210000004211 gastric acid Anatomy 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 description 2
- SBQLYHNEIUGQKH-UHFFFAOYSA-N omeprazole Chemical compound N1=C2[CH]C(OC)=CC=C2N=C1S(=O)CC1=NC=C(C)C(OC)=C1C SBQLYHNEIUGQKH-UHFFFAOYSA-N 0.000 description 2
- 229960000381 omeprazole Drugs 0.000 description 2
- 239000006191 orally-disintegrating tablet Substances 0.000 description 2
- 208000000689 peptic esophagitis Diseases 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
- 229940121819 ATPase inhibitor Drugs 0.000 description 1
- 208000033469 Gastrooesophageal heterotopia Diseases 0.000 description 1
- 241000167880 Hirundinidae Species 0.000 description 1
- 208000010728 Meckel diverticulum Diseases 0.000 description 1
- 102100021904 Potassium-transporting ATPase alpha chain 1 Human genes 0.000 description 1
- 108010083204 Proton Pumps Proteins 0.000 description 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 1
- 206010066969 Vitello-intestinal duct remnant Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000000362 adenosine triphosphatase inhibitor Substances 0.000 description 1
- 230000003872 anastomosis Effects 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 230000002183 duodenal effect Effects 0.000 description 1
- 210000003238 esophagus Anatomy 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 210000001156 gastric mucosa Anatomy 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 210000001630 jejunum Anatomy 0.000 description 1
- 229940057948 magnesium stearate Drugs 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 210000002954 meckel diverticulum Anatomy 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 210000001711 oxyntic cell Anatomy 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229940126409 proton pump inhibitor Drugs 0.000 description 1
- 239000000612 proton pump inhibitor Substances 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000003248 secreting effect Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000004206 stomach function Effects 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
- 125000003652 trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
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| 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 |
| 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 |
| 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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| US9925148B2 (en) | 2010-10-26 | 2018-03-27 | Capsugel Belgium Nv | Bulk enteric capsule shells |
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| 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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