CN107625736A - A kind of esomeprazole enteric capsules piece and preparation method thereof - Google Patents
A kind of esomeprazole enteric capsules piece and preparation method thereof Download PDFInfo
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- CN107625736A CN107625736A CN201710647904.7A CN201710647904A CN107625736A CN 107625736 A CN107625736 A CN 107625736A CN 201710647904 A CN201710647904 A CN 201710647904A CN 107625736 A CN107625736 A CN 107625736A
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Abstract
The present invention relates to a kind of preparation method of esomeprazole enteric capsules piece, step includes the preparation of esomeprazole enteric capsules and the preparation of micropill and excipient mixed pressuring plate；Esomeprazole enteric capsules, include pharmaceutical activity capsule core, separation layer and enteric coating layer, esomeprazole enteric capsules made from the inventive method have certain elastic, pressure-resistant, it is tabletted with together with excipient, micropill can be made to completely cut off air, more more stable than micro pill capsule, the term of validity was up to more than 3 years, and have the advantages that small volume, dosage can be split, increase patient compliance.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of preparation method of esomeprazole enteric capsules piece.
Background technology
Esomeprazole magnesium is used for GORD：The treatment of erosive reflux esophagitis, the oesophagus cured
Scorching patient prevents the long term maintenance therapy of recurrence, the symptom control of GORD；It is additionally operable to and the treatment of appropriate antibacterial
Method drug combination eradicates helicobacter pylori, and the duodenal ulcer related to helicobacter pylorus infection of healing, for preventing and
The related recurrent peptic ulcer of helicobacter pylori.
Esomeprazole magnesium less stable, easily degraded.Its stability is also influenceed by light, humidity, heat, organic solvent.
Therefore the weakness of raw material in itself is overcome by formulation and technology technology, prepares the U.S. drawing magnesium of Esso that stability is good, bioavilability is high
Azoles preparation seems most important.Therefore what is clinically used is esomeprazole magnesium enteric coated preparations.
CN102100671A discloses a kind of preparation method of esomeprazole enteric capsules, including esomeprazole magnesium activity
Preparation, spacer layer coating and the enteric layer coating of capsule core, wherein doing strength hydrophilic lubricant using sodium stearyl fumarate.
CN201510509446.1 provides a kind of esomeprazole enteric capsules and preparation method thereof, prepared by esomeprazole magnesium
Into enteric-coated micro-pill, wherein enteric-coated micro-pill is added alkaline stabiliser and resisted in drug-loaded layer by adding alkaline material in blank capsule core
Oxidant；The conditioning agent that alkalescence is higher and alkalescence is relatively low is separately added into two layers of separation layer；Enteric coated and film-coating is sprayed again,
Micropill finally is packed into gastric-dissolved capsule to be prepared.But it is still not very good in terms of stability, while this traditional side
Method, enteric-coated micro-pill is simply fitted into capsule, capsule volume is larger, and patient's poor compliance, particularly gerontal patient are being swallowed
In, capsule shells become sticky and are easily attached in oesophagus.In addition, capsule has an inseparability, dosage is single.
The content of the invention
In order to overcome above-mentioned prior art deficiency, there is provided a kind of brand-new of more stable esomeprazole enteric capsules piece
Agent, facilitate patient medication, the invention provides the preparation method of esomeprazole enteric capsules piece, in pharmaceutical activity capsule core
Meglumine composition is added, increases medicine stability, enteric-coated micro-pill and excipient are mixed tabletting, it is empty to have completely cut off enteric-coated micro-pill contact
Gas, medicine long-time stability are added, tablet is easily swallowed than capsule small volume, adds the compliance of the medication of patient
Property.
Esomeprazole enteric capsules piece prepared in accordance with the present invention, in 40 ± 2 DEG C, the constant temperature of relative humidity 75% ± 5%
Accelerate to investigate 6 months and deposit 3 years under conditions of 25 ± 2 DEG C, relative humidity 75% ± 5%, esomeprazole in constant humidity cabinet
The appearance character of magnesium enteric-coated micro-pill piece, had no significant change compared with 0 month about material, release and content, infer press accordingly
It can make the preparation term of validity up to more than 3 years according to the esomeprazole enteric capsules piece of the present invention.
Esomeprazole enteric capsules piece of the present invention, components by weight percentage are as follows：
Enteric-coated micro-pill：
A, pharmaceutical activity capsule core
B, separation layer
Coating agent 5-10%
Titanium dioxide 0.5-1.5%
Talcum powder 3-10%
C, enteric coating layer
Enteric material 20-30%
Talcum powder 5-10%
Plasticizer 1-5%
Piece：
Enteric-coated micro-pill 50-70%
Excipient 30-50%
The esomeprazole enteric capsules piece of the present invention, accounts for 50-70% by enteric-coated micro-pill and excipient 30-50% forms pressure
Piece forms.
The present invention esomeprazole enteric capsules in, active medicine capsule core, by esomeprazole magnesium, disintegrant, filler,
Adhesive, alkaline compositions, surfactant, talcum powder composition, it is micro- that esomeprazole magnesium raw material granularity is preferably less than 120
Rice, disintegrant may be selected from low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch and Ac-Di-Sol, crosslinked polyethylene
One or more combination in pyrrolidones；Adhesive is syrup, hydroxypropyl methyl cellulose, sodium carboxymethylcellulose, poly- second
One or more of combinations in alkene pyrrolidone；Meglumine and combinations thereof be meglumine or meglumine with disodium hydrogen phosphate,
One or more combination in sodium acid carbonate, sodium carbonate, sodium dihydrogen phosphate；Surfactant is Tween-80, dodecyl sulphate
One or both of sodium, poloxamer combine；Filler is one or both of Icing Sugar, dextrin, microcrystalline cellulose, starch
Combination.Enteric material is aqueous acrylic resin dispersion, cellulose acetate phthalate, hydroxypropyl methylcellulose phthalic acid
One or more of combinations in ester；The wherein preferred L30D-55 of acrylic resin；Plasticizer is triethyl citrate, adjacent benzene two
One or more of combinations in formic acid diethylester, Macrogol 6000, preferably triethyl citrate.
A kind of preparation method of esomeprazole enteric capsules piece provided by the invention, the piece are micro- by esomeprazole magnesium enteric
Ball and excipient composition, enteric-coated micro-pill can use centrifugal coating granulator, extrusion spheronization machine, fluidized bed coating granulator, height
Seed-coating machine is imitated to prepare.Specific preparation method is as described below：
(1) preparation of pharmaceutical activity capsule core：Using centrifugal coating granulator, extrusion spheronization machine prepare, by esomeprazole magnesium,
After disintegrant, filler, alkali compounds, surfactant, talcum powder are pulverized and mixed uniformly, medicine capsule core is made；
(2) spacer layer coating：Prepared, will be coated using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine
Agent, oxidant, titanium dioxide, talcum powder are made into suspension with purified water, then spray and be wrapped in active capsule core；
(3) enteric-coating layer：Prepared using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine, by enteric
Material, talcum powder and plasticizer are made into enteric coating liquid, and spray is wrapped on the pill of bag separation layer；
(4) tabletting：Enteric-coated micro-pill is well mixed with excipient, by specification dosage stator weight, tabletting produces enteric-coated micro-pill piece.
Esomeprazole enteric capsules piece prepared in accordance with the present invention, with the hydrochloric acid solution of sodium chloride (take sodium chloride 1g,
Adding hydrochloric acid 3.5ml, add water to 500ml) 500ml is dissolution medium, 100 turns of rotating speed, through 2 hours, this pellet tablet outward appearance is not found
On significant change, measure acid-resistant strength up to more than 95%；According to 2015 editions drug release determination methods of Chinese Pharmacopoeia, slurry processes, 100 turns, survey
45 minutes releases are obtained up to more than 90%.
Embodiment
Embodiment 1
Enteric-coated micro-pill formula of the present invention is made up of following component：(1000 are made altogether)
A, pharmaceutical activity capsule core
B, separation layer
C, enteric coating layer
D, enteric-coated micro-pill tabletting
Preparation method：
(1) preparation of pharmaceutical activity capsule core：Using centrifugal coating granulator, extrusion spheronization machine prepare, by esomeprazole magnesium,
After disintegrant, filler, meglumine, surfactant, talcum powder are pulverized and mixed uniformly, medicine capsule core is made；
(2) spacer layer coating：Prepared, will be coated using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine
Agent, oxidant, titanium dioxide, talcum powder are made into suspension with purified water, then spray and be wrapped in active capsule core；
(3) enteric-coating layer：Prepared using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine, by enteric
Material, talcum powder and plasticizer are made into enteric coating liquid, and spray is wrapped on the pill of bag separation layer；
(4) tabletting：Enteric-coated micro-pill is well mixed with excipient, by specification dosage stator weight, tabletting produces enteric-coated micro-pill piece.
Comparing embodiment 1
Above-mentioned enteric-coated micro-pill is loaded into capsule according to specification 20mg, produces esomeprazole magnesium capsulae enterosolubilis.
Estimation of stability：
First, accelerated test
To above-described embodiment esomeprazole enteric capsules piece, and comparing embodiment esomeprazole magnesium capsulae enterosolubilis, difference
It is placed in the glassware of opening；Placed ten days under the conditions of illumination (4500 ± 500Lx), 40 DEG C, RH92%, investigate 0 day, 10
Index, its stability result such as it micropill color, impurity, content are as follows：
As a result show：After the embodiment prepared by the present invention is placed ten days under illumination, high temperature, high humidity, micropill color
Unchanged, impurity increases without obvious, and less than 1%, acid-resistant strength is more than more than 96%, and after identical enteric-coated micro-pill filling capsule
Comparing embodiment, be positioned over illumination, high temperature, high humility after ten days, micropill color has significant change, and impurity is significantly increased,
More than 1%, some is even greater than 4%, and acid-resistant strength is decreased obviously, and some is less than 80%.
2nd, the long-term experiment that keeps sample
Listing packaging, and above-mentioned comparing embodiment esomeprazole are simulated to above-described embodiment esomeprazole enteric capsules piece
Magnesium capsulae enterosolubilis simulation listing packaging, is placed under room temperature condition and places the room 3 years of keeping sample, investigate micropill color, impurity, content etc. and refer to
Mark, its stability result are as follows：
As a result show：Embodiment " esomeprazole enteric capsules piece " is prepared according to the present invention, is put for a long time at ambient temperature
After putting 3 years, micropill color is unchanged, and impurity is without significant change, and less than 1%, acid-resistant strength is still greater than 95%.And by the present invention's
The comparing embodiment " esomeprazole magnesium capsulae enterosolubilis " that enteric-coated micro-pill is fitted into capsule, it is long-term at ambient temperature to place 3 years
Afterwards, micropill color is changed, and impurity is significantly increased, and more than 2%, acid-resistant strength substantially reduces, and some is less than 85%
Conclusion：The esomeprazole enteric capsules prepared using the technology of the present invention, the direct tablet compressing after the mixing of excessively excipient,
Manufactured " esomeprazole enteric capsules piece " its stability is than " the esomeprazole enteric capsules glue after loading capsule
Capsule " is higher by a lot, after placing 3 years, meets medicinal standard requirement, it is contemplated that its term of validity was up to more than 3 years.In addition, " Esso is beautiful to be drawn
Azoles magnesium enteric-coated micro-pill piece " has swallows smooth, Er Qiechang than capsule small volume, particularly patient's poor compliance, gerontal patient
Molten micropill tablet has per tablet amounts severability, realizes a variety of dosages.
Claims (9)
- A kind of 1. esomeprazole enteric capsules piece, it is characterised in that：Mixed by esomeprazole enteric capsules and excipient Combined pressure piece forms, and components by weight percentage is as follows：Enteric-coated micro-pill：A, pharmaceutical activity capsule coreB, separation layerCoating agent 5-10%Titanium dioxide 0.5-1.5%Talcum powder 3-10%C, enteric coating layerEnteric material 20-30%Talcum powder 5-10%Plasticizer 1-5%Piece：Enteric-coated micro-pill 50~70%Excipient 30~50%.
- 2. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that specifically preparation method is：(1) preparation of pharmaceutical activity capsule core：Using centrifugal coating granulator, extrusion spheronization machine prepare, by esomeprazole magnesium, After disintegrant, filler, meglumine and combinations thereof, surfactant, talcum powder are pulverized and mixed uniformly, medicine capsule core is made；(2) spacer layer coating：Prepared, will be coated using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine Agent, oxidant, titanium dioxide, talcum powder are made into suspension with purified water, then spray and be wrapped in active capsule core；(3) enteric-coating layer：Prepared using centrifugal coating granulator, fluidized bed coating granulator, high-efficiency coating machine, by enteric Material, talcum powder and plasticizer are made into enteric coating liquid, and spray is wrapped on the pill of bag separation layer；(4) tabletting：Enteric-coated micro-pill is well mixed with excipient, by specification dosage stator weight, tabletting produces enteric-coated micro-pill piece.
- 3. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that by the intestines of 50-70% mass parts The excipient tabletting of molten micropill and 30-50% mass parts forms, and excipient is starch, pregelatinized starch, microcrystalline cellulose, crosslinking One or more of combinations in sodium carboxymethylcellulose, lactose.
- 4. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that enteric layer have certain elasticity, Compressive property.
- 5. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that disintegrant is low substituted hydroxy-propyl One or more combination in cellulose, sodium carboxymethyl starch and Ac-Di-Sol, PVPP； Adhesive is one or more of groups in syrup, hydroxypropyl methyl cellulose, sodium carboxymethylcellulose, polyvinylpyrrolidone Close；Meglumine and combinations thereof is in meglumine or meglumine and disodium hydrogen phosphate, sodium acid carbonate, sodium carbonate, sodium dihydrogen phosphate One or more combination；Surfactant is one or both of Tween-80, lauryl sodium sulfate, poloxamer group Close；Filler is the combination of one or both of Icing Sugar, dextrin, microcrystalline cellulose, starch.
- 6. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that spacer layer coating is hydroxypropyl first Base cellulose.
- 7. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that enteric material is acrylic resin One or more of combinations in aqueous dispersion, cellulose acetate phthalate, hypromellose phthalate；Increase Modeling agent is one or more of combinations in triethyl citrate, diethyl phthalate, Macrogol 6000.
- 8. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that enteric material is Utech system Row.
- 9. esomeprazole enteric capsules piece as claimed in claim 1, it is characterised in that enteric material is Utech L30D-55。
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710647904.7A CN107625736A (en) | 2017-08-01 | 2017-08-01 | A kind of esomeprazole enteric capsules piece and preparation method thereof |
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| CN201710647904.7A CN107625736A (en) | 2017-08-01 | 2017-08-01 | A kind of esomeprazole enteric capsules piece and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1935139A (en) * | 2006-09-30 | 2007-03-28 | 邢为藩 | Substituted benzimidazole proton pump inhibitor composition, and its preparing method |
| CN102805735A (en) * | 2011-06-21 | 2012-12-05 | 寿光富康制药有限公司 | Esomeprazole enteric pellet tablets and preparation method thereof |
-
2017
- 2017-08-01 CN CN201710647904.7A patent/CN107625736A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1935139A (en) * | 2006-09-30 | 2007-03-28 | 邢为藩 | Substituted benzimidazole proton pump inhibitor composition, and its preparing method |
| CN102805735A (en) * | 2011-06-21 | 2012-12-05 | 寿光富康制药有限公司 | Esomeprazole enteric pellet tablets and preparation method thereof |
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