CN104523648A - Pantoprazole sodium enteric micro-pellet capsules and preparation method thereof - Google Patents
Pantoprazole sodium enteric micro-pellet capsules and preparation method thereof Download PDFInfo
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- CN104523648A CN104523648A CN201410798039.2A CN201410798039A CN104523648A CN 104523648 A CN104523648 A CN 104523648A CN 201410798039 A CN201410798039 A CN 201410798039A CN 104523648 A CN104523648 A CN 104523648A
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Abstract
The invention discloses pantoprazole sodium enteric micro-pellet capsules and a preparation method thereof. The micro-pellet capsules comprise a main medicine layer, a first isolation layer, a second isolation layer, an enteric layer, a pigment layer and a capsule layer from inside to outside. The micro-pellet capsules comprise the first and second isolation layers to ensure that an environment pH value of pantoprazole sodium can be slowly transited to a slightly acidic environment of the enteric layer, and under the protection of the enteric layer and two isolation layers, pantoprazole sodium and an enteric layer material with acidity can still exist stably under the condition of being placed for a long time, so that the stability of products can be ensured. Meanwhile, the preparation method disclosed by the invention is simple to operate, high in production efficiency, low in equipment investment and low in product cost.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of pantoprazole sodium enteric-pellets capsules and preparation method thereof.
Background technology
Pantoprazole Sodium is proton pump inhibitor, H+ on the secreted microtubule that parietal cell top film can be suppressed specifically to form and intracytoplasmic tubular foam, K+-ATP enzyme, cause the suppression of this enzyme irreversibility, thus the secretion of gastric acid inhibitory effectively, can not only Noncompetition inhibition gastrin, histamine, the gastric acid secretion that choline causes, and can suppress not by the part basis gastric acid secretion that choline or H2 receptor blocking agent affect, effectively can reduce gastric acid secretion, be used for the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis and Zollinger-Eillison syndrome, especially for ulcer, companion is hemorrhage, vomiting maybe can not be taken food and intractable ulcer and acute pancreatitis etc.Pantoprazole Sodium Enteric-Coated Capsules is the common drug of the digestive system disease such as treatment gastric ulcer, has been widely used in clinical.
The problem such as prescription and the preparation method existence and stability coefficient of variation that is poor, stripping of existing Pantoprazole Sodium Enteric-Coated Capsules is large, thus limit the application of Pantoprazole Sodium Enteric-Coated Capsules.
Summary of the invention
The object of the present invention is to provide a kind of pantoprazole sodium enteric-pellets capsules and preparation method thereof, be intended to the problem solving existing pantoprazole sodium enteric-pellets capsules poor stability, thus improve safety and the bioavailability of product.
For achieving the above object, the present invention adopts following technical scheme:
A kind of pantoprazole sodium enteric-pellets capsules, described pellet capsule comprises main medicament layer, the first sealing coat, the second sealing coat, enteric layer and capsule layer from inside to outside;
Described main medicament layer comprises the component of following weight portion:
| Celphere | 35-37 part |
| Pantoprazole Sodium | 5.5-6 part |
| Hydroxypropyl methylcellulose | 1.5-2 part |
| Sodium carbonate | 0.3-0.5 part |
| Sodium lauryl sulphate | 0.3-0.4 part |
| Tween 80 | 0.6-0.8 part |
| Purified water | 40-60 part |
Described first sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.5-4.5 part |
| Pulvis Talci | 0.15-0.25 part |
| Sodium carbonate | 0.025-0.035 part |
| Titanium dioxide | 0.65-0.75 part |
| Purified water | 30-50 part |
Described second sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.5-4.5 part |
| Pulvis Talci | 0.15-0.25 part |
| Titanium dioxide | 0.65-0.75 part |
| Purified water | 30-50 part |
Described enteric layer comprises the component of following weight portion:
| Triethyl citrate | 1-1.2 part |
| Pulvis Talci | 5.5-6 part |
| Polyacrylic resin | 35-42 part |
| Purified water | 80-100 part |
Further, described main medicament layer comprises the component of following weight portion:
| Celphere | 35.89 parts |
| Pantoprazole Sodium | 5.82 part |
| Hydroxypropyl methylcellulose | 1.75 part |
| Sodium carbonate | 0.40 part |
| Sodium lauryl sulphate | 0.35 part |
| Tween 80 | 0.70 part |
| Purified water | 50 parts |
Described first sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.90 part |
| Pulvis Talci | 0.20 part |
| Sodium carbonate | 0.03 part |
| Titanium dioxide | 0.70 part |
| Purified water | 40 parts |
Described second sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.90 part |
| Pulvis Talci | 0.20 part |
| Titanium dioxide | 0.70 part |
| Purified water | 40 parts |
Described enteric layer comprises the component of following weight portion:
| Triethyl citrate | 1.16 part |
| Pulvis Talci | 5.79 part |
| Polyacrylic resin | 38.39 parts |
| Purified water | 90 parts |
Also comprise uvea between described enteric layer and capsule layer, described uvea comprises the Opadry of 0.2-0.3 part weight portion, and described uvea is the aesthetics in order to increase medicine, and further, described uvea comprises the Opadry of 0.24 part of weight portion.
Another object of the present invention is to the preparation method that a kind of pantoprazole sodium enteric-pellets capsules is provided, comprise the following steps:
By the weight ratio of each component, take each component;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 50-70 part purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining purified water, after stirring, in colloid mill, grinds 30-40min, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 25-35min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) by above-mentioned Microcapsule filling in capsule shells, obtain pantoprazole sodium enteric-pellets capsules.
Further, described step 4) and step 5) between also comprise: wrap up uvea: ratio by weight, takes Opadry, Opadry added in purified water, after stirring, obtain uvea coating solution;
Step 4) obtained micropill, by weight, get 30-35% and be placed in coating of pellets machine, coating is carried out with uvea coating solution, obtain wrapping up uveal micropill, to wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
The present invention adopts above technical scheme, Pantoprazole Sodium pellet capsule is obtained owing to having wrapped up two-layer sealing coat containing pill core, because Pantoprazole Sodium is stable in summary alkaline environment, slightly then easily degrade in sour environment, and enteric layer is for slightly acid, the pellet capsule of this method comprises first, second sealing coat, make the environment pH of Pantoprazole Sodium can transit to the summary sour environment of enteric layer slowly, under the protection of two-layer sealing coat, Pantoprazole Sodium with there is the existence that acid enteric layer material still can be stable when placing for a long time, ensure that the stability of product.Usual enteric-coated pellet capsule can discharge the pastille micropill of parcel enteric layer uniformly after in stomach entering; Pantoprazole Sodium is alkalescence; owing to there being the protection of enteric layer and two-layer sealing coat; medicine still can ensure at stomach stable existence; after entering intestinal; dissolve under suitable pH condition and discharge medicine, playing drug effect.Meanwhile, preparation method of the present invention is simple to operate, and production efficiency is high, and equipment investment is low, and product cost is low.
Detailed description of the invention
A kind of pantoprazole sodium enteric-pellets capsules, described pellet capsule comprises main medicament layer, the first sealing coat, the second sealing coat, enteric layer and capsule layer from inside to outside;
Described main medicament layer comprises the component of following weight portion:
| Celphere | 35-37 part |
| Pantoprazole Sodium | 5.5-6 part |
| Hydroxypropyl methylcellulose | 1.5-2 part |
| Sodium carbonate | 0.3-0.5 part |
| Sodium lauryl sulphate | 0.3-0.4 part |
| Tween 80 | 0.6-0.8 part |
| Purified water | 40-60 part |
Described first sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.5-4.5 part |
| Pulvis Talci | 0.15-0.25 part |
| Sodium carbonate | 0.025-0.035 part |
| Titanium dioxide | 0.65-0.75 part |
| Purified water | 30-50 part |
Described second sealing coat comprises the component of following weight portion:
| Hydroxypropyl methylcellulose | 3.5-4.5 part |
| Pulvis Talci | 0.15-0.25 part |
| Titanium dioxide | 0.65-0.75 part |
| Purified water | 30-50 part |
Described enteric layer comprises the component of following weight portion:
| Triethyl citrate | 1-1.2 part |
| Pulvis Talci | 5.5-6 part |
| Polyacrylic resin | 35-42 part |
| Purified water | 80-100 part |
Further, also comprise uvea between described enteric layer and capsule layer, described uvea comprises the Opadry of 0.2-0.3 part weight portion.
The preparation method of described pantoprazole sodium enteric-pellets capsules, comprises the following steps:
By the weight ratio of each layer component, take each component;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 50-70 part purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining purified water, after stirring, in colloid mill, grinds 30-40min, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 25-35min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) uvea is wrapped up:
Ratio by weight, takes Opadry, is added by Opadry in appropriate purified water, after stirring, obtains uvea coating solution;
Step 4) obtained micropill, by weight, get 30-35% and be placed in coating of pellets machine, carry out coating with uvea coating solution, obtain wrapping up uveal micropill;
6) will wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
Described uvea is the aesthetics in order to increase medicine, also can not wrap up uvea.
Embodiment 1
A kind of preparation of pantoprazole sodium enteric-pellets capsules:
By weight, following each component is taken:
Main medicament layer:
| Celphere | 35.89 parts |
| Pantoprazole Sodium | 5.82 part |
| Hydroxypropyl methylcellulose | 1.75 part |
| Sodium carbonate | 0.40 part |
| Sodium lauryl sulphate | 0.35 part |
| Tween 80 | 0.70 part |
| Purified water | 50 parts |
First sealing coat:
| Hydroxypropyl methylcellulose | 3.90 part |
| Pulvis Talci | 0.20 part |
| Sodium carbonate | 0.03 part |
| Titanium dioxide | 0.70 part |
| Purified water | 40 parts |
Second sealing coat:
| Hydroxypropyl methylcellulose | 3.90 part |
| Pulvis Talci | 0.20 part |
| Titanium dioxide | 0.70 part |
| Purified water | 40 parts |
Enteric layer:
| Triethyl citrate | 1.16 part |
| Pulvis Talci | 5.79 part |
| Polyacrylic resin | 38.39 parts |
| Purified water | 90 parts |
Uvea: Opadry (pink) 0.24 part;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 35min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 35min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 60 parts of purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining 30 parts of purified water, in colloid mill, grind 35min after stirring, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 30min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) uvea is wrapped up:
Opadry is added in appropriate purified water, after stirring, obtain uvea coating solution;
Step 4) obtained micropill, by weight, get 30% and be placed in coating of pellets machine, carry out coating with uvea coating solution, obtain wrapping up uveal micropill;
6) will wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
Embodiment 2
A kind of preparation of pantoprazole sodium enteric-pellets capsules:
By weight, following each component is taken:
Main medicament layer:
| Celphere | 35 parts |
| Pantoprazole Sodium | 5.5 part |
| Hydroxypropyl methylcellulose | 2 parts |
| Sodium carbonate | 0.3 part |
| Sodium lauryl sulphate | 0.4 part |
| Tween 80 | 0.6 part |
| Purified water | 40 parts |
First sealing coat:
| Hydroxypropyl methylcellulose | 3.5 part |
| Pulvis Talci | 0.25 part |
| Sodium carbonate | 0.025 part |
| Titanium dioxide | 0.75 part |
| Purified water | 30 parts |
Second sealing coat:
| Hydroxypropyl methylcellulose | 4.5 part |
| Pulvis Talci | 0.25 part |
| Titanium dioxide | 0.75 part |
| Purified water | 30 parts |
Enteric layer:
| Triethyl citrate | 1 part |
| Pulvis Talci | 5.5 part |
| Polyacrylic resin | 35 parts |
| Purified water | 80 parts |
Uvea: Opadry (pink) 0.2 part;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 30min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 30min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 50 parts of purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining 30 parts of purified water, in colloid mill, grind 30min after stirring, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 25min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) uvea is wrapped up:
Opadry is added in appropriate purified water, after stirring, obtain uvea coating solution;
Step 4) obtained micropill, by weight, get 35% and be placed in coating of pellets machine, carry out coating with uvea coating solution, obtain wrapping up uveal micropill;
6) will wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
Embodiment 3
A kind of preparation of pantoprazole sodium enteric-pellets capsules:
By weight, following each component is taken:
Main medicament layer:
| Celphere | 37 parts |
| Pantoprazole Sodium | 6 parts |
| Hydroxypropyl methylcellulose | 1.5 part |
| Sodium carbonate | 0.5 part |
| Sodium lauryl sulphate | 0.3 part |
| Tween 80 | 0.8 part |
| Purified water | 60 parts |
First sealing coat:
| Hydroxypropyl methylcellulose | 4.5 part |
| Pulvis Talci | 0.15 part |
| Sodium carbonate | 0.035 part |
| Titanium dioxide | 0.65 part |
| Purified water | 50 parts |
Second sealing coat:
| Hydroxypropyl methylcellulose | 3.5 part |
| Pulvis Talci | 0.15 part |
| Titanium dioxide | 0.65 part |
| Purified water | 50 parts |
Enteric layer:
| Triethyl citrate | 1.2 part |
| Pulvis Talci | 6 parts |
| Polyacrylic resin | 42 parts |
| Purified water | 100 parts |
Uvea: Opadry (pink) 0.3 part;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 40min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 40min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 65 parts of purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining 35 parts of purified water, in colloid mill, grind 40min after stirring, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 35min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) uvea is wrapped up:
Opadry is added in appropriate purified water, after stirring, obtain uvea coating solution;
Step 4) obtained micropill, by weight, get 30% and be placed in coating of pellets machine, carry out coating with uvea coating solution, obtain wrapping up uveal micropill;
6) will wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
Embodiment 4
A kind of preparation of pantoprazole sodium enteric-pellets capsules:
By weight, following each component is taken:
Main medicament layer:
| Celphere | 36 parts |
| Pantoprazole Sodium | 5.75 part |
| Hydroxypropyl methylcellulose | 1.75 part |
| Sodium carbonate | 0.4 part |
| Sodium lauryl sulphate | 0.35 part |
| Tween 80 | 0.7 part |
| Purified water | 50 parts |
First sealing coat:
| Hydroxypropyl methylcellulose | 4 parts |
| Pulvis Talci | 0.2 part |
| Sodium carbonate | 0.03 part |
| Titanium dioxide | 0.7 part |
| Purified water | 40 parts |
Second sealing coat:
| Hydroxypropyl methylcellulose | 4 parts |
| Pulvis Talci | 0.2 part |
| Titanium dioxide | 0.7 part |
| Purified water | 40 parts |
Enteric layer:
| Triethyl citrate | 1.1 part |
| Pulvis Talci | 5.5 part |
| Polyacrylic resin | 38 parts |
| Purified water | 90 parts |
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 30min, obtain the first sealing coat Coating Solution;
By step 1) the obtained micropill containing main medicament layer is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 30min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 60 parts of purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining 30 parts of purified water, in colloid mill, grind 30min after stirring, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 25min, cross 80 mesh sieves, obtain enteric layer coating solution;
By step 3) obtained product is placed in coating of pellets machine, and carry out coating with enteric layer coating solution, obtain enteric coated mini-pill of pantoprazole sodium;
5) by above-mentioned Microcapsule filling in capsule shells, obtain pantoprazole sodium enteric-pellets capsules.
Contrast test:
Comparative example
Adopt the recipe quantity identical with embodiment 2 and preparation method to prepare pantoprazole sodium enteric-pellets capsules, described comparative example only has the first sealing coat.
By the pantoprazole sodium enteric-pellets capsules of comparative example and the embodiment of the present invention 1, embodiment 2, embodiment 3, carry out three months study on the stability under similarity condition, detect the changes of contents of its content (i.e. pantoprazole sodium content) and related substance (i.e. impurity).
Test method is as follows:
1 method of inspection: (Chinese Pharmacopoeia Commission .YBH35942005)
2 content detection are according to high performance liquid chromatography (Chinese Pharmacopoeia version in 2010 two annex IE).
Chromatographic condition and system suitability experiment octadecylsilane chemically bonded silica are filler; Be mobile phase with phosphate buffer (get sodium hydrogen phosphate 1.12g, sodium dihydrogen phosphate 0.18g, be dissolved in water and be diluted to 1000ml)-acetonitrile (70:50), determined wavelength is 292nm.Number of theoretical plate calculates should be not less than 1000 by Pantoprazole Sodium peak.
2.1 content (i.e. pantoprazole sodium content) mensuration gets the content under content uniformity item, porphyrize, precision takes in right amount (being about equivalent to pantoprazole 20mg), put in 100ml measuring bottle, add mobile phase dissolved dilution to scale, shake up, microporous filter membrane filters, get subsequent filtrate, as need testing solution; Separately get Pantoprazole Sodium reference substance (by anhydride calculating) appropriate, accurately weighed, add mobile phase dissolving and quantitatively dilute and make every 1ml about containing the solution of 0.2mg, product solution in contrast.Precision measures need testing solution and each 20 μ l of reference substance solution respectively, injection liquid chromatography, and record chromatogram, by external standard method with calculated by peak area, result is multiplied by 0.9458, to obtain final product.Limit should be the 90.0%--110.0% of labelled amount.
The content that the mensuration precision of 2.2 related substances (i.e. impurity) takes under content uniformity item is appropriate, and add mobile phase and dissolve and to make in every 1ml about containing by the solution dissolving holder and draw 0.2mg, filtration, gets subsequent filtrate as need testing solution; Precision measures in right amount, add mobile phase and make the solution about containing pantoprazole 3 μ g in every 1ml, product solution in contrast, according to the chromatographic condition under assay item, precision measures contrast solution 20 μ l injection liquid chromatography, regulate detection sensitivity, make the peak height of main constituent chromatographic peak be about 10% of monitor full scale; Precision measures need testing solution and each 20 μ l of reference substance solution again, injection liquid chromatography, and record chromatogram is to 2 times of main constituent peak retention time.As aobvious impurity peaks in the chromatogram of need testing solution, measure each impurity peak area sum, must not be greater than the main peak area (1.5%) of contrast solution, limit should be labelled amount≤1.5%.
3 experimental results
Get respectively 0 month and the comparative example of 3 months and each 3 of the sample of embodiment, detect by above method, testing result is as follows:
Table 1
Table 2
Table 3
4 analyze
From table 1, table 2, table 3, the pantoprazole sodium enteric-pellets capsules of prepared by prior art only have one deck sealing coat, Pantoprazole Sodium poor stability, degradation speed is fast, its related substance (impurity) the content rate of climb very fast (after 3 months, content rises 119.21%); And the pantoprazole sodium enteric-pellets capsules with two-layer sealing coat prepared by the present invention, Pantoprazole Sodium stability is high, after three months, pantoprazole sodium content maintains a metastable level, related substance (impurity) content increasing degree little (after three months, its related substances of embodiment 1,2,3 adds 29.17%, 7.56%, 12.95% respectively).
As can be seen here; pantoprazole sodium enteric-pellets capsules of the present invention comprises first, second sealing coat; make the environment pH of Pantoprazole Sodium can transit to the summary sour environment of enteric layer slowly; under the protection of enteric layer and two-layer sealing coat; Pantoprazole Sodium with there is the existence that acid enteric layer material still can be stable when placing for a long time, ensure that the stability of product.
Claims (5)
1. a pantoprazole sodium enteric-pellets capsules, is characterized in that: described pellet capsule comprises main medicament layer, the first sealing coat, the second sealing coat, enteric layer and capsule layer from inside to outside;
Described main medicament layer comprises the component of following weight portion:
Celphere 35-37 part;
Pantoprazole Sodium 5.5-6 part;
Hydroxypropyl methylcellulose 1.5-2 part;
Sodium carbonate 0.3-0.5 part;
Sodium lauryl sulphate 0.3-0.4 part;
Tween 80 0.6-0.8 part;
Purified water 40-60 part;
Described first sealing coat comprises the component of following weight portion:
Hydroxypropyl methylcellulose 3.5-4.5 part;
Pulvis Talci 0.15-0.25 part;
Sodium carbonate 0.025-0.035 part;
Titanium dioxide 0.65-0.75 part;
Purified water 30-50 part;
Described second sealing coat comprises the component of following weight portion:
Hydroxypropyl methylcellulose 3.5-4.5 part;
Pulvis Talci 0.15-0.25 part;
Titanium dioxide 0.65-0.75 part;
Purified water 30-50 part;
Described enteric layer comprises the component of following weight portion:
Triethyl citrate 1-1.2 part;
Pulvis Talci 5.5-6 part;
Polyacrylic resin 35-42 part;
Purified water 80-100 part.
2. a kind of pantoprazole sodium enteric-pellets capsules according to claim 1, is characterized in that:
Described main medicament layer comprises the component of following weight portion:
Celphere 35.89 parts;
Pantoprazole Sodium 5.82 parts;
Hydroxypropyl methylcellulose 1.75 parts;
Sodium carbonate 0.40 part;
Sodium lauryl sulphate 0.35 part;
Tween 80 0.70 part;
Purified water 50 parts;
Described first sealing coat comprises the component of following weight portion:
Hydroxypropyl methylcellulose 3.90 parts;
Pulvis Talci 0.20 part;
Sodium carbonate 0.03 part;
Titanium dioxide 0.70 part;
Purified water 40 parts;
Described second sealing coat comprises the component of following weight portion:
Hydroxypropyl methylcellulose 3.90 parts;
Pulvis Talci 0.20 part;
Titanium dioxide 0.70 part;
Purified water 40 parts;
Described enteric layer comprises the component of following weight portion:
Triethyl citrate 1.16 parts;
Pulvis Talci 5.79 parts;
Polyacrylic resin 38.39 parts;
Purified water 90 parts.
3. a kind of pantoprazole sodium enteric-pellets capsules according to claim 1, it is characterized in that: also comprise uvea between described enteric layer and capsule layer, described uvea comprises the Opadry of 0.2-0.3 part weight portion.
4. the preparation method of a kind of pantoprazole sodium enteric-pellets capsules as described in one of claims 1 to 3, is characterized in that: it comprises the following steps:
By the weight ratio of each component, take each component;
1) preparation of main medicament layer:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add sodium carbonate, Pantoprazole Sodium, sodium lauryl sulphate, tween 80 successively, after stirring, obtain main medicament layer coating solution;
Celphere is placed in coating of pellets machine, carries out coating with main medicament layer coating solution, obtain the micropill containing main medicament layer;
2) the first sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, sodium carbonate, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the first sealing coat Coating Solution;
The micropill containing main medicament layer step 1) obtained is placed in coating of pellets machine, carries out coating with the first sealing coat coating solution;
3) the second sealing coat is wrapped up:
Under agitation, hydroxypropyl methylcellulose is added in purified water, after dissolving completely, add Pulvis Talci, titanium dioxide successively, after stirring, in colloid mill, grind 30-40min, obtain the second sealing coat Coating Solution;
By step 2) obtained product is placed in coating of pellets machine, carries out coating with the second sealing coat coating solution;
4) enteric layer is wrapped up:
Polyacrylic resin is added 50-70 part purification dilution with water, then add triethyl citrate, stir, obtain solution A;
Pulvis Talci is added in remaining purified water, after stirring, in colloid mill, grinds 30-40min, obtain solution B;
Under agitation, solution B is added in solution A, after slowly stirring 25-35min, cross 80 mesh sieves, obtain enteric layer coating solution;
The product that step 3) is obtained is placed in coating of pellets machine, carries out coating, obtain enteric coated mini-pill of pantoprazole sodium with enteric layer coating solution;
5) by above-mentioned Microcapsule filling in capsule shells, obtain pantoprazole sodium enteric-pellets capsules.
5. the preparation method of a kind of pantoprazole sodium enteric-pellets capsules according to claim 4, is characterized in that: also comprise between described step 4) and step 5): wrap up uvea:
Ratio by weight, takes Opadry, is added by Opadry in purified water, after stirring, obtains uvea coating solution;
The micropill that step 4) is obtained, by weight, get 30-35% and be placed in coating of pellets machine, coating is carried out with uvea coating solution, obtain wrapping up uveal micropill, to wrap up uveal micropill and remainder does not wrap up after uveal micropill mixes, and is filled in capsule shells, obtains pantoprazole sodium enteric-pellets capsules.
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Application publication date: 20150422 |