CN105147616A - Medicine namely pantoprazole sodium composition dry suspension for treating gastric ulcer - Google Patents
Medicine namely pantoprazole sodium composition dry suspension for treating gastric ulcer Download PDFInfo
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- CN105147616A CN105147616A CN201510574779.2A CN201510574779A CN105147616A CN 105147616 A CN105147616 A CN 105147616A CN 201510574779 A CN201510574779 A CN 201510574779A CN 105147616 A CN105147616 A CN 105147616A
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- sodium
- pantoprazole
- dry suspension
- pantoprazole sodium
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Abstract
The invention relates to a medicine, namely a pantoprazole sodium composition dry suspension for treating gastric ulcer, and belongs to the field of medical technologies. The composition dry suspension is prepared from pantoprazole sodium, sucrose, dextrin, xanthan gum, sodium dodecyl sulfate, sodium dihydrogen phosphate and sodium cyclamate. The pantoprazole sodium is a new crystal form compound, an X-ray powder diffraction pattern measured by using Cu-K alpha rays is shown by a figure 1, the pantoprazole sodium is different from the pantoprazole sodium reported by the prior art, and experiments find that the compound with a new crystal form structure is good in fluidity and stability, and the dry suspension prepared from the pantoprazole sodium namely the new crystal form compound is simple in composition, so that the occurrence of adverse reactions is greatly reduced, and the dry suspension is good in stability and high in bioavailability.
Description
Technical field
The invention belongs to medical art, relate to a kind of medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer.
Background technology
Pantoprazole Sodium is proton pump inhibitor, by the H with parietal cell
+-K
+two site covalent bond of ATP enzyme system and final step that gastric acid inhibitory produces.This effect be dose dependent and make basis and stimulation state under gastric acid secretion all suppressed.H
+-K
+the combination of ATP enzyme can cause its anti-gastric acid secretion effect lasts more than 24 hours.Pantoprazole Sodium is the proton pump inhibitor of the 3rd listing after omeprazole and lansoprazole.Due to the substituted radical of Pantoprazole Sodium on pyridine ring and benzimidazole ring and omeprazole and lansoprazole different, thus determine its difference at biochemical, pharmacokinetics and pharmacological property, make it have stronger selectivity and specificity.
In prior art, for crystal formation and the hydrate of Pantoprazole Sodium, there is many research:
Patent application 02109182.X relates to anti-peptic ulcer medicine (±) 5-difluoro-methoxy-[[(3; 4-dimethoxy-2-pyridinyl) methyl] sulfinyl] left-handed (-) of-1H-benzimidazole and the salt of dextrorotation (+) enantiomer, i.e. S (-) pantoprazole potassium, sodium, magnesium, calcium, zinc salt R (+) pantoprazole potassium, sodium, magnesium, calcium, zinc salt.Additionally provide a kind of new preparation process of S (-) pantoprazole and R (+) pantoprazole, with chloroform or acetonitrile as solvents, under Sharpless reagent exists, carry out chiral oxidization obtain, be obtained by reacting with potassium hydroxide, potassium carbonate etc.
ZL201110228921.X discloses a kind of compound of pantoprazole sodium, this compound of pantoprazole sodium is crystal, and in the X-ray powder diffraction pattern using the measurement of Cu-K alpha ray to obtain, characteristic peak is 12.5 °, 12.6 °, 13.2 °, 16.2 °, 17.3 ° displays at 2 θ.
ZL201210306449.1 relates to a kind of pantoprazole sodium crystal, adopt X-diffraction powder diffraction, its collection of illustrative plates is followed successively by 9.5 °, 10.4 °, 11.6 °, 13.1 °, 13.8 °, 14.2 °, 15.0 °, 15.3 °, 15.9 °, 16.5 °, 17.5 °, 18.0 ° and 18.2 ° with the characteristic peak that 2 θ angles represent.
ZL201310093503.3 Pantoprazole Sodium crystalline compounds, pharmaceutical composition and preparation method thereof the invention provides a kind of new Pantoprazole Sodium crystalline compounds, its pharmaceutical preparation particularly enteric coated capsule, and their preparation method, the chemical stability of Pantoprazole Sodium crystalline compounds of the present invention is better, dissolubility is more excellent, improve Drug safety, be beneficial to the long term storage of medicine, for clinical drug application provides safety guarantee, but the dissolution of the enteric coated capsule preparation of the mobility of its Pantoprazole Sodium crystalline compounds and preparation thereof, stability is unsatisfactory.
In order to improve the performance of Pantoprazole Sodium further, the present invention develops a kind of Pantoprazole Sodium noval chemical compound, find through test, the compound flow of this novel crystal forms structure, good stability, dry suspension component prepared by this Pantoprazole Sodium crystal compound is simple, greatly reduce the generation of untoward reaction, good stability, bioavailability are high.
Summary of the invention
Goal of the invention of the present invention is to provide a kind of medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer.
In order to complete object of the present invention, the technical scheme of employing is:
The present invention relates to a kind of medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer, described compositions dry suspension is made up of Pantoprazole Sodium, sucrose, dextrin, xanthan gum, sodium lauryl sulphate, sodium dihydrogen phosphate, cyclamate; Described Pantoprazole Sodium is crystal, and the X-ray powder diffraction pattern that the measurement of use Cu-K alpha ray obtains as shown in Figure 1.
As preferably, with parts by weight, described compositions dry suspension is made up of the Pantoprazole Sodium of 0.1-0.6 weight portion, the sucrose of 3-3.4 weight portion, the dextrin of 0.7-0.9 weight portion, the xanthan gum of 0.15-0.25 weight portion, the sodium lauryl sulphate of 0.04-0.06 weight portion, the sodium dihydrogen phosphate of 0.07-0.09 weight portion, 0.005-0.015 cyclamate.
As preferably, with parts by weight, described compositions dry suspension is made up of the Pantoprazole Sodium of 0.4 weight portion, the sucrose of 3.2 weight portions, the dextrin of 0.8 weight portion, the xanthan gum of 0.2 weight portion, the sodium lauryl sulphate of 0.05 weight portion, the sodium dihydrogen phosphate of 0.08 weight portion, 0.01 cyclamate.
As preferably, the preparation method of described compositions dry suspension comprises the following steps:
1) supplementary material process: Pantoprazole Sodium was pulverized 100 mesh sieves with pulverizer;
2) weigh: weigh each supplementary material according to technology preparation amount;
3) always mix: whole supplementary materials of recipe quantity are joined in three-dimensional mixer, mixing velocity 12r/min, open mixer and mix 60 minutes;
4) subpackage: granule is joined subpackage in particles packing machine, controls content uniformity and meets inner quality standard.
The preparation method of the pantoprazole sodium crystal in present composition dry suspension comprises the following steps:
(1) get pantoprazole sodium, add in deionized water, the volumetric usage of deionized water is 5 times of the quality of Pantoprazole Sodium;
(2) be stirred to whole dissolving, regulate pH to 6-9;
(3) add activated carbon decolorizing, filter, obtain settled solution;
(4) settled solution is moved in pressure vessel, the pressure in pressure vessel being controlled at 2.0Mpa and drip isopropyl alcohol, the ether of 2 DEG C under the condition stirred, speed of agitator controls at 35rmp, the volumetric usage of isopropyl alcohol, ether is 3 times of the volume of deionized water, and the volume ratio of isopropyl alcohol, ether is 1:3;
(5) bleed off pressure after dripping, with the speed of 10 DEG C/min, solution is cooled to-5 DEG C, leave standstill 2h, filter, washing, drying under reduced pressure, obtains pantoprazole sodium crystal.
Below technical scheme of the present invention is made further explanation:
The present invention is by the precise controlling to crystallization condition, and prepared a kind of pantoprazole sodium novel crystal form unlike the prior art, the X-ray powder diffraction pattern of this pantoprazole sodium crystal unlike the prior art.Simultaneously due to the ins and outs of this crystal formation, find through test, the compound flow of this novel crystal forms structure, good stability, dry suspension component prepared by this Pantoprazole Sodium crystal compound is simple, greatly reduce the generation of untoward reaction, good stability, bioavailability are high.
Accompanying drawing explanation
Fig. 1 is the X-ray powder diffraction that the pantoprazole sodium crystal of the embodiment of the present invention 1 preparation uses the measurement of Cu-K alpha ray to obtain.
Detailed description of the invention
Below by specific embodiment, summary of the invention of the present invention is described in further detail, but does not therefore limit content of the present invention.
embodiment 1:the preparation of pantoprazole sodium crystal
(1) get pantoprazole sodium, add in deionized water, the volumetric usage of deionized water is 5 times of the quality of Pantoprazole Sodium;
(2) be stirred to whole dissolving, regulate pH to 6-9;
(3) add activated carbon decolorizing, filter, obtain settled solution;
(4) settled solution is moved in pressure vessel, the pressure in pressure vessel being controlled at 2.0Mpa and drip isopropyl alcohol, the ether of 2 DEG C under the condition stirred, speed of agitator controls at 35rmp, the volumetric usage of isopropyl alcohol, ether is 3 times of the volume of deionized water, and the volume ratio of isopropyl alcohol, ether is 1:3;
(5) bleed off pressure after dripping, with the speed of 10 DEG C/min, solution is cooled to-5 DEG C, leave standstill 2h, filter, washing, drying under reduced pressure, obtains pantoprazole sodium crystal.
The X-ray powder diffraction pattern that the pantoprazole sodium crystal prepared uses the measurement of Cu-K alpha ray to obtain as shown in Figure 1.
embodiment 2:the preparation of Pantoprazole Sodium dry suspension
Prescription: with parts by weight, the compound of pantoprazole sodium that 0.4 part of embodiment 1 is obtained, 3 portions of sucrose, 0.7 part of dextrin, 0.15 part of xanthan gum, 0.04 part of sodium lauryl sulphate, 0.07 part of sodium dihydrogen phosphate, 0.005 part of cyclamate.
Preparation method:
1) supplementary material process: Pantoprazole Sodium was pulverized 100 mesh sieves with pulverizer;
2) weigh: weigh each supplementary material according to technology preparation amount;
3) always mix: whole supplementary materials of recipe quantity are joined in three-dimensional mixer, mixing velocity 12r/min, open mixer and mix 60 minutes;
4) subpackage: granule is joined subpackage in particles packing machine, controls content uniformity and meets inner quality standard.
embodiment 3:the preparation of Pantoprazole Sodium dry suspension
Prescription: with parts by weight, the compound of pantoprazole sodium that 0.4 part of embodiment 1 is obtained, 3.2 portions of sucrose, 0.8 part of dextrin, 0.2 part of xanthan gum, 0.05 part of sodium lauryl sulphate, 0.08 part of sodium dihydrogen phosphate, 0.01 part of cyclamate.
Preparation method:
1) supplementary material process: Pantoprazole Sodium was pulverized 100 mesh sieves with pulverizer;
2) weigh: weigh each supplementary material according to technology preparation amount;
3) always mix: whole supplementary materials of recipe quantity are joined in three-dimensional mixer, mixing velocity 12r/min, open mixer and mix 60 minutes;
4) subpackage: granule is joined subpackage in particles packing machine, controls content uniformity and meets inner quality standard.
embodiment 4:the preparation of Pantoprazole Sodium dry suspension
Prescription: with parts by weight, the compound of pantoprazole sodium that 0.4 part of embodiment 1 is obtained, 3.4 portions of sucrose, 0.9 part of dextrin, 0.25 part of xanthan gum, 0.06 part of sodium lauryl sulphate, 0.09 part of sodium dihydrogen phosphate, 0.015 part of cyclamate.
Preparation method:
1) supplementary material process: Pantoprazole Sodium was pulverized 100 mesh sieves with pulverizer;
2) weigh: weigh each supplementary material according to technology preparation amount;
3) always mix: whole supplementary materials of recipe quantity are joined in three-dimensional mixer, mixing velocity 12r/min, open mixer and mix 60 minutes;
4) subpackage: granule is joined subpackage in particles packing machine, controls content uniformity and meets inner quality standard.
experimental example 1:mobility is tested
Pantoprazole Sodium crystalline compounds prepared by reference examples 1:ZL201310093503.3 embodiment 1
The mobility of this experimental example to the compound of pantoprazole sodium of the embodiment of the present invention 1 and reference examples 1 compound detects, adopt fixed funnel method, funnel is placed in the suitable height on graph paper, compound of pantoprazole sodium is freely flowed down from bell mouth, until the cone top formed contacts with bell mouth, measure hypotenuse and the horizontal angle (θ angle of repose) of compound of pantoprazole sodium accumulation horizon, experimental result is as shown in the table.
Mobility experimental result
From interpretation, the mobility of the compound of pantoprazole sodium that the embodiment of the present invention 1 prepares obviously is better than reference examples 1.
test example 2: stability test
The Pantoprazole Sodium dry suspension that Example 2-4 is obtained, under high temperature 40 DEG C, relative humidity 75% ± 5% condition 6 months, carry out accelerated test investigation, result was as following table:
Accelerated test investigates result
From above result, impurity content of the present invention is low, and accelerated test is after 6 months, and the sample indices of embodiment of the present invention 2-4 and related substance significant change do not occur, and the good stability of the Pantoprazole Sodium dry suspension that the present invention obtains is described.
Claims (5)
1. treat a medicine pantoprazole composition of sodium dry suspension for gastric ulcer, it is characterized in that: described compositions dry suspension is made up of Pantoprazole Sodium, sucrose, dextrin, xanthan gum, sodium lauryl sulphate, sodium dihydrogen phosphate, cyclamate; Described Pantoprazole Sodium is crystal, and the X-ray powder diffraction pattern that the measurement of use Cu-K alpha ray obtains as shown in Figure 1.
2. the medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer according to claim 1, it is characterized in that: with parts by weight, described compositions dry suspension is made up of the Pantoprazole Sodium of 0.1-0.6 weight portion, the sucrose of 3-3.4 weight portion, the dextrin of 0.7-0.9 weight portion, the xanthan gum of 0.15-0.25 weight portion, the sodium lauryl sulphate of 0.04-0.06 weight portion, the sodium dihydrogen phosphate of 0.07-0.09 weight portion, 0.005-0.015 cyclamate.
3. the medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer according to claim 2, it is characterized in that: with parts by weight, with parts by weight, described compositions dry suspension is made up of the Pantoprazole Sodium of 0.4 weight portion, the sucrose of 3.2 weight portions, the dextrin of 0.8 weight portion, the xanthan gum of 0.2 weight portion, the sodium lauryl sulphate of 0.05 weight portion, the sodium dihydrogen phosphate of 0.08 weight portion, 0.01 cyclamate.
4. prepare as arbitrary in claim 1-3 as described in the method for medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer, it is characterized in that comprising the following steps:
1) supplementary material process: Pantoprazole Sodium was pulverized 100 mesh sieves with pulverizer;
2) weigh: weigh each supplementary material according to technology preparation amount;
3) always mix: whole supplementary materials of recipe quantity are joined in three-dimensional mixer, mixing velocity 12r/min, open mixer and mix 60 minutes;
4) subpackage: granule is joined subpackage in particles packing machine, controls content uniformity and meets inner quality standard.
5. the medicine pantoprazole composition of sodium dry suspension for the treatment of gastric ulcer according to claim 1, it is characterized in that, in described compositions dry suspension, the crystal preparation method of Pantoprazole Sodium comprises the following steps:
(1) get pantoprazole sodium, add in deionized water, the volumetric usage of deionized water is 5 times of the quality of Pantoprazole Sodium;
(2) be stirred to whole dissolving, regulate pH to 6-9;
(3) add activated carbon decolorizing, filter, obtain settled solution;
(4) settled solution is moved in pressure vessel, the pressure in pressure vessel being controlled at 2.0Mpa and drip isopropyl alcohol, the ether of 2 DEG C under the condition stirred, speed of agitator controls at 35rmp, the volumetric usage of isopropyl alcohol, ether is 3 times of the volume of deionized water, and the volume ratio of isopropyl alcohol, ether is 1:3;
(5) bleed off pressure after dripping, with the speed of 10 DEG C/min, solution is cooled to-5 DEG C, leave standstill 2h, filter, washing, drying under reduced pressure, obtains pantoprazole sodium crystal.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510574779.2A CN105147616A (en) | 2015-09-11 | 2015-09-11 | Medicine namely pantoprazole sodium composition dry suspension for treating gastric ulcer |
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|---|---|---|---|
| CN201510574779.2A CN105147616A (en) | 2015-09-11 | 2015-09-11 | Medicine namely pantoprazole sodium composition dry suspension for treating gastric ulcer |
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Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007091276A3 (en) * | 2006-02-10 | 2007-12-06 | Rajasthan Antibiotic Ltd | Novel crystal form of omeprazol sodium |
| US20080132707A1 (en) * | 2002-12-19 | 2008-06-05 | Teva Pharmaceuticals Usa, Inc. For Barbados. | Solid states of pantoprazole sodium, processes for preparing them and processes for preparing known pantoprazole sodium hydrates |
| CN102166209A (en) * | 2011-03-18 | 2011-08-31 | 海南灵康制药有限公司 | Compound pantoprazole sodium pharmaceutical composition solid preparation |
| CN104814942A (en) * | 2015-05-26 | 2015-08-05 | 苗怡文 | Medicinal pantoprazole sodium composition capsule for treating digestive system disease |
| CN104856993A (en) * | 2015-05-26 | 2015-08-26 | 苗怡文 | Medical pantoprazole sodium freeze-dried powder injection composition for treating digestive system diseases |
| CN104856994A (en) * | 2015-05-26 | 2015-08-26 | 苗怡文 | Medical pantoprazole sodium composition tablet for treating gastric ulcer |
-
2015
- 2015-09-11 CN CN201510574779.2A patent/CN105147616A/en not_active Withdrawn
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080132707A1 (en) * | 2002-12-19 | 2008-06-05 | Teva Pharmaceuticals Usa, Inc. For Barbados. | Solid states of pantoprazole sodium, processes for preparing them and processes for preparing known pantoprazole sodium hydrates |
| WO2007091276A3 (en) * | 2006-02-10 | 2007-12-06 | Rajasthan Antibiotic Ltd | Novel crystal form of omeprazol sodium |
| CN102166209A (en) * | 2011-03-18 | 2011-08-31 | 海南灵康制药有限公司 | Compound pantoprazole sodium pharmaceutical composition solid preparation |
| CN104814942A (en) * | 2015-05-26 | 2015-08-05 | 苗怡文 | Medicinal pantoprazole sodium composition capsule for treating digestive system disease |
| CN104856993A (en) * | 2015-05-26 | 2015-08-26 | 苗怡文 | Medical pantoprazole sodium freeze-dried powder injection composition for treating digestive system diseases |
| CN104856994A (en) * | 2015-05-26 | 2015-08-26 | 苗怡文 | Medical pantoprazole sodium composition tablet for treating gastric ulcer |
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Application publication date: 20151216 |
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