CN103006691B - Compound capsule preparation containing omeprazole and sodium bicarbonate - Google Patents
Compound capsule preparation containing omeprazole and sodium bicarbonate Download PDFInfo
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- CN103006691B CN103006691B CN201310000622.XA CN201310000622A CN103006691B CN 103006691 B CN103006691 B CN 103006691B CN 201310000622 A CN201310000622 A CN 201310000622A CN 103006691 B CN103006691 B CN 103006691B
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- omeprazole
- capsule
- sodium bicarbonate
- piller
- disintegrating agent
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Abstract
The invention relates to a compound capsule containing omeprazole and sodium bicarbonate and a preparation method thereof. The compound capsule is characterized in that when the compound capsule is positioned in a hydrochloric acid solution, the sodium bicarbonate is quickly released, and the omeprazole is quickly released after the sodium bicarbonate is completely released.
Description
Technical field
The invention belongs to medical technical field, be specifically related to a kind of containing omeprazole sodium bicarbonate compound capsule.
Background technology
Peptic ulcer is a kind of commonly encountered diseases and frequently-occurring disease, and the people in the whole world nearly 5%～6% suffered from this disease.The appearance of the H+-K+-ATP enzyme eighties (proton pump) inhibitor, makes a breakthrough the treatment of peptic ulcer, becomes the strongest novel antisecretory at present.The proton pump inhibitors such as omeprazole (omeprazole) have been opened up the new role approach for the treatment of peptic ulcer, and the treatment that makes peptic ulcer is no longer a difficult problem.Omeprazole is benzimidazole proton pump inhibitors, can suppress parietal cell film inner proton pump (H+-K+-ATP enzyme system), H+ in cell wall can not be transported in gastric juice and go, thereby performance suppresses the effect of gastric secretion.It has been widely used in treating gastric ulcer, duodenal ulcer, reflux esophagitis, gastrinoma etc.But omeprazole acid labile, therefore can be by gastric acid fast degradation.Omeprazole chemical name 5-methoxy foundation stone-[(4-methoxyl group-3,5-dimethyl-2-pyridine radicals)-methyl] sulfenyl-1H-benzimidazole, structural formula is as follows:
Existing proton pump inhibitor destroys its decomposition in order to avoid gastric juice; mostly be oral enteric preparation; when production, need enteric coated; as Chinese patent literature CN101036633A, CN101120930A, CN101366703A, CN101579324B; and the omeprazole casing preparation reported of WO96/01623A1, WO98/52564A1, US4786503, EP247983; generally omeprazole to be made to micropill carry out again enteric coating; or omeprazole is packed in enteric hollow capsule, protection omeprazole exempts from stomach acids destroy.Thisly be designed with several shortcomings: in (1) production technology, need special coating equipment in sugar production line, technological requirement is higher, requires capsule coating even, and thickness is suitable, has increased production cost; (2) enteric coating preparation majority has moisture sensitivity; (3) owing to discharging in intestinal juice, at least wait until could be compared with Slow release when after gastric emptying, namely preparation arrives small intestinal, and medicine, from intestinal absorption, then just can take effect subsequently, this process almost wants time-consuming nearly 3 hours drug effects to slow down, and peak time postpones.
Chinese patent ZL200610098266 discloses the preparation method of a kind of fast releasing solid omeprazole and said preparation.Described preparation is combined by omeprazole and a certain amount of sodium hydroxide, makes medicine to summation gastric acid rapidly after stomach, and medicine is effectively absorbed.But the content to sodium hydroxide has strict demand, can be effectively in and gastric acid and don't can cause injury of gastrointestinal tract.
Chinese patent ZL200710141577.4 discloses the capsule that sodium bicarbonate that some enteric-coated pellets that the compositions of a kind of omeprazole and sodium bicarbonate is made up of omeprazole, sodium bicarbonate and arbitrary form exist forms.But complex process needs omeprazole enteric coatedly simultaneously, has lost medicine and discharge rapidly under one's belt the effect of onset.
Patent CN101816641B discloses the quick-acting proton pump inhibitors that a kind of oral quick release solid preparation that contains omeprazole is made up of omeprazole, sodium bicarbonate and pharmaceutic adjuvant.Said preparation prescription pharmaceutic adjuvant complexity, and in technique, require omeprazole, sodium bicarbonate and part pharmaceutic adjuvant associating facing-up to carry out micronization, both increase technology difficulty, increase again production cost.Simultaneously maximum problem is preparation under one's belt when stripping, if sodium bicarbonate can not discharge completely rapidly in and gastric acid, omeprazole will fast degradation, affects the treatment.
Capsule and the preparation method of a patent CN 102641285A compound recipe omeprazole, be made up of omeprazole, sodium bicarbonate and pharmaceutically acceptable pharmaceutical carrier.Sodium bicarbonate can improve the pH value of gastric environment and maintain the regular hour, make the unsettled omeprazole of acid absorb fast onset before by stomach acids destroy, its feature is that the granularity of the omeprazole of controlling one of its principal agent composition is in certain scope, make the preparation omeprazole that makes can be in gastric environment solution absorption fast.If but sodium bicarbonate can not discharge rapidly, in and gastric acid, once omeprazole first contacts with gastric juice, will cause the degraded of omeprazole.
Summary of the invention
For the deficiencies in the prior art, inventor sends out bright a kind of omeprazole sodium bicarbonate compound capsule, and this capsule arrives after stomach, under the effect of disintegrating agent, sodium bicarbonate discharges rapidly, fast in and gastric acid, then omeprazole discharges fast again, reaches therapeutic effect.
Further, inventor's process great many of experiments, determines omeprazole and appropriate disintegrating agent is made to piller, piller outsourcing gastric solubleness film-coat, then, with sodium bicarbonate, disintegrating agent, mix lubricant, is filled into capsule.After gastric solubleness layer dissolves, under the effect of the inner disintegrating agent of piller, the piller release medicine that breaks rapidly.
The present invention specifically realizes as follows:
Described omeprazole sodium bicarbonate compound capsule, is made up of omeprazole gastric solubleness piller and sodium bicarbonate, disintegrating agent, lubricant, and in hydrochloric acid solution, sodium bicarbonate discharges rapidly, and omeprazole discharges rapidly after sodium bicarbonate discharges completely again.
Described capsule, disintegrating agent is one or more in carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, hydroxypropyl cellulose, polyvinylpolypyrrolidone, preferably polyvinylpolypyrrolidone.
Described capsule, omeprazole gastric solubleness piller is formed by micronized omeprazole and the rear bag of hydroxypropyl cellulose preparation gastric solubleness film-coat, film-coat weightening finish 5-20%, the 10-18% that preferably increases weight, most preferably increases weight 12%.
Described capsule, the consumption of disintegrating agent accounts for the 5-20% of Capsule content gross weight, preferably accounts for the 8-12% of gross weight, and most preferably 10%.
Described capsule, micronized omeprazole particle diameter D90 < 30 μ m, preferable particle size D90 < 20 μ m, most preferably particle diameter D90 < 10 μ m.
Described capsule, gastric solubleness film-coat material is selected from one kind of multiple in hydroxypropyl emthylcellulose, polyethylene glycol-ethenol copolymer, hydroxypropyl cellulose
Described piller, is to be greater than 10 aqueous solution by omeprazole and hydroxypropyl cellulose pH to granulate, and extrudes round as a ball, dry forming.PH adjusting agent is selected from one or more in sodium hydroxide, sodium carbonate, sodium bicarbonate.
Compared with prior art, the omeprazole sodium bicarbonate capsule tool the present invention relates to has the following advantages and is progressive significantly:
(1) omeprazole sodium bicarbonate capsule of the present invention, first sodium bicarbonate discharges, in and gastric acid after, omeprazole more rapidly discharge, design ingenious.
(2) omeprazole sodium bicarbonate capsule of the present invention, its preparation process is fairly simple, easy to operate, is applicable to industrialized great production.
Detailed description of the invention
Now further describe beneficial effect of the present invention by following examples, embodiment is only for the object of illustration, do not limit the scope of the invention, within the apparent change that those of ordinary skill in the art make according to the present invention simultaneously and modification are also contained in the scope of the invention.
Embodiment 1:
(1) piller prescription
Omeprazole (m) 10g of D90 < 30 μ
Hydroxypropyl cellulose 90g
The aqueous sodium carbonate of pH10 is appropriate
(2) coating prescription
Omeprazole and hydroxypropyl cellulose mix homogeneously, add aqueous sodium carbonate appropriate, granulates, and extrudes round as a ballly, dry, obtains omeprazole piller, coating weightening finish 5%.
(3) capsule prescription
By omeprazole coated pellets and polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Embodiment 2:
(1) piller prescription
Omeprazole (m) 10g of D90 < 20 μ
Hydroxypropyl cellulose 70g
The sodium hydroxide sodium water solution of pH10 is appropriate
(2) coating prescription
Omeprazole and hydroxypropyl cellulose mix homogeneously, add aqueous sodium carbonate appropriate, granulates, and extrudes round as a ballly, dry, obtains omeprazole piller, coating weightening finish 20%.
(3) capsule prescription
By omeprazole coated pellets and polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Embodiment 3:
(1) piller prescription
Omeprazole (m) 10g of D90 < 10 μ
Hydroxypropyl cellulose 90g
The aqueous sodium carbonate of pH10 is appropriate
(2) coating prescription
Polyethylene glycol-ethenol copolymer 10g
Water 100g
Omeprazole and hydroxypropyl cellulose mix homogeneously, add aqueous sodium carbonate appropriate, granulates, and extrudes round as a ballly, dry, obtains omeprazole piller, coating weightening finish 12%.
(3) capsule prescription
By omeprazole coated pellets and polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Comparative example 1
By omeprazole, hydroxypropyl cellulose, polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Comparative example 2
(1) piller prescription
Omeprazole (m) 10g of D90 < 10 μ
Microcrystalline Cellulose 90g
The aqueous sodium carbonate of pH10 is appropriate
(2) coating prescription
Polyethylene glycol-ethenol copolymer 10g
Water 100g
Omeprazole and microcrystalline Cellulose mix homogeneously, add aqueous sodium carbonate appropriate, granulates, and extrudes round as a ballly, dry, obtains omeprazole piller, coating weightening finish 12%.
(3) capsule prescription
By omeprazole coated pellets and polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Comparative example 3
(1) piller prescription
Omeprazole (m) 10g of D90 < 10 μ
Polyvinylpolypyrrolidone 90g
The aqueous sodium carbonate of pH10 is appropriate
(2) coating prescription
Polyethylene glycol-ethenol copolymer 10g
Water 100g
Omeprazole and microcrystalline Cellulose mix homogeneously, add aqueous sodium carbonate appropriate, granulates, and extrudes round as a ballly, dry, obtains omeprazole piller, coating weightening finish 12%.
(3) capsule prescription
By omeprazole coated pellets and polyvinylpolypyrrolidone, sodium bicarbonate, magnesium stearate mix homogeneously, incapsulate and get final product.
Checking embodiment
Dissolution: get this product, according to dissolution method, taking 0.1mol/L hydrochloric acid solution 900ml as dissolution medium, rotating speed turns for minutes 75, operation in accordance with the law, in the time of 15 minutes, getting solution filters, detect, 5 minutes time, sodium bicarbonate dissolution is greater than 85%, and omeprazole stripping quantity is lower than 5% of labelled amount, 15 minutes time, omeprazole stripping quantity must not be lower than 85% of labelled amount, and in mensuration process, solution colour must not redden.
[note] omeprazole is unstable to acid, if in stripping mensuration process the dissolution medium color that reddens, represent the existing degraded of omeprazole.
Embodiment measurement result
Embodiment 1-3, in dissolution determination process, dissolution medium color is constant, and omeprazole not degraded is substantially described, and stripping in 15 minutes is complete; Comparative example 1 does not adopt piller packaging technique, although suppressed the degraded of omeprazole after sodium bicarbonate stripping, but due to the incipient stage, the stripping simultaneously of omeprazole and sodium bicarbonate, cause dissolution medium variable color, omeprazole stripping 80.2% in 15 minutes, illustrates the existing degraded largely of omeprazole; Comparative example 2 adopts piller packaging technique, but prepares the adjuvant employing microcrystalline Cellulose of piller, and result omeprazole is difficult to stripping, and reason is that piller is difficult to disintegrate; Comparative example 3 adopts piller packaging technique, and the adjuvant of preparing piller is disintegrating agent polyvinylpolypyrrolidone, although omeprazole stripping is very fast, degrades also fast, and reason is that piller disintegrate is very fast, and the stripping simultaneously of omeprazole and sodium bicarbonate, is destroyed by acid medium; Embodiment and comparative example's result has further been verified superiority of the present invention.
Claims (11)
1. an omeprazole sodium bicarbonate compound capsule, it is characterized in that: this capsule is even by omeprazole gastric solubleness piller and sodium bicarbonate, disintegrating agent, mix lubricant, filled capsules forms, in hydrochloric acid solution, sodium bicarbonate discharges rapidly, and omeprazole discharges rapidly after sodium bicarbonate discharges completely again; Described disintegrating agent is polyvinylpolypyrrolidone; The consumption of disintegrating agent accounts for the 5%-20% of Capsule content gross weight; In micropill, disintegrating agent accounts for 90% of micropill gross weight; Described omeprazole gastric solubleness piller is prepared and is wrapped gastric solubleness film-coat after piller and form by micronized omeprazole and hydroxypropyl cellulose.
2. capsule as claimed in claim 1, is characterized in that the consumption of disintegrating agent accounts for the 8%-12% of Capsule content gross weight.
3. capsule as claimed in claim 1, is characterized in that the consumption of disintegrating agent accounts for 10% of Capsule content gross weight.
4. capsule as claimed in claim 1, is characterized in that omeprazole gastric solubleness piller prepared and wrapped gastric solubleness film-coat after piller and form by micronized omeprazole and hydroxypropyl cellulose, film-coat weightening finish 5%-20%.
5. capsule as claimed in claim 4, is characterized in that film-coat weightening finish 10%-18%.
6. capsule as claimed in claim 4, is characterized in that film-coat weightening finish 12%.
7. capsule as claimed in claim 4, is characterized in that micronized omeprazole particle diameter D90 < 30 μ m.
8. capsule as claimed in claim 4, is characterized in that micronized omeprazole particle diameter D90 < 20 μ m.
9. capsule as claimed in claim 4, is characterized in that micronized omeprazole particle diameter D90 < 10 μ m.
10. capsule as claimed in claim 4, gastric solubleness film-coat material is selected from one or more in hydroxypropyl emthylcellulose, polyethylene glycol-ethenol copolymer, hydroxypropyl cellulose.
11. capsules as claimed in claim 4, is characterized in that described piller is greater than 10 aqueous solution by omeprazole and hydroxypropyl cellulose pH and granulates, and extrude round as a ball, dry forming; PH adjusting agent is selected from one or more in sodium hydroxide, sodium carbonate, sodium bicarbonate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310000622.XA CN103006691B (en) | 2013-01-05 | 2013-01-05 | Compound capsule preparation containing omeprazole and sodium bicarbonate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310000622.XA CN103006691B (en) | 2013-01-05 | 2013-01-05 | Compound capsule preparation containing omeprazole and sodium bicarbonate |
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| CN103006691A CN103006691A (en) | 2013-04-03 |
| CN103006691B true CN103006691B (en) | 2014-10-08 |
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| CN201310000622.XA Expired - Fee Related CN103006691B (en) | 2013-01-05 | 2013-01-05 | Compound capsule preparation containing omeprazole and sodium bicarbonate |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11813285B2 (en) | 2018-01-29 | 2023-11-14 | Chong Kun Dang Pharmaceutical Corp. | Stable pharmaceutical composition comprising esomeprazole and sodium bicarbonate |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102006777B1 (en) | 2018-01-29 | 2019-10-08 | 주식회사 종근당 | Pharmaceutical formulation comprising esomeprazole and sodium bicarbonate |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101120930A (en) * | 2006-08-11 | 2008-02-13 | 石药集团中奇制药技术（石家庄）有限公司 | Omeprazole composition and preparing process thereof |
| CN102119927A (en) * | 2010-01-11 | 2011-07-13 | 石药集团中奇制药技术（石家庄）有限公司 | Enteric-coated pellet preparation of proton pump inhibitor and preparation method thereof |
| CN102688196A (en) * | 2012-05-21 | 2012-09-26 | 杭州华东医药集团生物工程研究所有限公司 | Omeprazole pellets and preparation method thereof |
-
2013
- 2013-01-05 CN CN201310000622.XA patent/CN103006691B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101120930A (en) * | 2006-08-11 | 2008-02-13 | 石药集团中奇制药技术（石家庄）有限公司 | Omeprazole composition and preparing process thereof |
| CN102119927A (en) * | 2010-01-11 | 2011-07-13 | 石药集团中奇制药技术（石家庄）有限公司 | Enteric-coated pellet preparation of proton pump inhibitor and preparation method thereof |
| CN102688196A (en) * | 2012-05-21 | 2012-09-26 | 杭州华东医药集团生物工程研究所有限公司 | Omeprazole pellets and preparation method thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11813285B2 (en) | 2018-01-29 | 2023-11-14 | Chong Kun Dang Pharmaceutical Corp. | Stable pharmaceutical composition comprising esomeprazole and sodium bicarbonate |
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| CN103006691A (en) | 2013-04-03 |
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| C14 | Grant of patent or utility model | ||
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| EE01 | Entry into force of recordation of patent licensing contract |
Application publication date: 20130403 Assignee: Guangzhou Ren Heng Pharmaceutical Technology Co., Ltd Assignor: Qingdao University Contract record no.: 2015440000145 Denomination of invention: Compound capsule preparation containing omeprazole and sodium bicarbonate Granted publication date: 20141008 License type: Exclusive License Record date: 20150520 |
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