CN102225050A - Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same - Google Patents
Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same Download PDFInfo
- Publication number
- CN102225050A CN102225050A CN2011101758376A CN201110175837A CN102225050A CN 102225050 A CN102225050 A CN 102225050A CN 2011101758376 A CN2011101758376 A CN 2011101758376A CN 201110175837 A CN201110175837 A CN 201110175837A CN 102225050 A CN102225050 A CN 102225050A
- Authority
- CN
- China
- Prior art keywords
- famotidine
- beta
- sulfobutyl ether
- sodium chloride
- schardinger dextrin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Abstract
The invention relates to a method for preparing a famotidine sodium chloride injection by an inclusion method and a product prepared by using the same. The method is characterized in that sulfobutyl ether-beta-cyclodextrin is used as an including agent of famotidine, and famotidine is firstly dissolved in glacial acetic acid and then added into a sulfobutyl ether-beta-cyclodextrin saturated solution to allow sulfobutyl ether-beta-cyclodextrin to include famotidine, and the sulfobutyl ether-beta-cyclodextrin including famotidine is dissolved in water; the weight part ratio of famotidine to sulfobutyl ether-beta-cyclodextrin is (1:5)-(1:10); the quantity of glacial acetic acid is 5-7 times of that of famotidine based on weight part; and excessive sterilization at 121 DEG C for 15 minutes is adopted. The method provided by the invention has the following advantages: related substances are controlled within 2%, which is far lower than 5% of domestic like-products, and the sterilization is changed from a residual probability method to an excessive sterilization method, which ensures 100% sterilization, greatly improves product quality and enhances the safety of medicine in clinical applications.
Description
Technical field
The present invention relates to a kind of enclose legal system and be equipped with method of famotidine sodium chloride injection and products thereof, belong to biomedicine field.
Background technology
Famotidine chemistry 3-[[[2-[(diamino methylene by name)-and the 4-thiazolyl] methyl] sulfo-]-N-sulfonamides third amidine, be the crystalline powder of white or off-white color; Mildly bitter flavor; Meet photochromic deepening; Slightly soluble in methanol, soluble,very slightly in acetone, almost insoluble in water or chloroform, easily molten in glacial acetic acid.Its fusing point is 160～165 ℃, decomposes simultaneously during fusion.The famotidine sodium chloride injection is mainly used in upper gastrointestinal hemorrhage, the Zhuo-Emhorn syndrome due to treatment peptic ulcer, acute stress ulcer and the hemorrhagic gastritis; The upper gastrointestinal hemorrhage that prevention aggressive stress (various major operations, as: cerebrovascular disorders, injury of head, multiple organs failure, large-area burns etc.) causes.Prior art is to use glacial acetic acid as cosolvent, and directly soluble in water, sterilising conditions adopts remaining probabilistic method, i.e. 115 degree sterilization in 30 minutes, because of the famotidine case of thermal instability, related substance reaches 5%, and can not sterilize with the method for excessively killing, can not guarantee the gentle product quality of product sterilized water.
Make inclusion agents with sulfobutyl ether-β-Cyclodextrin in the present technique, make the famotidine sodium chloride injection.Sulfobutyl ether-β-Cyclodextrin is the novel ionizable cyclodextrin derivative of nineties listing, and animal toxicity studies show that similar (the malicious LD50 of the oral urgency of rat＞2g/kg) to present widely used hydroxypropyl cyclodextrin of sulfobutyl ether-beta-schardinger dextrin-oral administration safety; But adjuvant as the vascular drug delivery preparation, SBE-β-CD does not have significant cytotoxicity, renal function is not had influence, and have higher water solublity, an advantage such as enclose performance preferably, be widely used in injecting, different route of administration such as oral, eye and nasal cavity, have broad application prospects at field of medicaments.
Summary of the invention
One of purpose of the present invention provides the method that a kind of enclose legal system is equipped with the famotidine sodium chloride injection.
Two of purpose of the present invention provides a kind of famotidine sodium chloride injection of enclose method preparation.
One of purpose of the present invention is achieved in that employing sulfobutyl ether-beta-schardinger dextrin-is the inclusion agents of famotidine, be dissolved in famotidine in the glacial acetic acid earlier, add again that sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, by sulfobutyl ether-beta-schardinger dextrin-with the famotidine enclose after, soluble in water again.
The scope that preferably is the weight part ratio of famotidine and sulfobutyl ether-beta-schardinger dextrin-is 1:5～1:10;
Earlier sulfobutyl ether-beta-schardinger dextrin-is dissolved in the water for injection of 1～2 times of weight portion, makes that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, standby; After being dissolved in famotidine in 5～7 times of weight portion glacial acetic acid earlier, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, enter next step technology again.
Sterilization is adopted and is excessively killed method, selects the sterilization in 15 minutes of 121 degree for use.
More preferably: earlier sulfobutyl ether-beta-schardinger dextrin-is dissolved in the water for injection of 1.5 times of weight portions, makes that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, standby; After being dissolved in famotidine in 6 times of weight portion glacial acetic acid earlier, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, enter next step technology again.
Sulfobutyl ether-beta-schardinger dextrin-s of 1000～2000 parts are dissolved in the water for injection of 1.5 times of weight portions, make that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, standby; After being dissolved in 200 parts of famotidines in 1200 parts of glacial acetic acid, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, stirred 30 minutes, add 600000 parts of waters for injection, stir, add 9000 parts of sodium chloride again and be stirred to dissolving, add water for injection again, total amount to water for injection is 1000000 parts, stir, add 200 parts of pin charcoals, stir 30 minutes after-filtration, the filtrate embedding, the method of excessively killing is adopted in sterilization, the sterilization in 15 minutes of 121 degree, and the content of described famotidine raw material is more than 99%, related substance is below 1%, and the related substance of the famotidine sodium chloride injection of preparation is below 2%.
Two of purpose of the present invention is achieved in that it is made up of following substances in parts by weight: 200 parts of famotidines, 1000～1400 parts in glacial acetic acid, 1000～2000 parts of sulfobutyl ether-beta-schardinger dextrin-s, 9000 parts in sodium chloride, 1000000 parts of waters for injection; The content of described famotidine raw material is more than 99%, and related substance is below 1%, and the related substance of famotidine sodium chloride injection is below 2%.
The present invention has obvious improvement at this aspect two, after selecting for use sulfobutyl ether-beta-schardinger dextrin-with the medicinal liquid enclose, soluble in water again, the dissolubility of famotidine is improved greatly, stability is better, more stable to heat especially, select the sterilization in 15 minutes of 121 degree for use, to there be the related substance of famotidine sodium chloride injection can be controlled in 2%, be far superior to 5% of domestic like product, significantly reduce related substance, sterilising conditions has become the method for excessively killing by remaining probabilistic method, guarantee that product 100% is aseptic, improved product quality greatly, increased clinical application safety.
The specific embodiment
The present invention is by the following examples can the invention will be further described, yet scope of the present invention is not limited to following embodiment.
Embodiment 1:
Material by following weight portion constitutes prescription:
Famotidine 200g
Glacial acetic acid 1200g
Sulfobutyl ether-beta-schardinger dextrin-1000g
Sodium chloride 9000g
Water for injection 1000000g
Make 10000 bottles altogether
Its preparation process is:
Feedstock production by following weight portion forms, and sulfobutyl ether-beta-schardinger dextrin-of 1000g is dissolved in the 1500g water for injection, making fullly to close solution, and is standby; The 200g famotidine is dissolved in the 1200g glacial acetic acid, and adds in the full sulfobutyl ether-beta-schardinger dextrin-solution that closes, stirred 30 minutes, add 600000g water for injection, stir, add 9000g sodium chloride again and be stirred to dissolving, now add 398500g water for injection, stir, add 200g pin charcoal, stir 30 minutes after-filtration, 10000 bottles of filtrate embeddings, the method of excessively killing is adopted in sterilization, the sterilization in 15 minutes of 121 degree.
The content of described famotidine raw material is more than 99%, and related substance is below 1%, and the related substance of the famotidine sodium chloride injection of preparation is below 2%.
Embodiment 2:
Material by following weight portion constitutes prescription:
Famotidine 200g
Glacial acetic acid 1200g
Sulfobutyl ether-beta-schardinger dextrin-1500g
Sodium chloride 9000g
Water for injection 1000000g
Make 10000 bottles altogether
Its preparation process is:
Feedstock production by following weight portion forms, and sulfobutyl ether-beta-schardinger dextrin-of 1500g is dissolved in the 2250g water for injection, making fullly to close solution, and is standby; The 200g famotidine is dissolved in the 1200g glacial acetic acid, and adds in the full sulfobutyl ether-beta-schardinger dextrin-solution that closes, stirred 30 minutes, add 600000 parts of waters for injection, stir, add 9000g sodium chloride again and be stirred to dissolving, now add 397750 waters for injection, stir, add 200g pin charcoal, stir 30 minutes after-filtration, the filtrate embedding, the method of excessively killing is adopted in sterilization, the sterilization in 15 minutes of 121 degree.
The content of described famotidine raw material is more than 99%, and related substance is below 1%, and the related substance of the famotidine sodium chloride injection of preparation is below 2%.
Embodiment 3:
Material by following weight portion constitutes prescription:
Famotidine 200g
Glacial acetic acid 1200g
Sulfobutyl ether-beta-schardinger dextrin-2000g
Sodium chloride 9000g
Water for injection 1000000g
Make 10000 bottles altogether
Its preparation process is:
Feedstock production by following weight portion forms, and sulfobutyl ether-beta-schardinger dextrin-of 2000g is dissolved in the 3000g water for injection, making fullly to close solution, and is standby; The 200g famotidine is dissolved in the 1200g glacial acetic acid, and adds in the full sulfobutyl ether-beta-schardinger dextrin-solution that closes, stirred 30 minutes, add 600000g water for injection, stir, add 9000g sodium chloride again and be stirred to dissolving, now add 397000g water for injection, stir, add 200g pin charcoal, stir 30 minutes after-filtration, the filtrate embedding, the method of excessively killing is adopted in sterilization, the sterilization in 15 minutes of 121 degree.
The content of described famotidine raw material is more than 99%, and related substance is below 1%, and the related substance of the famotidine sodium chloride injection of preparation is below 2%.
Claims (7)
1. an enclose legal system is equipped with the method for famotidine sodium chloride injection, it is characterized in that being to adopt sulfobutyl ether-beta-schardinger dextrin-is the inclusion agents of famotidine, be dissolved in famotidine in the glacial acetic acid earlier, add again that sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, by sulfobutyl ether-beta-schardinger dextrin-with the famotidine enclose after, soluble in water again.
2. a kind of enclose legal system according to claim 1 is equipped with the method for famotidine sodium chloride injection, it is characterized in that being that the scope of the weight part ratio of famotidine and sulfobutyl ether-beta-schardinger dextrin-is 1:5～1:10.
3. a kind of enclose legal system according to claim 1 and 2 is equipped with the method for famotidine sodium chloride injection, it is characterized in that being earlier sulfobutyl ether-beta-schardinger dextrin-being dissolved in the water for injection of 1～2 times of weight portion, make that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, standby; After being dissolved in famotidine in 5～7 times of weight portion glacial acetic acid earlier, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, enter next step technology again.
4. a kind of enclose legal system according to claim 3 is equipped with the method for famotidine sodium chloride injection, it is characterized in that being earlier sulfobutyl ether-beta-schardinger dextrin-being dissolved in the water for injection of 1.5 times of weight portions, makes that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, and is standby; After being dissolved in famotidine in 6 times of weight portion glacial acetic acid earlier, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, enter next step technology again.
5. the method that is equipped with the famotidine sodium chloride injection according to the described a kind of enclose legal system of arbitrary claim in the claim 1 to 4 is characterized in that being sterilizing adopting and excessively kills method, selects the sterilization in 15 minutes of 121 degree for use.
6. a kind of enclose legal system according to claim 3 is equipped with the method for famotidine sodium chloride injection, it is characterized in that: sulfobutyl ether-beta-schardinger dextrin-s of 1000～2000 parts are dissolved in the water for injection of 1.5 times of weight portions, make that sulfobutyl ether-beta-schardinger dextrin-is full to close solution, standby; After being dissolved in 200 parts of famotidines in 1200 parts of glacial acetic acid, add again that described sulfobutyl ether-beta-schardinger dextrin-is full to be closed in the solution, stirred 30 minutes, add 600000 parts of waters for injection, stir, add 9000 parts of sodium chloride again and be stirred to dissolving, add water for injection again, total amount to water for injection is 1000000 parts, stir, add 200 parts of pin charcoals, stir 30 minutes after-filtration, the filtrate embedding, the method of excessively killing is adopted in sterilization, the sterilization in 15 minutes of 121 degree, and the content of described famotidine raw material is more than 99%, related substance is below 1%, and the related substance of the famotidine sodium chloride injection of preparation is below 2%.
7. a kind of enclose legal system according to claim 1 is equipped with the famotidine sodium chloride injection of the method preparation of famotidine sodium chloride injection, it is characterized in that being that it is made up of following substances in parts by weight: 200 parts of famotidines, 1000～1400 parts in glacial acetic acid, 1000～2000 parts of sulfobutyl ether-beta-schardinger dextrin-s, 9000 parts in sodium chloride, 1000000 parts of waters for injection; The content of described famotidine raw material is more than 99%, and related substance is below 1%, and the related substance of famotidine sodium chloride injection is below 2%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011101758376A CN102225050B (en) | 2011-06-28 | 2011-06-28 | Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011101758376A CN102225050B (en) | 2011-06-28 | 2011-06-28 | Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102225050A true CN102225050A (en) | 2011-10-26 |
| CN102225050B CN102225050B (en) | 2012-06-20 |
Family
ID=44806081
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011101758376A Active CN102225050B (en) | 2011-06-28 | 2011-06-28 | Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102225050B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103446048A (en) * | 2013-09-12 | 2013-12-18 | 南京正宽医药科技有限公司 | Famotidine injection and preparation method thereof |
| CN114767626A (en) * | 2022-03-31 | 2022-07-22 | 天津金耀集团湖北天药药业股份有限公司 | Famotidine injection and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101380313A (en) * | 2008-10-16 | 2009-03-11 | 沈阳药科大学 | Famotidine high density type gastric retention osmotic pump controlled release preparation and preparation method thereof |
-
2011
- 2011-06-28 CN CN2011101758376A patent/CN102225050B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101380313A (en) * | 2008-10-16 | 2009-03-11 | 沈阳药科大学 | Famotidine high density type gastric retention osmotic pump controlled release preparation and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 《JOURNAL OF PHARMACEUTICAL SCIENCES》 20101030 FATMA M. MADY等 Enhancement of the Aqueous Solubility and Masking the Bitter 4285-4294 1-7 第99卷, 第10期 * |
| 《解放军药学学报》 20020430 文爱东等 法莫替丁氯化钠注射液的稳定性研究 83 1-7 第18卷, 第2期 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103446048A (en) * | 2013-09-12 | 2013-12-18 | 南京正宽医药科技有限公司 | Famotidine injection and preparation method thereof |
| CN114767626A (en) * | 2022-03-31 | 2022-07-22 | 天津金耀集团湖北天药药业股份有限公司 | Famotidine injection and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102225050B (en) | 2012-06-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HU229571B1 (en) | Aqueous compositions containing moxifloxacin and common salt and process for its preparation | |
| CN106166143B (en) | Plant hard hollow capsule shell and preparation method thereof | |
| US11896598B2 (en) | Appetite suppressant compositions and methods thereof | |
| CN102091028A (en) | Edaravone injection and preparation method thereof | |
| CN103547257B (en) | Viscoelastic fluid is in the application of producing for the drug products by operative treatment eye | |
| CN102225050B (en) | Method for preparing famotidine sodium chloride injection by inclusion method and product prepared by using the same | |
| CN105726473A (en) | Oral solution of tomoxetine or medicinal salt thereof and preparation method thereof | |
| CN102579329B (en) | Milrinone lactate injection and preparation method thereof | |
| CN100512804C (en) | Preparing process of botanical hollow enteric hard capsule | |
| JP4394447B2 (en) | Acetaminophen composition | |
| EP3669879B1 (en) | Pharmaceutical composition in the form of an oral suspension including a flavonoid fraction comprising diosmin and xanthan gum | |
| CN114126583A (en) | Ornidazole injection and S-ornidazole injection | |
| CN103784426A (en) | Aripiprazole oral membrane and preparation method thereof | |
| JP5298028B2 (en) | Treatment for cerebral ischemic injury | |
| CN103690516A (en) | Aripiprazole oral membrane and preparation method thereof | |
| CN102440957B (en) | Terlipressin acetate nasal cavity spray and preparation method thereof | |
| CN105163732A (en) | Methods for treatment of ophthalmic diseases and disorders | |
| CN102240261A (en) | Preparation method and medicinal purpose of glucomannan injection | |
| CA3074541A1 (en) | Appetite suppressant compositions and methods thereof | |
| CN105496954B (en) | A kind of preparation method of the injection of muscle relaxants rocuronium bromide | |
| CN104887622A (en) | Stable ambroxol hydrochloride huge capacity injection and preparation method thereof | |
| CN104666335A (en) | Preparation method of peritoneal dialysis solution (lactate) (low-calcium) composition | |
| CN109010268A (en) | A kind of ophthalmic composition and preparation method thereof improving chloramphenicol stability | |
| CN102784122A (en) | Isoniazid composition freeze-dried orally disintegrating tablet and preparation method thereof | |
| CN103550142A (en) | Medicinal solution preparation prepared from acetylcysteine clathrate and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CP03 | Change of name, title or address | ||
| CP03 | Change of name, title or address |
Address after: 331800 No. 6, Dongshan Industrial Park, Dongxiang Economic Development Zone, Fuzhou, Jiangxi. Patentee after: Hui Yin group Jiangxi East Asia Pharmaceutical Co., Ltd. Address before: 331800 Dongxiang Province Economic Development Zone, Dongshan Industrial Park, Fuzhou, Hui Road, No. 6, No. Patentee before: Huiyinbi Group (Jiangxi) Dongya Pharmaceutical Co., Ltd. |