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Sulbenicillin sodium injection

A technology for sulfobenicillin sodium and injection, which is applied in the field of high-purity D(-)-sulfobenicillin sodium powder injection and its preparation, can solve the problems of unfavorable labor protection, low product purity, large adverse reactions, etc. Low cost, good curative effect, and the effect of reducing adverse reactions

Inactive Publication Date: 2013-07-10
辽宁科泰生物基因制药股份有限公司
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0013] Chinese patent CN101912365B discloses a preparation process of sulbenicillin sodium powder injection, sulbenicillin in the powder injection is sulbenicillin sodium containing a crystal water, D (-)-Sulbenicillin sodium content is 75%-99%, L(+)-Sulbenicillin sodium content is 1%-25%, product purity is low
[0014] Chinese patent CN101912370B discloses a preparation process of D(-)-sulfbenicillin sodium powder injection, the method is used in the preparation of D(-)-sulfbenicillin sodium Diethyl ether is used in the process, and there is also n-butanol extraction operation, which is time-consuming and expensive to produce
[0015] Chinese patent CN10194103B discloses a kind of preparation method of sulbenicillin sodium, uses a large amount of diethyl ether in the operation of this method, and adopts the operating procedure of n-butanol extraction, is unfavorable for Labor protection, time-consuming production, high cost, and low purity of the resulting product
[0017] Chinese patent CN101906108B discloses a sulbenicillin containing D(-)-sulbenicillin sodium and L(+)-sulbenicillin sodium at a ratio of 3:1 A sodium compound and a preparation method thereof, in which a large amount of diethyl ether is used and n-butanol extraction is used, which is not conducive to labor protection, time-consuming production, high cost, low purity of the obtained product, low activity, and large adverse reactions
[0019] Chinese patent CN102161667B discloses a preparation process of sulfbenicillin sodium using 6-APA and N, O-bistrimethylsilylacetamide to form an organic salt dissolved in di Chloromethane, triethylamine sulfophenylacetic acid and pivaloyl chloride are used to make mixed anhydrides, anhydrous condensation is carried out in dichloromethane, and then freeze-dried with sodium to obtain the finished product. The product obtained by this method is not high-purity D(- )-Sulbenicillin Sodium, while the yield of this method is low
[0020] After a lot of systematic creative research work, the inventor obtained sterile D(-)-sulfonylbenzyl with higher purity, white color, good properties and low production cost Cillin sodium, creatively solves the existing technical problems, and has a significant improvement compared with the existing technology. The production materials and operations used have produced unexpected results. So far, there have been no relevant reports and public use at home and abroad.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 Preparation of sterile sulbenicillin sodium raw materials:

[0065]1) Preparation of D(-)-α-sulfophenylacetic acid: Weigh 50kg of (±)-α-sulfophenylacetic acid, dissolve it in 500L of water, add 40.58kg of D-p-hydroxyphenylglycine (the molar ratio of feed is 1: 1.05), heated to 60°C, stirred for 2 hours, cooled to 20°C, filtered, collected the filtrate, adjusted the pH to 6.5 with 1mol / L sodium hydroxide, filtered, and collected the solid D-p-hydroxyphenylglycine in another device for reuse, the filtrate Concentrate to dryness, add 250L ethanol, adjust pH to 1.5 with concentrated hydrochloric acid, stir for 1 hour, add 50L acetone, precipitate solid matter, filter to obtain 21.55kg of D(-)-α-sulfophenylacetic acid, yield 86.2%, HPLC content 96.8%;

[0066] 2) Preparation of D(-)-α-sulfophenylacetyl chloride: Dissolve 20kg of D(-)-α-sulfophenylacetic acid and 12L of triethylamine in 200L of methyl tert-butyl ether, stir and add chlorination Sulfoxide 6.7L, co...

Embodiment 2

[0069] Example 2 Sulbenicillin Sodium Powder Injection (0.5g specification)

[0070] Sulbenicillin Sodium Sterile Powder 5kg

[0071] -------------------------------------------------- --

[0072] 10,000 made

[0073] Preparation method:

[0074] (1) Bottle washing and sterilization: Take the soda-lime glass injection bottle, rinse it with drinking water, and irradiate it with ultraviolet light for 30 minutes, then enter the bottle washing machine, rinse it with water for injection, blow off the residual water with compressed air, and enter the 330°C tunnel The oven is dried, sterilized, and cooled for later use;

[0075] (2) Cleaning and sterilization of rubber stoppers: take bromobutyl rubber stoppers, rough wash with purified water, rinse, then finely wash with water for injection, dry and sterilize for later use;

[0076] (3) Clean and sterilize the aluminum cap for the injection bottle: take the aluminum cap and put it into the alumi...

Embodiment 3

[0081] Example 3 Sulbenicillin Sodium Powder Injection (1.0g specification)

[0082] Sulbenicillin Sodium Sterile Powder 10kg

[0083] -------------------------------------------------- ----

[0084] 10,000 made

[0085] Preparation method:

[0086] (1) Bottle washing and sterilization: Take the soda-lime glass injection bottle, rinse it with drinking water, and irradiate it with ultraviolet light for 30 minutes, then enter the bottle washing machine, rinse it with water for injection, blow off the residual water with compressed air, and enter the 330°C tunnel The oven is dried, sterilized, and cooled for later use;

[0087] (2) Cleaning and sterilization of rubber stoppers: take bromobutyl rubber stoppers, rough wash with purified water, rinse, then finely wash with water for injection, dry and sterilize for later use;

[0088] (3) Clean and sterilize the aluminum cap for the injection bottle: take the aluminum cap and put it into the alu...

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Abstract

The invention provides sulbenicillin sodium injection. Freeze-dried sterile sulbenicillin sodium is used as a raw material and prepared into a product free of any solid auxiliary material or excipient by virtue of a sterile sub-packaging process; in terms of anhydrous substances, the content of the D(-)-sulbenicillin sodium is bigger than 99%, the content of the L(+)-sulbenicillin sodium is smaller than 0.5%, the content of the sulbenicillin sodium polymer is smaller than 0.3% and the content of moisture is smaller than 5%. Moreover, the sulbenicillin sodium injection has high product purity, strong anti-bacterial activity and good stability, so that medication safety of the human body can be ensured better.

Description

technical field [0001] The invention relates to an injection of sulfbenicillin sodium, which belongs to the technical field of pharmacy, and more specifically relates to a high-purity D(-)-sulfbenicillin sodium powder injection and a preparation method thereof. Background technique [0002] Sulbenicillin sodium is a semi-synthetic penicillin, which was first developed by the Japanese Takeda Pharmaceutical Company Research Institute. It was included in the Chinese Pharmacopoeia in 1990 and included in the "National Basic Medical Insurance Drug Catalog" by the Chinese government in 2009. Compared with other types of penicillins, it has a broad antibacterial spectrum. , High stability to β-lactamase, good in vivo absorption and bioavailability, etc., and it is effective against Gram-negative bacteria such as Pseudomonas aeruginosa, Proteus, Influenza Bacillus, Enterobacter, Staphylococcus, Streptococcus It has antibacterial activity against Gram-positive bacteria; it is also ac...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/19A61K31/43A61P31/04
Inventor 张侠黄玉新王斐鹤潘晓旭张春萍李斌周娜曹晓峰
Owner 辽宁科泰生物基因制药股份有限公司
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