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Tiamulin alkali ointment and preparation method thereof

A technology of tiamulin base and tiamulin, which is applied in the direction of antibacterial drug, ointment delivery, emulsion delivery, etc., can solve the problems of failure to meet customer requirements, complicated process, cumbersome process, etc., and achieve safety and Guaranteed effectiveness, simple preparation process, and improved work efficiency

Active Publication Date: 2013-04-03
山东胜利生物工程有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the Tiamulin products currently produced at home and abroad are all tiamulin fumarate powder raw materials. The production process of tiamulin fumarate powder is complicated and the cost is high, and the production process of tiamulin fumarate powder raw materials has already been completed. It is very mature, and has basically reached a high level in terms of product yield and quality, and it is difficult to improve quality and yield through technological innovation
[0003] Nowadays, there are many domestic and foreign companies producing tiamulin fumarate powder raw materials, no other tiamulin drugs have appeared, and the market competitiveness of tiamulin is strong. In addition, tiamulin fumarate powder The preparation of raw materials requires salt formation and crystallization, and the process is cumbersome, and the current market is full of tiamulin fumarate powder raw materials, and the product is single, which cannot meet the requirements of all customers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Take 2L of tiamulin alkali solution, the content of tiamulin alkali is 21.5%, add 2L of water, stir and add 98% concentrated sulfuric acid to adjust the pH to 3.0, after standing for 2 hours, collect a total of 2.1L from the water phase, and recover the solvent from the ketone phase;

[0029] Add 2.1L tetramethyldipentanone to 2.1L water phase, then add 40wt% NaOH solution to adjust the pH to 12.0, and separate the ketone phase 2.2L after standing for 2 hours;

[0030] Turn on the vacuum rotary evaporation equipment, raise the temperature of the tiamulin alkali solution to 70°C, and carry out concentrated evaporation. The vacuum degree is -0.07~-0.09MPa, 1.7L is evaporated, and the remaining solution is 0.5L;

[0031] The tiamulin alkali solution is cooled at a rate of 8-10°C / h. When the temperature drops to 20°C, add 3.5g of propyl gallate and 5.2g of butylparaben, and stir for 1h;

[0032] Continue to cool down to 0°C at a rate of 3-5°C / h, and after holding at 0°C for...

Embodiment 2

[0036] Take 4L of tiamulin alkali solution with a content of 19%, add 4L of water, stir and add 85% phosphoric acid to adjust the pH to 4.0, after standing for 2 hours, collect a total of 4.3L from the water phase, and recover the solvent from the ketone phase;

[0037] Add 4.3L tetramethyldipentanone to 4.3L water phase, then add 40% NaOH solution to adjust the pH to 12.5, and separate the ketone phase 4.5L after standing for 2 hours;

[0038] Turn on the vacuum rotary evaporation equipment, raise the temperature of the tiamulin alkali solution to 75°C, and carry out concentrated evaporation. The vacuum degree is -0.07~-0.09MPa, 3.6L is evaporated, and the remaining solution is 0.9L;

[0039] The tiamulin alkali solution was cooled at a rate of 8-10°C / h. When the temperature dropped to 15°C, 8.4g of propyl gallate and 11.4g of butylparaben were added and stirred for 1h;

[0040] Continue to cool down to 0°C at a rate of 3-5°C / h, and after holding at 0°C for 2~3 hours, take sa...

Embodiment 3

[0044] Take 2L of tiamulin alkali solution, the content of tiamulin is 24%, add 3L of water, stir and add 40% hydrochloric acid to adjust the pH to 5.0, after standing for 2 hours, collect a total of 3.2L from the water phase, and recover the solvent from the ketone phase;

[0045] Add 4.8L tetramethyldipentanone to 3.2L water phase, then add 30wt% KOH solution to adjust the pH to 13.0, and separate the ketone phase 5.0L after standing for 2 hours;

[0046] Turn on the vacuum rotary evaporation equipment, raise the temperature of the tiamulin alkali solution to 70°C, and carry out concentrated evaporation. The vacuum degree is -0.07~-0.09MPa, 4.4L is evaporated, and the remaining solution is 0.6L;

[0047] The tiamulin alkali solution was cooled at a rate of 8-10°C / h. When the temperature dropped to 10°C, 6.7g of propyl gallate and 8.6g of butylparaben were added and stirred for 1h;

[0048] Continue to cool down to 0°C at a rate of 3-5°C / h, and after holding at 0°C for 2~3 ho...

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Abstract

The invention discloses a tiamulin alkali ointment and a preparation method thereof. The tiamulin alkali ointment comprises the following components in percentage by weight:75-85% of tiamulin, 0.8-1.4% of propylgallate, 1.2-1.8% of butylparaben and the balance of solvent. The invention provides a liquid tiamulin alkali ointment and provides a new option for the tiamulin crude drug. The ointment preparation process disclosed by the invention is simple; compared with the preparation method of tiamulin fumarate powder crude drug, the steps of salifying, crystallizing, drying, breaking and the like are omitted, so that the working efficiency is greatly enhanced, the labor strength is reduced and the production cost is reduced; after the special auxiliary material is added into the product, the safety and effectiveness are well guaranteed; and the preparation method disclosed by the invention is more suitable for industrialized mass production.

Description

technical field [0001] The invention relates to a raw material drug of tiamulin and its preparation, in particular to a tiamulin alkali ointment and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Tiamulin is a diterpene (pluromulin) antibiotic, which has special effects on many Gram-positive bacteria and Mycoplasma (Mycoplasma). Maintaining a high concentration in the respiratory tract, especially has a strong effect on Staphylococcus aureus, Streptococcus, various mycoplasma and some spirochetes, and this drug has been widely used in the world. However, the Tiamulin products currently produced at home and abroad are all tiamulin fumarate powder raw materials. The production process of tiamulin fumarate powder is complicated and the cost is high, and the production process of tiamulin fumarate powder raw materials has already been completed. It is very mature and has basically reached a relatively high level in term...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/22A61P31/04
Inventor 张宗鹏王振华杜敏辉郭文营张巨平张翠芬景巍李玉清
Owner 山东胜利生物工程有限公司
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