CN103070820A - Preparation method of compound anticoccidial medicine sulfachloropyrazine sodium solution - Google Patents

Preparation method of compound anticoccidial medicine sulfachloropyrazine sodium solution Download PDF

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Publication number
CN103070820A
CN103070820A CN 201110328661 CN201110328661A CN103070820A CN 103070820 A CN103070820 A CN 103070820A CN 201110328661 CN201110328661 CN 201110328661 CN 201110328661 A CN201110328661 A CN 201110328661A CN 103070820 A CN103070820 A CN 103070820A
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solution
preparation
nsc
medicine
cosolvent
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CN 201110328661
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栾明娜
郝智慧
王春元
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Qingdao Continent Pharmaceutical Co Ltd
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Qingdao Continent Pharmaceutical Co Ltd
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Priority to CN 201110328661 priority Critical patent/CN103070820A/en
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Abstract

The invention relates to a preparation method of a compound high-efficiency anticoccidial medicine sulfachloropyrazine sodium and diaveridine solution. The solution is provided mainly for overcoming defects such as mixing difficulty, inconvenient dosing, inaccurate dose, and the like of existing powders. The solution comprises main components of: main medicines of sulfachloropyrazine sodium and diaveridine, and auxiliary materials of dimethyl sulfoxide, N-methylpyrrolidone, a cosolvent, and triethanolamine. A preparation process provided by the invention comprises the steps that: dimethyl sulfoxide, N-methylpyrrolidone, and sulfachloropyrazine sodium are dissolved in a liquid blending tank; diaveridine well dissolved by the cosolvent is added; and triethanolamine with a formulated dose is added. The method has the advantages of simple production process, stable product quality, simple feeding method, and accurate dose.

Description

The preparation method of composite anti-coccidium medicine sulfaclozine sodium solution
Technical field
The present invention relates to the preparation method of a kind of compound high-efficient coccidiostat sulfaclozine sodium, NSC 408735 solution.
Background technology
Sulfaclozine sodium, chemistry N-(5-chloro-3-pyrazinyl by name)-4-aminobenzenesul fonamide sodium salt sulfuric monohydrate, molecular weight 324.72, molecular formula C 10H 8ClN 4NaO 2SH 2O, white or pale yellow powder; Tasteless.In water or methanol, dissolve, slightly soluble in ethanol or acetone, insoluble in chloroform.NSC 408735, chemistry 5-(3 by name, 4-veratryl)-2,4-thonzylamine, molecular weight 260.29, molecular formula C 13H 16N 4O 2, white or little yellow crystalline powder; Odorless almost.Soluble,very slightly in chloroform, insoluble in water, ethanol or ether; In hydrochloric acid, dissolve slightly soluble in dilute hydrochloric acid.Lipid LogP 3=1.
Coccidiosis is the parasitic disease that chicken is common and harm is very serious.At present, the Main Means of control chicken coccidiosis still relies on coccidiostat.But the use of coccidiostat has also brought some problems.A most outstanding problem is that coccidiosis is easy to medicine is produced drug resistance, it is reported that nearly all medicine has the appearance of drug-resistant worm plant.For fear of or delay the chemical sproof generation of coccidiosis, people adopt more increases drug level, by turns medication, the measures such as medication and matching medication of shuttling back and forth.Matching medication can increase the curative effect of medicine, reduces drug dose, reduces untoward reaction, also can delay chemical sproof generation, and can reduce the residual quantity of medicine.Therefore, the research of carrying out coccidiostat fit applications aspect has certain realistic meaning.
Trimethoprim is the diamino pyrimidines of synthetic, and its Antibacterial Mechanism is that the dihydrofolate reductase by anti-bacteria can not reduce dihydrofoilic acid to become tetrahydrofolic acid, thereby stops the nucleic acid metabolism of antibacterial, the growth and breeding of anti-bacteria.This class medicine and sulphonamides use in conjunction can make the antibacterial efficacy of sulphonamides strengthen, and present bactericidal action, and can enlarge the antibacterial range of sulphonamides.Sulphonamides and synergist are basic identical with it to the mechanism of action of coccidiosis.Sulfaclozine sodium, NSC 408735 solution mainly suppress the growth of coccidiosis second filial generation schizont, and first generation schizont is also had effect, and Peak of action is at metainfective the 4th day, and the coccidiosis of fowl, rabbit is had good prevention effect.How when breaking out, to use in coccidiosis.
The sulfaclozine soluble powder of sodium, as traditional anticoccidial drug, by a plurality of national extensive uses decades, produced at present more serious coccidiosis Drug resistance, for overcoming this phenomenon, carry out compatibility with the synergist NSC 408735 of sulphonamides, then can obtain comparatively ideal effect.Simultaneously, select solution to be studied, the reasons are as follows:
(1) on the mechanism of action, synthesizes but NSC 408735 and sulphonamides share the double blocking tetrahydrofolic acid, strengthen antibiotic (coccidiosis) effect several times and the decades of times of sulphonamides.The two compatibility not only can reduce the chemical sproof generation of coccidiosis, and the strain of anti-sulphonamides worm is also had effect;
(2)Why select solution but not soluble powder is because NSC 408735 is water insoluble, add if make the pre-mixing agent spice, have mixed inhomogeneous problem, easily cause poisoning; And the accurate dosage when selecting suitable adjuvant that this product is made solution and just greatly improved dispersibility behind the mixed water and administration by preparation technique, thereby increased the safety of administration;
(3)Under chicken morbidity or stress state, often having and searching for food decline or do not eat phenomenon, but general drinking-water is normal, pre-mixing agent just can not well be brought into play its pharmacologic action like this.The administration of solution drinking-water then can make chicken obtain enough doses, thereby the morbidity chicken is got timely medical treatment.
Compound sulfonamide chloropyrazine sodium solution there is not yet report at home and abroad or approval is used, and patent retrieval is there are no patent protection.
Summary of the invention
The object of the present invention is to provide the compound anti-parasitic medicine sulfaclozine sodium solution that a kind of processing technology is simple, the throwing clothes are convenient, anthelminthic effect is good.Ingredients of the present invention is sulfaclozine sodium, NSC 408735, dimethyl sulfoxide, N-Methyl pyrrolidone, cosolvent, triethanolamine.The degree of above-mentioned each component: sulfaclozine sodium 15%, NSC 408735 3%, dimethyl sulfoxide 15% ~ 25%, N-Methyl pyrrolidone 20% ~ 40%, cosolvent 1% ~ 5%, triethanolamine 5% ~ 10%.Preparation technology: dimethyl sulfoxide, N-Methyl pyrrolidone and sulfaclozine sodium poured in the Agitation Tank dissolve, add with cosolvent and dissolve good NSC 408735, the triethanolamine that adds at last formula ratio is regulated pH value (6.5-8.0).Medicinal liquid filters 100 ℃ of high temperature sterilize 30min through the micropore filter element of 0.45 μ m again.
The invention has the advantages that production technology is simple, constant product quality, but the room temperature placement was never degenerated in 2 years.This medicine is solution, than the more convenient administration of existing dispersant and easy for dividing dose, especially is fit to large-scale cultivation factory and uses the labor intensity in the time of can greatly alleviating people's administration.
The specific embodiment
Accurately weighing dimethyl sulfoxide 25L, N-Methyl pyrrolidone 40L and sulfaclozine sodium 15kg pour stirring at normal temperature in the Agitation Tank into, until dissolving, adding is dissolved good NSC 408735 3kg with cosolvent, regulate pH value (6.5-8.0) with triethanolamine at last, N-Methyl pyrrolidone is settled to 100L.Medicinal liquid filters through the micropore filter element of 0.45 μ m again, 100 ℃ of high temperature sterilize 30min and get final product.

Claims (3)

1. the preparation method of a compound high-efficient coccidiostat sulfaclozine sodium, NSC 408735 solution is characterized in that its component is sulfaclozine sodium, NSC 408735, dimethyl sulfoxide, N-Methyl pyrrolidone, cosolvent, triethanolamine.
2. a kind of compound high-efficient coccidiostat sulfaclozine sodium according to claim 1, NSC 408735 solution, it is characterized in that: the percentage composition of above-mentioned each component is: sulfaclozine sodium 15%, NSC 408735 3%, dimethyl sulfoxide 15% ~ 25%, N-Methyl pyrrolidone 20% ~ 40%, cosolvent 1% ~ 10%, triethanolamine 5% ~ 10%.
3. the preparation method of a kind of compound high-efficient coccidiostat sulfaclozine sodium according to claim 1, NSC 408735 solution, it is characterized in that: dimethyl sulfoxide, N-Methyl pyrrolidone and sulfaclozine sodium are poured in the Agitation Tank dissolved, adding is dissolved good NSC 408735 with cosolvent, and the triethanolamine that adds at last formula ratio is regulated pH value (6.5-8.0).
CN 201110328661 2011-10-26 2011-10-26 Preparation method of compound anticoccidial medicine sulfachloropyrazine sodium solution Pending CN103070820A (en)

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CN 201110328661 CN103070820A (en) 2011-10-26 2011-10-26 Preparation method of compound anticoccidial medicine sulfachloropyrazine sodium solution

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CN 201110328661 CN103070820A (en) 2011-10-26 2011-10-26 Preparation method of compound anticoccidial medicine sulfachloropyrazine sodium solution

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CN103070820A true CN103070820A (en) 2013-05-01

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102920716A (en) * 2012-11-02 2013-02-13 青岛康地恩药业股份有限公司 Method for preparing sulfachloropyrazine sodium solution serving as compound anti-coccidium medicine
CN116570556A (en) * 2023-05-17 2023-08-11 郑州福源动物药业有限公司 Compound sulfachlordazine sodium solution for treating escherichia coli and pasteurellosis infection of livestock and poultry and preparation method thereof

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102920716A (en) * 2012-11-02 2013-02-13 青岛康地恩药业股份有限公司 Method for preparing sulfachloropyrazine sodium solution serving as compound anti-coccidium medicine
CN102920716B (en) * 2012-11-02 2015-02-25 青岛蔚蓝生物股份有限公司 Method for preparing sulfachloropyrazine sodium solution serving as compound anti-coccidium medicine
CN116570556A (en) * 2023-05-17 2023-08-11 郑州福源动物药业有限公司 Compound sulfachlordazine sodium solution for treating escherichia coli and pasteurellosis infection of livestock and poultry and preparation method thereof
CN116570556B (en) * 2023-05-17 2023-11-07 郑州福源动物药业有限公司 Compound sulfachlordazine sodium solution for treating escherichia coli and pasteurellosis infection of livestock and poultry and preparation method thereof

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Application publication date: 20130501