CN1507864A - Endermatic feeding preparation of anti parastic medicine containing benzimidazole - Google Patents
Endermatic feeding preparation of anti parastic medicine containing benzimidazole Download PDFInfo
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- CN1507864A CN1507864A CNA021566933A CN02156693A CN1507864A CN 1507864 A CN1507864 A CN 1507864A CN A021566933 A CNA021566933 A CN A021566933A CN 02156693 A CN02156693 A CN 02156693A CN 1507864 A CN1507864 A CN 1507864A
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- albendazole
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Abstract
The present invention relates to a sprinkling preparation containing benzimidazole medicine for preventing and curing animal parasitic helminthiasis. Its composition comprises (a) inorganic acid salt or organic acid salt of benzimidazole medicine 1-20 (W/V), (2). transdermal promotor 1-60% (V/V); and (c) diluting agent or solvent added to 100% (V/V) or antiparasitic medicine benzimidazole 1-20% (W/V), transdermal promotor 1-60 % (V/V) and diluting agent and organic solvent containing inorganic acid or organic acid added to 100% (V/V).
Description
The benzimidazole anti-parasite medicine is dissolving hardly in water, also is difficult to dissolving in most of medical solvents, therefore, is difficult to be prepared into solution-type non-intestinal drug delivery agent (as injection or dashing agent).After some benzimidazole medicines and organic acid or inorganic acid reaction formation salt, great changes have taken place for its dissolubility.This experiment shows, after albendazole (albendazole), albendazole sulfoxide (albendazole oxide), Phenbendasol (fenbendazole) or oxfendazole (oxfendazole) form hydrochlorate with hydrochloric acid reaction, or be under the condition of " cosolvent " with hydrochloric acid, dissolve in 1, organic solvents such as 2-propylene glycol, glycerol, Polyethylene Glycol, formal glycerine, and in soluble in water (example hydrochloric acid albendazole sulfoxide).
Based on this, the present invention is prepared into acylate or inorganic acid salt with albendazole, albendazole sulfoxide, Phenbendasol or oxfendazole or under acid condition they in water-soluble or some organic solvents, further is prepared into percutaneous drug administration preparation (as dashing agent).Therefore, preparation of the present invention is different from the preparation of describing among patent US5925374 and the US6340672.
Formulation preparation method of the present invention is as follows:
Method 1:(a) albendazole, albendazole sulfoxide, Phenbendasol or oxfendazole are dissolved in contain in mineral acid or the organic acid solution, after treating its salify, make solution evaporation or add small amount of seeds and make it crystallize, filter, with the solids drying under reduced pressure, pulverize, promptly get albendazole, albendazole sulfoxide, Phenbendasol or oxfendazole's acylate or inorganic acid salt.Above-mentioned acylate that (b) will obtain or inorganic acid salt are dissolved in 12-propylene glycol or other medium and the auxiliary agent, promptly get preparation of the present invention.
Method 2: 1, add an amount of organic acid or mineral acid in the 2-propylene glycol equal solvent, add benzimidazole medicines such as albendazole again, stir and make it dissolving, add remaining media and auxiliary agent afterwards promptly.
Acetic acid, propanoic acid, lactic acid or Albendazole oxide monohydrochloride and hydrochloric acid, lactic acid or acetic acid oxfendazole's preparation also can the directly oxidation acquisition under acid condition with its corresponding precursor albendazole or Phenbendasol.
The dashing agent of optimization of the present invention consists of:
(a) inorganic acid salt of benzimidazole or acylate 1-20% (W/V)
(b) transdermal enhancer 1-60% (V/V)
(c) diluent or solvent add to 100% (V/V)
Or (a) benzimidazole anti-parasite medicine 1-20% (W/V)
(b) transdermal enhancer 1-60% (V/V)
(c) contain mineral acid or organic acid organic solvent and diluent and add to 100% (V/V)
Described transdermal enhancer comprises: surfactant (non-ionic surface active agent or ionic surfactant), azone class, contain the above organic acid of 8 carbon, decyl methyl sulfoxide etc.These transdermal enhancers have detailed description in " percutaneous drug administration preparation " (Chinese Medicine science and technology publishing house,, 127-163 page or leaf in 1992) book of Liang Bingwen chief editor.Described solvent or diluent comprise: dimethyl acetylamide, dimethyl formamide, N-methyl-ketopyrrolidine, 1,2-propylene glycol, Polyethylene Glycol (low-molecular-weight), formal glycerine, glycerol, second alcohol and water.
The preparation of optimization of the present invention consists of:
(a) albendazole sulfoxide or oxfendazole's acylate or inorganic acid salt 2-10% (W/V)
(b) azone 2-3.5% (V/V)
(c) N-methyl-ketopyrrolidine or dimethyl acetylamide or they and ethanol use in conjunction
20-70％(V/V)
(d) 1, the 2-propylene glycol adds to 100% (V/V)
The preparation that the present invention further optimizes consists of:
(a) Albendazole oxide monohydrochloride or oxfendazole chloride 3-7.5% (W/V)
(b) N-methyl-ketopyrrolidine and ethanol 40-60% (V/V)
(c) azone 3.5% (V/V)
(d) 1, the 2-propylene glycol adds to 100% (V/V)
The present invention is special, and the preparation of optimizing consists of;
(a) Albendazole oxide monohydrochloride or oxfendazole chloride 5% (W/V)
(b) N-methyl-ketopyrrolidine 40% (V/V)
(c) ethanol 20% (V/V)
(d) azone 3.5% (V/V)
(e) 1, the 2-propylene glycol adds to 100% (V/V)
In preparation of the present invention, with 1,2-propylene glycol or formal glycerine or 1,2-propylene glycol/formal glycerine cosolvent are the hydrochloric albendazole of medium preparation or hydrochloric acid Phenbendasol or oxfendazole chloride's liquid preparation, also are suitable for injection or oral administration.Preferred preparation consists of: hydrochloric acid albendazole or oxfendazole chloride or hydrochloric acid Phenbendasol 10～20% (W/V), 1,2-propylene glycol or formal glycerine or use in conjunction add to 100% (V/V).This agent is used for cattle, sheep parasite control.Oral or drug administration by injection dosage is 1-10mg/kg.b.w
With example preparation of the present invention is described below, but example do not limit the scope of the invention, scope of the present invention and core content are determined according to claims.
Example one: the dashing agent of hydrochloric albendazole sulfoxide 5%
Get Albendazole oxide monohydrochloride 5.5g, add 40ml N-methyl-ketopyrrolidine and make it dissolving, after mass crystallization to be had is separated out, add 20ml ethanol, 40ml 1 again, 2-propylene glycol and 3.5ml azone make it dissolving, promptly get this dashing agent.
This preparation is used for the anthelmintic control of animals such as pig, sheep, cat, Canis familiaris L., pours in the back, and 1-4kg body weight using dosage is 1-2ml.
Example two: the dashing agent of hydrochloric albendazole sulfoxide 10%
Get Albendazole oxide monohydrochloride 11g, add 30ml N-methyl-ketopyrrolidine and 30ml dimethyl acetylamide and make it dissolving, after mass crystallization to be had is separated out, add 10ml ethanol and 4ml azone again, add 1, the 2-propylene glycol makes it dissolving to 100ml, promptly gets this dashing agent.
This preparation is used for the control of cattle parasitic worm, and the back pours, and 10kg body weight using dosage is 1-3ml.
Example three: hydrochloric oxfendazole's 7.5% dashing agent
Get oxfendazole chloride 8g, add 30ml N-methyl-ketopyrrolidine, 30ml dimethyl acetylamide, 10ml ethanol and 4ml azone, add 1, the 2-propylene glycol makes it dissolving to 100ml, promptly gets this dashing agent.
This preparation is used for the control of cattle parasitic worm, and the back pours, and 10kg body weight using dosage is 1-2ml.
Example four: hydrochloric oxfendazole's 15% liquid preparation
Get oxfendazole chloride 16g, add 30ml formal glycerine, 20mlPEG-200, add 1, the 2-propylene glycol makes it dissolving to 100ml, promptly gets this liquid preparation.
This preparation is used for cattle, the control of sheep parasitic worm, oral or injection, and 30-60kg body weight using dosage is 1ml.
Claims (10)
1, a kind of dashing agent that contains the benzimidazole medicine is characterized in that preparation consists of:
(a) inorganic acid salt of benzimidazole medicine or acylate 1-20% (W/V)
(b) transdermal enhancer 1-60% (V/V)
(c) diluent or solvent add to 100% (V/V)
Or (a) benzimidazole anti-parasite medicine 1-20% (W/V)
(b) transdermal enhancer 1-60% (V/V)
(c) contain mineral acid or organic acid organic solvent and diluent and add to 100% (V/V)
2, by the described preparation of claim 1, it is characterized in that the preferred albendazole of described benzimidazole medicine, albendazole sulfoxide, Phenbendasol or oxfendazole.
3,, it is characterized in that described organic acid or mineral acid or be used for the inorganic acid salt of synthesizing benzimidazole class medicine and the organic acid or the mineral acid of acylate comprises acetic acid, propanoic acid, lactic acid and hydrochloric acid by the described preparation of claim 1.
4, by the described preparation of claim 1, it is characterized in that described transdermal enhancer, solvent and diluent comprise: surfactant (non-ionic surface active agent or ionic surfactant), azone class, contain 8 carbon above organic acid, decyl methyl sulfoxide, dimethyl acetylamide, dimethyl formamide, N-methyl-ketopyrrolidine, ethanol, 1,2-propylene glycol, glycerol, low-molecular-weight Polyethylene Glycol, formal glycerine and water.
5, by the described preparation of claim 1, it is characterized in that the preparation of optimizing consists of:
(a) albendazole sulfoxide or oxfendazole's acylate or inorganic acid salt 2-10% (W/V)
(b) azone 2-3.5% (V/V)
(c) N-methyl-ketopyrrolidine or dimethyl acetylamide or they and ethanol use in conjunction
20-70％(V/V)
(d) 1, the 2-propylene glycol adds to 100% (V/V)
6, by the described preparation of claim 5, it is characterized in that the preparation of optimizing consists of:
(a) Albendazole oxide monohydrochloride or lactic acid albendazole sulfoxide 3-7.5% (W/V)
(b) N-methyl-ketopyrrolidine and ethanol 40-60% (V/V)
(c) azone 3.5% (V/V)
(d) 1, the 2-propylene glycol adds to 100% (V/V)
7, by the described preparation of claim 5, it is characterized in that the preparation of optimizing consists of:
(a) hydrochloric acid or lactic acid oxfendazole 3-7.5% (W/V)
(b) N-methyl-ketopyrrolidine and ethanol 40-60% (V/V)
(c) azone 3.5% (V/V)
(d) 1, the 2-propylene glycol adds to 100% (V/V)
8,, it is characterized in that the preparation of further optimizing consists of by claim 6 and 7 described preparations:
(a) Albendazole oxide monohydrochloride or oxfendazole chloride 5% (W/V)
(b) N-methyl-ketopyrrolidine 40% (V/V)
(c) ethanol 20% (V/V)
(d) azone 3.5% (V/V)
(e) 1, the 2-propylene glycol adds to 100% (V/V)
9, by the described preparation of claim 8, it is characterized in that described preparation is used for the control of animal parasitic worm, pour in back part of animal, using dosage is 3-30mg/kg b.w.; The Sq of Albendazole oxide monohydrochloride is 15-30mg/kg b.w.; Oxfendazole chloride's Sq is 5-20mg/kg b.w..
10, press the preparation of claim 1, but it is characterized in that said preparation removes percutaneous dosing, also can oral or drug administration by injection.The preparation of optimizing consists of: hydrochloric acid albendazole or hydrochloric acid Phenbendasol or oxfendazole chloride 10-20% (W/V), and 1,2-propylene glycol or formal glycerine or use in conjunction add to 100% (V/V).Can add N-methyl-ketopyrrolidine of 10～30% in case of necessity.The suitable consumption of cattle, sheep injection or oral agent is 1-10mg/kgb.w.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021566933A CN1507864A (en) | 2002-12-19 | 2002-12-19 | Endermatic feeding preparation of anti parastic medicine containing benzimidazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021566933A CN1507864A (en) | 2002-12-19 | 2002-12-19 | Endermatic feeding preparation of anti parastic medicine containing benzimidazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1507864A true CN1507864A (en) | 2004-06-30 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA021566933A Pending CN1507864A (en) | 2002-12-19 | 2002-12-19 | Endermatic feeding preparation of anti parastic medicine containing benzimidazole |
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| CN (1) | CN1507864A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101536983B (en) * | 2009-04-23 | 2011-06-01 | 华中农业大学 | Albendazole oxide hydrochloride premix for animals |
| CN101312727B (en) * | 2005-09-15 | 2011-10-05 | 梅瑞尔有限公司 | Anti-worm formulation |
-
2002
- 2002-12-19 CN CNA021566933A patent/CN1507864A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101312727B (en) * | 2005-09-15 | 2011-10-05 | 梅瑞尔有限公司 | Anti-worm formulation |
| CN101536983B (en) * | 2009-04-23 | 2011-06-01 | 华中农业大学 | Albendazole oxide hydrochloride premix for animals |
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