CN106075458A - Moxidectin preparation and preparation method thereof - Google Patents
Moxidectin preparation and preparation method thereof Download PDFInfo
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- CN106075458A CN106075458A CN201610404280.1A CN201610404280A CN106075458A CN 106075458 A CN106075458 A CN 106075458A CN 201610404280 A CN201610404280 A CN 201610404280A CN 106075458 A CN106075458 A CN 106075458A
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- moxidectin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
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- Health & Medical Sciences (AREA)
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- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
The invention discloses a kind of moxidectin preparation and preparation method thereof, wherein, described preparation method includes: is inoculated in culture medium by cyaneogriseus streptomyces strain and cultivates, obtains suspension M；Described suspension M is carried out sucking filtration, obtains filter cake N；Described filter cake N is dried, obtains dry mycelium；By described dry mycelium and methanol mixed, it is filtrated to get lixiviating solution；Described lixiviating solution is obtained moxidectin through overprotection reaction, oxidation reaction and oximation reaction；Water, described moxidectin, first propanol, ethyl acetate and surfactant being mixed, obtain described moxidectin preparation, the killing rate solving traditional moxidectin preparation is relatively low, and preparation is the most volatile after using simultaneously, the problem easily causing secondary pollution.
Description
Technical field
The present invention relates to moxidectin preparation field, in particular it relates to moxidectin preparation and preparation method thereof.
Background technology
Moxidectin is a kind of novel antiparasitic, is by the Macrolide antibiosis of the single component of streptomycete fermentation
Element, this type of antiparasitic is widely used in the agricultural of the basis such as animal husbandry, aquaculture.The parasite killing of traditional moxidectin preparation
Rate is relatively low, and preparation is the most volatile after using simultaneously, easily causes secondary pollution.
Therefore it provides a kind of killing rate is high and after use, volatile moxidectin preparation and preparation method thereof is this
The bright problem needing solution badly.
Summary of the invention
It is an object of the invention to provide a kind of moxidectin preparation and preparation method thereof, solve traditional moxidectin system
The killing rate of agent is relatively low, and preparation is the most volatile after using simultaneously, the problem easily causing secondary pollution.
To achieve these goals, the invention provides the preparation method of a kind of moxidectin preparation, wherein, described preparation
Method includes:
(1) cyaneogriseus streptomyces strain is inoculated in culture medium cultivates, obtain suspension M；
(2) described suspension M is carried out sucking filtration, obtain filter cake N；
(3) described filter cake N is dried, obtain dry mycelium；
(4) by described dry mycelium and methanol mixed, it is filtrated to get lixiviating solution；
(5) described lixiviating solution is obtained moxidectin through overprotection reaction, oxidation reaction and oximation reaction；
(6) water, described moxidectin, first propanol, ethyl acetate and surfactant are mixed, obtain described moxidectin
Preparation, wherein, relative to the water of 100 weight portions, the consumption of described moxidectin is 70-90 weight portion, the use of described first propanol
Amount is 20-40 weight portion, and the consumption of described ethyl acetate is 10-15 weight portion, and the consumption of described surfactant is 1-5 weight
Part.
The invention provides a kind of moxidectin preparation, described moxidectin preparation is prepared by above-mentioned preparation method.
By technique scheme, the invention provides the preparation method of a kind of moxidectin preparation, wherein, described preparation
Method includes: is inoculated in culture medium by cyaneogriseus streptomyces strain and cultivates, obtains suspension M；Described suspension M is carried out
Sucking filtration, obtains filter cake N；Described filter cake N is dried, obtains dry mycelium；By described dry mycelium and methanol mixed, filter
Obtain lixiviating solution；Described lixiviating solution is obtained moxidectin through overprotection reaction, oxidation reaction and oximation reaction；By water, described
Moxidectin, first propanol, ethyl acetate and surfactant mixing, obtain described moxidectin preparation, between each raw material
Synergism so that prepared moxidectin preparation possesses excellent killing ability, and preparation is volatile, does not results in secondary dirty
Dye, meanwhile, for preparing, the method for this moxidectin preparation is simple, raw material is easy to get.
Other features and advantages of the present invention will be described in detail in detailed description of the invention part subsequently.
Detailed description of the invention
Hereinafter the detailed description of the invention of the present invention is described in detail.It should be appreciated that described herein specifically
Embodiment is merely to illustrate and explains the present invention, is not limited to the present invention.
The invention provides the preparation method of a kind of moxidectin preparation, wherein, described preparation method includes: by bluish grey chain
Mold species is inoculated in culture medium and cultivates, and obtains suspension M；Described suspension M is carried out sucking filtration, obtains filter cake N；Will
Described filter cake N is dried, and obtains dry mycelium；By described dry mycelium and methanol mixed, it is filtrated to get lixiviating solution；By described
Lixiviating solution obtains moxidectin through overprotection reaction, oxidation reaction and oximation reaction；By water, described moxidectin, first propanol, second
Acetoacetic ester and surfactant mixing, obtain described moxidectin preparation, wherein, relative to the water of 100 weight portions, described Moses
The consumption of rhzomorph is 70-90 weight portion, and the consumption of described first propanol is 20-40 weight portion, and the consumption of described ethyl acetate is 10-
15 weight portions, the consumption of described surfactant is 1-5 weight portion.
The present invention one preferred embodiment in so that prepare moxidectin preparation possess the most excellent
Killing ability, relative to the water of 100 weight portions, the consumption of described moxidectin is 75-85 weight portion, the use of described first propanol
Amount is 25-35 weight portion, and the consumption of described ethyl acetate is 12-14 weight portion, and the consumption of described surfactant is 2-3 weight
Part.
The present invention one preferred embodiment in so that filter cake can fully be dried, simultaneously do not affect filter
Dry mycelium in cake, the temperature of described drying is 55-60 DEG C, and drying time is 5-10min.
The present invention one preferred embodiment in so that suspension M can keep higher concentration, convenient dry
Mycelial extraction, the time of described cultivation is 3-5 days, and cultivation temperature is 30-35 DEG C.
The present invention one preferred embodiment in so that cyaneogriseus streptomyces strain can the most more
Good growth, described culture medium selects LB culture medium.
So that the moxidectin preparation prepared possesses the most excellent killing ability, described surfactant is two pungent
One or more in base sodium sulfosuccinate, dodecylbenzene sodium sulfonate and sodium glycocholate.
Present invention also offers a kind of moxidectin preparation, described moxidectin preparation is prepared by above-mentioned preparation method.
Hereinafter will be described the present invention by embodiment.
Embodiment 1
Cyaneogriseus streptomyces strain is inoculated in LB culture medium and cultivates, obtain suspension M；Described suspension M is entered
Row sucking filtration, obtains filter cake N；Carry out described filter cake N drying (drying temperature 55 DEG C, time 5min), obtain dry mycelium；By institute
State dry mycelium and methanol mixed, be filtrated to get lixiviating solution；Described lixiviating solution is anti-through overprotection reaction, oxidation reaction and oximate
Moxidectin should be obtained；By moxidectin, 25g first propanol, 12g ethyl acetate and the acid of 2g dioctyl succinate described in 100g water, 75g
Sodium sulfonate mixes, and obtains moxidectin preparation A1.
Embodiment 2
Cyaneogriseus streptomyces strain is inoculated in LB culture medium and cultivates, obtain suspension M；Described suspension M is entered
Row sucking filtration, obtains filter cake N；Carry out described filter cake N drying (drying temperature 60 C, time 10min), obtain dry mycelium；Will
Described dry mycelium and methanol mixed, be filtrated to get lixiviating solution；By described lixiviating solution through overprotection reaction, oxidation reaction and oximate
Reaction obtains moxidectin；By moxidectin, 35g first propanol, 14g ethyl acetate and 3g detergent alkylate described in 100g water, 85g
Sodium sulfonate mixes, and obtains moxidectin preparation A2.
Embodiment 3
Cyaneogriseus streptomyces strain is inoculated in LB culture medium and cultivates, obtain suspension M；Described suspension M is entered
Row sucking filtration, obtains filter cake N；Carry out described filter cake N drying (drying temperature 58 DEG C, time 8min), obtain dry mycelium；By institute
State dry mycelium and methanol mixed, be filtrated to get lixiviating solution；Described lixiviating solution is anti-through overprotection reaction, oxidation reaction and oximate
Moxidectin should be obtained；Moxidectin, 30g first propanol, 13g ethyl acetate and 2.5g sodium glycocholate described in 100g water, 80g are mixed
Close, obtain moxidectin preparation A3.
Embodiment 4
Being prepared according to the method for embodiment 1, except for the difference that, the consumption of water is 100g, the consumption of described moxidectin
For 70g, the consumption of described first propanol is 20g, and the consumption of described ethyl acetate is 10g, described dioctyl succinate disulfonate acid
Consumption is 1g, obtains moxidectin preparation A4.
Embodiment 5
Being prepared according to the method for embodiment 3, except for the difference that, the consumption of water is 100g, the consumption of described moxidectin
For 90g, the consumption of described first propanol is 40g, and the consumption of described ethyl acetate is 15g, and the consumption of described sodium glycocholate is 5g,
To moxidectin preparation A5.
Comparative example 1
Being prepared according to the method for embodiment 1, except for the difference that, the consumption of water is 100g, the consumption of described moxidectin
For 60g, the consumption of described first propanol is 10g, and the consumption of described ethyl acetate is 5g, the use of described dioctyl succinate disulfonate acid
Amount is 0.5g, obtains moxidectin preparation D1.
Comparative example 2
Being prepared according to the method for embodiment 3, except for the difference that, the consumption of water is 100g, the consumption of described moxidectin
For 95g, the consumption of described first propanol is 45g, and the consumption of described ethyl acetate is 20g, and the consumption of described sodium glycocholate is 8g,
To moxidectin preparation D2.
Table 1
| Embodiment is numbered | Killing rate (%) |
| A1 | 95 |
| A2 | 92 |
| A3 | 96 |
| A4 | 85 |
| A5 | 88 |
| D1 | 65 |
| D2 | 70 |
By above table data it can be seen that within the scope of the present invention prepare moxidectin preparation A1-A5, its killing rate
It is higher than outside the scope of the invention moxidectin preparation D1 and D2 prepared, and the Moses prepared in currently preferred scope
Rhzomorph preparation A1-A3 possesses the most excellent killing ability.
The preferred embodiment of the present invention described in detail above, but, the present invention is not limited in above-mentioned embodiment
Detail, in the technology concept of the present invention, technical scheme can be carried out multiple simple variant, this
A little simple variant belong to protection scope of the present invention.
It is further to note that each the concrete technical characteristic described in above-mentioned detailed description of the invention, at not lance
In the case of shield, can be combined by any suitable means, in order to avoid unnecessary repetition, the present invention to various can
The compound mode of energy illustrates the most separately.
Additionally, combination in any can also be carried out between the various different embodiment of the present invention, as long as it is without prejudice to this
The thought of invention, it should be considered as content disclosed in this invention equally.
Claims (7)
1. the preparation method of a moxidectin preparation, it is characterised in that described preparation method includes:
(1) cyaneogriseus streptomyces strain is inoculated in culture medium cultivates, obtain suspension M；
(2) described suspension M is carried out sucking filtration, obtain filter cake N；
(3) described filter cake N is dried, obtain dry mycelium；
(4) by described dry mycelium and methanol mixed, it is filtrated to get lixiviating solution；
(5) described lixiviating solution is obtained moxidectin through overprotection reaction, oxidation reaction and oximation reaction；
(6) water, described moxidectin, first propanol, ethyl acetate and surfactant are mixed, obtain described moxidectin system
Agent, wherein, relative to the water of 100 weight portions, the consumption of described moxidectin is 70-90 weight portion, the consumption of described first propanol
For 20-40 weight portion, the consumption of described ethyl acetate is 10-15 weight portion, and the consumption of described surfactant is 1-5 weight
Part.
Preparation method the most according to claim 1, wherein, relative to the water of 100 weight portions, the consumption of described moxidectin
For 75-85 weight portion, the consumption of described first propanol is 25-35 weight portion, and the consumption of described ethyl acetate is 12-14 weight portion,
The consumption of described surfactant is 2-3 weight portion.
Preparation method the most according to claim 1, wherein, the temperature of described drying is 55-60 DEG C, and drying time is 5-
10min。
Preparation method the most according to claim 1, wherein, the time of described cultivation is 3-5 days, and cultivation temperature is 30-35
℃。
Preparation method the most according to claim 1, wherein, described culture medium selects LB culture medium.
Preparation method the most according to claim 1, wherein, described surfactant be dioctyl succinate disulfonate acid, ten
One or more in dialkyl benzene sulfonic acids sodium and sodium glycocholate.
7. a moxidectin preparation, it is characterised in that described moxidectin preparation is by described in any one in claim 1-6
Preparation method prepare.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610404280.1A CN106075458A (en) | 2016-06-08 | 2016-06-08 | Moxidectin preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610404280.1A CN106075458A (en) | 2016-06-08 | 2016-06-08 | Moxidectin preparation and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN106075458A true CN106075458A (en) | 2016-11-09 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610404280.1A Pending CN106075458A (en) | 2016-06-08 | 2016-06-08 | Moxidectin preparation and preparation method thereof |
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| Country | Link |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108096564A (en) * | 2017-12-29 | 2018-06-01 | 塔里木大学 | A kind of externally applied drug for preventing livestock and poultry vermin |
Citations (4)
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|---|---|---|---|---|
| CN1947507A (en) * | 2006-05-19 | 2007-04-18 | 东北农业大学 | Method for preparing microemulsion aqueous emulsion and suspending agent contg. Nimoctin and Mosictin |
| CN103127058A (en) * | 2011-11-29 | 2013-06-05 | 金坛市凌云动物保健品有限公司 | Moxidectin preparation and preparing method thereof |
| CN104846030A (en) * | 2015-05-07 | 2015-08-19 | 芜湖福民生物药业有限公司 | Preparation method of moxidectin |
| CN105079019A (en) * | 2015-08-31 | 2015-11-25 | 重庆布尔动物药业有限公司 | Compound ivermectin vitamin B oral liquid and preparation method thereof |
-
2016
- 2016-06-08 CN CN201610404280.1A patent/CN106075458A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1947507A (en) * | 2006-05-19 | 2007-04-18 | 东北农业大学 | Method for preparing microemulsion aqueous emulsion and suspending agent contg. Nimoctin and Mosictin |
| CN103127058A (en) * | 2011-11-29 | 2013-06-05 | 金坛市凌云动物保健品有限公司 | Moxidectin preparation and preparing method thereof |
| CN104846030A (en) * | 2015-05-07 | 2015-08-19 | 芜湖福民生物药业有限公司 | Preparation method of moxidectin |
| CN105079019A (en) * | 2015-08-31 | 2015-11-25 | 重庆布尔动物药业有限公司 | Compound ivermectin vitamin B oral liquid and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 计亮年等: "《生物无机化学导论》", 30 September 2001, 中山大学出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108096564A (en) * | 2017-12-29 | 2018-06-01 | 塔里木大学 | A kind of externally applied drug for preventing livestock and poultry vermin |
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Application publication date: 20161109 |
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