CN103845327A - Broad-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases - Google Patents
Broad-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases Download PDFInfo
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- CN103845327A CN103845327A CN201210510365.XA CN201210510365A CN103845327A CN 103845327 A CN103845327 A CN 103845327A CN 201210510365 A CN201210510365 A CN 201210510365A CN 103845327 A CN103845327 A CN 103845327A
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Abstract
The invention relates to a b road-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases and a preparation method of the solution. The solution comprises the following components in percentage by mass: 0.5-1 percent of closantel sodium, 0.5-1 percent of fenbendazole, 40-70 percent of propylene glycol, 15-30 percent of isopropanol, 10-20 percent of polyethylene glycol, 1-5 percent of glycerinum, and 2-5 percent of azone, wherein the main drug is prepared by dissolving, mixing, filtering and filling. Compared with a traditional anti-parasitic medicine, the broad-spectrum effective anti-parasitic transdermal solution can be used for improving absorption of skin to medicines and avoiding the first-pass effect of liver, and can reach a target position to achieve a better clinical effect.
Description
Technical field
The present invention relates to the compound closantel sodium transdermal solution of a kind of wide spectrum parasiticide disease.Belong to field of veterinary.
Background technology
Closantel sodium (Closantel Sodium) is anti-parasite medicine, calls as CLOSANTEL BASE Tech .98min sodium salt, closantel sodium salt, and chemical name is the chloro-4[(4-chlorphenyl of N-{5-) cyanogen methyl]-2-tolyl }-2-hydroxyl-3,5-diiodo-benzene formyl sodium salt.Character is buff powder, odorless.Easily molten in ethanol or acetone, in methanol, dissolve, insoluble in water or chloroform, be mainly used in preventing cattle, sheep distoma hepaticum, Biocontrol of Gastrointestinal Nematodes and oestriasis etc.This product all has to cattle, sheep fasciola, haemonchus contortus and some arthropod the activity of expeling.To most gastrointestinal nematode parasites, Bunostomum trigonoce phalum, Oesophagostomum, expeling rate all exceedes 90%.Closantel sodium can effectively be driven away dog ancylostome, and the common strongylid that also can prevent or reduce horse infects.In addition, this medicine all has 100% killing effect to one, two, three phase sheep nose fly larvae, and bomb fly stageⅢlarvae is also had to better repelling and killing efficacy.Its pest-resistant mechanism is by increasing parasite mitochondria permeability, oxidative phosphorylation being carried out to uncoupling, thereby effect is killed in performance.After absorption, be distributed widely in body tissue, the half-life reaches 14.5 days, and the highest with concentration in liver, fat, nephridial tissue, and drug main will be discharged through feces (80%), and the medicine of less than 0.5% excretes through urine.
Fenbendazole is the novel benzimidazoles anthelmintic of wide spectrum, efficient, low toxicity.It not only has height anthelmintic activity to animal gastrointestinal tract nematicide adult, larva, and net filaria, fasciola lanceolata, fasciola and cestode are also had to better effect.Fenbendazole abroad, not only for various animals, even also has the special preparation of wild animal.
Anti-parasite medicine for animals mostly is powder, solution etc. in the market, preparation capable of permeating skin is a kind of new form of administration, this dosage form has been avoided first pass effect of hepar and medicine and the gastrointestinal interaction of medicine, and can produce constant controlled blood drug level, reduces the toxic and side effects of medicine; Therefore in order to enrich clinical application, developed the transdermal solution of the parasiticide disease of new wide spectrum.
Summary of the invention
Based on above-mentioned situation, the object of this invention is to provide the compound closantel sodium transdermal solution of a kind of wide spectrum parasiticide disease.
Another object of the present invention is to provide a kind of preparation method of described compound closantel sodium transdermal solution.
A kind of antiparasitic compound closantel sodium transdermal solution for wide spectrum, it is characterized in that, forming component and weight mass fraction thereof is respectively: closantel sodium 0.5%-1%, Phenbendasol 0.5%-1%, propylene glycol 40%-70%, dimethyl sulfoxide 10%-20%, isopropyl alcohol 15%-30%, PEG400 10%-20%, glycerol 1%-5%, azone 2%-5%.
A preparation method for antiparasitic compound closantel sodium transdermal solution for wide spectrum, is characterized in that, the step of preparation is: a small amount of propylene glycol of closantel sodium of getting recipe quantity dissolves, and makes solution A; Get the Phenbendasol of recipe quantity with the dmso solution of recipe quantity, make solution B; A solution is mixed with B solution, add isopropyl alcohol, PEG400, glycerol, the azone of recipe quantity, stir, use propylene glycol standardize solution; By the solution filtering with microporous membrane obtaining, the qualified rear fill of clarity, obtains compound closantel sodium transdermal solution.
Described microporous filter membrane is 1-5 μ m.
Skin forms the barrier that is difficult to together infiltration to most drug, transdermal is more difficult.Azone is the current generally acknowledged good Percutaneous absorption enhancer of one, and the lipoid increase Drug Percutaneous Absorption that it mainly flows and dissolve skin by accelerating horny layer lipoid, is widely used in external preparation research.The present invention uses azone and dimethyl sulfoxide transdermal amount can reach more than 90% in 12h.Technique of the present invention is simple, and drug effect is remarkable, has made up the blank on house pet medicine market.
The specific embodiment
Embodiment 1:
A kind of antiparasitic compound closantel sodium transdermal solution for wide spectrum, forms component and weight mass fraction thereof and is respectively (carrying out proportioning by every 100g raw material):
Closantel sodium 1 g
Phenbendasol 0.5 g
Propylene glycol 50 g
Dimethyl sulfoxide 13.5 g
Isopropyl alcohol 15 g
PEG400 10 g
Glycerol 5 g
Azone 5 g
Preparation method: a small amount of propylene glycol of closantel sodium of getting recipe quantity dissolves, and makes solution A; Get the Phenbendasol of recipe quantity with the dmso solution of recipe quantity, make solution B; A solution is mixed with B solution, add isopropyl alcohol, PEG400, glycerol, the azone of recipe quantity, stir, be settled to 100ml with propylene glycol; By 2 μ m filtering with microporous membranes for the solution obtaining, the qualified rear fill of clarity, obtains compound closantel sodium transdermal solution.
Claims (3)
1. the compound closantel sodium transdermal solution of a broad-spectrum anti-parasite, it is characterized in that, forming component and weight mass fraction thereof is respectively: closantel sodium 0.5%-1%, Phenbendasol 0.5%-1%, propylene glycol 40%-70%, dimethyl sulfoxide 10%-20%, isopropyl alcohol 15%-30%, PEG400 10%-20%, glycerol 1%-5%, azone 2%-5%.
2. according to the preparation method of the compound closantel sodium transdermal solution of a kind of broad-spectrum anti-parasite described in claims 1, it is characterized in that, the step of preparation is: a small amount of propylene glycol of closantel sodium of getting recipe quantity dissolves, and makes solution A; Get the Phenbendasol of recipe quantity with the dmso solution of recipe quantity, make solution B; A solution is mixed with B solution, add isopropyl alcohol, PEG400, glycerol, the azone of recipe quantity, stir, use propylene glycol standardize solution; By the solution filtering with microporous membrane obtaining, the qualified rear fill of clarity, obtains compound closantel sodium transdermal solution.
3. according to the preparation method of the compound closantel sodium transdermal solution of a kind of broad-spectrum anti-parasite described in claims 2, it is characterized in that: described microporous filter membrane is 1-5 μ m.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210510365.XA CN103845327A (en) | 2012-12-04 | 2012-12-04 | Broad-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201210510365.XA CN103845327A (en) | 2012-12-04 | 2012-12-04 | Broad-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases |
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| CN103845327A true CN103845327A (en) | 2014-06-11 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201210510365.XA Pending CN103845327A (en) | 2012-12-04 | 2012-12-04 | Broad-spectrum compound closantel sodium transdermal solution for resisting parasitic diseases |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112294793A (en) * | 2020-10-21 | 2021-02-02 | 青岛海洋生物医药研究院股份有限公司 | Use of closantel or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the prevention and/or treatment of a coronavirus infection |
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2012
- 2012-12-04 CN CN201210510365.XA patent/CN103845327A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112294793A (en) * | 2020-10-21 | 2021-02-02 | 青岛海洋生物医药研究院股份有限公司 | Use of closantel or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the prevention and/or treatment of a coronavirus infection |
| CN112294793B (en) * | 2020-10-21 | 2022-03-22 | 青岛海洋生物医药研究院股份有限公司 | Use of closantel or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the prevention and/or treatment of a coronavirus infection |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20140611 |