CN109674739A - A kind of transdermal liniment and preparation method thereof for preventing and treating Yak parasitoses - Google Patents

A kind of transdermal liniment and preparation method thereof for preventing and treating Yak parasitoses Download PDF

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Publication number
CN109674739A
CN109674739A CN201910072142.1A CN201910072142A CN109674739A CN 109674739 A CN109674739 A CN 109674739A CN 201910072142 A CN201910072142 A CN 201910072142A CN 109674739 A CN109674739 A CN 109674739A
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China
Prior art keywords
transdermal
auxiliary material
praziquantel
preparation
liniment
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CN201910072142.1A
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Chinese (zh)
Inventor
李家奎
高兴
张丽鸿
参木有
罗晓林
石红梅
索朗斯珠
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Xizang Agriculture and Animal Husbandry College
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Xizang Agriculture and Animal Husbandry College
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Priority to CN201910072142.1A priority Critical patent/CN109674739A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention provides a kind of transdermal liniments for preventing and treating Yak parasitoses, belong to field of veterinary, the transdermal liniment includes praziquantel and auxiliary material;The mass volume ratio of the praziquantel and auxiliary material is 200~400mg:1mL;The auxiliary material includes the raw material of following volumes percentage: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 78%.Transdermal liniment of the invention passes through reasonable compatibility, overcomes that praziquantel dissolubility is poor, defect of transdermal effect difference;And transdermal liniment convenient drug administration of the invention, and can effectively play drug effect.

Description

A kind of transdermal liniment and preparation method thereof for preventing and treating Yak parasitoses
Technical field
The present invention relates to field of veterinary more particularly to a kind of transdermal liniment for preventing and treating Yak parasitoses and its preparation sides Method.
Background technique
Yak is the pillar industry of Qinghai-xizang Plateau Region Alpine Grasslands economic development, is the distinctive domestic animal kind in Qinghai-Tibet Platean One of.The existing yak in China nearly 14,000,000, it is mainly distributed on the provinces and regions such as Qinghai, Tibet, Sichuan, Gansu.Yak is as plateau The main body of grassland agriculture raises kind, has the status that do not replace in Tibetan husbandry production.The steady and sound of Industry of Yaks can Sustainable development plays an important role the development of entire Tibetan area economy.
For yak at present still based on traditional herd, parasitic disease is to endanger the disease the most serious of production of yak at present One of disease causes extremely serious loss to yak animal husbandry every year.Up to more than 20 kinds of helminth for endangering yak at present, wherein Especially with gastrointestinal nematode parasites, the harm such as bomb fly, echinococcus, burnt worm, fluke, tapeworm are serious.
Prevention and treatment Yak parasitoses are still using oral and drug administration by injection traditional approach at present, since the wild nature of yak is big It is low with the prevention and control consciousness of herdsman, in addition traditional administration mode herdsman's inconvenience is grasped, so that Yak parasitoses cannot be fine Control, cause huge economic loss.
Summary of the invention
The purpose of the present invention is to provide a kind of transdermal liniments and preparation method thereof for preventing and treating Yak parasitoses, this is transdermal Liniment convenient drug administration and it can effectively play drug effect.
In order to achieve the above-mentioned object of the invention, the present invention the following technical schemes are provided:
The present invention provides a kind of transdermal liniments for preventing and treating Yak parasitoses, including praziquantel and auxiliary material;The pyrrole quinoline The mass volume ratio of ketone and auxiliary material is 200~400mg:1mL;The auxiliary material includes the raw material of following volumes percentage: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 78%.
Preferably, the mass volume ratio of the praziquantel and auxiliary material is 280~350mg:1mL.
The present invention also provides the preparation method of the transdermal liniment described in above scheme, steps are as follows: by auxiliary material and praziquantel Mixing, is dissolved, obtains transdermal liniment.
Preferably, the temperature of the dissolution is 50~70 DEG C.
Preferably, the process of the dissolution is with stirring.
Preferably, the revolving speed of the stirring is 60~90rpm.
Beneficial effects of the present invention: the present invention provides a kind of transdermal liniments for preventing and treating Yak parasitoses, including pyrrole quinoline Ketone and auxiliary material;The mass volume ratio of the praziquantel and auxiliary material is 200~400mg:1mL;The auxiliary material includes following volumes hundred The raw material of score: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 78%.Of the invention is saturating Skin liniment passes through reasonable compatibility, overcomes that praziquantel dissolubility is poor, defect of transdermal effect difference, and transdermal liniment of the invention dissolves Degree is 358mg/mL;Transdermal characteristic is 19.9mg/100mg;Resultant effect is 71.24mg/mL;And transdermal liniment of the invention is given Prescription just, and can effectively play drug effect.
Detailed description of the invention
Fig. 1 shows relative bioavailability experimental measurements in embodiment 2.
Specific embodiment
The present invention provides a kind of transdermal liniments for preventing and treating Yak parasitoses, including praziquantel and auxiliary material;The pyrrole quinoline The mass volume ratio of ketone and auxiliary material is 200~400mg:1mL, preferably 280~350mg:1mL, more preferably 300mg:1mL; The auxiliary material includes the raw material of following volumes percentage: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, second Glycol phenylate 78%.
In the present invention, the praziquantel is active drug ingredient;The praziquantel is preferred purchased from remote from commercially available At chemical industry store.
In the present invention, the auxiliary material includes 3% azone;In the present invention, the azone is transdermal enhancer;The azone comes Derived from commercially available, it is preferably purchased from Shanghai Aladdin biochemical technology limited liability company.
In the present invention, the auxiliary material includes 3% oleic acid;In the present invention, the oleic acid is transdermal enhancer;The oleic acid comes Derived from commercially available, it is preferably purchased from Sinopharm Chemical Reagent Co., Ltd..
In the present invention, the auxiliary material includes 11% propylene glycol;In the present invention, the propylene glycol is transdermal enhancer;It is described Propylene glycol is preferably purchased from Sinopharm Chemical Reagent Co., Ltd. from commercially available.
In the present invention, the auxiliary material includes 5% dimethyl sulfoxide;In the present invention, the dimethyl sulfoxide is transdermal promotion Agent and transdermal protective agent;The dimethyl sulfoxide is preferably purchased from Sinopharm Chemical Reagent Co., Ltd. from commercially available.
In the present invention, the auxiliary material includes 78% ethylene glycol phenyl ether;In the present invention, the ethylene glycol phenyl ether is solvent;Institute Ethylene glycol phenyl ether is stated from commercially available, is preferably purchased from Suzhou City Mike woods medical instrument Products Co., Ltd.
The present invention also provides the preparation method of the transdermal liniment described in above scheme, steps are as follows: by auxiliary material and praziquantel Mixing, is dissolved, obtains transdermal liniment;The temperature of the dissolution is preferably 50~70 DEG C, and more preferably 60 DEG C;The present invention couple The time of the dissolution is not particularly limited, and dissolution of being subject to is complete;The process of the dissolution is preferably water-bath dissolution;It is described molten The process of solution is preferably with stirring;The revolving speed of the stirring is preferably 60~90rpm.
Below with reference to embodiment to it is provided by the invention it is a kind of prevent and treat Yak parasitoses transdermal liniment and its preparation side Method is described in detail, but they cannot be interpreted as limiting the scope of the present invention.
Embodiment 1
Formula components: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, 78% (volume of ethylene glycol phenyl ether Than), praziquantel 300mg/mL, 10mL/ bottle.
Preparation method: 60 DEG C of water-bath hand operated mixings to whole dissolutions obtain transdermal liniment.
Transdermal liniment solubility and transdermal characteristic are detected, and calculates resultant effect according to following formula:
Resultant effect=solubility × transdermal characteristic
Testing result are as follows: solubility 358mg/mL;Transdermal characteristic is 19.9mg/100mg;Resultant effect is 71.24mg/ mL.Wherein resultant effect is higher represents transdermal characteristic and the comprehensive performance of solubility is better, is more conducive to the performance of drug effect.
Comparative example 1
Formula components: azone 2%, oleic acid 7%, propylene glycol 13%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 73%, pyrrole quinoline Ketone 300mg/mL, 10mL/ bottle.
The preparation method is the same as that of Example 1;
Solubility is 262mg/mL;Transdermal characteristic is 23.2mg/100mg;Resultant effect is 60.78mg/mL.
Comparative example 2
Formula components: azone 4%, oleic acid 1%, propylene glycol 11%, dimethyl sulfoxide 15%, ethylene glycol phenyl ether 69%, pyrrole Quinoline ketone 300mg/mL, 10mL/ bottle.
The preparation method is the same as that of Example 1;
Solubility is 269mg/mL;Transdermal characteristic is 18.83mg/100mg;Resultant effect is 50.65mg/mL.
Comparative example 3
Formula components: azone 2%, oleic acid 3%, propylene glycol 9%, dimethyl sulfoxide 35%, ethylene glycol phenyl ether 51%, pyrrole quinoline Ketone 300mg/mL, 10mL/ bottle.
The preparation method is the same as that of Example 1;
Solubility is 131mg/mL;Transdermal characteristic is 36.4mg/100mg;Resultant effect is 47.68mg/mL.
Comparative example 4
Formula components: azone 2%, oleic acid 5%, propylene glycol 11%, dimethyl sulfoxide 45%, ethylene glycol phenyl ether 37%, pyrrole Quinoline ketone 300mg/mL, 10mL/ bottle.
The preparation method is the same as that of Example 1;
Solubility is 100mg/mL;Transdermal characteristic is 44.7mg/100mg;Resultant effect is 44.7mg/mL.
Comparative example 5
Formula components: azone 2%, oleic acid 7%, propylene glycol 13%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 73%, pyrrole quinoline Ketone 300mg/mL, 10mL/ bottle.
The preparation method is the same as that of Example 1;
Solubility is 352mg/mL;Transdermal characteristic is 18.9mg/100mg;Resultant effect is 66.53mg/mL.
Transdermal liniment relative bioavailability verifying in 2 embodiment 1 of embodiment
Clinical test: by 2 groups of 6 yaks point, after taking blank serum, by one group of 25mg/kg weight to transdermal agent, one group is pressed The administration of 25mg/kg bodyweight p praziquantel original powder, 5,15,30,45,60,90,150,240min, 360min distinguishes upon administration Blood sampling, centrifuging and taking plasma freezing save, and measure blood concentration (μ g/mL).Measurement result is referring to Fig. 1, as the result is shown: cutaneous penetration It is higher earlier to there are peak plasma concentrations, while cutaneous penetration is more more convenient than being administered orally with yak.
As seen from the above embodiment, the present invention provides a kind of transdermal liniment for preventing and treating Yak parasitoses, change transdermal put on the skin Agent convenient drug administration, and can effectively play drug effect.
The above is only a preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art For member, various improvements and modifications may be made without departing from the principle of the present invention, these improvements and modifications are also answered It is considered as protection scope of the present invention.

Claims (6)

1. a kind of transdermal liniment for preventing and treating Yak parasitoses, including praziquantel and auxiliary material;The quality of the praziquantel and auxiliary material Volume ratio is 200~400mg:1mL;
The auxiliary material includes the raw material of following volumes percentage: azone 3%, oleic acid 3%, propylene glycol 11%, dimethyl sulfoxide 5%, ethylene glycol phenyl ether 78%.
2. transdermal liniment according to claim 1, which is characterized in that the mass volume ratio of the praziquantel and auxiliary material is 280~350mg:1mL.
3. the preparation method of transdermal liniment of any of claims 1 or 2, step are as follows: mix auxiliary material and praziquantel, carry out molten Solution, obtains transdermal liniment.
4. preparation method according to claim 3, which is characterized in that the temperature of the dissolution is 50~70 DEG C.
5. preparation method according to claim 3, which is characterized in that the process of the dissolution is with stirring.
6. preparation method according to claim 5, which is characterized in that the revolving speed of the stirring is 60~90rpm.
CN201910072142.1A 2019-01-25 2019-01-25 A kind of transdermal liniment and preparation method thereof for preventing and treating Yak parasitoses Pending CN109674739A (en)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101669906A (en) * 2009-07-28 2010-03-17 中国农业科学院上海兽医研究所 Praziquantel injection, preparation method and application thereof
CN101693009A (en) * 2009-10-27 2010-04-14 天津必佳药业集团有限公司 Antiparasitic closantel sodium transdermal solution for ox and sheep and preparation method thereof
CN102138890A (en) * 2011-04-01 2011-08-03 中国农业科学院上海兽医研究所 Praziquantel transdermal preparation and applications thereof
CN102450282A (en) * 2010-10-20 2012-05-16 周端午 Green long-acting zoonosis vector prevention and control medicament
CN102860981A (en) * 2012-10-26 2013-01-09 天津必佳药业集团有限公司 Schistosomiasis resistant praziquantel transdermal solution for flocks and herds and preparation method
CN111991411A (en) * 2020-09-28 2020-11-27 吉林吉力生物技术研究有限公司 Application of composition in preparation of veterinary anthelmintic drug, transdermal anthelmintic solution for veterinary use and preparation method of transdermal anthelmintic solution

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101669906A (en) * 2009-07-28 2010-03-17 中国农业科学院上海兽医研究所 Praziquantel injection, preparation method and application thereof
CN101693009A (en) * 2009-10-27 2010-04-14 天津必佳药业集团有限公司 Antiparasitic closantel sodium transdermal solution for ox and sheep and preparation method thereof
CN102450282A (en) * 2010-10-20 2012-05-16 周端午 Green long-acting zoonosis vector prevention and control medicament
CN102138890A (en) * 2011-04-01 2011-08-03 中国农业科学院上海兽医研究所 Praziquantel transdermal preparation and applications thereof
CN102860981A (en) * 2012-10-26 2013-01-09 天津必佳药业集团有限公司 Schistosomiasis resistant praziquantel transdermal solution for flocks and herds and preparation method
CN111991411A (en) * 2020-09-28 2020-11-27 吉林吉力生物技术研究有限公司 Application of composition in preparation of veterinary anthelmintic drug, transdermal anthelmintic solution for veterinary use and preparation method of transdermal anthelmintic solution

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LEI WANG,ET AL: ""Transdermal Evaporation Delivery System of Praziquantel for Schistosomiasis Japonicum Chemotherapy"", 《JOURNAL OF PHARMACEUTICAL SCIENCES》 *

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Application publication date: 20190426