CN106377504A - Praziquantel premix and preparation method thereof - Google Patents
Praziquantel premix and preparation method thereof Download PDFInfo
- Publication number
- CN106377504A CN106377504A CN201610882926.7A CN201610882926A CN106377504A CN 106377504 A CN106377504 A CN 106377504A CN 201610882926 A CN201610882926 A CN 201610882926A CN 106377504 A CN106377504 A CN 106377504A
- Authority
- CN
- China
- Prior art keywords
- praziquantel
- mixing agent
- agent according
- inclusion agents
- preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
Abstract
The invention discloses a medicien for treating coccidiosis, particularly a praziquantel premix and a preparation method thereof. The anti-coccidiosis medicine is characterized by comprising praziquantel, a high-polymer carrier, an inclusion agent and a diluter. Therefore, the infusible praziquantel is made into water-soluble substances by a solid dispersion technique and an inclusion technique, thereby enhancing the curative effect and reducing the drug resistance.
Description
Technical field
The invention belongs to field of veterinary is and in particular to a kind of praziquantel pre-mixing agent.
Background technology
Praziquantel is all effective to schistosomicide, cestode, cysticercosis, clonorchis sinensises, lung fluke, fasciloopsis.This product is mainly passed through
The effect of 5-HT sample makes schistosomicide in host's body, cestode generation spastic paralysis come off, to most cestode adults and immaturity polypide
There are better effects, calcium ion permeability in polypide myocyte can be affected simultaneously, so that flow of calcium ions is increased, suppress sarcoplasmic reticulum calcium
The reuptake of pump, in polypide myocyte, calcium ion content increases, and so that polypide is benumbed and comes off.It is mainly used on veterinary treating cattle pig
Taeniasiss.Praziquantel is slightly soluble in water, and in water, dissolubility is low, cattle is gavaged or pig drinking-water use not very convenient.
Content of the invention
For overcoming prior art not enough, the invention provides a kind of praziquantel pre-mixing agent.
For achieving the above object, the technical scheme is that and be achieved in that：
A kind of praziquantel pre-mixing agent, is characterized in that：It is made up of praziquantel, macromolecule carrier, inclusion agents, diluent.
Further, percentage by weight consists of：Praziquantel 2%, macromolecule carrier 10-30%, inclusion agents 25-50%, diluent
Polishing.
Further, described macromolecule carrier be Macrogol 4000, polyethylene glycol 6000, Polyvinylpyrrolidone wherein
A kind of or their several combinations；
Further, described inclusion agents are the mixture of beta-schardinger dextrin-or hydroxypropylβ-cyclodextrin or alpha-cyclodextrin and sodium carbonate.
Further, described diluent be anhydrous glucose, Lactose, Mannitol, in soluble starch one or two with
On.
Present invention also offers a kind of preparation method of praziquantel pre-mixing agent, for realizing this purpose, the technical side of the present invention
Case is realized in：
By praziquantel, macromolecule carrier mix homogeneously, heating under the conditions of 100 DEG C -120 DEG C melts to liquid condition, then certainly
So it is cooled to room temperature, under the conditions of 30 DEG C -40 DEG C, is vacuum dried 30-40 minute, add inclusion agents after pulverizing, add dilution
Agent stirs and obtains final product.
Beneficial effect of the present invention
Using solid dispersion technology and inclusion technique, the praziquantel of indissoluble is prepared into water-soluble substanceses, improves curative effect, reduce resistance to
The mesh of the property of medicine, using more convenient.
Specific embodiment
Embodiment 1：
Praziquantel 2%, Macrogol 4000 10%, beta-schardinger dextrin -15%, sodium carbonate 10%, anhydrous glucose polishing.
Embodiment 2:
Praziquantel 2%, polyethylene glycol 6000 30%, hydroxypropylβ-cyclodextrin 30%, sodium carbonate 20%, Lactose polishing.
Embodiment 3：
Praziquantel 2%, Polyvinylpyrrolidone 20%, alpha-cyclodextrin 10%, sodium carbonate 25%, Lactose and soluble starch mixture
（1:1）Polishing.
Embodiment 4：
Praziquantel 2%, Macrogol 4000:Polyvinylpyrrolidone (1:1）25%th, beta-schardinger dextrin -20%, sodium carbonate 20%, Mannitol
Polishing.
Embodiment 5：
A kind of preparation method of praziquantel pre-mixing agent, employs the following technical solutions realization：
By praziquantel, macromolecule carrier mix homogeneously, heating under the conditions of 100 DEG C -120 DEG C melts to liquid condition, then certainly
So it is cooled to room temperature, under the conditions of 30 DEG C -40 DEG C, is vacuum dried 30-40 minute, add inclusion agents after pulverizing, add dilution
Agent stirs and obtains final product.
Below by way of concrete test example, the present invention is described further and explains.
Test example 1：Stability test
By the embodiment of the present invention 1～4 according to the stability test principle of Chinese veterinary pharmacopoeia, carry out influence factor, acceleration and long-term
Test, result show, the embodiment of the present invention 1～4 has good stability, in continuous 6 months of accelerated test and long term test 1 year half
Observe, appearance without exception.
Test example 2：Water solublity and the test that is suspended
Take the made medicine 1g of the embodiment of the present invention 1～4, add in 100ml water, shaking, so that dissolving is suspended completely, timing, observe
Solution settling particulate matter.Result shows, after 10h, embodiment 1～4 solution is still uniform solution, and no substantially granule goes out
Existing.
Test example 1, the result of test example 2 show, the medicine of present invention preparation has good stability and water solublity, can
Drinking-water uses.
The foregoing is only presently preferred embodiments of the present invention, not in order to limit the present invention, all essences in the present invention
Within god and principle, any modification, equivalent substitution and improvement made etc., should be included within the scope of the present invention.
Claims (4)
1. a kind of praziquantel pre-mixing agent, is characterized in that：It is made up of praziquantel, macromolecule carrier, inclusion agents, diluent.
2. a kind of praziquantel pre-mixing agent according to claim 1, is characterized in that：Described praziquantel 2%, macromolecule carrier 10-
30%th, inclusion agents 25-50%, diluent polishing.
3. a kind of praziquantel pre-mixing agent according to claim 1 and 2, is characterized in that：Described macromolecule carrier is poly- second
The combination that glycol 4000, polyethylene glycol 6000, Polyvinylpyrrolidone are therein a kind of or they are several.
4. a kind of praziquantel pre-mixing agent according to claim 1 and 2, is characterized in that：Described inclusion agents be beta-schardinger dextrin-or
Hydroxypropylβ-cyclodextrin or the mixture of alpha-cyclodextrin and sodium carbonate.
A kind of preparation method of the praziquantel pre-mixing agent according to claim 1, is characterized in that：Praziquantel, macromolecule are carried
Body mix homogeneously, under the conditions of 100 DEG C -120 DEG C heating melt to liquid condition, then naturally cool to room temperature, 30 DEG C -
It is vacuum dried 30-40 minute under the conditions of 40 DEG C, after pulverizing, adds inclusion agents, add diluent and stir and obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610882926.7A CN106377504A (en) | 2016-10-10 | 2016-10-10 | Praziquantel premix and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610882926.7A CN106377504A (en) | 2016-10-10 | 2016-10-10 | Praziquantel premix and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106377504A true CN106377504A (en) | 2017-02-08 |
Family
ID=57937209
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610882926.7A Pending CN106377504A (en) | 2016-10-10 | 2016-10-10 | Praziquantel premix and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN106377504A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109432440A (en) * | 2018-11-30 | 2019-03-08 | 佛山科学技术学院 | A kind of praziquantel hydroxypropyl cyclodextrin inclusion and its preparation method and application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103800297A (en) * | 2014-02-18 | 2014-05-21 | 四川农业大学 | Intragastric floating sustained release tablet of praziquantel composition and preparation method thereof |
-
2016
- 2016-10-10 CN CN201610882926.7A patent/CN106377504A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103800297A (en) * | 2014-02-18 | 2014-05-21 | 四川农业大学 | Intragastric floating sustained release tablet of praziquantel composition and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 王天梓 等: "《第十一届北京畜牧兽医青年科技工作者"新思想、新观点、新方法"论文集》", 22 September 2016 * |
| 罗延红 等: "吡喹酮固体分散体泡腾片的制备", 《中国农学通报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109432440A (en) * | 2018-11-30 | 2019-03-08 | 佛山科学技术学院 | A kind of praziquantel hydroxypropyl cyclodextrin inclusion and its preparation method and application |
| CN109432440B (en) * | 2018-11-30 | 2022-04-26 | 佛山科学技术学院 | Praziquantel hydroxypropyl cyclodextrin inclusion compound and preparation method and application thereof |
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Application publication date: 20170208 |
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