CN106727350A - A kind of lincomycin solid dispersion preparation and preparation method thereof - Google Patents
A kind of lincomycin solid dispersion preparation and preparation method thereof Download PDFInfo
- Publication number
- CN106727350A CN106727350A CN201611235758.9A CN201611235758A CN106727350A CN 106727350 A CN106727350 A CN 106727350A CN 201611235758 A CN201611235758 A CN 201611235758A CN 106727350 A CN106727350 A CN 106727350A
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- CN
- China
- Prior art keywords
- lincomycin
- preparation
- solid dispersion
- poloxamer
- pvp
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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
- 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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
Abstract
The invention discloses a kind of lincomycin solid dispersion preparation and preparation method thereof, belong to veterinary drug solid dispersions novel form technical field, preparation is made up of the raw material of following mass percent：Lincomycin 10%~50%, PVP 30%~50%, poloxamer 10%~50%, excipient substance 0%~50%.Lincomycin is prepared into solid dispersions, using hot-melt extruded inclusion technique, pharmaceutical carrier can be in a short time set to melt and uniform packaging medicine, the lincomycin solid dispersions of preparation have covers medicine material bad smell, the oral palatability of livestock and poultry and absorbability are preferable, medicine is water-soluble high, bioavilability advantage high.
Description
Technical field
The invention belongs to veterinary drug solid dispersions novel form technical field, and in particular to a kind of lincomycin solid dispersions
Preparation and preparation method thereof.
Background technology
Solid dispersions refer to medicine is highly dispersed in formed in solid carrier a kind of exist in solid form point
The system of dissipating.Medicine particle diameter in the carrier is mainly used in accelerating and increasing insoluble drug between 0.001~0.1 millimeter
Dissolution, improves its bioavilability.90% medicine is all to be administered in the form of dispersion in current veterinary drug Clinical practice, and its is excellent
Point is simple production process, packed and transported and easy to use, and artificial and production can be reduced for manufacturing enterprise and cultivation industry
Cost.
The method that the preparation of solid dispersions is conventional has fusion method, solvent method, solvent-fusion method, solvent spray freezing dry
Dry method, polishing etc.；It is divided into quick-releasing type solid dispersions by pharmacy Release Performance, slow (control) type solid dispersions and targeting are released
Types of Medicine solid dispersions.After medicine is prepared to solid dispersions, drug molecule is presented superfine crystallite or ultra-fine in carrier
Particulate, or even exist with molecular state, the surface area of medicine is substantially increased, dissolving of the medicine in water can be significantly improved
Degree, improves the dissolution rate of medicine and covers bad smell, improves the palatability of livestock and poultry, improves the utilization rate of medicine.
Lincomycin can suppress the protein synthesis of bacterium also known as lincomycinum, to most of gram-positive bacterias and some
Anaerobic bacteria has antibacterial action.At present, livestock and poultry in the market mainly has the formulations such as lincomycin supensoid agent, lincomycin pre-mixing agent, all
Be simple medicine material and the mixture of excipient substance, the subject matter that this kind of product is present be after mixing with drinking water due to
Lincomycin solubility is low, and medicine occurs sedimentation causes the animal can not to drink enough medicines；Pre-mixing agent is due to lincomycin
Dosage is low, so it is difficult to well mixed, influence using effect；Also it is exactly poor lincomycin palatability, Clinical practice
In the presence of certain defect.
Once there is the patent (patent No.：201310023751.0) report prepares the content of lincomycin soluble powder, the patent
Using the method for heating melting packaging medicine, it is improved the water-soluble and palatability of medicine, but there is medicine and carrier
Melting time is more long, is coated with shortcoming that is uneven and being difficult to realize mechanization production, is not suitable for promoting the use of on a large scale, consults
Pertinent literature and patent in recent years, development and application at present on lincomycin solid dispersions are rarely reported at home, because
This prepares a kind of good water solubility, and dissolution rate is high, and the lincomycin solid dispersion preparation of good palatability improves the biology of medicine
Availability, it is very necessary to expand the Clinical practice of medicine.
The content of the invention
The present invention provides a kind of lincomycin solid dispersion preparation and preparation method thereof, and lincomycin is prepared into solid
Dispersion, using hot-melt extruded inclusion technique, can in a short time be such that pharmaceutical carrier melts and uniform packaging medicine, the woods of preparation
Can mycin solid dispersions have and cover medicine material bad smell, the oral palatability of livestock and poultry and absorbability preferably, drug-eluting
Spend higher, bioavilability advantage high.
The present invention uses following technical scheme：
A kind of lincomycin solid dispersion preparation, is made up of following raw material：Lincomycin, solid dispersions material and medicine
Thing auxiliary material, the solid dispersions material is PVP and poloxamer；The mass percent of the raw material is：Lincomycin
10%~50%, PVP 30%~50%, poloxamer 10%~50%, excipient substance 0%~50%.
Preferably, the mass percent of the raw material is：Lincomycin 40%, PVP 30%, poloxamer 20%, medicine
Thing auxiliary material 10%.
Preferably, the PVP is PVP-K30, and the poloxamer is poloxamer -188.
Preferably, the excipient substance is any one of DEXTROSE ANHYDROUS, water soluble starch or cyclodextrin.
A kind of preparation method of lincomycin solid dispersion preparation, comprises the following steps：Woods is weighed by mass percentage
Can mycin and solid dispersions material, stirred using three-dimensional mixer, by the mixture for stirring send into heat
Extruder melting extrusion；After above-mentioned extrudate cool drying, size-reduced sieving adds excipient substance to mix according to mass percent
After even dilution, you can obtain the lincomycin solid dispersion preparation of different size.
Advantageous Effects of the invention are：
1. the method that lincomycin solid dispersions preparation method of the invention is included using melting extrusion, can be in the short time
The pharmaceutical carrier is inside set to melt and uniform packaging medicine, it is to avoid influence of the melting to drug effect for a long time；
2. lincomycin solid dispersions of the invention, effectively cover the bad smell of material medicine, increase the suitable of livestock and poultry
Mouth property, can be completely water-soluble, improves dissolution rate, with bioavilability higher, can be clinically used for spice or drinking-water is used；
3. the lincomycin solid dispersions process is simple that prepared by this method, can large-scale promotion production, without expensive
Equipment, operation difficulty is relatively low, and operating personnel carry without Special Training and requested knowledge higher, production process low power consuming, environmental protection
The utilization rate of lincomycin high, makes medicine using obtaining bigger popularization.
Specific embodiment
With reference to specific embodiment, the invention will be further described.
Embodiment 1
Lincomycin 40.0g, PVP 30.0g, poloxamer 20.0g accurately are weighed, is fully stirred using three-dimensional mixer
Mix uniform, the mixture for stirring is sent into hot-melt extruded machine melting extrusion.It is size-reduced after by above-mentioned extrudate cool drying
Sieving, after adding excipient substance glucose 10.0g to mix dilution, you can obtain 40% lincomycin solid dispersion preparation.
Embodiment 2
Lincomycin 30.0g, PVP 35.0g, poloxamer 25.0g accurately are weighed, is fully stirred using three-dimensional mixer
Mix uniform, the mixture for stirring is sent into hot-melt extruded machine melting extrusion.It is size-reduced after by above-mentioned extrudate cool drying
Sieving, after adding excipient substance DEXTROSE ANHYDROUS 10.0g to mix dilution, you can obtain 30% lincomycin solid dispersions system
Agent.
Embodiment 3
Lincomycin 20.0g, PVP 40.0g, poloxamer 30.0g accurately are weighed, is fully stirred using three-dimensional mixer
Mix uniform, the mixture for stirring is sent into hot-melt extruded machine melting extrusion.It is size-reduced after by above-mentioned extrudate cool drying
Sieving, after adding excipient substance soluble starch 10.0g to mix dilution, you can obtain 20% lincomycin solid dispersions system
Agent.
Embodiment 4
Lincomycin 10.0g, PVP 50.0g, poloxamer 30.0g accurately are weighed, is fully stirred using three-dimensional mixer
Mix uniform, the mixture for stirring is sent into hot-melt extruded machine melting extrusion.It is size-reduced after by above-mentioned extrudate cool drying
Sieving, after adding excipient substance soluble starch 10.0g to mix dilution, you can obtain 10% lincomycin solid dispersions system
Agent.
Embodiment 5
The lincomycin solid dispersions 1.0g that respectively prepared by Example 1~4, stirring is dissolved in 200mL water under normal temperature,
Commercially available 10% lincomycin pulvis (10.0g of raw material containing lincomycin, auxiliary material DEXTROSE ANHYDROUS in 100g medicines is taken in addition
90.0g) 1.0g, stirring is dissolved in conduct control in 200mL water under similarity condition, and solution state is observed after 30min, and lincomycin is solid
Body dispersion is as shown in table 1 with common dispersion water solubility comparative test result.
Table 1
From table 1 it follows that there is preferable water according to lincomycin solid dispersions prepared by technique of the invention
Dissolubility, water-soluble effect is better than common commercially available lincomycin pulvis.This be due in technique of the invention lincomycin by water
Solubleness carrier PVP and poloxamer considerably increase degree of scatter of the medicine in water by uniform hot melt inclusion, show
Write the solubility for improving medicine in water.
Presently preferred embodiments of the present invention is the foregoing is only, is not intended to limit the invention, it is all in skill of the invention
On the basis of art scheme, the various modifications or deformation that those skilled in the art make by need not paying creative work still exist
In protection scope of the present invention.
Claims (5)
1. a kind of lincomycin solid dispersion preparation, it is characterised in that be made up of following raw material：Lincomycin, solid dispersion
Body material and excipient substance, the solid dispersions material are PVP and poloxamer；The mass percent of the raw material is：
Lincomycin 10%~50%, PVP 30%~50%, poloxamer 10%~50%, excipient substance 0%~50%.
2. a kind of lincomycin solid dispersion preparation according to claim 1, it is characterised in that the quality of the raw material
Percentage is：Lincomycin 40%, PVP 30%, poloxamer 20%, excipient substance 10%.
3. a kind of lincomycin solid dispersion preparation according to claim 1 and 2, it is characterised in that the PVP
It is PVP-K30, the poloxamer is poloxamer -188.
4. a kind of lincomycin solid dispersion preparation according to claim 1 and 2, it is characterised in that the medicine is auxiliary
Expect for DEXTROSE ANHYDROUS, water soluble starch or cyclodextrin any one.
5. the preparation method of a kind of lincomycin solid dispersion preparation described in any one of claim 1-3, it is characterised in that
Comprise the following steps：Lincomycin and solid dispersions material are weighed by mass percentage, are sufficiently stirred for using three-dimensional mixer
Uniformly, the mixture for stirring is sent into hot-melt extruded machine melting extrusion；After above-mentioned extrudate cool drying, size-reduced mistake
Sieve, after adding excipient substance to mix dilution according to mass percent, you can obtain the lincomycin solid dispersions of different size
Preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611235758.9A CN106727350A (en) | 2016-12-28 | 2016-12-28 | A kind of lincomycin solid dispersion preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611235758.9A CN106727350A (en) | 2016-12-28 | 2016-12-28 | A kind of lincomycin solid dispersion preparation and preparation method thereof |
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| CN106727350A true CN106727350A (en) | 2017-05-31 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611235758.9A Pending CN106727350A (en) | 2016-12-28 | 2016-12-28 | A kind of lincomycin solid dispersion preparation and preparation method thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102665693A (en) * | 2009-10-27 | 2012-09-12 | 鲁平有限公司 | Solid dispersion of rifaximin |
| CN102988363A (en) * | 2012-11-19 | 2013-03-27 | 河南新正好生物工程有限公司 | Medicine for treating poultry proventriculitis and necrotic enteritis and preparation method thereof |
| CN103932987A (en) * | 2013-01-23 | 2014-07-23 | 青岛康地恩药业股份有限公司 | Novel lincomycin soluble powder and preparing method thereof |
-
2016
- 2016-12-28 CN CN201611235758.9A patent/CN106727350A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102665693A (en) * | 2009-10-27 | 2012-09-12 | 鲁平有限公司 | Solid dispersion of rifaximin |
| CN102988363A (en) * | 2012-11-19 | 2013-03-27 | 河南新正好生物工程有限公司 | Medicine for treating poultry proventriculitis and necrotic enteritis and preparation method thereof |
| CN103932987A (en) * | 2013-01-23 | 2014-07-23 | 青岛康地恩药业股份有限公司 | Novel lincomycin soluble powder and preparing method thereof |
Non-Patent Citations (1)
| Title |
|---|
| FOUSTERIS E.,ET AL.: "Poly(vinyl pyrrolidone)-poloxamer-188 solid dispersions prepared by hot melt extrusion", 《JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY》 * |
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| RJ01 | Rejection of invention patent application after publication | ||
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Application publication date: 20170531 |