CN105982854A - Fenbendazole nano suspension and preparation method thereof - Google Patents
Fenbendazole nano suspension and preparation method thereof Download PDFInfo
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- CN105982854A CN105982854A CN201510040787.9A CN201510040787A CN105982854A CN 105982854 A CN105982854 A CN 105982854A CN 201510040787 A CN201510040787 A CN 201510040787A CN 105982854 A CN105982854 A CN 105982854A
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Abstract
The invention discloses a fenbendazole nano suspension which is composed of, by mass, 2-8% of fenbendazole, 0.5-2% of a suspending agent, 0.05-0.15% of a wetting agent, 0.5-2% of a flocculating agent, 0.05-0.15% of an antibacterial agent and the balanced being water for injection. Compared with the prior art, the fenbendazole is processed into the nano suspension, so that saturated solubility, dissolving rate and mucous membrane adhesion are improved, a problem of low bioavailability of the medicine is overcome and effectiveness, safety and stability of the medicine are improved. The preparation method and formula in the invention are simple. The fenbendazole nano suspension has uniform particle size distribution, is easy to apply and is suitable for industrial production. The nano suspension has excellent stability, improves solubility and oral-taking bioavailability of fenbendazole, is reduced in toxic and side effects and has excellent practical value and application prospect.
Description
Technical field
The invention belongs to technical field of veterinary, be specifically related to a kind of fenbendazole nano suspension and preparation method thereof.
Background technology
Fenbendazole has another name called albendazole, it it is benzimidazoles derivative, the pest-resistant spectrum of this medicine is wide, low toxicity, efficient and inexpensive, it is widely used in treatment and ancylostomiasis, ascariasis, trichuriasis, enterobiasis, thichinelliasis, taeniasis and the cysticercosis etc. that prevent humans and animals to be suffered from, is also used for treating strongyloidiasis.Up to the present, fenbendazole be considered as in benzimidazoles residues anthelmintic spectrum relatively wide, one of anthelmintic that insecticidal action is the strongest.Water insoluble and the most organic solvent of fenbendazole, development recently as preparation technique, formulation scientist takes a lot of method to solve this problem, as: use mixed solvent, use inclusion technique, micronization or make Emulsion etc., but these methods all exist some problems: mixed solvent method requires that medicine has specific physicochemical characteristics；Inclusion technique requires that medicine has suitable molecular size；Micronization increases bioavailability DeGrain；The physical stability of Emulsion is bad, and organic solvent uses more, and manufacturing cost is higher, and toxicity is relatively large etc..
Nano suspension is a kind of nano-grade medicine transmission system that development in recent years is got up, and is the colloidal dispersion of pure medicine submicron particles, relies on surfactant to remain stable.The medicine of slightly water-soluble and water, oil all indissolubles all can make corresponding nano suspension by this method.As a kind of new preparation technique, nano suspension can increase drug dissolution, improve bioavailability and drug effect.This dosage form is the submicron particles cavity dispersion in a liquid of pure medicine, in system Nano Particle pure drug particles rely on surfactant charge effect or/and stereoeffect stably suspendible in the solution, the mean diameter of its Chinese medicine is less than 1 μm, typically between 200 ~ 500nm.
Nano suspension can improve the safety of pharmaceutical preparation, the use of dangerous adjuvant can be reduced or eliminated by medicine is made nano suspension, and the content that simultaneously can improve medicine reduces taking dose；Secondly, dissolubility and the dissolution rate of medicine can be improved, strengthen the oral absorption of medicine, improve bioavailability；3rd, surfactant molecule and high molecular polymer in nano suspension improve the chemical stability of preparation to the protective effect of medicament nano granule and the medicine crystal structure of nano-scale；4th, owing to the grain diameter of nano suspension Chinese medicine is little, there is good bioadhesive, the absorption of medicine can be promoted.
Summary of the invention
The technical problem to be solved in the present invention is the water insoluble and most organic solvent of fenbendazole, development recently as preparation technique, formulation scientist takes a lot of method to solve this problem, as: use mixed solvent, use inclusion technique, micronization or make Emulsion etc., but all there are some problems in these methods, for solving the problems referred to above, it is provided that a kind of fenbendazole nano suspension and preparation method thereof.
It is an object of the invention to realize in the following manner:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 2 ~ 8%, suspending agent 0.5 ~ 2%, wetting agent 0.05 ~ 0.15%, flocculant 0.5 ~ 2%, antibacterial 0.05 ~ 0.15%, and surplus is water for injection.
Described suspending agent is at least one in methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, sodium alginate, arabic gum.
Described suspending agent is sodium carboxymethyl cellulose.
Described wetting agent is at least one in ethanol, propylene glycol, glycerol, tween 80, polyethylene glycol 200.
Described wetting agent is tween 80.
Described flocculant is at least one in tartaric acid, phosphate, citric acid.
Described flocculant is citric acid.
Described antibacterial is at least one in benzyl alcohol, phenol, sodium benzoate.
Described antibacterial is sodium benzoate.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 3 ~ 5 times under 10 ~ 30MPa pressure, homogenisation cycle 10 ~ 15 times under 100 ~ 150MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Relative to prior art, fenbendazole is made nano suspension by the present invention can increase the saturation solubility of medicine, dissolution velocity and mucosa adhesion, overcomes the problem that drug bioavailability is low, improves the effectiveness of medicine, safety and stability.
Preparation technology of the present invention and prescription composition are simple, and gained diameter of aspirin particle is evenly distributed, it is easy to operation, production suitable for industrialized.This nano suspension has good stability, can improve the dissolubility of fenbendazole, improves its oral administration biaavailability, reduces toxic and side effects, has good practical value and application prospect.
Detailed description of the invention
Embodiment 1:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 2 ~ 8%, suspending agent 0.5 ~ 2%, wetting agent 0.05 ~ 0.15%, flocculant 0.5 ~ 2%, antibacterial 0.05 ~ 0.15%, and surplus is water for injection.
Described suspending agent is at least one in methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, sodium alginate, arabic gum.
Described wetting agent is at least one in ethanol, propylene glycol, glycerol, tween 80, polyethylene glycol 200.
Described flocculant is at least one in tartaric acid, phosphate, citric acid.
Described antibacterial is at least one in benzyl alcohol, phenol, sodium benzoate.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 3 ~ 5 times under 10 ~ 30MPa pressure, homogenisation cycle 10 ~ 15 times under 100 ~ 150MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
After 0.45 μm filtering with microporous membrane, be not transmitted through filter membrane thick suspension concentration be identical through the concentration of fenbendazole contained in the nanosuspension of filter membrane and the concentration of suspending agent, wetting agent, flocculant and antibacterial.
Embodiment 2:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 2%, methylcellulose 0.5%, ethanol 0.05%, tartaric acid 0.5%, benzyl alcohol 0.05%, and surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 3 times under 10MPa pressure, homogenisation cycle 10 times under 100MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 3:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 3%, sodium carboxymethyl cellulose 0.6%, propylene glycol 0.06%, phosphate 0.6%, phenol 0.06%, and surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 4 times under 15MPa pressure, homogenisation cycle 11 times under 110MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 4:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 4%, hydroxypropyl cellulose 0.7%, glycerol 0.07%, citric acid 0.7%, sodium benzoate 0.07%, and surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 5 times under 20MPa pressure, homogenisation cycle 12 times under 120MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 5:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 5%, sodium alginate 0.8%, tween 80 0.08%, tartaric acid 0.4%, phosphate 0.4%, benzyl alcohol 0.04%, phenol 0.04%, and surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 5 times under 25MPa pressure, homogenisation cycle 13 times under 130MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 6:
A kind of fenbendazole nano suspension, is made up of the component of following mass fraction: fenbendazole 6%, arabic gum 0.9%, polyethylene glycol 200 0.09%, tartaric acid 0.5%, citric acid 0.4%, benzyl alcohol 0.05%, sodium benzoate 0.04%, and surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 5 times under 30MPa pressure, homogenisation cycle 14 times under 140MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 7:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 7%, methylcellulose 0.5%, sodium carboxymethyl cellulose 0.5%, ethanol 0.05%, propylene glycol 0.05%, phosphate 0.5%, citric acid 0.5%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 5 times under 30MPa pressure, homogenisation cycle 15 times under 150MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
Embodiment 8:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.6%, hydroxypropyl cellulose 0.5%, ethanol 0.06%, glycerol 0.05%, tartaric acid 0.1%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.01%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 9:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.6%, sodium alginate 0.6%, ethanol 0.06%, tween 80 0.06%, tartaric acid 0.2%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.02%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 10:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, arabic gum 0.6%, ethanol 0.07%, polyethylene glycol 200 0.06%, tartaric acid 0.3%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.03%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 11:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.7%, hydroxypropyl cellulose 0.7%, propylene glycol 0.07%, glycerol 0.07%, tartaric acid 0.4%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.04%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 12:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.8%, sodium alginate 0.7%, propylene glycol 0.08%, tween 80 0.07%, tartaric acid 0.5%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 13:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.8%, arabic gum 0.8%, propylene glycol 0.08%, polyethylene glycol 200 0.07%, tartaric acid 0.6%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 14:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, hydroxypropyl cellulose 0.9%, sodium alginate 0.8%, glycerol 0.08%, tween 80 0.07%, tartaric acid 0.7%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 15:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, hydroxypropyl cellulose 0.9%, arabic gum 0.9%, glycerol 0.08%, polyethylene glycol 200 0.07%, tartaric acid 0.8%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 16:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium alginate 1.0%, arabic gum 0.9%, tween 80 0.08%, polyethylene glycol 200 0.07%, tartaric acid 0.9%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 17:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, sodium carboxymethyl cellulose 0.7%, hydroxypropyl cellulose 0.6%, ethanol 0.05%, propylene glycol 0.05%, glycerol 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 18:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, sodium carboxymethyl cellulose 0.7%, sodium alginate 0.6%, ethanol 0.05%, propylene glycol 0.05%, tween 80 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 19:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, sodium carboxymethyl cellulose 0.7%, arabic gum 0.6%, ethanol 0.05%, propylene glycol 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 20:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, hydroxypropyl cellulose 0.7%, sodium alginate 0.6%, ethanol 0.05%, glycerol 0.05%, tween 80 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 21:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, hydroxypropyl cellulose 0.7%, arabic gum 0.6%, ethanol 0.05%, glycerol 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 22:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.7%, sodium alginate 0.7%, arabic gum 0.6%, ethanol 0.05%, tween 80 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 23:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.7%, hydroxypropyl cellulose 0.7%, sodium alginate 0.6%, propylene glycol 0.05%, glycerol 0.05%, tween 80 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 24:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.7%, hydroxypropyl cellulose 0.7%, arabic gum 0.6%, propylene glycol 0.05%, glycerol 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 25:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.7%, sodium alginate 0.7%, arabic gum 0.6%, propylene glycol 0.05%, tween 80 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 26:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, hydroxypropyl cellulose 0.7%, sodium alginate 0.7%, arabic gum 0.6%, glycerol 0.05%, tween 80 0.05%, polyethylene glycol 200 0.05%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 27:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.5%, sodium carboxymethyl cellulose 0.5%, hydroxypropyl cellulose 0.5%, sodium alginate 0.5%, ethanol 0.03%, propylene glycol 0.04%, glycerol 0.04%, tween 80 0.04%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 28:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.5%, sodium carboxymethyl cellulose 0.5%, hydroxypropyl cellulose 0.5%, arabic gum 0.5%, ethanol 0.03%, propylene glycol 0.04%, glycerol 0.04%, polyethylene glycol 200 0.04%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 29:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.5%, sodium carboxymethyl cellulose 0.5%, sodium alginate 0.5%, arabic gum 0.5%, ethanol 0.03%, propylene glycol 0.04%, tween 80 0.04%, polyethylene glycol 200 0.04%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 30:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.5%, hydroxypropyl cellulose 0.5%, sodium alginate 0.5%, arabic gum 0.5%, ethanol 0.03%, glycerol 0.04%, tween 80 0.04%, polyethylene glycol 200 0.04%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 31:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, sodium carboxymethyl cellulose 0.5%, hydroxypropyl cellulose 0.5%, sodium alginate 0.5%, arabic gum 0.5%, propylene glycol 0.03%, glycerol 0.04%, tween 80 0.04%, polyethylene glycol 200 0.04%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Embodiment 32:
A kind of fenbendazole nano suspension, being made up of the component of following mass fraction: fenbendazole 8%, methylcellulose 0.4%, sodium carboxymethyl cellulose 0.4%, hydroxypropyl cellulose 0.4%, sodium alginate 0.4%, arabic gum 0.4%, ethanol 0.03%, propylene glycol 0.03%, glycerol 0.03%, tween 80 0.03%, polyethylene glycol 200 0.03%, tartaric acid 1.0%, phosphate 0.5%, citric acid 0.5%, benzyl alcohol 0.05%, phenol 0.05%, sodium benzoate 0.05%, surplus is water for injection.
Other are with embodiment 1.
Test example
Test example 1: color changes with pH
Observe and record the outward appearance of fenbendazole nano suspension, color and luster, clarity, measure its pH simultaneously.
The fenbendazole nano suspension that embodiment 2 prepares is: milky, uniformly, muddy, nanosuspension without Tyndall effect.Having slight lamination, supernatant water white transparency after standing a period of time, lower floor's precipitum is creamy white, and recovers again uniformly, present good resuspendability after jog.In placement process, pH is without substantially changing, and excursion is 5.5～6.2.
Test example 2: sedimentation volumn is than measuring
The ratio of the volume of sedimentation volumn suspensoid more front with sedimentation than the volume being precipitum, can be by sedimentation volumn than the stability that judge suspensoid.The fenbendazole nano suspension 25mL that Example 3 prepares is placed in graduated cylinder, records original height H of suspensoid after close plug0, after forced oscillation 1min, above suspensoid is stood 1,2,3,4,5,6,7d, records the height H of precipitum respectively, then calculate the sedimentation volumn of suspensoid than F (F=H/H0).F should be not less than 0.90, and F is the biggest, shows that suspensoid is the most stable.Sedimentation volumn in the fenbendazole nano suspension 7d after the production of embodiment 3,4,5,6,7 preparation is shown in Table 1 than measurement result.
Table 1 respectively organizes the sedimentation volumn of nano suspension than measuring
Test example 3: redispersion is tested
The fenbendazole nano suspension that embodiment 3,4,5,6,7 after storage 30d prepares is placed in the graduated cylinder of 100 mL, by graduated cylinder spin inversion 180 ° after close plug, reverses 1 time, stop 5s, be calculated as shaking 1 time.The required number of times rotated of record redispersion, is evaluated with " good ", " good ", " typically ", " poor ", investigates stability and the redispersibility of preparation system.Wherein homodisperse for " good " i.e. to occur less than 12 times；Needing to occur homodisperse 12 ~ 60 times is " good "；More than 60 times, but still can homodisperse be " typically "；Cannot homodisperse be " poor ".Under room temperature environment, after the fenbendazole nano suspension of preparation stands 30d, can again disperse, and without precipitation at the bottom of bottle, without grumeleuse in suspensoid, redispersibility the results are shown in Table 2.
The test of nano suspension redispersibility respectively organized by table 2
Above-described is only the preferred embodiment of the present invention, it is noted that for a person skilled in the art, without departing under general idea premise of the present invention, it is also possible to making some changes and improvements, these also should be considered as protection scope of the present invention.
Claims (10)
1. a fenbendazole nano suspension, it is characterised in that: being made up of the component of following mass fraction: fenbendazole 2 ~ 8%, suspending agent 0.5 ~ 2%, wetting agent 0.05 ~ 0.15%, flocculant 0.5 ~ 2%, antibacterial 0.05 ~ 0.15%, surplus is water for injection.
A kind of fenbendazole nano suspension the most according to claim 1, it is characterised in that: described suspending agent is at least one in methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, sodium alginate, arabic gum.
A kind of fenbendazole nano suspension the most according to claim 2, it is characterised in that: described suspending agent is sodium carboxymethyl cellulose.
A kind of fenbendazole nano suspension the most according to claim 1, it is characterised in that: described wetting agent is at least one in ethanol, propylene glycol, glycerol, tween 80, polyethylene glycol 200.
A kind of fenbendazole nano suspension the most according to claim 4, it is characterised in that: described wetting agent is tween 80.
A kind of fenbendazole nano suspension the most according to claim 1, it is characterised in that: described flocculant is at least one in tartaric acid, phosphate, citric acid.
A kind of fenbendazole nano suspension the most according to claim 6, it is characterised in that: described flocculant is citric acid.
A kind of fenbendazole nano suspension the most according to claim 1, it is characterised in that: described antibacterial is at least one in benzyl alcohol, phenol, sodium benzoate.
A kind of fenbendazole nano suspension the most according to claim 8, it is characterised in that: described antibacterial is sodium benzoate.
The preparation method of a kind of fenbendazole nano suspension the most according to claim 1, it is characterised in that: comprise the following steps:
(1) suspending agent, flocculant, antibacterial being dissolved in water for injection, stir to obtain mixture A；
(2) taking wetting agent to be dissolved in water for injection, be subsequently adding fenbendazole, stir to obtain mixture B；
(3) mixture A is joined in mixture B, add to the full amount of water for injection, mix homogeneously, grinds with colloid mill, obtains thick suspension；
(4) the thick suspension of gained in step (3) is mixed by high speed homogenization dispersion machine, homogenisation cycle 3 ~ 5 times under 10 ~ 30MPa pressure, homogenisation cycle 10 ~ 15 times under 100 ~ 150MPa pressure, with 0.45 μm filtering with microporous membrane, obtain fenbendazole nano suspension.
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| CN106727300A (en) * | 2016-12-15 | 2017-05-31 | 河南牧翔动物药业有限公司 | A kind of thiabendazolum supensoid agent and preparation method thereof |
| CN106727304A (en) * | 2017-04-06 | 2017-05-31 | 江西博莱大药厂有限公司 | A kind of Fenbendazole supensoid agent and preparation method thereof |
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| RU2013129100A (en) * | 2013-06-25 | 2014-12-27 | Александр Александрович Кролевец | METHOD FOR ENCapsulating Phenbendazole |
| CN104274398A (en) * | 2013-07-04 | 2015-01-14 | 青岛康地恩动物药业有限公司 | Suspension containing albendazole, and preparation method thereof |
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| RU2013129100A (en) * | 2013-06-25 | 2014-12-27 | Александр Александрович Кролевец | METHOD FOR ENCapsulating Phenbendazole |
| CN104274398A (en) * | 2013-07-04 | 2015-01-14 | 青岛康地恩动物药业有限公司 | Suspension containing albendazole, and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106727300A (en) * | 2016-12-15 | 2017-05-31 | 河南牧翔动物药业有限公司 | A kind of thiabendazolum supensoid agent and preparation method thereof |
| CN106727304A (en) * | 2017-04-06 | 2017-05-31 | 江西博莱大药厂有限公司 | A kind of Fenbendazole supensoid agent and preparation method thereof |
| CN106727304B (en) * | 2017-04-06 | 2019-09-03 | 江西博莱大药厂有限公司 | A kind of Fenbendazole suspension and preparation method thereof |
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Application publication date: 20161005 |