Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of esafoxolaner eprinomectin and praziquantel topical solution in China. Welcome to wholesale bulk high quality esafoxolaner eprinomectin and praziquantel topical solution for sale here from our factory. Good service and reasonable price are available.
Esafoxolaner Eprinomectin And Praziquantel Topical Solution is a broad-spectrum antiparasitic topical drug designed specifically for cats, which combines three active ingredients to prevent and treat a variety of parasitic infections both inside and outside the body, including fleas, ticks, roundworms, hookworms, heartworms, and tapeworms. It is highly effective, safe, and easy to use. It is the first and only broad-spectrum antiparasitic drug for cats that can simultaneously prevent and treat fleas, ticks, roundworms, hookworms, heartworms, and tapeworms. Comprehensive parasite protection can be provided through a one-time application, without the need for cat owners to use multiple medications simultaneously. The killing effect of this drug on adult fleas can reach 92.1% to 99.7% within 24 hours after treatment, and the preventive effect remains above 95.5% in subsequent weekly reinfection for at least one month.
 |
 |
| Esafoxolaner Eprinomectin And Praziquantel Topical Common specifications |
| (1)0.3ml:esafoxolaner 3.6mg+eprinomectin 1.2mg+praziquantel 24.9mg (1.8-5.5 lb) |
| (2)0.9ml:esafoxolaner 10.8mg+eprinomectin 3.6mg+praziquantel 74.7mg (5.6-16.5 lb) |
 |
||
| Certificate of Analysis | ||
| Compound name | Esafoxolaner Eprinomectin And Praziquantel Topical | |
| Grade | Pharmaceutical grade | |
| Quantity | 337.3kg | |
| Packaging standard | 25kg/drum | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090054 | |
| MFG | Jan 9th 2025 | |
| EXP | Jan 8th 2028 | |
| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.48% |
| Loss on drying | ≤1.0% | 0.36% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.90% |
| Single impurity | <0.8% | 0.47% |
| Total microbial count | ≤750cfu/g | 80 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage | Store in a sealed, dark, and dry place below 2-8°C | |
|
|
||
Pet parasitic infections are one of the core challenges in global pet health management. According to the World Association of Small Animal Veterinarians (WSAVA), approximately 60% of cats worldwide are at risk of at least one parasitic infection, with external parasites such as fleas and ticks having an infection rate of up to 45%, and internal parasites such as heartworms, roundworms, hookworms, and tapeworms having an infection rate of 30% -50%. The traditional deworming regimen requires the combined use of multiple drugs (such as oral ivermectin+topical flea drops+oral praziquantel), which has problems such as poor compliance, drug interaction risks, and complex operation. Esafoxolaner Eprinomectin And Praziquantel Topical Solution, as the first broad-spectrum antiparasitic drug for cats, achieves synchronous prevention and control of fleas, ticks, heartworms, roundworms, hookworms, and tapeworms through a single monthly use. The core breakthrough lies in the precise delivery mechanism of three active ingredients through the skin barrier.
Anatomy and Physiology Basis of Skin Barrier
Cat skin, as the first line of defense against external pathogens, is composed of epidermis, dermis, and subcutaneous tissue, forming a triple physical and chemical barrier. Its specificity directly affects drug penetration efficiency and local irritation.
The cat's stratum corneum is composed of 15-20 layers of keratinized cells, with a thickness of approximately 10-15 μ m (20-30 μ m for dogs). The cells form a dense structure through tight junctions and desmosomes. The lipids (ceramides, cholesterol, free fatty acids) between keratinocytes form a hydrophobic matrix in a molar ratio of 1:1:1, forming a "brick wall structure" that restricts the penetration of water-soluble substances.
The resistance of the stratum corneum to drug penetration mainly comes from:
Lipid matrix: Only lipophilic substances with a molecular weight<500 Da and a LogP value of 1-3 are allowed to penetrate through passive diffusion;
Keratinocytes: They absorb large molecules through endocytosis, but the metabolic activity of cat keratinocytes is low, and the efficiency of this pathway is limited;
PH gradient: The surface pH value of cat skin (5.5-7.0) is close to neutral, and the dissociation degree of weakly acidic drugs (such as certain antibiotics) decreases, resulting in a decrease in penetration efficiency.
Epidermal: Chemical defense of the living cell layer
The multi-layered structure and function of the epidermis consist of a basal layer, a spinous layer, a granular layer, and a transparent layer (cats lack a transparent layer):
Basal layer: containing stem cells and melanocytes, maintaining epidermal renewal by secreting growth factors;
Thorn layer: mechanically supported by intercellular bridging granules and secreting antimicrobial peptides (such as defense factor β -1);
Granular layer: Contains Lamellar Bodies, which secrete lipid precursors to participate in the repair of the stratum corneum barrier.
The bidirectional regulation of drug penetration is influenced by the epidermal layer through the following mechanisms:
Metabolic enzyme expression: CYP450 enzyme activity is low in cat epidermal cells, but esterase and amidase activities are high, which may degrade some prodrugs;
Transport protein expression: P-glycoprotein (P-gp) is highly expressed in the basal layer and can pump lipophilic drugs back to the dermis, forming an "efflux pump" effect;
Inflammatory response: During infection or injury, the permeability of the epidermal layer increases, but at the same time, P-gp expression is upregulated, which may reduce drug efficacy.
The density of cat skin hair follicles is 50-100/cm ² (10-50/cm ² for humans), and the diameter of the follicular funnel is about 20-50 μ m, which is the main channel for lipid soluble drug penetration. The sebum secreted by sebaceous glands (containing triglycerides, wax esters, and squalene) forms an acidic lipid membrane (pH 4-5.5), which can dissolve some lipophilic drugs, but excessive sebum may hinder drug release.
The limitation of sweat glands is that they are only distributed in the foot pads of cats, with very little secretion and negligible contribution to drug penetration. However, electrolytes in sweat (such as Na ⁺, Cl ⁻) may alter local pH values and affect drug dissociation status.
The particularity of cat skin barrier
The thickness of the cat's stratum corneum is only one-third of that of dogs, but its lipid content (30% of the dry weight of the stratum corneum) is comparable to that of dogs, resulting in a higher density of lipid matrix and greater resistance to the penetration of water-soluble drugs.
The pH value of cat skin is close to neutral, similar to that of dogs (pH 6.2-7.4), but higher than that of humans (pH 4.5-6.0). A neutral environment may reduce the penetration efficiency of weakly acidic drugs (such as certain antibiotics), but it is beneficial for maintaining the balance of the skin microbiome (such as reducing the colonization of opportunistic pathogens).
Cat hair follicles go through a growth phase (70% -80%), a regression phase (5% -10%), and a resting phase (10% -20%). The drug penetration efficiency varies with the hair follicle cycle: during the growth phase, the funnel part of the hair follicle opens, and the penetration efficiency is highest; During the resting period, hair follicles contract and osmotic resistance increases.
The permeation mechanism and synergistic effect of three active ingredients
Esafoxolaner Eprinomectin And Praziquantel Topical Solution Through molecular modification, nanocrystal technology, and synergistic mechanisms, we break through the cat skin barrier and achieve broad-spectrum anti parasitic effects.
Esafoxolaner: a neurotoxin targeting arthropods
Chemical characteristics and permeation advantages
Esafoxolane is the S-enantiomer of Afoxolane, with a molecular weight of 625.9 g/mol, a LogP value of 4.8, and high lipid solubility. The trifluoromethylphenyl and imidazole rings in its molecular structure endow it with strong penetration ability:
Liposoluble groups: trifluoromethyl (- CF ∝) and imidazole ring enhance molecular hydrophobicity and promote passage through the stratum corneum lipid matrix;
Hydrogen bond receptor: The nitrogen atom in the imidazole ring can act as a hydrogen bond receptor, interacting with the lipid head group of the stratum corneum to reduce osmotic resistance.
Target and insecticidal mechanism
Esafoxolane, as a potent inhibitor of gamma aminobutyric acid (GABA) - gated chloride channels and glutamate gated chloride channels (GluCl), kills arthropods through the following mechanisms:
Neuroinhibition: Blocking GABA/GluCl channels in the postsynaptic membrane of flea and tick neurons leads to increased chloride ion influx, neuronal hyperpolarization, and paralysis induced death;
Selective toxicity: The affinity for mammalian GABA receptors is more than 1000 times lower (cat GABA receptor IC50>10 μ M), ensuring safety;
Autotoxicity effect: When a flea bites, the drug accumulates in the flea's digestive tract through a blood sucking process, killing the flea and preventing it from laying eggs.
The dynamic process of barrier crossing
Initial penetration: After external application, Esafoxolane rapidly penetrates into the dermis layer through the follicular funnel (with a penetration rate of 30% within 1 hour);
System distribution: It is absorbed into the bloodstream through the dermal capillary network and distributed to the skin and subcutaneous tissues throughout the body;
Accumulation effect: Accumulation in adipose tissue (half-life t ₁/₂=12 days), forming long-lasting protection.
Epinomectin: Penetration optimization of broad-spectrum anti parasitic agents
Molecular modification and skin affinity
Molecular modification and skin affinity
Epinomectin is a derivative of avermectin B1, and its permeability is optimized through the following modifications: introducing an acetylamino group to acetylate the C4-OH of avermectin B1, improving its water solubility (solubility 0.5 mg/mL) while retaining its lipophilic skeleton (LogP value 3.8); Add flexible ring structures (such as pentacyclic ethers) to reduce skin penetration resistance. Its molecular weight is 914.13 g/mol, and its surface area is further increased through nanocrystal technology (particle size<200 nm) to promote permeation. Preclinical studies have shown that the dermal concentration reaches its peak (Cmax 4.2 μ g/g) 12 hours after topical application, with a distribution volume of Vd=3.2 L/kg, indicating that the drug can penetrate deep tissues.
Multi target anti parasitic mechanism
Epinomectin kills nematodes and arthropods through the following mechanisms:
GluCl channel activation: induces parasitic neuromuscular paralysis, leading to motor disorders and death;
GABA receptor regulation: enhances GABA mediated chloride ion influx, inhibits parasite feeding and reproduction;
Penetration of blood-brain barrier: The blood-brain barrier permeability in cats is three times higher than that in dogs, and Epinomectin can effectively kill parasites (such as heartworm microfilaments) in tissues.
Skin penetration and systemic distribution
Hair follicle absorption: Within 30 minutes after external application, it is rapidly absorbed through hair follicles and sweat glands (with a penetration rate of 25%);
Lymphatic system transport: entering the bloodstream through dermal lymphatic vessels to avoid first pass effects;
Adipose tissue accumulation: Accumulation in subcutaneous fat (concentration 5-10 times that of plasma), forming a drug reservoir.
Praziquantel: Breakthrough in the penetration of tapeworm specific agents
Molecular properties and skin penetration challenges
Praziquantel has a molecular weight of 312.41 g/mol and a LogP value of 2.8. It belongs to hydrophilic drugs (water-soluble 4 mg/mL) and is traditionally considered difficult to pass through the skin barrier. Its permeation resistance mainly comes from:
Low fat solubility: LogP value<3, difficult to penetrate the lipid matrix of the stratum corneum;
High polarity: The molecule contains pyrazine rings and benzene rings, forming a strongly polar structure that limits passive diffusion.
Mechanism and targeting of tapeworm resistance
Praziquantel kills tapeworms through the following mechanisms:
Calcium channel disruption: activates L-type calcium channels on the surface membrane of tapeworms, leading to increased influx of calcium ions and sustained muscle contraction and spasms;
Surface membrane injury: destroys the glycoprotein structure of tapeworm surface membrane, increases membrane permeability, and leads to parasite dehydration and death;
Immune activation: Exposure to tapeworm antigens activates the host immune system (such as macrophage phagocytosis) to eliminate parasites.
Its LC50 for Dipylidium caninum in dogs is 0.1 μ g/mL, and it is sensitive to common tapeworms in cats such as Taenia solium.
Enhanced penetration of innovative delivery systems
Nano crystal dispersion: Praziquantel nanocrystals rapidly penetrate through the funnel of hair follicles, with a penetration rate of 15% within 1 hour;
Lipid carrier effect: The lipophilic groups of Esafoxolane and Epinomectin form hydrogen bonds with Praziquantel, promoting their passage through the stratum corneum;
PH adjustment: Add citric acid buffer (pH 5.5) to the formula to increase the proportion of non dissociated Praziquantel (from 30% to 70%) and enhance permeation efficiency.
Hot Tags: esafoxolaner eprinomectin and praziquantel topical solution, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale