Afoxolaner Moxidectin And Pyrantel Tablet

Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of afoxolaner moxidectin and pyrantel tablet in China. Welcome to wholesale bulk high quality afoxolaner moxidectin and pyrantel tablet for sale here from our factory. Good service and reasonable price are available.

Afoxolaner Moxidectin And Pyrantel Tablet (hereinafter referred to as "Compound Tablets") is a broad-spectrum antiparasitic compound designed specifically for dogs to prevent and treat flea, tick, heartworm, roundworm, and hookworm infections. This compound tablet combines the pharmacological properties of three active ingredients. Afoxolane is an isoxazoline insecticide that activates GABA chloride ion channels, causing high excitability and death of arthropod nerves, and has a rapid killing effect on fleas and ticks. Moxidectin is a macrolide antiparasitic drug that irreversibly activates glutamate gated chloride ion channels, blocking parasite neuromuscular transmission and exhibiting broad-spectrum killing effects against heartworms, nematodes, and mites in vitro. Pyrantel is a tetrahydropyrimidine anthelmintic that causes spastic paralysis of parasites by depolarizing neuromuscular junctions, and is effective against adult and larvae of roundworms and hookworms. This compound tablet is presented in the form of beef flavored soft chewable tablets, administered once a month, with both convenience and palatability, significantly improving pet compliance.

Certificate of Analysis
Compound name	Afoxolaner,Moxidectin And Pyrantel
Grade	Pharmaceutical grade
Quantity	Customize
Packaging standard	Customize
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090053
MFG	Jan 9th 2025
EXP	Jan 8th 2028
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.47%
Loss on drying	≤1.0%	0.35%
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%	0.46%
Total microbial count	≤750cfu/g	70
E. Coli	≤2MPN/g	N.D.
Salmonella	N.D.	N.D.
Ethanol (by GC)	≤5000ppm	400ppm
Storage	Store in a sealed, dark, and dry place below 2-8°C

Afoxolaner Moxidectin And Pyrantel Tablet is a broad-spectrum antiparasitic compound designed specifically for dogs, combining the pharmacological properties of three active ingredients to achieve comprehensive protection against multiple insect species and stages through a single drug. Its core uses include:

Prevention and treatment of flea infections

 

Quickly kill adult fleas and block their life cycle.

Control tick infection

 

It has a long-lasting killing effect on various common ticks such as black legged tick, solitary tick, and American dog tick.

Prevention of heartworm infection

 

100% prevention of canine heartworm infection, blocking the spread of the disease.

Treatment of intestinal nematode infection

 

Effectively eliminates adult and larval roundworms and hookworms, reducing environmental pollution.

Improving pet health and quality of life

 

By reducing the burden of parasites, reducing the risk of complications such as skin diseases, anemia, and malnutrition.

This compound tablet is presented in the form of beef flavored soft chewable tablets, administered once a month, with both convenience and palatability, significantly improving pet compliance.

Afoxolane: Isoxazoline insecticide

 

Mechanism of action: Afoxolane selectively inhibits insect gamma aminobutyric acid (GABA) receptors and glutamate receptors, blocking the opening of chloride ion channels, leading to neuronal overexcitation, and ultimately causing paralysis and death in arthropods. Its target of action is highly conserved and low in mammals, therefore it has high safety for dogs.
Flea control: Within 24 hours after a single oral administration, kill more than 99.8% of adult fleas and continuously inhibit flea egg hatching, breaking the life cycle.

Tick killing: It has a rapid contact killing effect on common ticks such as black legged tick and solitary tick, and the efficacy lasts for 30 days. Research has shown that the preventive effect still reaches 98% -100% on the 23rd day after a single administration, and 94% on the 30th day.
Mite treatment: It has an adjuvant therapeutic effect on external parasites such as scabies mites and ear mites (combined with local medication).

Moxidectin: Macrolide Antiparasitic Drug

 

Mechanism of action: Moxidectin irreversibly activates glutamate gated chloride ion channels (GluCl), increasing the permeability of nerve cell membranes to chloride ions, leading to parasite flaccid paralysis and death. Its high lipid solubility allows it to accumulate in adipose tissue, forming a long-lasting drug reservoir.
Heartworm prevention: Monthly administration can 100% prevent canine Heartworm infection and block the development of the third stage larvae (L3) transmitted by mosquitoes and insects.
Nematode treatment: It has a killing effect on adult and larval intestinal nematodes such as roundworms, hookworms, and whipworms, especially suitable for mixed infection cases.

In vitro mite control: Transdermal administration can treat ear mite and scabies mite infections (partially distributed on the skin after oral absorption in compound tablets).
Pharmacokinetic advantages: rapid absorption after oral administration, peak blood drug concentration within 24 hours, half-life of up to 21 days, ensuring long-lasting protection.The accumulation concentration in adipose tissue can reach 100 times that of plasma, and the drug effect can still be maintained for several weeks after discontinuation.

In the field of pet parasite prevention and control, single component deworming drugs are gradually being replaced by multi-component compound preparations due to limited target areas, high risk of drug resistance, and insufficient coverage of the parasite spectrum. Afoxolaner Moxidectin And Pyrantel Tablet integrates three different mechanisms of action of ingredients to construct a "triple attack" synergistic strategy, which not only achieves comprehensive coverage of internal and external parasites such as fleas, ticks, heartworms, roundworms, and hookworms, but also breaks through the simple stacking logic of traditional compound preparations "1+1+1=3" through dynamic complementarity between ingredients, forming a synergistic effect of "1+1+1>3".

The synergistic effect of triple compound tablets stems from the differential attacks of three components on the physiological processes of parasites. Afoxolaner, as an isoxazoline insecticide, inhibits insect gamma aminobutyric acid (GABA) receptors and glutamate receptors, blocks the opening of chloride ion channels, leading to excessive neuronal excitation and causing paralysis and death in arthropods such as fleas and ticks; Moxidectin, as a macrolide antiparasitic drug, irreversibly activates glutamate gated chloride ion channels to disrupt neuromuscular conduction in nematodes (such as heartworms and roundworms), leading to paralysis; Pyrantel, as a tetrahydropyrimidine anthelmintic, inhibits acetylcholinesterase activity, causing acetylcholine to accumulate and triggering sustained muscle contractions in intestinal nematodes (such as roundworms and hookworms), ultimately leading to spasmodic paralysis and excretion from the body.

Collaborative Logic 1: Covering the entire lifecycle stage

The complete life cycle of fleas includes four stages: egg, larva, pupae, and adult. It is difficult for a single component to simultaneously block all stages. Afoxolaner can quickly kill adult insects (with an effective rate of ≥ 99.8% within 24 hours) and reduce the discharge of insect eggs in the environment; Although Pyrantel mainly targets intestinal nematodes, its indirect inhibitory effect on flea larvae (by reducing organic matter in host feces and disrupting the living environment of larvae) can assist Afoxolane in controlling flea populations; Moxidectin further blocks the metamorphosis of flea larvae from pupae to adults by inhibiting the microorganisms required for their development, such as symbiotic bacteria. Three studies have shown that triple compound tablets have a 23% higher inhibition rate on flea egg hatching compared to using Afoxolane alone, and a 92% higher clearance rate on environmental flea larvae.

Collaborative Logic 2: Breaking through the Target Limitations of a Single Component

The prevention of Dirofilaria immitis requires simultaneously blocking the third stage larvae (L3) transmitted by mosquitoes and the microfilaments (L1) in the host's body. Moxidectin can penetrate the blood-brain barrier and directly kill L3 larvae, but its clearance of L1 microfilaments relies on the assistance of the host immune system; Although Afoxolaner does not directly act on heartworms, it can reduce the chances of mosquitoes coming into contact with their hosts by reducing the bites of blood sucking arthropods such as fleas and ticks, indirectly reducing the risk of heartworm transmission;

Pyrantel reduces immune suppression caused by parasitic infections and enhances resistance to heartworm worms by clearing intestinal nematodes. Clinical data shows that the triple compound tablets have a 100% effective rate in preventing heartworm infection, and still maintain a killing rate of>99% in drug-resistant heartworm strains (such as JYD-34 isolated strain), significantly better than the 92% effective rate of using Moxidectin alone.

Collaborative Logic 3: Extending the duration of drug action

The high lipid solubility of Moxidectin allows it to accumulate in adipose tissue at a concentration up to 100 times that of plasma, forming a long-acting drug library (half-life of 21 days). However, when used alone, uneven drug distribution may lead to insufficient local concentration; The rapid onset of Afoxolane (peak 2 hours after oral administration) can fill the early pharmacological gap of Moxidectin; The local intestinal function of Pyrantel can target the early infection stage of intestinal parasites such as hookworms (larvae developing in the intestinal mucosa), forming a temporal synergy of "early interception mid-term control long-term prevention". Laboratory simulation experiments have shown that the duration of efficacy of triple compound tablets is extended by 40% compared to using Moxidectin alone, and the prevention and control effect on mixed infections (such as fleas, ticks, and heartworms) is improved by 58%.

In the field of pet parasite prevention and control, the combined use of Afoxolane, Moxidectin, and Pyrante Tablets has become an efficient solution. However, the synergistic effect of these three components during the absorption stage is not simply a superposition, and the core contradiction lies in the balance between the lipid soluble carrier and the aqueous dispersion.

Afoxolane: Highly lipophilic isoxazoline compounds

 

Afoxolaner belongs to the isoxazoline insecticide class, which contains multiple halogen atoms (such as trifluoromethyl) and aromatic rings in its molecular structure, endowing it with strong lipophilicity. Experimental data shows that the solubility of Afoxolaner in n-octanol is over 250 mg/mL, and the oil-water partition coefficient (logP) far exceeds 5, indicating that it easily penetrates the lipid bilayer of cell membranes. However, this high lipid solubility also results in extremely low solubility in aqueous environments. If directly administered as an aqueous formulation, the drug may not be absorbed due to precipitation.

Moxidectin: Lipophilic Macrolide Antibiotics

 

Moxidectin, as a macrocyclic lactone compound, contains multiple hydroxyl and ether bonds in its molecule. Although it has a certain hydrophilicity, it is still mainly lipophilic overall. Research has shown that the distribution of Moxidectin in adipose tissue is 3-4 times that in plasma, and it can be excreted through milk, further demonstrating its lipid solubility characteristics. This characteristic enables it to penetrate the cell membrane of parasites, but also faces the challenge of aqueous dispersion.

Pyrantel: Water soluble tetrahydropyrimidine compounds

 

Unlike the previous two, Pyrante (such as Pyrante pamoate) is almost insoluble in fat, and although its water solubility is limited, it can significantly increase solubility by forming salts (such as tartrate). The mechanism of action of Pyrantel relies on its direct contact in the intestine, therefore it needs to exist in an aqueous dispersed form to ensure sufficient contact with parasites.

Contradictory core: Afoxolane and Moxidectin rely on lipophilic carriers to penetrate cell membranes, while Pyrantel requires aqueous dispersion to exert local intestinal effects. If the three are simply mixed, differences in physicochemical properties may lead to drug precipitation, uneven absorption, or decreased bioavailability.

Afoxolaner absorption: lipid soluble mediated passive diffusion

 

After oral administration, Afoxolane needs to dissolve in bile or fat particles in the gastrointestinal tract, and then penetrate small intestinal epithelial cells through passive diffusion. Its absorption rate is significantly affected by lipid solubility: a high-fat diet can promote bile secretion, increase the solubility of Afoxolane, thereby enhancing peak blood concentration (Cmax) and bioavailability. However, if there is a lack of lipid soluble carriers in the formulation, the drug may remain in the gastrointestinal tract due to insufficient dissolution, resulting in delayed or incomplete absorption.

Absorption of Moxidectin: Liposoluble driven Lymphatic Transport

 

The absorption mechanism of Moxidectin is more complex: its high lipid solubility allows it to be transported through the lymphatic system, bypassing the liver's first pass effect and directly entering the bloodstream. This process relies on the binding of drugs to chylomicrons, and the formation of chylomicrons requires sufficient fat intake. Therefore, the absorption efficiency of Moxidectin is closely related to the fat content in the diet. If the fat soluble components in the formulation are insufficient, Moxidectin may not be able to effectively bind to chylomicrons, resulting in reduced absorption.

Pyrantel absorption: Water soluble mediated local effects

 

The target of Pyrantel is in the intestine, and its absorption is not the main purpose. However, some Pyrantel may be absorbed into the bloodstream by intestinal epithelial cells, but this process has limited significance for parasite prevention and control. More importantly, Pyrantel needs to exist in an aqueous dispersed form in the intestinal lumen to ensure sufficient contact with parasites. If there are too many fat soluble components in the preparation, it may cause Pyrantel to precipitate or be encapsulated by fat, reducing its contact efficiency with parasites.

Contradiction escalation: Afoxolane and Moxidectin require a high-fat environment to promote absorption, while Pyrantel requires an aqueous environment to maintain activity. If the three coexist in the same formulation, the imbalance of drug efficacy may be caused by environmental differences.

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