Milbemycin Oxime And Praziquantel Tablets

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

Milbemycin Oxime and Praziquantel Tablets are a broad‑spectrum antiparasitic formulation specifically developed for dogs and cats, providing comprehensive parasite control through the synergistic action of two active ingredients. This dual‑agent combination delivers multi‑species coverage against a wide range of internal parasites, including nematodes, cestodes, and developmental stages of heartworms. Milbemycin oxime exerts its anthelmintic effect by binding to gamma‑aminobutyric acid (GABA) receptors and glutamate‑gated chloride channels on the membranes of parasitic nerve and muscle cells. This binding inhibits the closure of chloride ion channels, leading to sustained chloride ion influx, neuronal hyperpolarization, and blockade of action potential conduction. As a result, neuromuscular transmission is disrupted, causing paralysis and loss of contractile function in the body‑wall muscles of susceptible nematodes. Unable to maintain normal body‑cavity pressure or coordinated movement, the parasites become non‑viable and are eliminated. Additionally, milbemycin oxime effectively targets microfilariae and third‑stage (L3) larvae in the bloodstream, interrupting the life cycle of *Dirofilaria immitis* and helping to prevent heartworm disease in dogs. Praziquantel acts primarily against cestodes (tapeworms) by inducing rapid, sustained contraction and spastic paralysis of the parasite's body‑wall musculature. This immediate muscular disruption leads to structural damage, vacuolar degeneration of the tegument, and exposure of parasite surface antigens. The damaged tegument not only compromises the parasite's integrity but also triggers an immune response from the host, further contributing to parasite destruction. Praziquantel also interferes with nucleic acid synthesis and impairs glycogen uptake and energy metabolism, leading to progressive energy depletion and irreversible damage. Ultimately, the affected tapeworms disintegrate and are expelled from the gastrointestinal tract in the feces. Together, milbemycin oxime and praziquantel provide complementary activity against nematodes, cestodes, and developing heartworm stages, making this combination a widely used and effective option for broad‑spectrum internal parasite control in companion animals.

Certificate of Analysis
Compound name	Milbemycin Oxime And Praziquantel
Grade	Pharmaceutical grade
Quantity	35g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090052
MFG	Jan 9th 2025
EXP	Jan 8th 2028
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.46%
Loss on drying	≤1.0%	0.34%
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

Milbemycin Oxime And Praziquantel Tablets are a broad-spectrum antiparasitic medicine designed specifically for dogs and cats, achieving multi species coverage by combining two active ingredients. Its core applications include prevention of heartworms, eradication of nematodes and tapeworms, and control of ectoparasites.

 

 

Core component analysis

01.

Milbemycin Oxime

Belonging to macrolide antibiotic derivatives, it disrupts the neural transmission system of nematodes and arthropods by interfering with the release of parasitic neurotransmitter gamma aminobutyric acid (GABA). Its target is the chloride ion channel controlled by glutamate, which enhances the permeability of the cell membrane to chloride ions, leading to hyperpolarization of the insect's neuromuscular membrane and ultimately causing paralysis and death. This ingredient has a potent killing effect on nematodes such as heartworm larvae, roundworms, and hookworms, and is relatively safe for mammals (as GABA only exists in the central nervous system and is minimally affected in the peripheral nervous system).

02.

Praziquantel

As a derivative of isoquinoline, it increases the permeability of insect cell membranes to calcium ions, causing muscle rigidity and cortical damage. It has a 100% clinical cure rate for tapeworms (such as canine tapeworm and tapeworm) and flukes (such as schistosomiasis), and its mechanism of action includes:
Muscle rigidity effect: Within 20 seconds after exposure to medicine, the tension of the insect body increases, and a concentration of 1mg/L can cause strong contraction.
Cortical disruption effect: medicine cause vacuolar degeneration of the insect's epidermis, swelling of the syncytial outer skin, ultimately leading to epidermal erosion and rupture, exposing surface antigens and activating the host's immune system for attack.

Neuroblocking effect: Milbeixime binds to GABA receptors on the membrane of parasitic nerve cells, inhibiting the closure of chloride ion channels, leading to sustained hyperpolarization of neurons and blocking action potential conduction. The nematode's body wall muscles lose their ability to contract due to the interruption of nerve signals, and eventually rupture and die due to the inability to maintain body cavity pressure. 

The pathway of action of milberoxime

 

Prevention mechanism of heartworm: By killing microfilaments and L3 stage larvae in the blood, the life cycle of heartworm is blocked. Experiments have shown that the killing rate of heartworm larvae can reach over 98% after a single administration.
External parasite control: It has a killing effect on external parasites such as hair follicle mites, scabies mites, lice, fleas, etc., by disrupting the nerve conduction of arthropods.

Dual insecticidal mechanism of praziquantel

 

Muscle rigidity effect: Praziquantel causes instantaneous rigidity and contraction of the tapeworm's body wall muscles, leading to the rupture of the parasite and its excretion with feces. For example, within 1 minute of exposure to medication, the canine tapeworm developed strong contractions.
Cortical disruption effect: medicine induce vacuolar degeneration of the insect's epidermis, exposing surface antigens and activating the host's immune system for attack. 15 minutes after taking the medication, vacuolar degeneration of the outer layer of the parasite can be seen, and within 24 hours, the inner layer is completely ruptured.
Metabolic interference effect: Inhibits the synthesis of nucleic acid and glycogen uptake in insects.

Advantages of combination therapy

 

Complementary insect spectrum: Milberoxime covers nematodes and heartworms, while praziquantel targets tapeworms and flukes, achieving triple protection of nematodes tapeworms heartworms. For example, for dogs infected with both roundworms and tapeworms, a single dose can eliminate both parasites.
Effective time: Milbeixime reaches its peak blood medicine value in 2.6 hours after oral administration, and praziquantel reaches its peak in 1.1 hours. Combined use can shorten the deworming cycle. The experiment showed that the killing rate of roundworms was 100% within 24 hours after combination therapy, and the clearance rate of tapeworms was 95% within 48 hours.
Medicine resistance prevention and control: By targeting different medicine, we can reduce the pressure of single medicine selection and delay the development of parasite medicine resistance. At present, there have been no reports of resistance to the combination therapy of Mirxexime and Praziquantel.

Milbemycin Oxime And Praziquantel Tablets are a broad-spectrum antiparasitic medicine mainly used for the prevention and treatment of parasites in pets (such as dogs and cats) both inside and outside the body. Milbemycin Oxime belongs to the class of macrolide antibiotics, which have efficient killing effects on nematodes, mites, and heartworm larvae by interfering with the transmission of parasitic neurotransmitter gamma aminobutyric acid (GABA); Praziquantel causes muscle spasms and death by disrupting the calcium ion channels on the surface of parasites, particularly effective against tapeworms and flukes. The combination of the two can achieve broad-spectrum anti parasitic effects

 

 

Raw material preparation

01.

Preparation of Milbemycin Oxime

The preparation of Milbemycin Oxime usually starts from the fermentation products of Streptomyces hygroscopicus var. aureolacerimosus. The fermentation process requires strict control of temperature, pH value, and dissolved oxygen to obtain a high-purity mixture of Milbemycin A3 and A4 (with a ratio of approximately 30:70). Subsequently, Milbemycin A3 and A4 were converted to Milbemycin Oxime through chemical oxidation and oximation reactions. This step requires the use of oxidants (such as hydrogen peroxide) and oxime reagents (such as hydroxylamine), and the reaction conditions need to be precisely controlled to avoid the generation of by-products.

02.

Preparation of Praziquantel

The synthesis of Praziquantel uses cyclohexanediamine as the raw material and generates the target molecule through multi-step substitution reactions. The specific steps include:

Acylation reaction: Cyclohexanediamine reacts with chloroacetyl chloride to produce the intermediate N, N '- bis (chloroacetyl) cyclohexanediamine.
Cyclization reaction: The intermediate is cyclized under alkaline conditions to form a pyrazine isoquinoline skeleton.
Oxidation reaction: The cyclization product is oxidized and introduced into the carbonyl group to generate Praziquantel.

 

Preparation of compound tablets

 

Mix Milbemycin Oxime and Praziquantel active ingredients with excipients (such as starch, lactose, microcrystalline cellulose, cross-linked carboxymethyl cellulose sodium) in a certain proportion to ensure uniform distribution.

Subsequently, adhesive (such as polyvinylpyrrolidone) and wetting agent (such as water or ethanol) are added to form particles through wet granulation technology. The granulation process requires control of stirring speed and drying temperature to avoid particles becoming too hard or too soft.

Drying and whole granules:Place wet particles in a fluidized bed dryer and remove moisture through hot air circulation to obtain dry particles. The dried particles need to be sieved to ensure uniform particle size and facilitate compression.

Packaging and Storage:Put the finished tablets into aluminum foil blister packaging or plastic bottles, seal and store. The packaging materials must comply with the medicine packaging standards to ensure that the medicine do not get damp or spoil during storage

 

 

Tablet pressing and coating

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