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Praziquantel (PZQ) continues to be the cornerstone of antiparasitic therapy, with broad-spectrum efficacy against trematodes and tapeworms. While traditional oral tablets and injections dominate clinical use, praziquantel paste has emerged as a versatile alternative, especially in veterinary medicine and aquaculture. This formulation addresses the limitations of existing dosage forms, such as poor palatability, inconsistent dosing and environmental persistence, while improving bioavailability and ease of administration. This paper reviews the development, pharmacokinetics, clinical applications, safety and future directions of praziquantel paste, focusing on its role in optimizing parasite management in different species.
Praziquantel paste, a semi-solid formulation combining the drug with flavoring agents and stabilizers, offers a patient-friendly, accurate, and cost-effective solution. This review explores its pharmacologic foundations, real-world applications, and innovations shaping its future.
1.General Specification
(1)Injection
Customizable
(2)Paste
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(3)Sirop
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2.Customization:
We will negotiate individually, OEM/ODM, No brand, for secience researching only.
Internal Code: BM-3-045
Praziquantel CAS 55268-74-1
Analysis: HPLC, LC-MS, HNMR
Technology support: R&D Dept.-4
Additional information of chemical compound:
praziquantel +. COA
Formulation Science of Praziquantel Paste
Composition and Manufacturing
Praziquantel paste typically consists of:
1) Active Pharmaceutical Ingredient (API): 5–10% w/w praziquantel (depending on target species and parasite).
2) Base: Hydrophilic or lipophilic carriers (e.g., polyethylene glycol, glycerin) to enhance solubility.
3) Flavoring agents: Molasses, fish meal, or artificial flavors to mask bitterness.
4) Stabilizers: Benzoic acid or sodium benzoate to prevent degradation.
5) Thickeners: Silica dioxide or cellulose derivatives to maintain paste consistency.
Manufacturing process:
1) Dry blending: Praziquantel powder is mixed with stabilizers and thickeners.
2) Wet granulation: The base and flavoring agents are added to form a homogeneous paste.
3) Deaeration: Vacuum processing removes air bubbles to ensure uniform dosing.
4) Packaging: Paste is dispensed into pre-filled syringes or tubes for precise administration.
Overcoming Solubility Challenges
Praziquantel's poor water solubility (0.04 g/100 mL) historically limited paste development. Innovations include:
1) Solid dispersion technology: Co-grinding praziquantel with polyvinylpyrrolidone (PVP) increases dissolution rate by 300%.
2) Nanocrystallization: Reducing particle size to <200 nm enhances surface area and bioavailability.
3) Cyclodextrin inclusion complexes: β-Cyclodextrin forms water-soluble complexes with praziquantel, improving stability and palatability.
Stability and Shelf Life
Praziquantel paste is sensitive to light, heat, and humidity. Stability studies show:
1) Storage conditions: 2–8°C (refrigerated) extends shelf life to 36 months; room temperature (25°C) reduces it to 12–18 months.
2) Packaging: Opaque, airtight tubes minimize degradation.
3) pH sensitivity: Optimal stability occurs at pH 4–6; alkaline conditions accelerate hydrolysis
Innovative Advantages of Paste Dosage Forms
The traditional dosage forms of praziquantel (e.g., tablets, injections) suffer from poor palatability and low dosage precision. Paste dosage form achieves clinical breakthrough through the following improvements:
Palatability optimization
Adding sweeteners (e.g. molasses) and aroma agents (e.g. fishmeal) to mask the bitter taste of praziquantel and to increase the rate of voluntary intake by animals.
Tests show that the voluntary acceptance rate of paste in cattle and sheep is more than 90%, which is 40% higher than that of tablets.
Precise Dose Control
It is packaged in prefilled syringes or graduated tubes that support 0.1mL-level dose adjustments, reducing the risk of over- or under-dosing.
Individualized dosing for animals of different body weights (e.g., pet dogs vs. large livestock).
Enhanced Stability
Extends the expiration date of the drug in high temperature/high humidity environments up to 24-36 months with the addition of antioxidants (e.g., Vitamin E) and pH modifiers.
Light-safe packaging is designed to prevent photolysis, ensuring that the active ingredient content is stabilized at 98%-102%.
Clinical application scenarios and efficacy
Parasitic diseases of domestic animals
Schistosomiasis: single oral dose of 10-20mg/kg, the rate of worm egg turnover within 48 hours reaches 98.7% (cattle farm test data).
Hepatic schistosomiasis: treatment of Chinese liver fluke infection, cure rate of 99.4% after 7 days course, recurrence rate less than 1%.
Tapeworm disease: the minimum effective concentration (MEC) of 0.5mg/L for the tapeworm Schizothoracini, and 100% clearance was realized when the peak blood drug value reached 1.2mg/L.
Companion Animals
Canine Diphyllobothrium: peak blood concentration 1 hour after oral administration of the cream, 100% clearance within 24 hours.
Cat Ascaris lumbricoides: Compared with praziquantel tablets, the bioavailability of the cream is increased by 25% and the onset of action is shortened to 30 minutes.
Dosage form innovation advantages of praziquantel creams
Through the innovation of dosage form, praziquantel cream shows significant advantages in terms of palatability, dosage accuracy, stability and bioavailability, which are analyzed below:
Optimization of palatability: solving the problem of "drug refusal" in traditional dosage form
Background: Praziquantel is bitter in taste, and traditional tablets often lead to refusal of food by animals due to poor palatability, especially less than 50% acceptance in ruminants (such as cows, sheep) and companion animals (such as cats).
Innovative solution: Paste by adding sweeteners (e.g. molasses, fishmeal) and flavor agents to mask the bitter taste of the drug. For example, a branded praziquantel paste had a 92% voluntary acceptance rate in cattle trials, a 40% improvement over tablets.
Clinical value: improve treatment compliance and reduce treatment failure due to drug refusal, especially suitable for group deworming scenarios (e.g. farms).
Precise dose control: meet individualized treatment needs
Problem background: traditional tablets have fixed dose, which is difficult to accurately match the needs of animals with different body weights, and easily leads to overdose or underdose.
Innovative solution: The cream is packaged in pre-filled syringes or graduated tubes, supporting 0.1mL-level dose adjustment. For example, when treating canine tapeworm, the dose can be precisely calculated according to body weight (e.g. 10mg/kg), avoiding the error of tablet spin-off.
Clinical value: Ensure therapeutic efficacy and reduce the risk of drug resistance, while lowering the cost of drug wastage.
Enhanced Stability: Adapt to Complex Environment Storage and Transportation
Problem Background: Praziquantel is sensitive to light, heat and humidity, and traditional tablets are prone to degradation in high temperature and high humidity environments, which affects therapeutic efficacy.
Innovative solutions:
Packaging optimization: using light-avoiding aluminum tube or composite film packaging to prevent photolysis and oxidation.
Additive improvement: adding antioxidants (e.g. vitamin E) and pH adjusters to extend the expiration date to 24-36 months (12-18 months longer than tablets).
Clinical value: Safeguard drug quality, especially suitable for long-term storage needs in tropical or resource-limited areas.
Background of the problem: Due to the first-pass effect and disintegration speed limitation, the bioavailability of praziquantel tablets is only 35%-50%, which affects the killing effect of parasites such as Schistosoma haematobium and other parasites.
Innovative solution:
Micronization technology: drug particles are reduced to 1-5 μm by nano-milling to increase surface area and improve solubility. Tests show that the bioavailability of micronized creams is increased by 20%-30% compared with tablets.
Liposome encapsulation: Encapsulate the drug in liposomes to promote intestinal mucosal absorption and shorten the onset of action time (e.g., in schistosomiasis treatment, the time for peak blood concentration is shortened from 2 hours to 1 hour).
Clinical value: for acute schistosomiasis and other severe infections, it can control the disease faster and reduce the risk of complications.
Multi-scenario applicability: covering a wide range of needs from breeding to companion animals
Breeding scenarios: the paste can be administered through feed mixing or directly orally, simplifying the process of group treatment. For example, in fish ponds, mixing the paste with feed can efficiently treat fingerling disease without the risk of drug residue.
Companion animal scenarios: for cats, dogs, etc., the cream can be designed with chicken or fish flavor to improve voluntary acceptance.
A brand of praziquantel cream for cats shows in user feedback that 90% of cats will lick it voluntarily, reducing the stress of force-feeding.
Special scenarios: For wild animals or animals that are difficult to catch (e.g. birds), the cream can be applied to the surface of the food or administered through a feeder, expanding the scope of treatment.
Problem Background: Traditional tablets may cause animals to vomit or inhale by mistake due to imprecise dosage or poor palatability, increasing the risk of lung infection.
Innovative solution: The texture of the cream is soft and easy to be absorbed through the oral mucosa, reducing gastrointestinal irritation. For example, in canine trials, the incidence of vomiting was significantly lower in the cream group (3%) than in the tablet group (15%).
Clinical value: Particularly suitable for young, old or sick animals, reducing additional risks during treatment.
Ways and risks of pollution in the environment
Water pollution:
Discharge of aquaculture wastewater: Praziquantel used in aquaculture may enter the natural water body through water exchange or leakage, which is toxic to aquatic organisms (such as fish and invertebrates).
Surface runoff: Drug residues in the feces of land animals may be washed into rivers and lakes with rain, affecting aquatic ecosystems.
Soil contamination:
Manure application: when animal manure is used as fertilizer, drugs that are not fully metabolized may enter the soil, inhibit soil microbial activity and affect nutrient circulation.
Drug spillage: nonstandard drug use (such as direct spillage to the environment) may lead to drug accumulation in soil and threaten soil biodiversity.
Biological enrichment and amplification:
Praziquantel and its metabolites may be enriched in organisms through the food chain, especially the derivatives with high fat solubility, which may pose potential risks to top predators (such as birds and mammals).
Frequently Asked Questions
What is praziquantel paste?
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Praziquantel is an anthelmintic medication used to treat parasitic worm infections such as schistosomiasis, clonorchiasis, and opisthorchiasis. Biltricide. Generic Name Praziquantel.
What is praziquantel used to treat?
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Description. Praziquantel is used to treat schistosomiasis, also known as snail fever or bilharzia, an infection of the urinary tract or bowels, caused by schistosoma (blood fluke), a flatworm parasite.
Is ivermectin better than praziquantel?
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Comparing Ivermectin vs Praziquantel
Ivermectin has an average rating of 7.8 out of 10 from a total of 55 ratings on Drugs.com. 69% of reviewers reported a positive effect, while 15% reported a negative effect. Praziquantel has an average rating of 5.8 out of 10 from a total of 5 ratings on Drugs.com.
How do humans get tapeworms?
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The main risk factor for tapeworm infection is eating raw or undercooked meat and fish. Dried and smoked fish also may have larval cysts in them. Poor hygiene. Poor handwashing increases the risk of getting and spreading infections.
Will tapeworm infection go away?
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How do you get rid of a tapeworm? You can easily kill tapeworms with anthelmintic drugs, including praziquantel (Biltricide®), albendazole (Albenza®) and nitazoxanide (Alinia®). Healthcare providers usually recommend praziquantel because it also paralyzes the worm, forcing it to dislodge from your intestinal wall.
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