Milbemycin oxime tablets are a high-efficiency broad-spectrum oral antiparasitic veterinary medicine, mainly developed for regular prevention and systematic treatment of diverse internal and external parasitic infestations that commonly afflict companion animals including domestic dogs and cats. Chemically, this active ingredient falls under the large category of macrolide antibiotic derivatives with special antiparasitic biological activity. Once absorbed into the parasite's body, milbamycin oxime can specifically interfere with the normal signal transmission of the parasite's central nervous system by acting on gamma-aminobutyric acid.
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Our products
Milbemycin Oxime Powder
Milbemycin Oxime Tablets
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| Product Name | Milbemycin Oxime Powder | Milbemycin Oxime Tablets |
| Product Type | Powder | Tablet |
| Product Purity | ≥99% | ≥99% |
| Product Specifications | 100g/1kg/etc. | For dogs:2.3mg/5.75mg/11.5mg/23.0mg For cats: 5.75mg/11.5mg/23.0mg |
| Product Form | Organic synthesis | Take Orally |
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Milbemycin Oxime COA
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| Certificate of Analysis | ||
| Compound name | Milbemycin oxime | |
| Grade | Pharmaceutical grade | |
| CAS No. | 129496-10-2 | |
| Quantity | Customized | |
| Packaging standard | Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202601090034 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |  |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.38% |
| Loss on drying | ≤1.0% | 0.29% |
| 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% | 99.80% |
| Single impurity | <0.8% | 0.43% |
| 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 -20°C | |
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Its core clinical application scenarios cover two major directions. First, heartworm disease prevention: through standardized regular oral administration at the conventional frequency of once every month.The active ingredient can effectively block the developmental process of invasive heartworm larvae and stop them from maturing into harmful adult heartworms, thus drastically cutting down the overall heartworm infection risk for pets living in high-risk environments.
Second, intestinal parasite clearance: it delivers reliable killing activity against widespread intestinal nematode pathogens carried by pets, including hookworms, roundworms and whipworms, thoroughly removing these intestinal parasites to protect pets' gastrointestinal health and normal nutrient absorption.Milbemycin oxime tablets are a broad-spectrum antiparasitic drug widely used in pets (dogs, cats). Its core component, Milbamycin Oxime, achieves its killing effect by interfering with the parasite's neural transmission system.The chemical structure of Milberoxime belongs to the class of macrolide antibiotic derivatives, and its synthesis pathway requires multiple organic reactions to achieve high-purity.
Chemical synthesis: precise construction from natural products to active molecules
Selection of starting materials
Inspired by natural sources: The chemical structure of Mirbeixime is based on the modification of natural macrolide compounds (such as avermectin), and its anti parasitic activity and pharmacokinetic properties are enhanced by introducing oxymethyl and oxime groups.
Key intermediates: The synthesis usually starts with Mirbeimycin A3/A4 (extracted from Streptomyces fermentation broth), which contains a 16 membered macrocyclic lactone ring as the active core.
Core synthesis steps
Step 1: Oxymethylation reaction- ---Mix Milbermycin A3/A4 with Chloromethyl Methyl Ether (CMME) under alkaline conditions, introduce an oxymethyl group, and generate Oxymethyl Milbermycin. This step requires strict control of the reaction temperature (0-5 ℃) and pH value (8-9) to avoid side reactions.
Step 2: Oxmation reaction------Oxymethylmilbamycin reacts with hydroxylamine hydrochloride (NH ₂ OH · HCl) in an organic solvent (such as methanol) to form an oxime group, ultimately yielding milbamycin oxime. The reaction needs to be carried out in the presence of a catalyst (such as sodium acetate) to improve reaction selectivity.
Step 3: Purification and Crystallization----- Separate the target product through silica gel column chromatography or recrystallization techniques (such as ethyl acetate n-hexane system), with a purity of over 98% to meet pharmaceutical requirements.
Direct compression method (optional)
It is applicable to active ingredients sensitive to moisture and heat. The process is simplified by selecting highly compressible excipients (such as spray dried lactose), but particle fluidity needs to be optimized.
Coating process
Objective: To mask the bitter taste of Mirbeixime and improve pet palatability.
Method: A fluidized bed coating machine was used to spray HPMC aqueous solution (containing pigments and sweeteners), controlling weight gain (2% -5%) and coating uniformity.
Direction of process optimization
Green Chemistry: Exploring biocatalytic methods (such as enzymatic oxygen methylation) to replace traditional chemical synthesis and reduce the use of organic solvents.
Continuous flow reaction: using microchannel reactor to achieve precise control of temperature and pH, shorten reaction time and improve yield.
Raw material selection: Quality comes from the core principle of design
The raw materials of Milbemycin Oxime Tablets include active ingredients (APIs) and excipients, and their quality directly affects the stability and efficacy of the formulation.
Active ingredient (milberoxime)
Supplier Qualification: It is necessary to select raw material manufacturers that have passed GMP certification to ensure compliance with EP (European Pharmacopoeia) or USP (United States Pharmacopeia) standards.
Key quality control indicators:
Content: 98.0% -102.0% (HPLC method).
Regarding substances: single impurities ≤ 0.5%, total impurities ≤ 1.0%.
Residual solvents: methanol ≤ 0.3%, ethyl acetate ≤ 0.5% (GC method).
Accessory selection&Compatibility Study
Diluents: Lactose and Microcrystalline Cellulose (MCC) are used to adjust the weight and hardness of tablets.Adhesive: Polyvinylpyrrolidone (PVP) or hydroxypropyl methylcellulose (HPMC) improves particle compressibility.
Lubricant: Magnesium stearate or silica reduces friction during the compression process.Disinfectant: Crosslinked carboxymethyl cellulose sodium (CCNa) ensures rapid disintegration of tablets.
Coating material: Hydroxypropyl methylcellulose (HPMC) or polyethylene glycol (PEG) is used for masking or moisture resistance.
Formulation process: precision manufacturing from powder to tablet
The preparation process of Milberoxime tablets requires consideration of content uniformity, disintegration time limit, and stability. Common processes include wet granulation and compression method.
Wet granulation and compression method
1
Pre mixing
Combine milbamycin oxime powder with partial diluent like MCC and blend for 10–15 min to evenly spread the key active component across all powder materials fully blend milbamycin oxime with partial diluent such as MCC for 10 to 15 minutes to achieve even.
2
Granulation
Add adhesive solution (such as 5% PVP ethanol solution), form wet particles through high-speed stirring granulator, and sieve (16-20 mesh) to remove oversized or undersized particles.
3
Drying and whole granules
Dry the prepared wet particles thoroughly in a fluidized bed dryer at 40–50 ℃ until the measured moisture content falls to ≤ 3.0%, then crush all large hard agglomerates using a standard industrial dry granulator.
4
Total mixing
Add all the leftover functional excipients including lubricants and disintegrants and blend fully for 20–30 minutes to guarantee consistent uniform drug content with RSD strictly kept below 5%.
5
Tablet pressing
Utilize a precise rotary tablet press to control tablet weight difference within ±5% and hardness between 50–100 N, while maintaining disintegration time strictly limited to no more than 15 minutes as required by specifications
Quality control of Milbamycin Oxime: full process monitoring from raw materials to finished products
The quality control of Mirbexime tablets should cover raw materials, intermediates, and finished products to ensure compliance with GMP and pharmacopoeia standards.
Raw material inspection
Appearance: White to off white crystalline powder, odorless.Identification: The infrared spectrum (IR) is consistent with the spectrum of the test sample.Content determination: HPLC method (C18 column, acetonitrile water as mobile phase, detection wavelength 245 nm).
Stability study
Long term test: Place under 25 ℃± 2 ℃/60% RH ± 5% conditions for 12 months, and regularly test the content and related substances.Accelerated test: Place at 40 ℃± 2 ℃/75% RH ± 5% for 6 months to evaluate the compatibility of packaging materials.
Intermediate control
Particle content: Take the granulated sample and determine the content of Milberoxime (RSD ≤ 2%).Moisture content: determined by Karl Fischer method, with a drying loss of ≤ 3.0%.
Finished product inspection
Content uniformity: Take 10 pieces for measurement, A+1.8S ≤ 15 (USP standard).
Dissolution rate: Paddle method (50 rpm), dissolution rate ≥ 80% in 30 minutes.Microbial limit: Total aerobic bacteria count ≤ 1000 CFU/g, mold and yeast count ≤ 100 CFU/g.
Research and Development Innovation: Technology Driven Product Iteration
The research and development of Milbeixime tablets continues to focus on improving efficacy and optimizing ease of administration.
Development of compound preparations
Combining praziquantel (anti tapeworm) or moxifloxacin (anti parasite antibody) to expand the deworming spectrum, such as Heartgard Plus (milberoxime+praziquantel).
New drug delivery system
Chewable tablets: Improve pet acceptance by adding meat flavorings.Transdermal patch: Exploring non oral administration routes to reduce liver first pass effects.
Green production technology
Using supercritical fluid technology (SCF) to replace organic solvents and reduce environmental pollution.
Production Standards: Standardized Operations under the GMP System
The production of milbemycin oxime tablets must strictly follow GMP standards to ensure traceability and controllable risks throughout the entire process.
Personnel and Training
Operators need to undergo GMP training and be familiar with sterile operation and cleaning validation requirements.
Equipment and Cleaning
Key equipment: Granulator, tablet press, and coating machine need to be regularly calibrated and cleaned.
Environmental control
Clean area: D-level area (10000 level) controls the number of dust particles (≥ 0.5 μ m ≤ 3520000/m ³).
Recording and tracing
Batch production records should provide detailed records of raw material batch numbers, process parameters.
references
In vitro effects of milbamycin oxime: mechanism of action against Angiostrongylus cantonensis and Dirofilaria immitis, 1992
Chemoprophylactic effects of milbamycin oxime against larvae of Dirofilaria immitis during prepatent development, 1991
Development and validation of an LC–MS/MS method for the simultaneous quantification of milbamycin oxime and praziquantel in plasma: application to a pharmacokinetic study in cats, 2023
Frequently Asked Questions
Is milbemycin oxime the same as ivermectin?
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Milbemycin oxime (Interceptor, Ciba-Geigy) is in the same drug family as ivermectin and is also not approved by the Food and Drug Administration for the treatment of canine demodicosis. It may be safer in sensitive breeds as it requires a higher dose to produce side effects.
What does milbamycin oxime do?
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Milbemycin oxime, sold under the well-known brand name Interceptor®, acts as a reliable heartworm disease preventive and effectively treats common internal gastrointestinal parasites including hookworms and roundworms for both domestic dogs and cats. This active ingredient is also widely incorporated into popular multi-active combination veterinary products like Sentinel®, Sentinel Spectrum®, and Trifexis®, paired with complementary parasitic control drugs such as lufenuron or spinosad to deliver broad-spectrum pest protection.
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