Milbemycin Oxime Tablets

Milbemycin Oxime Tablets are a broad-spectrum antiparasitic drug primarily used for the prevention and treatment of various parasitic infections in pets such as dogs and cats. They belong to the class of macrolide antibiotic derivatives. It interferes with the parasitic nervous system (gamma aminobutyric acid, GABA), Causing parasite paralysis and death. Effective against nematodes (such as heartworms, hookworms, roundworms) and certain arthropods (such as fleas and ticks in the larval stage). Mainly used for preventing heartworm disease: By regular administration (usually once a month), it can effectively prevent heartworm larvae from developing into adults and reduce the risk of pet infection; Treating intestinal parasites: targeting common intestinal nematodes such as hookworms, roundworms, and whipworms, it has a killing effect.

At the same time, our company not only provides pure powders, but also tablets and injections. If needed, please feel free to contact us at any time.

Our products

Milbemycin Oxime Powder

Milbemycin Oxime Tablets

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Milbemycin Oxime COA

Certificate of Analysis
Compound name	Milbemycin oxime
Grade	Pharmaceutical grade
CAS No.	129496-10-2
Quantity	337.3kg
Packaging standard	25kg/drum
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090034
MFG	Jan 9th 2025
EXP	Jan 8th 2028
Structure
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

Milbemycin Oxime Tablets are a broad-spectrum antiparasitic drug widely used in pets (dogs, cats). Its core component, Milbemycin 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 and high-yield preparation of the target product.

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------Oxymethylmilbemycin reacts with hydroxylamine hydrochloride (NH ₂ OH · HCl) in an organic solvent (such as methanol) to form an oxime group, ultimately yielding milbemycin 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.

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.

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.

01.

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).

02.

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.

Evaluate the interaction between raw materials and excipients through forced degradation tests (such as high temperature, high humidity, and light exposure) to avoid compatibility taboos.

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

Pre mix milberoxime with a partial diluent (such as MCC) for 10-15 minutes to ensure uniform dispersion of the active ingredient.

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

Wet particles are dried in a fluidized bed dryer at 40-50 ℃ until the moisture content is ≤ 3.0%, and then crushed and agglomerated by a granulator.

4

 

Total mixing

Add the remaining excipients (lubricants, disintegrants) and mix for 20-30 minutes to ensure uniformity of content (RSD ≤ 5%).

5

 

Tablet pressing

Use a rotary tablet press to control the weight difference (± 5%) and hardness (50-100 N) of the tablets, ensuring a disintegration time limit (≤ 15 minutes).

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.

• 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.

The quality control of Mirbexime tablets should cover raw materials, intermediates, and finished products to ensure compliance with GMP and pharmacopoeia standards.

The production of Milbemycin Oxime Tablets must strictly follow GMP standards to ensure traceability and controllable risks throughout the entire process.

The research and development of Milbeixime tablets continues to focus on improving efficacy and optimizing ease of administration.

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