Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of prilocaine powder in China. Welcome to wholesale bulk high quality prilocaine powder for sale here from our factory. Good service and reasonable price are available.
Prilocaine powder, CAS 721-50-6, The molecular formula C13H20N2O usually appears as a white crystalline powder at room temperature and pressure. Has a certain degree of granularity and fluidity. This physical state is beneficial for its processing and handling during the formulation process, for example, it can be easily mixed with other excipients to make different dosage forms of drugs, such as ointments, creams, etc. At the same time, the state of crystalline powder also makes it relatively stable during storage and less likely to undergo changes in physical form. As a local anesthetic, it has significant value in clinical applications. It achieves local anesthesia and pain relief by blocking nerve impulse conduction, and is widely used in epidermal anesthesia, skin discomfort relief, and special scenarios such as premature ejaculation treatment. However, it should be noted that our company's products are only for scientific research purposes and are strictly prohibited from being used for other purposes.
Our product
Additional information of chemical compound:
| Product Name | Ketoconazole powder | Prilocaine Ointment |
| Product Type | Powder | Ointment |
| Product Purity | HPLC≥99.0% | ≥99% |
| Product Specifications | Customizable | Customizable |
| Product Package | PE/Al foil bag/ paper box for Pure powder |
Customizable |
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Propionacaine+. COA
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Certificate of Analysis |
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Compound name |
Ketoconazole | |
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CAS No. |
65277-42-1 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2028 |
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Structure |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Chemical Formula |
C13H20N2O |
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Exact Mass |
220 |
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Molecular Weight |
220 |
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m/z |
220 (100.0%), 221 (14.1%) |
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Elemental Analysis |
C, 70.87; H, 9.15; N, 12.72; O, 7.26 |
Solubility
Solubility in water
Prilocaine powder is easily soluble in water. This characteristic is of great significance for its application in medicine. When preparing water-based preparations such as injection solutions, prilocaine can be easily dissolved in water to form a uniform solution, which is convenient for injection administration. Moreover, its good solubility in water also contributes to the absorption and distribution of drugs in the body, as the physiological environment of the human body is mainly aqueous, and drugs can quickly dissolve and enter the bloodstream, thereby exerting their therapeutic effects.
Solubility in ethanol
Propionacaine is easily soluble in ethanol. Ethanol is often used as a solvent or excipient in the pharmaceutical field. The good solubility of prilocaine in ethanol allows it to be mixed with ethanol to prepare some special preparations, such as tinctures. In addition, ethanol may also serve as an effective solvent for extracting prilocaine during the extraction and purification processes of drugs.
Solubility in other solvents
Propionine is slightly soluble in chloroform, but not easily soluble in non-polar solvents such as benzene and ether. The difference in solubility is related to the molecular structure of prilocaine and the polarity of the solvent. Chloroform has a certain polarity, so it can partially dissolve prilocaine; Benzene and ether are non-polar solvents, and according to the principle of "similar solubility", the solubility of prilocaine in these solvents is relatively low. This solubility characteristic has important guiding significance in the separation, purification, and formulation processes of drugs. For example, when selecting solvents for drug extraction, the appropriate solvent system can be chosen based on its solubility.
Boiling point
Boiling point data
The boiling point of prilocaine varies under different conditions. At 760mmHg (standard atmospheric pressure), its boiling point is 361.6 ± 25.0 ℃; Under low pressure conditions of 0.133kPa, the boiling point is 159-162 ℃. Boiling point is the temperature at which a liquid transforms into a gas, influenced by factors such as pressure. At standard atmospheric pressure, prilocaine has a high boiling point, indicating that it is not easily volatile at room temperature and pressure, and has good chemical stability. Under low pressure conditions, the boiling point is significantly reduced, which may be utilized in some special drug preparation processes, such as vacuum distillation, where prilocaine can be evaporated at lower temperatures to achieve separation and purification of the drug.
The relationship between boiling point and drug preparation
Boiling point information is crucial for selecting appropriate separation and purification methods in the production process of drugs. For example, if it is necessary to separate prilocaine from a mixture, methods such as distillation can be used to separate prilocaine powder based on its boiling point difference from other substances. At the same time, during the drying process of drugs, the boiling point of prilocaine also needs to be considered to avoid decomposition or deterioration of the drug due to high temperature.
melting point
Melting point range
The melting point of prilocaine is 37-38 ℃. The melting point is the temperature at which a substance transitions from a solid state to a liquid state, and is an important physical constant. The relatively low melting point of prilocaine allows it to undergo a state change under conditions close to human body temperature. In practical applications, this characteristic may affect the stability of drugs and the storage conditions of formulations. For example, in high temperature environments, prilocaine may gradually melt, affecting the appearance and quality of the drug.
The Effect of Melting Point on Drugs
The stability of melting point is crucial for the quality control of drugs. If the melting point of prilocaine changes, it may indicate a change in the purity, crystal structure, etc. of the drug, thereby affecting its efficacy and safety. Therefore, in the production and storage process of drugs, it is necessary to strictly control temperature and other conditions to ensure the stability of the melting point of prilocaine.
The mechanism of action is mainly based on its blocking effect on sodium ion channels on the membrane of nerve cells. The transmission of nerve impulses depends on the opening and closing of ion channels on the nerve cell membrane, and sodium ion channels play a crucial role in the generation and transmission of nerve impulses. Propavacaine can bind to specific sites of sodium ion channels, preventing the influx of sodium ions and thereby inhibiting the generation and transmission of nerve impulses. This blocking effect is reversible. When the drug concentration decreases or is metabolized, the function of sodium ion channels will gradually recover, and the transmission of nerve impulses will also return to normal. Through this mechanism, prilocaine ointment can produce anesthetic effects in the local area and alleviate patients' pain.
Pharmacokinetic characteristics
After local application, its absorption and metabolism processes have certain characteristics. When the ointment is applied to intact skin, the drug gradually penetrates through the skin into subcutaneous tissue, but is relatively less absorbed systemically. The degree of absorption is influenced by various factors, including dosage, application time, skin thickness in different parts of the body, and other skin conditions. For example, on undamaged skin, after applying the cream to the thighs of adults (260g cream per 400cm ²) for 3 hours, approximately 5% lidocaine and prilocaine are absorbed. The metabolism of prilocaine in the body is mainly carried out through the liver, and its metabolites are mainly excreted through the kidneys. Due to its fast metabolism and low accumulation, Prilocaine powder is relatively safe. However, excessive or long-term use may still cause allergies or toxic reactions, and strict adherence to medical advice is necessary.
adverse reaction
Prilocaine, as an amide local anesthetic, has been widely used in clinical practice since the 1950s and has become a core drug in fields such as invasive anesthesia, nerve block, and epidural block. It inhibits pain signal transduction by blocking sodium channels on the neuronal membrane, and as a Na/K-ATPase inhibitor, it has a unique neurotoxic mechanism. However, with the expansion of clinical applications, the diversity and severity of its adverse reactions have gradually become apparent.
Local reactions: from stimulation to tissue damage
Contact allergy and dermatitis
Prilocaine can induce type IV hypersensitivity reactions, manifested as redness, itching, blisters, and even ulcers at the injection site. Research has shown that the incidence of allergies to EMLA cream (containing lidocaine and prilocaine) is 1.2% -3.5%, with prilocaine being the main allergen. The mechanism is related to the binding of drug molecules as haptens to skin proteins, activating T lymphocyte mediated delayed type reactions.
Neurological damage and sensory abnormalities
High concentrations or repeated injections of Prilocaine may cause axonal damage, leading to numbness, tingling, or decreased sensation at the injection site. Animal experiments have shown that injecting 10% prilocaine around the sciatic nerve of rats significantly reduces nerve conduction velocity, and the degree of damage is positively correlated with concentration.
Local tissue necrosis
Venous extravasation is a serious complication of Prilocaine injection. In the case, a 10 month old child suffered from skin necrosis in the left lower limb due to extravasation of prilocaine via intravenous infusion, requiring one month of treatment for recovery. The mechanism is that the drug directly stimulates endothelial cells, triggering inflammatory reactions and thrombosis, and blocking local blood supply.
Systemic reactions: from metabolic disorders to organ toxicity
Methemoglobinemia
Prilocaine's metabolite, alpha toluidine, can oxidize divalent iron in hemoglobin, leading to the production of methemoglobin (MetHb). When the concentration of MetHb exceeds 15%, patients may experience cyanosis, headache, and fatigue; When the concentration exceeds 50%, it may cause coma or even death. Research has shown that after a single injection of 10mg/kg prilocaine, the concentration of MetHb can reach 6% -8%, and anemia patients are at a higher risk.
Cardiovascular toxicity
Prilocaine can inhibit sodium channels in myocardial cells, prolong action potential duration, and induce arrhythmia. In clinical cases, patients who received injection of prilocaine experienced bradycardia, ventricular premature beats, and even cardiac arrest. In addition, the vasodilatory effect of drugs may lead to hypotension, especially when used in combination with vasoactive drugs.
Central nervous system toxicity
Excessive or rapid absorption of prilocaine can break through the blood-brain barrier and inhibit the central nervous system. Manifested as dizziness, tinnitus, anxiety, convulsions, and in severe cases, respiratory depression. Animal experiments have shown that after intraperitoneal injection of prilocaine in mice, the LD50 is 85mg/kg, and toxic symptoms include tremors, ataxia, and coma.
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