Lidocaine hydrochloride CAS No:73-78-9
Lidocaine hydrochloride, CAS 73-78-9 ,Local anesthesia,Lidocaine hydrochloride CAS No:73-78-9
Content
Product Introduction
Product Name: Lidocaine hydrochloride
Chemical Name: 2-diallylamino-N-2,6-dimethylphenylacetylamine
Product Purity: ≥ 99.0%
CAS No ：73-78-9
Product Appearance: white crystalline powder
Product Packaging: aluminum foil bag/cardboard drum
Product Storage: Store in a dry and cool place, avoiding sunlight and high temperature
Molecular Formula: C14H23ClN2O
Molecular Weight: 270.80
EINECS No：200-803-8
Shelf Life：24 months
Product Description
Lidocaine hydrochloride is a high-purity pharmaceutical-grade amide-type local anesthetic and Class Ib antiarrhythmic API. As a white crystalline powder with no odor, a bitter taste, and a characteristic numbing sensation, it is highly soluble in water and ethanol, slightly soluble in chloroform, and practically insoluble in ether. Chemically named N-(2,6-Dimethylphenyl)-2-(diethylamino)acetamide hydrochloride monohydrate, our product is synthesized via a refined GMP-compliant process to ensure consistent purity and stable pharmacological activity. It fully complies with USP 43, EP 11, BP 2023, and CP 2020 international pharmacopoeia standards, serving as a core raw material for injectable, topical, and mucosal anesthetic formulations.
Note: The anhydrous form (molecular weight 270.80) is less stable and rarely used in pharmaceutical production; the monohydrate form is the industry standard for medicinal applications.
Product Advantages
Advantage | Details |
Pharmacopoeia-Compliant Purity | HPLC purity ≥99.0% (meets USP/EP/BP requirements), total related substances ≤0.5%, heavy metals ≤10 ppm, and loss on drying ≤1.0% (monohydrate standard). Each batch undergoes strict quality testing including IR identification, pH value, and residue on ignition to ensure clinical safety and efficacy. |
Stable GMP Production Capacity | Equipped with a 100,000-level clean production workshop and automated synthesis lines, with an annual output of 300+ tons. Adheres to GMP guidelines throughout the production process, ensuring batch-to-batch consistency and reliable supply for global pharmaceutical manufacturers. |
Comprehensive Regulatory Support | Provides complete documentation package including batch-specific COA, MSDS, GMP certificate, and DMF (Drug Master File) for major markets. Assists customers in import registration and compliance verification in Europe, America, Southeast Asia, and other regions. |
Customized One-Stop Service | Offers customized packaging (1kg/aluminum foil bag, 25kg/fiber drum with double PE liner) and flexible delivery terms (FOB Qingdao, CIF). Professional technical team provides formulation guidance and post-sales support for dosage form development. |
Controlled Toxicity Profile | Low systemic toxicity when used as directed; no cross-allergy with procainamide or quinidine. Optimized synthesis process reduces toxic intermediates, ensuring higher safety margin for clinical application. |
Product COA
Test Item | Specification | Result | Test Method |
Appearance | White crystalline powder | Conforms | Visual Inspection |
Identification (IR) | Matches standard spectrum | Conforms | USP 43 <197K> |
Assay (HPLC) | 99.0% – 101.0% | 99.5% | USP 43 Chromatographic Method |
pH (1% Aqueous Solution) | 4.0 – 5.5 | 4.8 | USP 43 <791> |
Loss on Drying | ≤1.0% (Monohydrate) | 0.45% | 105℃ for 2 hours |
Residue on Ignition | ≤0.1% | 0.06% | USP 43 <281> |
Heavy Metals | ≤10 ppm | <8 ppm | USP 43 <231> Method II |
Related Substances | Total impurities ≤0.5% | 0.17% | HPLC Gradient Elution |
Conclusion | Complies with USP 43 standards for pharmaceutical-grade API | ||
Note: Full COA with batch number, test date, and signature is available upon customer request. Custom testing items can be arranged based on specific market requirements.
Product Function
Local Anesthetic Effect
Blocks nerve impulse conduction by inhibiting voltage-gated sodium channels in nerve fibers, reducing the permeability of nerve cell membranes to sodium ions and preventing the generation and propagation of action potentials. It features fast onset (2-5 minutes after administration), strong diffusion ability, and moderate duration (1-2 hours; prolonged to 2-4 hours when combined with epinephrine). Compared with ester-type anesthetics, it has lower allergenicity and higher clinical safety.
Antiarrhythmic Effect
As a Class Ib antiarrhythmic drug, it shortens the action potential duration of ventricular myocytes, reduces myocardial自律性 (automaticity), and inhibits abnormal ventricular electrical activity without significantly affecting atrioventricular conduction or myocardial contractility at therapeutic doses. It is highly effective for ventricular arrhythmias such as ventricular premature beats, ventricular tachycardia, and ventricular fibrillation caused by myocardial infarction, digitalis toxicity, or cardiac surgery.
Pharmacokinetic Characteristics
Rapidly distributed in tissues after absorption, with a large volume of distribution and ability to cross the blood-brain barrier and placenta. Metabolized in the liver by microsomal enzymes to form monoethylglycinexylidide (MEGX), an active metabolite with local anesthetic activity. Approximately 10% of the drug is excreted in its original form via the kidneys, with a half-life of 1.5-2 hours (prolonged to 3+ hours in premature infants and patients with liver dysfunction).
Product Application
Application Field | Specific Uses & Dosage Forms |
Clinical Anesthesia | • Infiltration anesthesia, epidural anesthesia, nerve block anesthesia (e.g., brachial plexus block), and surface anesthesia (mucosal anesthesia for thoracoscopy, laparoscopy, or urethroscopy). • Dosage forms: 0.25%-2% injection, 2% gel, 4% spray, and 2% jelly. |
Cardiology | • Treatment of ventricular arrhythmias secondary to acute myocardial infarction, cardiac surgery, or digitalis poisoning. • Dosage form: 1%/2% injection for intravenous injection or drip, with a maximum loading dose of 300mg within 1 hour. |
Pain Management | • Relief of postherpetic neuralgia via transdermal administration (lidocaine patch). • Local analgesia for minor surgical incisions and dental procedures. |
Medical Devices | • Lubrication and anesthesia for urinary catheters, endoscopes, and other medical devices to reduce insertion discomfort. • Dosage form: 2% lubricating gel. |
Pharmaceutical R&D | • Used as a reference substance in pharmacological studies on anesthesia and arrhythmia. • Raw material for new dosage form development (e.g., sustained-release microspheres). |
Production Process Diagram
Raw Materials:
2,6-Dimethylaniline (99.5%+), Chloroacetyl Chloride (98.0%+), Diethylamine (99.0%+), Hydrochloric Acid (Pharmaceutical Grade) → Precision Preprocessing: Purify raw materials to remove heavy metals and impurities, control moisture content ≤0.1%
Step 1: Synthesis of Intermediate (2,6-Dimethylchloroacetanilide)
React 2,6-dimethylaniline with chloroacetyl chloride at 0-5℃ under anhydrous conditions; maintain pH 7.0-7.5 with triethylamine. After reaction, filter, wash with ice water, and dry at 60℃ to obtain the intermediate with purity ≥98.5%.
Step 2: Formation of Lidocaine Base
Add the intermediate to diethylamine solution, heat to 80-85℃ for reflux reaction for 6 hours. Cool to room temperature, adjust pH to 10-11 with sodium hydroxide solution, extract with chloroform, and distill to recover solvent to obtain lidocaine base (purity ≥99.0%).
Step 3: Acidification & Crystallization
Dissolve lidocaine base in ethanol, slowly add dilute hydrochloric acid to adjust pH 4.0-5.0, heat to dissolve completely. Add activated carbon for decolorization (0.5% w/w) at 70℃, filter while hot, and cool the filtrate to 0-5℃ for crystallization for 8 hours.
Step 4: Refinement & Drying
Filter the crystal, wash with cold ethanol, and recrystallize once with purified water to enhance purity. Dry under vacuum (60℃, -0.09MPa) to constant weight, controlling moisture content at 3.0%-4.0% (monohydrate standard).
Step 5: Quality Control (QC) Inspection
Conduct full-item testing (HPLC purity, related substances, heavy metals, pH, IR identification) in accordance with USP 43 standards. Only qualified products enter the packaging process.
Step 6: Packaging & Storage
Package in 25kg fiber drums with double PE liners (sterilized by gamma radiation) in a 100,000-level clean room. Label with batch number, production date, and expiry date. Store in a cool, dry warehouse (15-25℃, RH ≤65%).
Packaging
Payment Methods
Delivery methods
Products FAQ
What is the MOQ and delivery lead time for this product?
The MOQ is 1kg (aluminum foil bag) for R&D/small-batch trials and 25kg (fiber drum) for commercial orders. With an annual output of 300+ tons and regular inventory, we ensure 7-10 working days for stock orders and 3-4 weeks for bulk customized orders.
Can you provide customized packaging and labeling?
Yes. We offer customized packaging such as 5kg, 10kg drums or vacuum-sealed aluminum foil bags. Labeling can be tailored to include your required information (batch number, expiry date, pharmacopoeia standard, etc.) in multiple languages, complying with international pharmaceutical packaging regulations.
How is the product transported, and is it classified as a hazardous chemical?
Lidocaine Hydrochloride is non-hazardous (no UN number required). We adopt moisture-proof packaging (double PE liners + fiber drum) and ship via sea (FOB Qingdao) or air (CIF) as per your request. The product is transported separately from oxidizing agents and toxic substances to ensure safety and stability.
What is the shelf life, and how to store the product properly?
The shelf life is 2 years when stored in sealed packaging, in a cool dry place (15-25℃, RH ≤65%), away from direct sunlight and high temperature (≥30℃). We recommend retesting the product before use if stored beyond the expiry date.
How do you handle quality complaints or non-conforming products?
We provide full-process quality tracking. If the product is non-conforming to the agreed standards, please contact us within 7 working days of receipt. We will arrange re-testing immediately; if confirmed, we will provide a replacement, refund, or compensate according to the contract, ensuring your interests are protected.