Xi'an Kintai Biotech Inc is one of the most experienced manufacturers and suppliers of lappaconitine hbr in China. Please feel free to wholesale high quality lappaconitine hbr for sale here from our factory. For price consultation, contact us.
Pharmaceutical-Grade Lappaconitine HBr Active Pharmaceutical Ingredient (API)
Kintaibio®, as a professional supplier of plant-based active ingredients, is committed to providing global pharmaceutical companies with high-purity, high-standard Lappaconitine derived from the roots of *Aconitum sinomontanum* Nakai, meeting pharmaceutical raw material requirements. We primarily offer 96% Lappaconitine HBr tested by titration. Our precise extraction and purification processes ensure high purification of the active ingredient and batch-to-batch stability.
The core value of our Lappaconitine lies in achieving a balance between potent analgesia and non-addictiveness. Its mechanism of action differs from traditional opioids, primarily by blocking peripheral nerve voltage-gated sodium channels (Nav 1.7/1.8) with high affinity, thereby inhibiting the generation and conduction of action potentials and blocking pain signals at their source. This provides an ideal alternative or adjunct to traditional analgesics for developing a new generation of safe, effective, and non-addictive analgesics, especially for chronic pain management such as cancer pain and neuropathic pain.
Lappaconitine HBr quality standard
This product strictly follows the cGMP principles to establish a quality control system, ensuring high consistency and stability between batches. The control of key quality attributes (CQAs) is as follows:
| Test Item | Standard Specifications & Methods | Specific Parameters & Control Significance |
|---|---|---|
| Appearance & Physical Properties | White or off-white crystalline powder; Visual inspection | Uniform color, no visible foreign matter, ensuring uniformity of raw material. |
| Identification | A. HPLC retention time consistency; B. UV absorption spectrum | The retention time of the main peak in the HPLC chromatogram deviates ≤ ±2% from the reference standard; maximum absorption at 252 nm wavelength, ensuring the identity of the component. |
| Content Determination (HPLC-UV) | Area normalization method or external standard method | ≥ 98.0%, ensuring sufficient and efficient active ingredient. |
| Related Substances (HPLC) | Single impurity ≤ 0.5%, Total impurity ≤ 1.5% | Strict control of process impurities and degradation products, ensuring product purity and medication safety. |
| Loss on Drying | Dry at 105°C to constant weight | ≤ 5.0%, strictly controlling moisture to ensure product stability and formulation process adaptability. |
| Ignition Residue | Ignition at 800°C | ≤ 0.5%, controlling inorganic impurities. |
| Heavy Metals | Atomic absorption spectrophotometry or colorimetry | Lead (Pb) ≤ 10 ppm, Cadmium (Cd) ≤ 2 ppm, Arsenic (As) ≤ 3 ppm, Mercury (Hg) ≤ 1 ppm; Total ≤ 20 ppm, far exceeding general standards. |
| Microbial Limits | Plate method | Total aerobic bacteria ≤ 10³ CFU/g, Total molds and yeasts ≤ 10² CFU/g; E. coli, Salmonella, Staphylococcus aureus must not be detected (10g). |
| Bacterial Endotoxins | Dynamic turbidity method | < 10 EU/mg (lower endotoxin level products can be provided based on customer requirements for injectable grade). |
| Particle Size Distribution | Laser diffraction method | D90 ≤ 80μm (≥ 90% pass through 80 mesh), customized micronization services can be provided based on formulation requirements (e.g., D90 ≤ 30μm). |
| Storage & Stability | Long-term stability investigation (ongoing) | Recommended storage conditions: 2-8°C, sealed, protected from light. Accelerated test (40°C ± 2°C/ RH 75% ± 5%, 6 months) and long-term test (25°C ± 2°C/ RH 60% ± 5%, 24 months completed) show no significant changes in quality indicators. Tentative shelf life is three years. |
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Lappaconitine HBr Pharmacological Advantages
Potential Non-Addictive Analgesia: Highly selectively acts on voltage-gated sodium channels (VGSCs), particularly Nav 1.7 and Nav 1.8 subtypes (closely related to pain signal transduction), stabilizing cell membranes and blocking nerve impulses by inhibiting the recovery of their inactivated state.
In various animal pain models (such as the acetic acid writhing test, hot plate test, and neuropathic pain model), its analgesic ED₅₀ ranges from 0.1-0.5 mg/kg (intraperitoneal or intravenous injection), with an analgesic intensity approximately 1/5 to 1/10 that of morphine, but with a longer duration (lasting 4-6 hours after a single dose).
Non-Addictive: Because it does not act on opioid receptors, no psychological dependence (addiction) was observed in drug dependence assessment experiments (such as conditioned place preference tests).
In guinea pig intradermal papule experiments, its half-maximal effective dose (ED₅₀) for infiltration anesthesia was 0.05%, approximately 150 times more potent than procaine. In an isolated toad sciatic nerve block model, its minimum blocking concentration was 3.2 μM, 5-6 times more potent than cocaine. Local anesthesia takes effect in approximately 5-10 minutes and lasts for 60-120 minutes, superior to most commonly used local anesthetics.
Anti-inflammatory and antipyretic activity: In a carrageenan-induced rat paw swelling model, intraperitoneal injection of 2 mg/kg inhibited swelling by more than 50%. Its mechanism is related to the inhibition of inflammatory mediators (such as PGE2 and TNF-α) production and the reduction of capillary permeability. In yeast-induced fever rats, a dose of 1-2 mg/kg showed an antipyretic effect comparable to aspirin, with a longer duration of action.
Lappaconitine HBr Production Process and Process Control
We employ an optimized, stable, and controllable industrial extraction and purification process. The core steps and process control points (IPCs) are as follows:
step 1 Raw Material Pretreatment and Extraction: *Aconitum carmichaelii* rhizomes are pulverized to 20-40 mesh. Using 70% ethanol as the solvent, dynamic countercurrent percolation extraction is performed at 50-60°C until the extract is colorless, ensuring extraction efficiency and energy saving.
Concentration and Preliminary Enrichment: The percolate is concentrated under vacuum membrane conditions at -0.08 MPa and 65±5°C. Ethanol is recovered, yielding an extract with a relative density of 1.10-1.15 (60°C).
step 2 Acid-Base Purification: The extract is adjusted to pH 1.5-2.0 with 2% (v/v) hydrochloric acid solution. After thorough stirring, it is allowed to stand for 12 hours, and centrifuged to remove acid-insoluble impurities. The supernatant is adjusted to pH 9.5-10.0 with concentrated ammonia to fully release the alkaloids.
step 3 Solvent Extraction and Dehydration: The alkalized solution was subjected to three countercurrent extractions using chloroform (solid-to-solution ratio 1:1). The chloroform layers were combined, and 3% (w/v) anhydrous sodium sulfate was added for dehydration overnight, followed by filtration.
step 4 Crude Product Crystallization and Purification: Chloroform was recovered to a small volume, and 95% ethanol (volume ratio 1:2) was added. The mixture was aged at 4°C for 24 hours, resulting in crude crystals. These crystals were filtered, washed with pre-cooled ethanol, and yielded crude high-albinocyanin (purity ≥93%, acid-base titration method).
step 5 Salt Formation and Recrystallization: The crude product was dissolved in an appropriate amount of hot ethanol, and a calculated amount of 40% hydrobromic acid solution was added to adjust the pH to 4.0-4.5. The mixture was then slowly cooled for crystallization. The crystals were recrystallized using an ethanol-water mixed solvent to obtain white crystals of high-albinocyanin hydrobromide monohydrate.
step 6 Final purification and drying: The crystallized product was vacuum dried at 40°C and -0.09 MPa for 8 hours, pulverized through an 80-mesh sieve, and samples were taken for comprehensive testing. Only qualified samples were stored.
Process quality control: Intermediate control points were established at critical steps (such as after extraction and before salt formation). The content of main components and impurity profiles were monitored by TLC or rapid HPLC to ensure process robustness.
Lappaconitine HBr Application Range
Lappaconitine HBr is an ideal raw material for developing the following innovative dosage forms and drugs:
Injectable formulations: For the management of postoperative acute pain and cancer breakthrough pain. Our low-endotoxin grade products are specifically developed for this application.
Oral solid dosage forms: Tablets, capsules, and extended-release tablets for the long-term treatment of chronic cancer pain, trigeminal neuralgia, sciatica, etc.
Topical formulations: Gels, patches, and creams for local joint and muscle pain and postherpetic neuralgia, providing both local analgesia and local anesthesia with low systemic exposure and enhanced safety.
Combination formulations: Can be used in combination with acetaminophen, nonsteroidal anti-inflammatory drugs (NSAIDs), etc., to achieve synergistic analgesic effects and reduce the dosage and side effects of single-drug administration.
Why Choose Kintaibio's Lappaconitine Hbr?
Expertise: We have over 15 years of R&D and manufacturing experience in the field of diterpenoid alkaloids, possessing expertise across the entire technology chain from plant breeding to API production.
Quality: Our quality system not only meets standard requirements but also has enhanced internal control standards specifically for the characteristics of high aconitine (such as related substances and stability). We can provide complete DMF (Drug Master File) support to assist your global registration and application.
Production Capacity: We have a dedicated high aconitine production line with an annual capacity of 100 kg, ensuring a stable supply from clinical research to commercial production.
If you are committed to developing analgesic solutions with enhanced safety advantages, high aconitine, a clinically proven, non-addictive, and potent ingredient, is your strategic choice. We look forward to in-depth discussions with you, providing samples and detailed technical information to jointly promote the development of excellent drugs. Please feel free to contact us at sales@kintaibio.com
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