Digoksin

Digoksin

1.Nama Inggris:Digoxin Productoxin

  1. Spesifikasi
    • Kemurnian: Digoxin ≥ 99.0% (HPLC); high – purity grade: ≥ 99.5% (HPLC)
    • Kelarutan: Sparingly soluble in water (0.06 g/L at 25°C), soluble in chloroform, ethanol, and dimethylformamide
    • Penampilan – terkait: Loss on drying ≤ 1.0%, heavy metals ≤ 10 ppm, residual solvents ≤ 0.5%
    • Ukuran Partikel: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for better dissolution in pharmaceutical formulations
  2. Penampilan
    • White to off – white crystalline powder, odorless
  3. NOMOR CAS.：20830 – 75 – 5
  4. Waktu tunggu: 7 – 10 Working Days
  5. Kemasan
    • 0.25 mg/tablet (blister pack or bottle), 10 mg/vial (sterile glass vial for injectable formulation), sealed under nitrogen
  6. Pasar Utama: Global pharmaceutical market, with significant demand in North America, Europe, Asia, especially in cardiology departments and for the treatment of heart conditions
  7. Skenario Aplikasi

Properti Inti

  • Rumus Molekul: C₄₁H₆₄O₁₄
  • Struktur Kimia: A cardiac glycoside composed of a steroid nucleus (aglycone) attached to a trisaccharide (digitoxose) sugar chain.
  • Fitur Utama
    • Inotropic Effect: Inhibits the sodium – potassium ATPase pump in cardiac muscle cells, leading to an increase in intracellular calcium levels. This enhances myocardial contractility, improving cardiac output in patients with heart failure.
    • Rate – Controlling Action: Slows the conduction velocity through the atrioventricular (AV) node, making it effective in controlling the ventricular rate in atrial fibrillation and atrial flutter.
    • Low Therapeutic Index: The margin between the therapeutic and toxic doses is narrow, requiring close monitoring of plasma levels (therapeutic range: 0.5 – 2.0 ng/mL) to avoid adverse effects.
    • Biotransformation: Metabolized primarily in the liver by cytochrome P450 enzymes, with about 60 – 80% excreted unchanged in the urine.

Skenario Aplikasi

1. Cardiovascular Medicine

  • Chronic Heart Failure:
    • A mainstay in the treatment of mild to moderate chronic heart failure, especially in patients with reduced ejection fraction. It improves symptoms such as dyspnea and fatigue, and reduces hospitalizations. Usually prescribed at low doses (0.125 – 0.25 mg/day), with the dosage adjusted based on patient response and serum digoxin levels.
  • Atrial Fibrillation and Atrial Flutter:
    • Used to control the ventricular rate, helping to maintain a more regular and manageable heart rhythm. By slowing the conduction through the AV node, it prevents the ventricles from beating too rapidly in response to the irregular atrial contractions.
  • Supraventricular Tachycardia:
    • In some cases, employed to terminate or prevent episodes of supraventricular tachycardia by affecting the electrical conduction in the heart.

2. Penelitian Klinis

  • Cardiac Physiology Studies:
    • Serves as a tool for researchers to study the function of the sodium – potassium ATPase pump and its role in cardiac muscle contraction and electrical activity. By manipulating digoxin levels, scientists can observe the impact on various cardiac parameters.
  • Drug Interaction Research:
    • Investigated to understand its interactions with other medications commonly used in cardiovascular patients, such as diuretics (which can increase the risk of digoxin toxicity due to potassium depletion) and certain antibiotics. This knowledge helps in optimizing drug regimens and preventing adverse drug – drug interactions.
  • Development of New Therapies:
    • Studied to inspire the development of novel inotropic agents or drugs that target the cardiac electrical system. Its mechanism of action provides insights for creating more effective and safer treatments for heart diseases.

Metode Deteksi

  • Kromatografi Cair Kinerja Tinggi (HPLC):
    • Column: C18 (250 × 4.6 mm, 5 μm), Mobile Phase: Acetonitrile – 0.1% formic acid (25:75 v/v), Flow Rate: 1.0 mL/min, Detection Wavelength: 230 nm for quantification.
  • Immunoassay:
    • Widely used in clinical laboratories for rapid measurement of digoxin levels in serum or plasma. Methods such as fluorescence polarization immunoassay (FPIA) and chemiluminescent immunoassay (CLIA) offer high sensitivity and specificity, allowing for quick assessment of therapeutic and toxic levels.
  • Kromatografi Cair – Spektrometri Massa (LC – MS):
    • Employed for more accurate identification and quantification, especially in research settings or when dealing with complex biological samples. It can distinguish digoxin from its metabolites and other interfering substances, providing detailed information about the drug’s presence and concentration.

Sumber & Keuntungan

  • Sumber Alami: Originally isolated from the leaves of the foxglove plant (Digitalis lanata). However, most digoxin used today is synthetically produced to ensure consistent quality and meet the global demand.
  • Therapeutic Significance: A long – established medication in cardiology, with decades of clinical use, providing effective management of heart failure and cardiac arrhythmias, and improving the quality of life and prognosis for many patients.
  • Research Value: Facilitates fundamental research in cardiovascular physiology and pharmacology, contributing to a deeper understanding of heart function and the development of new treatment strategies.

Kepatuhan Peraturan

  • US FDA: Approved for the treatment of heart failure and cardiac arrhythmias, strictly regulated under the Federal Food, Drug, and Cosmetic Act. Stringent manufacturing, labeling, and safety standards are enforced to ensure the quality, efficacy, and safe use of digoxin – containing products.
  • EMA (European Medicines Agency): Licensed for similar indications, with continuous pharmacovigilance programs in place to monitor adverse effects and ensure patient safety throughout the product lifecycle.
  • China NMPA: Registered for clinical use in the treatment of relevant cardiovascular conditions, subject to Good Manufacturing Practice (GMP) requirements and regular quality inspections to comply with national pharmaceutical standards.
Kategori:

Digoxin: Nature’s Potent Cardiac Glycoside | High-Purity Extracts by Zhonghong Tech

1. What is Digoxin?

Digoxin is a potent cardiac glycoside derived primarily from the foxglove plant (Digitalis lanata Dan purpurea). This bioactive compound exerts profound positive inotropic effects, increasing the force of myocardial contraction, and negative chronotropic effects, slowing heart rate. It achieves this by selectively inhibiting the sodium-potassium ATPase pump (Na+/K+-ATPase) in cardiac myocytes, leading to increased intracellular sodium and subsequently elevated calcium concentrations via the sodium-calcium exchanger (NCX). This mechanism underpins its critical role in managing congestive heart failure (CHF) and controlling atrial fibrillation with rapid ventricular response.

2. Source, Chemical Properties & Identifiers

  • Sumber: Bio-extracted from leaves of Digitalis lanata (preferred for higher yield) via multi-step solvent extraction and chromatography.

  • Sifat Kimia: Steroidal glycoside (Cardenolide). Core structure: Cyclopentanoperhydrophenanthrene nucleus with a lactone ring and trisaccharide chain (Digitoxose x3).

  • Nomor CAS: 20830-75-5

  • Rumus Molekul (MF): C₄₁H₆₄O₁₄

  • Berat Molekul (BM): 780.95 g/mol

  • EINECS: 244-068-1

3. Benefits, Potency, Dosage & Safety

  • Best Source & Highest Content: Zhonghong Tech utilizes premium D. lanata cultivars and proprietary kromatografi arus berlawanan (CCC) technology, yielding digoxin extracts exceeding 99.5% HPLC purity – significantly above industry standard (typically 98%). This minimizes toxic impurities like digitoxin.

  • Manfaat Kesehatan & Mekanisme:

    • Heart Failure: Enhances cardiac output by strengthening systolic contraction (positive inotropy).

    • Arrhythmia Control: Slows AV node conduction, controlling ventricular rate in atrial fibrillation/flutter.

    • Neurohormonal Modulation: May indirectly modulate maladaptive neurohormonal systems (RAAS, SNS) in CHF.

  • Daily Intake (Therapeutic Use ONLY): Crucially, digoxin is a prescription medication, NOT a dietary supplement. Dosing is highly individualized (typical range: 0.125 – 0.25 mg/day). Requires strict medical supervision and therapeutic drug monitoring (TDM) targeting serum levels of 0.5-0.9 ng/mL to avoid toxicity.

  • Critical Precautions & Side Effects:

    • Narrow Therapeutic Index (NTI): Small dose changes can cause toxicity.

    • Interaksi Obat: High risk with diuretics (hypokalemia), amiodarone, verapamil, macrolides, PPIs.

    • Kontraindikasi: Ventricular fibrillation, hypertrophic cardiomyopathy, significant sinus/AV block.

    • Efek Samping: Anorexia, nausea, vomiting, visual disturbances (xanthopsia), fatigue, life-threatening ventricular arrhythmias (esp. in toxicity).

    • Essential: Requires baseline and periodic ECG monitoring, renal function assessment (eGFR), Dan serum electrolyte checks (K+, Mg2+, Ca2+).

4. Memperkenalkan Shaanxi Zhonghong Investment Technology Co., Ltd.
As a premier perusahaan teknologi tinggi dengan 28 years of bioactives expertise, Zhonghong Tech specializes in advanced botanical extraction and purification for chemical, pharmaceutical, and life science sectors. Our core competencies include:

  • Agile R&D: Kolaboratif laboratorium bersama with 5 top-tier universities fuel innovation.

  • Kemurnian yang Tak Tertandingi: Leveraging HPLC (Kromatografi Cair Kinerja Tinggi) Dan superconducting NMR (Nuclear Magnetic Resonance) ensures purity standards exceeding industry norms by 20%.

  • Jangkauan Global: Supplies customized API solutions to multinational pharma and research institutions across 80+ countries.

  • Proprietary Assets: 20+ teknologi yang dipatenkan and a unique perpustakaan gabungan global create significant scientific barriers.

5. Product Benefits & Health Applications
Zhonghong’s ultra-pure digoxin is essential for:

  • Pharmaceutical Manufacturing: Active Pharmaceutical Ingredient (API) for cardiology drugs (tablets, injectables).

  • Clinical Research: Reference standard for pharmacokinetic/toxicokinetic studies and mechanism of action research.

  • Advanced Drug Delivery Systems: Enabling development of nano-formulations or sustained-release matrices for improved NTI management.

6. Usage Guidelines (For Pharmaceutical Formulators & Researchers)

  • Handling: Use in controlled environments (GLP/GMP). Employ appropriate PPE (gloves, mask).

  • Kelarutan: Soluble in pyridine, slightly soluble in chloroform/ethanol, insoluble in water/ether. Formulations often use co-solvents.

  • Stabilitas: Store below 25°C in airtight, light-resistant containers. Monitor for degradation (hydrolysis of sugar moieties).

7. Critical Precautions (Reiterated for Emphasis)

  • STRICT PRESCRIPTION USE ONLY. Not for consumer self-administration.

  • Mandatory TDM: Essential for safe therapeutic use.

  • Vigilance for Toxicity: Recognize early signs (GI, vision changes) and manage aggressively (Digoxin Immune Fab for severe toxicity).

  • Renal Dosing Adjustment: Required in impaired kidney function.

8. Rigorous Product Specifications (Digoxin API – USP/EP Grade)

KategoriParameterSpesifikasiTest Method (Pharmacopoeia)
Residu PestisidaTotal Organochlorine Pesticides≤ 0,1 ppmUSP <561>, GC-MS
Total Organophosphorus Pesticides≤ 0,1 ppmUSP <561>, GC-MS
Piretroid≤ 0,05 ppmUSP <561>, GC-MS
Logam BeratTimbal (Pb)≤ 5 ppmUSP <232>, ICP-MS
Arsenik (As)≤ 2 ppmUSP <232>, ICP-MS
Kadmium (Cd)≤ 1 ppmUSP <232>, ICP-MS
Merkuri (Hg)≤ 0,5 ppmUSP <232>, CV-AAS
MikrobiologiJumlah Total Mikroba Aerobik≤ 1000 CFU/gramUSP <61>, Plate Count
Total Gabungan Ragi & Jamur≤ 100 CFU/gramUSP <61>, Plate Count
Bakteri Escherichia coliTidak ada dalam 1gUSP <62>
Salmonella spp.Tidak ada dalam 10gUSP <62>
Bile-Tolerant Gram-Negative Bacteria≤ 100 CFU/gramUSP <62>
Assay (HPLC)Digoksin99.0% – 101.0%USP Monograph, EP 10.0
Zat TerkaitTotal Impurities≤ 0,5%USP/EP HPLC Method
Kerugian pada Pengeringan≤ 1.0% w/wUSP <731>

9. Proses Produksi Lanjutan

  1. Sumber: Premi D. lanata leaves from audited sustainable farms.

  2. Ekstraksi Primer: Maceration/Percolation with optimized ethanol-water mixtures.

  3. Defatting: Solvent partitioning (e.g., hexane).

  4. Pemurnian: Multi-stage Liquid-Liquid Extraction (LLE) Dan Kromatografi Arus Berlawanan (CCC) for initial separation.

  5. Critical Chromatography: HPLC preparatif using C18 columns under gradient elution for final isolation.

  6. Kristalisasi: Controlled crystallization for particle size distribution.

  7. Liofilisasi: Freeze-drying (lyophilization) to enhance stability.

  8. Rilis QC: Rigorous testing per specifications (Table above) using metode yang tervalidasi.

10. Application Scenarios

  • Pharma: Tablet/capsule API, parenteral solutions for heart failure/arrhythmia.

  • Biomedical Research: Investigating Na+/K+-ATPase signaling roles in cancer/cell growth.

  • Reference Standards: Calibrating diagnostic assays (immunoassays, LC-MS/MS).

11. Comprehensive Quality Control
Zhonghong Tech’s QC framework is GMP/ISO 9001 certified, ensuring batch-to-batch consistency and regulatory compliance. Konfirmasi identitas memanfaatkan FT-IR spectroscopy Dan co-injection HPLC against USP/EP reference standards. Assay and impurity profiling employs validated stability-indicating HPLC-UV/DAD methods, capable of detecting and quantifying digoxigenin, digitoxigenin, and other related glycosides down to 0.05%. Residual solvent analysis (RSA) follows ICH Q3C guidelines menggunakan GC-FID/HS-GC-MS. Elemental impurities are strictly controlled per ICH Q3D menggunakan ICP-MS/OES. Microbiological quality is assured through filtrasi membran Dan bioburden testing in our ISO Class 7 cleanrooms. Studi stabilitas (accelerated & long-term per ICH Q1A(R2)) under defined conditions (25°C/60% RH, 40°C/75% RH) guarantee shelf life (typically 36 months). All analytical methods undergo full validation per ICH Q2(R1) for specificity, accuracy, precision, linearity, range, LOD, LOQ, and robustness. Data integrity is managed via 21 CFR Part 11 compliant LIMS.

12. Pengemasan Aman & Logistik Global

  • Kemasan Utama: Sealed double LDPE/HDPE bags di dalam aluminum foil laminate sachets for light/moisture protection.

  • Kemasan Sekunder: Sturdy Drum HDPE with desiccant.

  • Pelabelan: Compliant with destination regulations (GHS, CLP, DOT, IATA). Includes CAS, LOT#, Expiry, handling warnings.

  • Logistik: Shipped under controlled ambient temperature (15-25°C). Cold chain options available. Global reach via air/sea freight with full traceability Dan certificates (CoA, CoC, MSDS).

13. Deep Dive: Health, Industry & Research

  • Health & Mechanism: Beyond direct cardiac effects, research explores digoxin’s potential anti-inflammatory properties via NF-κB modulation and its complex interplay with endogenous cardiotonic steroids (CTS) like marinobufagenin.

  • Industry & Tech Innovation: Zhonghong focuses on green chemistry (reducing solvent use), continuous manufacturing, and developing highly sensitive LC-MS/MS methods for impurity fingerprinting. Process Analytical Technology (PAT) optimizes extraction yields.

  • Batasan dan Tantangan Penelitian: Key areas include elucidating digoxin’s potential in oncology (ATPase α-subunit isoforms), mitigating toxicity risks melalui therapeutic drug monitoring devices atau antibody fragments (DigiFab), overcoming bioavailability variability, and exploring genetic polymorphisms (e.g., *MDR1/ABCB1*) affecting response/toxicity.

14. FAQ: Digoxin Essentials
* Q: Is digoxin safe as a supplement?
A: Absolutely not. Digoxin is a potent prescription drug with a narrow therapeutic index. Self-administration is dangerous and potentially fatal.
* Q: What makes Zhonghong’s digoxin superior?
A: Unmatched purity (>99.5%) via proprietary CCC/HPLC, rigorous QC exceeding pharmacopoeia, and elimination of toxic contaminants like digitoxin.
* Q: What are the biggest risks with digoxin?
A: Toxicity due to overdose or interactions (esp. causing hypokalemia), manifesting as severe arrhythmias. Requires constant medical monitoring.
* Q: What is digoxin used for primarily?
A: Management of symptomatic chronic heart failure (reduced ejection fraction) and rate control in atrial fibrillation.
* Q: How is digoxin quality ensured?
A: Through validated HPLC-UV/DAD, GC-MS, ICP-MS methods, strict adherence to USP/EP monographs, and comprehensive stability testing.

15. Source High-Purity Digoxin
Procure Zhonghong Tech’s premium cGMP-grade Digoxin API or reference standards:

16. Kesimpulan
Digoxin remains a cornerstone therapy in cardiology, demanding exceptional purity and consistency for efficacy and safety. Shaanxi Zhonghong Investment Technology Co., Ltd. sets the global benchmark through vertically integrated botanical extraction, proprietary purification technologies (CCC, prep-HPLC), Dan rigorous quality systems exceeding pharmacopoeial standardsKomitmen kami untuk scientific barriers, advanced analytical capabilities (NMR, HPLC-MS), Dan kepatuhan peraturan global provides pharmaceutical partners and researchers with a trusted, high-performance digoxin API essential for developing life-saving cardiac medications and groundbreaking research. Partner with Zhonghong for unparalleled quality in bioactive compounds.

17. References (Examples – Use Actual Sources)

  1. Digitalis Investigation Group. (1997). The effect of digoxin on mortality and morbidity in patients with heart failure. N Engl J Med, 336, 525-533. DOI: 10.1056/NEJM199702203360801

  2. USP-NF Monograph: Digoxin. United States Pharmacopeia.

  3. European Pharmacopoeia (Ph. Eur.) 10th Edition: Digoxin Monograph (01/2013:0073).

  4. ICH Q7: Panduan Praktik Pembuatan yang Baik untuk Bahan Farmasi Aktif.

  5. ICH Q3D: Guideline for Elemental Impurities.

  6. Hauptman PJ, Kelly RA. (1999). Digitalis. Circulation, 99(9), 1265-1270. DOI: 10.1161/01.CIR.99.9.1265

  7. Eichhorn EJ, Gheorghiade M. (2002). Digoxin. Prog Cardiovasc Dis, 44(4), 251-266. DOI: 10.1053/pcad.2002.31591

  8. Review on Advanced Extraction Techniques for Plant Glycosides. Journal of Chromatography A. (Hypothetical – use recent reviews).

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