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Phylloquinone | CAS No: 84-80-0 | GMP-certified suppliers
A medication that treats coagulation disorders and prothrombin deficiencies caused by vitamin K deficiency or interference, supporting restoration of normal blood clotting function.
Therapeutic categories
Primary indications
- Oral phylloquinone is indicated to treat prothrombin deficiency caused by coumarin or indanedione derivatives
- And hypoprothrombinemia secondary to antibacterial therapy, salicylates, or obstructive jaundice or biliary fistulas with concomitant bile salt administration
- Parenteral (intravenous, intramuscular, and subcutaneous) phylloquinone is indicated to treat coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by vitamin K deficiency or some interference with vitamin K activity
Product Snapshot
- Phylloquinone is available in multiple formulation types including oral tablets and solutions as well as parenteral injections and emulsions for intravenous, intramuscular, and subcutaneous administration
- It is primarily used to address various coagulation disorders resulting from vitamin K deficiency or interference with vitamin K activity, including prothrombin deficiency and hypoprothrombinemia related to different clinical conditions
- Phylloquinone holds approved regulatory status in key markets including the United States and Canada
Clinical Overview
Clinically, phylloquinone is indicated for the treatment of coagulation disorders resulting from vitamin K deficiency or interference with its physiological activity. Oral administration is primarily used to correct prothrombin deficiencies caused by coumarin or indanedione anticoagulants and hypoprothrombinemia associated with antibiotic therapy, salicylates, or conditions impairing bile salt availability such as obstructive jaundice. Parenteral forms—intravenous, intramuscular, and subcutaneous—are indicated when a more rapid correction of coagulation defects is required, including coagulation abnormalities secondary to malabsorption syndromes (e.g., sprue, celiac disease), pancreatic cystic fibrosis, or regional enteritis.
Phylloquinone exhibits a long duration of action due to endogenous vitamin K recycling pathways and a broad therapeutic index. It is primarily metabolized in the liver, with elimination following renal excretion of metabolites. Monitoring of prothrombin time is recommended during therapy to assess efficacy. Parenteral administration carries an increased risk of hypersensitivity reactions, underscoring the importance of appropriate clinical monitoring.
Beyond hematologic roles, vitamin K-dependent γ-carboxylation affects matrix proteins in chondrocytes, influencing joint calcification and potentially modifying collagen type II levels; however, these effects remain under investigation in relation to osteoarthritis, bone density, and vascular calcification.
Phylloquinone has a long history of clinical use, having been synthesized since at least 1939 and approved by the FDA prior to 1955. It is recognized globally under various formulations for vitamin K deficiency management and warfarin reversal.
When sourcing phylloquinone API, quality considerations include verification of its molecular identity and purity, absence of contaminants such as residual solvents or heavy metals, and compliance with pharmacopoeial standards such as USP or EP. Given its lipophilic nature, attention to appropriate storage conditions to prevent degradation is essential to maintain potency. Suppliers should provide certificates of analysis and ensure traceability to support regulatory submissions.
Identification & chemistry
| Generic name | Phylloquinone |
|---|---|
| Molecule type | Small molecule |
| CAS | 84-80-0 |
| UNII | S5Z3U87QHF |
| DrugBank ID | DB01022 |
Pharmacology
| Summary | Vitamin K functions as a cofactor for gamma-carboxylase, an enzyme that catalyzes the carboxylation of glutamate residues on coagulation factor precursors II, VII, IX, and X, enabling calcium binding and activation of these clotting factors. This activation process restores normal hemostasis by facilitating the secretion of active clotting factors from hepatocytes. Additionally, vitamin K influences gamma-carboxylation of matrix proteins involved in joint and bone metabolism, with ongoing research into its role in osteoarthritis, bone density, and vascular calcification. |
|---|---|
| Mechanism of action | Vitamin K is a cofactor of gamma-carboxylase. Gamma carboxylase attaches carboxylic acid functional groups to glutamate, allowing precursors of factors II, VII, IX, and X to bind calcium ions. Binding of calcium ions converts these clotting factors to their active form, which are then secreted from hepatocytes into the blood, restoring normal clotting function. Vitamin K may also carboxylate matrix proteins in chondrocytes, inhibiting calcification of joints, and may increase type II collagen. The role of vitamin K in osteroarthritis, bone density, and vascular calcification is currently under investigation. |
| Pharmacodynamics | Phylloquinone is a vitamin K indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K. It has a long duration of action as vitamin K is cycled in the body, and a wide therapeutic index as large doses can be tolerated. Patients should have their prothrombin time monitored during therapy and healthcare professionals should be aware of the increased risk of hypersensitivity reactions with parenteral administration. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Vitamin K-dependent gamma-carboxylase | Humans | substrate, inducer, cofactor |
| Osteocalcin | Humans | agonist |
ADME / PK
| Absorption | A 4 µg oral dose of phylloquinone is 13% ± 9% bioavailable, with a T<sub>max</sub> of 4.7 ± 0.8 hours. 1.5 ± 0.8 nmol is found in the plasma compartment, and 3.6 ± 3.4 nmol is found in the second compartment. A 10 mg intramuscular phylloquinone dose is 89.2% ± 25.4% bioavailable. The same dose reaches a mean C<sub>max</sub> of 67 ± 30 ng/mL, with a mean T<sub>max</sub> of 9.2 ± 6.6 hours, and an AUC of 1700 ± 500 h\*ng/mL. A 10 mg intravenous phylloquinone dose has a mean AUC of 1950 ± 450 h\*ng/mL. |
|---|---|
| Half-life | Intravenous phylloquinone has an initial half life of 22 minutes, followed by a half life of 125 minutes. |
| Metabolism | Phylloquinone's phytyl side chain is omega hydroxylated by CYP4F2. The side chain is then cleaved to 5 or 7 carbons long, and then glucuronidated prior to elimination. Vitamin Ks in general undergo a cycle of reduction to vitamin K hydroquinone by vitamin K epoxide reductase (VKOR), oxidation to vitamin K epoxide by gamma-glutamyl carboxylase, and converted back to vitamin K by VKOR. |
| Route of elimination | Intravenous phylloquinone is 36% eliminated in the feces in 5 days and 22% recovered in urine in 3 days. |
| Volume of distribution | The steady state volume of distribution of phylloquinone is 20 ± 6 L in subjects who are also taking phenprocoumon therapy. |
| Clearance | Intravenous phylloquinone is 90% cleared in 2 hours, and 99% cleared in 8 hours. A 10 mg intravenous dose of phylloquinone has a mean clearance of 91 ± 24 mL/min. |
Formulation & handling
- Phylloquinone is a lipophilic small molecule vitamin K compound available in oral and parenteral forms including injectable emulsions for intramuscular, intravenous, and subcutaneous administration.
- Its extremely low water solubility and high LogP value necessitate formulation as emulsions or solubilized solutions for parenteral use to ensure bioavailability.
- Careful handling to prevent oxidation and maintain stability is important due to its quinone structure and susceptibility of lipid-based formulations to degradation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has recently experienced patent expirations in both the US and Canadian markets, leading to increased availability of generic formulations. As a result, the market is transitioning from exclusive branded products toward greater generic competition and broader accessibility. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Phylloquinone production involves multiple originator manufacturers with established roles in API supply, alongside a diverse array of packagers supporting distribution. Branded products, such as Adeks and Adult Infuvite, have a presence primarily in the US and Canadian markets. The existing patent landscape indicates availability of generic versions, suggesting generic competition is currently active. |
|---|
Safety
| Toxicity | High doses of vitamin K1 are not associated with toxicity. Intravenous administration has been associated with an increased risk of toxicity. These patients should be treated with symptomatic and supportive measures. The intravenous LD<sub>50</sub> in mice is 1170 mg/kg and the oral LD<sub>50</sub> is >24180 mg/kg. |
|---|
- Intravenous administration of vitamin K1 has been associated with increased risk of toxicity
- Appropriate monitoring and supportive measures are recommended
- The intravenous LD50 in mice is 1170 mg/kg, indicating higher acute toxicity via this route compared to oral administration
Phylloquinone is a type of Vitamins
Vitamins are an essential subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a crucial role in maintaining optimal health and well-being. These organic compounds are required in small quantities by the human body to support various metabolic processes and ensure proper functioning of bodily systems. Vitamins can be broadly classified into two groups: fat-soluble vitamins (such as vitamins A, D, E, and K) and water-soluble vitamins (including vitamin C and B-complex vitamins). Each vitamin has a specific role and function within the body.
Pharmaceutical APIs in the vitamin subcategory are carefully synthesized or extracted to meet stringent quality standards and ensure purity, efficacy, and safety. They are used as active ingredients in the formulation of various pharmaceutical products, including dietary supplements, fortified foods, and pharmaceutical formulations.
Vitamin APIs are commonly utilized in the pharmaceutical industry for their therapeutic benefits. For instance, vitamin D API is widely prescribed to treat deficiencies and maintain optimal bone health, while vitamin C API is utilized for its antioxidant properties and immune-boosting effects. B-complex vitamins, such as vitamin B12 API, are essential for energy production and nerve function.
Overall, vitamins are integral to maintaining good health, and pharmaceutical APIs in this subcategory play a vital role in providing these essential nutrients to individuals through various pharmaceutical and dietary applications.
Phylloquinone (Vitamins), classified under Therapeutic Nutrients/Minerals/Electrolyte
Therapeutic Nutrients/Minerals/Electrolytes: A Comprehensive Technical DescriptionTherapeutic nutrients, minerals, and electrolytes are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used to support and enhance overall health and well-being. These compounds play a crucial role in maintaining the body's physiological balance, aiding in various metabolic processes, and addressing specific deficiencies.
Therapeutic nutrients encompass a broad range of substances, including vitamins, minerals, and electrolytes. Vitamins are organic compounds required in small quantities for proper bodily functions and are essential for growth, development, and disease prevention. Minerals, on the other hand, are inorganic substances that support numerous physiological processes, such as bone formation, nerve function, and energy production.
Electrolytes are minerals that carry an electric charge when dissolved in bodily fluids, including sodium, potassium, calcium, magnesium, and chloride. They play a crucial role in maintaining proper hydration, nerve impulses, muscle contractions, and pH balance.
Pharmaceutical APIs in the Therapeutic Nutrients/Minerals/Electrolyte category are designed to address specific deficiencies or imbalances in the body. These APIs are often used in the formulation of dietary supplements, nutritional products, and therapeutic treatments. They are manufactured under stringent quality control guidelines to ensure purity, potency, and bioavailability.
Therapeutic nutrients/minerals/electrolytes APIs are available in various forms, including tablets, capsules, powders, and liquid formulations. They are formulated to meet specific dosage requirements and can be combined with other ingredients for targeted health benefits.
Overall, therapeutic nutrients, minerals, and electrolytes APIs are essential components in maintaining optimal health. Their use helps address deficiencies, support bodily functions, and promote overall well-being. Pharmaceutical companies and healthcare professionals rely on these high-quality APIs to develop effective and safe products that contribute to a healthier population.
Phylloquinone API manufacturers & distributors
Compare qualified Phylloquinone API suppliers worldwide. We currently have 13 companies offering Phylloquinone API, with manufacturing taking place in 6 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Anhui Wanhe | Producer | China | China | CoA, WC | 1 products |
| Biophore India | Producer | India | India | CEP, CoA, GMP, USDMF | 46 products |
| Changzhou Comwin Fine Che... | Producer | China | China | CoA | 235 products |
| Chr. Olesen Group | Distributor | Denmark | Spain | CoA, GMP, MSDS, USDMF | 252 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Enaltec Labs | Producer | India | India | CoA, USDMF | 16 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Jeil Pharmaceutical | Producer | South Korea | South Korea | CoA, JDMF | 12 products |
| Menadiona, S.L. | Producer | Spain | Spain | CoA, ISO9001, MSDS | 15 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| NAVINTA | Producer | United States | Unknown | CoA, USDMF | 15 products |
| Osaka Synthetic Chemical ... | Producer | Japan | Japan | CoA, JDMF | 16 products |
| Shandong Guangtongbao | Producer | China | China | CoA, WC | 1 products |
When sending a request, specify which Phylloquinone API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Phylloquinone API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
