Benoxil (Oxybuprocaine) API Manufacturers & Suppliers
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Oxybuprocaine | CAS No: 99-43-4 | GMP-certified suppliers
A medication that provides temporary topical anesthesia of the eye, facilitating diagnostic procedures and foreign body removal with minimal systemic absorption and rapid onset.
Therapeutic categories
Primary indications
- Used to temporarily numb the front surface of the eye so that the eye pressure can be measured or a foreign body removed
Product Snapshot
- Oxybuprocaine is available primarily as ophthalmic solutions and drops for topical application, with some tablet and liquid formulations
- It is used mainly for ocular anesthesia to facilitate diagnostic procedures or foreign body removal
- The product is approved for use in the US and Canada and also has investigational status
Clinical Overview
Pharmacologically, oxybuprocaine belongs to the class of benzoic acid esters. It exerts its anesthetic effect through reversible binding to voltage-gated sodium channels in neuronal membranes. This interaction stabilizes the membrane and decreases its permeability to sodium ions, thereby inhibiting depolarization and blocking the initiation and propagation of nerve impulses. The resultant effect is a reversible interruption of sensory nerve conduction in the treated area.
Clinical onset and duration of action for oxybuprocaine are comparable to those of tetracaine, with potentially less irritation upon administration. The compound is administered topically and acts locally with minimal systemic absorption. However, due to limited systemic exposure in typical ophthalmic use, detailed ADME (Absorption, Distribution, Metabolism, Excretion) profiles are not extensively characterized in literature. Nevertheless, systemic toxicity risk is low with recommended dosing, though hypersensitivity reactions or local toxicity may occur with repeated or excessive use.
Safety considerations include avoidance of prolonged or repeated dosing, which may lead to corneal epithelial toxicity. Appropriate formulation, sterility, and concentration control are important in minimizing adverse reactions. Oxybuprocaine is available in various ophthalmic preparations under multiple brands globally, often as sterile solutions.
From an API sourcing and quality perspective, oxybuprocaine must meet stringent purity criteria due to its local application in sensitive tissues. Ensuring compliance with pharmacopeial standards and regulatory requirements for residual solvents, impurities, and microbial limits is critical. Reliable suppliers should provide detailed certificates of analysis and evidence of Good Manufacturing Practice (GMP) compliance to support regulatory submissions and maintain product safety and efficacy.
Identification & chemistry
| Generic name | Oxybuprocaine |
|---|---|
| Molecule type | Small molecule |
| CAS | 99-43-4 |
| UNII | AXQ0JYM303 |
| DrugBank ID | DB00892 |
Pharmacology
| Summary | Oxybuprocaine is a local anesthetic that targets voltage-gated sodium channels, specifically the sodium channel protein type 10 subunit alpha. It reversibly stabilizes neuronal membranes by inhibiting sodium ion permeability, which blocks nerve impulse initiation and conduction. This leads to temporary numbness of the ocular surface for diagnostic or minor procedural use. |
|---|---|
| Mechanism of action | Oxybuprocaine binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions. Depolarization of the neuronal membrane is inhibited thereby blocking the initiation and conduction of nerve impulses. |
| Pharmacodynamics | Oxybuprocaine is a local anaesthetic. It may be less irritating than tetracaine, and the onset and duration of action are similar to tetracaine. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium channel protein type 10 subunit alpha | Humans | inhibitor |
Formulation & handling
- Oxybuprocaine is a small molecule local anesthetic suitable for oral, buccal, topical, and ophthalmic formulations.
- Due to moderate water solubility and LogP of 3.05, consideration of solubilization and stability in aqueous ophthalmic solutions is necessary.
- Handling should ensure protection from hydrolysis and maintain sterility in ophthalmic and topical liquid dosage forms.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently protected by patents in the United States until November 15, 2037. It is marketed in the US and Canada, with market maturity expected to progress as patent protection remains in place. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | Oxybuprocaine is supplied by a limited number of originator manufacturers with packaging handled by a separate company, serving primarily the US and Canadian markets. Branded products are established within these regions, but all key US patents extend until 2037, indicating that generic competition is not currently present and is unlikely to emerge in the near term. |
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Oxybuprocaine is a type of Local anesthetics
Local anesthetics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) commonly used to numb a specific area of the body during medical procedures or surgeries. They work by blocking the transmission of nerve signals, preventing the sensation of pain in the targeted region. Local anesthetics are vital for various medical applications, including dental procedures, minor surgeries, and childbirth.
The main mechanism of action for local anesthetics involves the reversible inhibition of sodium channels, which are responsible for the conduction of nerve impulses. By binding to these channels, local anesthetics prevent the influx of sodium ions, which blocks the generation and propagation of nerve signals. This results in temporary loss of sensation in the area where the medication is administered.
Local anesthetics can be categorized into two main types: esters and amides. Esters, such as procaine and benzocaine, are metabolized by plasma esterases, while amides, including lidocaine and bupivacaine, undergo hepatic metabolism. The choice of local anesthetic depends on factors such as the duration of action required, the specific procedure being performed, and the patient's medical history.
It is important to note that local anesthetics should be administered with caution, as they can have potential side effects, including allergic reactions, systemic toxicity, and nerve damage if used improperly. Therefore, proper dosage and administration techniques must be followed to ensure patient safety.
In summary, local anesthetics are essential pharmaceutical APIs used to temporarily block nerve signals, providing localized pain relief during medical procedures. Understanding the different types and their mechanisms of action allows healthcare professionals to select the most appropriate local anesthetic for each patient and procedure, ensuring optimal outcomes and patient comfort.
Oxybuprocaine API manufacturers & distributors
Compare qualified Oxybuprocaine API suppliers worldwide. We currently have 2 companies offering Oxybuprocaine API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Okami Chemical Industry | Producer | Japan | Japan | CoA, JDMF | 7 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001, MSDS | 762 products |
When sending a request, specify which Oxybuprocaine 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 Oxybuprocaine 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.
