LABETALOL HYDROCHLORIDE LAMOTRIGINE

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Ketotifen API

Ketotifen is a second-generation antihistamine and mast cell stabilizer used primarily for the management of allergic conditions. It acts mainly by blocking histamine H1 receptors and reducing the release of inflammatory mediators from mast cells.

Ketotifen is available in oral and ophthalmic formulations and is widely studied for allergic disorders, including allergic conjunctivitis and respiratory allergic conditions.

Ketotifen API Manufacturer in India

Ketotifen is a specialized antiallergic pharmaceutical API manufactured through controlled chemical synthesis, purification and crystallization.

Important quality attributes include identity, assay, related substances, water content, residual solvents, elemental impurities, residue on ignition and stability.

Chemical Information

CAS Number: 34580-13-7
Molecular Formula: C19H19NOS
Molecular Weight: 309.43 g/mol
Drug Class: Antihistamine / Mast Cell Stabilizer
Pharmacological Class: H1 Histamine Receptor Antagonist
Therapeutic Class: Antiallergic Agent
Therapeutic Area: Allergy / Respiratory / Ophthalmology

Mechanism of Action

Ketotifen primarily blocks histamine H1 receptors, reducing the effects of histamine released during allergic reactions.

It also exhibits mast cell-stabilizing properties, which can reduce the release of inflammatory mediators.

Its pharmacological effects include:

  • H1 histamine receptor blockade
  • Reduction of histamine-mediated allergic responses
  • Stabilization of mast cells
  • Reduction of inflammatory mediator release
  • Relief of allergic symptoms

Pharmaceutical Applications

Ketotifen is used in formulations for:

  • Allergic conjunctivitis
  • Allergic rhinitis
  • Allergic respiratory conditions
  • Other histamine-mediated allergic disorders

The specific indication depends on the formulation and applicable regulatory labeling.

Antihistamine Characteristics

Ketotifen combines antihistaminic activity with mast-cell-stabilizing effects, making it useful in the management of allergic disorders.

Unlike corticosteroids, ketotifen does not primarily act by broad suppression of inflammatory gene transcription; its main pharmacological activity involves histamine receptor antagonism and modulation of mast-cell mediator release.

Manufacturing Process

Typical API manufacturing may involve:

  1. Preparation of substituted benzocycloheptathiophene intermediates
  2. Controlled chemical synthesis
  3. Introduction of the piperidine-containing side chain
  4. Purification
  5. Crystallization
  6. Filtration
  7. Drying
  8. Milling where required
  9. Final analytical testing
  10. Controlled packaging

Quality and Analytical Testing

Ketotifen API quality evaluation may include:

  • Identification by IR
  • Identification by HPLC
  • Assay
  • Related substances
  • Organic impurities
  • Water content
  • Residual solvents
  • Elemental impurities
  • Residue on ignition
  • Melting range
  • Particle-size distribution where required
  • Stability testing

Storage

Ketotifen should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light. Final storage conditions should be established through validated stability studies.

Pharmaceutical Research and Development

Ketotifen is relevant to research involving:

  • Histamine H1 receptors
  • Mast-cell stabilization
  • Allergy pharmacology
  • Allergic conjunctivitis
  • Allergic rhinitis
  • Respiratory allergy
  • Antihistamine drug development
  • Ophthalmic formulations
  • Inflammatory mediator research

Ketotifen API Summary

Ketotifen is a second-generation antihistamine and mast cell stabilizer with CAS Number 34580-13-7, molecular formula C19H19NOS, and molecular weight 309.43 g/mol. It primarily blocks H1 histamine receptors and helps reduce allergic responses and mast-cell mediator release.

Detailed Specifications

Parameter Specification
Appearance White to off-white crystalline powder
Identification IR & HPLC compliant
Assay (HPLC) 98.0% – 102.0%
Loss on Drying NMT 1.0%
Residue on Ignition NMT 0.5%
Individual Impurity NMT 0.5%
Total Impurities ≤ 1.5%
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