Levocabastine API | Antihistamine API Manufacturer in India

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Levocabastine API

Levocabastine is a potent, selective histamine H1-receptor antagonist used primarily for the symptomatic treatment of allergic rhinitis and allergic conjunctivitis. It reduces histamine-mediated allergic responses such as itching, redness, sneezing and watery discharge.

Levocabastine is commonly formulated for topical nasal and ophthalmic administration, providing local antihistamine activity at the site of allergic symptoms.

Levocabastine API Manufacturer in India

Levocabastine is a specialized antihistamine pharmaceutical API manufactured through controlled chemical synthesis, purification and crystallization.

Important quality attributes include identity, assay, related substances, stereochemical purity, water content, residual solvents, elemental impurities and stability.

Chemical Information

CAS Number: 79547-78-1
Molecular Formula: C26H29FN2O2
Molecular Weight: 404.52 g/mol
Drug Class: Antihistamine
Pharmacological Class: H1-Receptor Antagonist
Therapeutic Class: Antiallergic Agent
Therapeutic Area: Allergy / Ophthalmology / Respiratory

Mechanism of Action

Levocabastine selectively antagonizes histamine H1 receptors.

During an allergic reaction, histamine contributes to symptoms such as vasodilation, increased vascular permeability, itching and smooth-muscle stimulation. By blocking H1 receptors, levocabastine helps reduce these effects.

It can therefore reduce:

  • Nasal itching
  • Sneezing
  • Rhinorrhea
  • Ocular itching
  • Ocular redness
  • Watery eyes

Pharmaceutical Applications

Levocabastine is used primarily in topical formulations for:

  • Allergic rhinitis
  • Allergic conjunctivitis
  • Seasonal allergic symptoms
  • Perennial allergic symptoms

Antihistamine Characteristics

Levocabastine is a highly selective H1 antagonist designed for local treatment of allergic symptoms. Its topical administration allows the active ingredient to act directly at nasal or ocular tissues.

Manufacturing Process

Typical API manufacturing may involve:

  1. Preparation of substituted aromatic intermediates
  2. Construction of the piperidine-related intermediate
  3. Controlled chemical transformations
  4. Introduction of the fluorinated phenyl group
  5. Purification
  6. Crystallization
  7. Filtration
  8. Drying
  9. Milling where required
  10. Final analytical testing
  11. Controlled packaging

Quality and Analytical Testing

Levocabastine API quality evaluation may include:

  • Identification by IR
  • Identification by HPLC
  • Mass spectrometry
  • Assay
  • Related substances
  • Stereochemical purity
  • Optical rotation where applicable
  • Water content
  • Residual solvents
  • Elemental impurities
  • Residue on ignition
  • Particle-size distribution where required
  • Stability testing

Storage

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

Pharmaceutical Research and Development

Levocabastine is relevant to research involving:

  • Histamine H1 receptors
  • Antihistamines
  • Allergic rhinitis
  • Allergic conjunctivitis
  • Seasonal allergies
  • Perennial allergies
  • Ophthalmic antihistamines
  • Nasal antihistamines
  • Allergy pharmacology

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 ≤ 0.5%
Total Impurities ≤ 1.5%
Water Content NMT 1.0%
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