Labetalol Hydrochloride API | Beta Blocker API Manufacturer in India

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Labetalol Hydrochloride API

Labetalol Hydrochloride is a combined alpha-1 adrenergic receptor blocker and beta-adrenergic receptor blocker used primarily for the management of hypertension. It reduces blood pressure through a combination of decreased peripheral vascular resistance and reduced cardiac activity.

Labetalol Hydrochloride is commonly used in the management of hypertension, including certain acute hypertensive situations where rapid blood-pressure control is required.

Labetalol Hydrochloride API Manufacturer in India

Labetalol Hydrochloride is a specialized cardiovascular pharmaceutical API manufactured through controlled chemical synthesis, purification and salt formation.

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

Chemical Information

CAS Number: 32780-06-6
Molecular Formula: C19H24N2O3·HCl
Molecular Weight: 364.87 g/mol
Drug Class: Adrenergic Blocker
Pharmacological Class: Alpha-1 and Beta Adrenergic Receptor Blocker
Therapeutic Class: Antihypertensive
Therapeutic Area: Cardiovascular

Mechanism of Action

Labetalol blocks both alpha-1 adrenergic receptors and beta adrenergic receptors.

Alpha-1 blockade causes peripheral vasodilation and decreases systemic vascular resistance, while beta blockade reduces cardiac stimulation.

The combined activity results in:

  • Reduced peripheral vascular resistance
  • Decreased blood pressure
  • Reduced heart rate and cardiac stimulation
  • Reduced sympathetic effects on the cardiovascular system

Pharmaceutical Applications

Labetalol Hydrochloride is used for:

  • Hypertension
  • Severe hypertension requiring rapid control
  • Hypertensive emergencies
  • Pregnancy-associated hypertension in appropriate clinical settings

The specific route and indication depend on the approved formulation and applicable regulatory labeling.

Adrenergic Blocking Characteristics

Labetalol has a distinctive pharmacological profile because it combines alpha-1 blockade with non-selective beta blockade. This allows reduction of blood pressure through both vasodilation and suppression of beta-adrenergic cardiovascular activity.

Manufacturing Process

Typical API manufacturing may involve:

  1. Preparation of substituted phenoxy intermediates
  2. Controlled chemical synthesis
  3. Formation of the labetalol base
  4. Purification
  5. Formation of the hydrochloride salt
  6. Crystallization
  7. Filtration
  8. Drying
  9. Milling where required
  10. Final analytical testing
  11. Controlled packaging

Quality and Analytical Testing

Labetalol Hydrochloride API quality evaluation may include:

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

Storage

Labetalol Hydrochloride 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

Labetalol Hydrochloride is relevant to research involving:

  • Beta-adrenergic receptors
  • Alpha-1 adrenergic receptors
  • Hypertension
  • Cardiovascular pharmacology
  • Adrenergic receptor antagonists
  • Blood-pressure regulation
  • Antihypertensive drug development

Labetalol Hydrochloride API Summary

Labetalol Hydrochloride is a combined alpha-1 and beta-adrenergic receptor blocker with CAS Number 32780-06-6, molecular formula C19H24N2O3·HCl, and molecular weight 364.87 g/mol. It is primarily used as an antihypertensive agent and is relevant to cardiovascular pharmaceutical development.

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 NMT 1.0%
Water Content NMT 2.0%
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