Neostigmine Methylsulphate API Manufacturer in India

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Neostigmine Methylsulphate API

Neostigmine Methylsulphate is a synthetic reversible acetylcholinesterase inhibitor and cholinergic pharmaceutical active pharmaceutical ingredient (API). It increases the availability of acetylcholine by reducing its enzymatic breakdown, thereby enhancing cholinergic transmission.

Neostigmine Methylsulphate is an important pharmaceutical form of neostigmine used in formulations associated with neuromuscular transmission and reversal of non-depolarizing neuromuscular blockade. It is also relevant to pharmaceutical research involving cholinergic and neuromuscular pharmacology.

Neostigmine Methylsulphate API Manufacturer in India

Neostigmine Methylsulphate is a well-characterized anticholinesterase pharmaceutical API used in pharmaceutical formulation development, manufacturing, analytical testing and research.

The compound is the methyl sulfate salt of neostigmine and is chemically distinct from Neostigmine Bromide. Neostigmine Methylsulphate has the molecular formula C₁₃H₂₂N₂O₆S and molecular weight 334.39 g/mol.

Chemical Information

CAS Number: 51-60-5

Molecular Formula: C₁₃H₂₂N₂O₆S

Molecular Weight: 334.39 g/mol

Chemical Name: 3-[(Dimethylcarbamoyl)oxy]-N,N,N-trimethylbenzenaminium methyl sulfate

Drug Class: Cholinesterase Inhibitor

Therapeutic Class: Anticholinesterase / Cholinergic Agent

Therapeutic Area: Neurology / Anesthesiology

Molecule Type: Synthetic Small Molecule

Salt Form: Methylsulphate

Synonyms: Neostigmine Methylsulphate, Neostigmine Methylsulfate, Neostigmine Methosulfate

Mechanism of Action

Neostigmine Methylsulphate acts as a reversible acetylcholinesterase inhibitor.

Its mechanism includes:

  • Reversible inhibition of acetylcholinesterase
  • Reduced enzymatic breakdown of acetylcholine
  • Increased acetylcholine availability
  • Enhanced cholinergic neurotransmission
  • Improved neuromuscular transmission
  • Increased skeletal-muscle response
  • Increased parasympathetic activity

Pharmaceutical Applications

Neostigmine Methylsulphate API is relevant to:

  • Neuromuscular blockade reversal formulations
  • Anesthesia-related pharmaceutical preparations
  • Cholinergic pharmaceutical formulations
  • Myasthenia gravis-related applications
  • Neuromuscular pharmacology research
  • Acetylcholinesterase inhibitor research
  • Pharmaceutical formulation development
  • Pharmaceutical API manufacturing
  • Analytical quality control
  • Cholinergic drug development

Neuromuscular Applications

Neostigmine Methylsulphate increases acetylcholine concentrations at the neuromuscular junction through inhibition of acetylcholinesterase.

This enhances neuromuscular transmission and makes the API particularly relevant to pharmaceutical preparations used for reversal of non-depolarizing neuromuscular blocking agents.

Cholinesterase Inhibition

Neostigmine Methylsulphate belongs to the reversible cholinesterase inhibitor class. By slowing the breakdown of acetylcholine, it enhances acetylcholine-mediated activity at cholinergic sites.

Physical Characteristics

Neostigmine Methylsulphate is generally described as a white crystalline powder and is hygroscopic.

It is very soluble in water and freely soluble in ethanol.

Manufacturing Process

A controlled Neostigmine Methylsulphate API manufacturing process may involve:

  1. Qualification of starting materials
  2. Preparation of substituted aromatic intermediates
  3. Formation of the dimethylcarbamate functionality
  4. Controlled quaternization of the tertiary amine
  5. Formation of the methylsulphate salt
  6. Reaction monitoring
  7. Purification
  8. Crystallization
  9. Filtration and washing
  10. Controlled drying
  11. Milling, where required
  12. Final analytical testing
  13. GMP-compliant packaging

Quality Control Testing

Typical Neostigmine Methylsulphate API testing may include:

  • Identification by IR
  • Chromatographic identification
  • Assay
  • Related substances
  • Specified impurities
  • Loss on drying
  • Residue on ignition
  • pH
  • Chloride
  • Sulfate-related testing
  • Melting range
  • Residual solvents
  • Elemental impurities
  • Stability testing

Storage

Store Neostigmine Methylsulphate API in a tightly closed container protected from light and moisture.

Because the material is hygroscopic, appropriate moisture protection should be maintained during storage and handling.

Detailed Specifications

Parameter Specification
Appearance White crystalline powder or crystals
Identification IR & HPLC compliant
Assay (HPLC) 98.0% – 102.0%
Loss on Drying NMT 1.0%
Residue on Ignition NMT 0.1%
Heavy Metals NMT 10 ppm
pH (1% Solution) 3.0 – 5.0
Water Content NMT 1.0%
Melting Point 145 – 149°C
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