Description

Technical Parameters

Linagliptin is a selective dipeptidyl peptidase-4 inhibitor indicated for type 2 diabetes mellitus management. The active pharmaceutical ingredient is synthesized through optimized multi-step pathways ensuring high stereochemical integrity and stringent impurity control. This compound sustains incretin hormone activity to regulate glycemic levels effectively. The manufacturing process maintains precise control over critical parameters to yield a stable raw material suited for immediate-release tablets and combination formulations.

Technical Specifications

Parameter	Specification
International Nonproprietary Name	Linagliptin
CAS Registry Number	668270-12-0
Chemical Name	8-[(3R)-3-aminopiperidin-1-yl]-3-methyl-7-(2-butyn-1-yl)-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Molecular Formula	C25H28N8O2
Molecular Weight	472.54 g/mol
Physical Appearance	White to off-white crystalline powder
Solubility Profile	Practically insoluble in water; sparingly soluble in methanol; slightly soluble in ethanol
Storage Conditions	Store in tight, light-resistant containers at controlled room temperature (15°C to 30°C)
Retest Period	24 months from manufacturing date

Quality and Analytical Standards

Test Parameter	Acceptance Criteria	Analytical Method
Identification	Retention time and infrared spectrum conform to reference standard	FTIR and HPLC-DAD
Assay	98.5 percent to 101.5 percent (anhydrous, solvent-free basis)	High-Performance Liquid Chromatography
Chiral Purity	Greater than or equal to 99.5 percent enantiomeric excess of R-isomer	Chiral HPLC
Individual Specified Impurity	Maximum 0.10 percent	Gradient HPLC
Total Impurities	Maximum 0.50 percent	Gradient HPLC
Water Content	Maximum 0.5 percent	Volumetric Karl Fischer
Residue on Ignition	Maximum 0.1 percent	Gravimetric analysis
Heavy Metals	Maximum 20 parts per million	Inductively Coupled Plasma Mass Spectrometry
Residual Solvents	Complies with ICH Q3C limits	Headspace Gas Chromatography

Manufacturing Standards

01/

Synthetic Route: Multi-step convergent synthesis utilizing specialized heterocyclic building blocks designed for high purity and consistent yield.

02/

Reaction Facilities: Advanced glass-lined multi-purpose reactors and hydrogenation autoclaves operating under automated temperature and pressure controls.

03/

Purification Protocols: Recrystallization and activated carbon treatment cycles engineered to isolate pure active ingredients and eliminate trace impurities.

04/

Cleanroom Environment: Micronization and final packaging executed within ISO Class 8 cleanroom facilities to prevent particulate cross-contamination.

05/

Scalability: Production capacity ranges from laboratory sample quantities to multi-kilogram commercial manufacturing batches.

Documentation and Regulatory Support

Regulatory Dossier

Comprehensive Drug Master File package prepared in Common Technical Document format for international regulatory submissions.

Analytical Documentation

Certified Certificate of Analysis provided with every commercial lot detailing complete raw data profiles.

Process Validation

Full validation documentation covering process optimization, cleaning validation, and analytical method validation.

Compliance Declarations

Certified statements confirming non-use of specified animal-origin materials and adherence to residual solvent guidelines.

Packaging and Storage

Primary Packaging: Double low-density polyethylene bags heat-sealed under a nitrogen purge to eliminate oxidative degradation and moisture absorption.

Secondary Packaging: Rigid fiber drums equipped with tamper-evident seals.

Moisture Control: Food-grade silica gel packets placed between packaging layers to maintain internal relative humidity below threshold limits.

Labeling Standards: Lot number, manufacturing date, retest date, net weight, storage instructions, and hazard symbols displayed on weather-resistant barcode labels.

Pharmaceutical Applications

Immediate-Release Tablets: Serves as the active raw material for standard oral solid dosage forms targeting glycemic control.

Fixed-Dose Combinations: Integrated into multi-active pharmaceutical ingredient solid dose formulations paired with metformin or sodium-glucose co-transporter-2 inhibitors.

Generic Formulations: Provides consistent physicochemical profiles and impurity tracking required for bioequivalence studies and clinical trial batches.

Extended-Release Matrices: Acts as a stable core compound for polymer-coated extended-release tablet development.

FAQ

Q: What is the regulatory status of this active pharmaceutical ingredient?

A: Complete analytical validation packages and Common Technical Document format documentation are fully prepared for immediate evaluation.

Q: What are the standard packaging sizes available for orders?

A: Evaluation samples are supplied in amber glass bottles or double polyethylene pouches, while commercial quantities are packed in fiber drums.

Q: Are impurity reference standards provided alongside shipments?

A: Process-related impurities and degradation standards can be supplied upon request to support internal method verification and quality control testing.

Q: What is the standard lead time for order fulfillment?

A: Standard delivery ranges from two to four weeks for existing stock batches and six to eight weeks for scheduled campaign production runs.

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