CALCIUM DOBESILATE-A VENOTONIC DRUG

Venotonics are a class of medicinal which are used to alleviate venous diseases and disorders and are used to treat chronic venous insufficiency and edema.

These vasoprotective agents are a broad group of drugs that acts over the smooth muscle fibers from the venous wall, through calcium-dependant mechanisms modulated by an alpha-adrenergic neurohormonal regulation.

CALCIUM DOBESILATE (2,5 dihydroxy-benzene-sulfonate) is one such venotonic or vasoprotective agent that shows well defined pharmacological properties. 

Calcium Dobesilate works by acting on endothelium and capillary basement membrane thereby blocking hyperpermeability inhibiting platelet aggregation and inhibiting blood hyperviscosity and hence improving lymphatic drainage.

Calcium Dobesilate which was discovered more than 40 years ago is also used for the treatment of diabetic retinopathy and it is the only angio-protective agent that reduces the progression of this disease. It also shows antioxidant properties.

Synthesis of Calcium Dobesilate Monohydrate involves sulfonation of hydroquinone. Hydroquinone is present as CALCIUM DOBESILATE MONOHYDRATE - IMPURITY A.

Reference standards of Calcium Dobesilate Monohydrate API and Calcium DobesilateMonohydrate - Impurity A are available at Pharmaffiliates Analytics and Synthetics P. Ltd.

Pharmaffiliates is one of the leading integrated CRO which deals with the Custom synthesis of Reference standards, Impurities, Metabolites, Deuterated compounds and Phyto standards. We also offer our expertise in Analytical research, Stability studies, Formulation & Development, Quality assurance and Regulatory services.

Pharmaffiliates has a huge database of reference standards for over 10,000 products and all the reference materials are provided in pack sizes of 25mg and 50mg with over 98% purity. Customized pack sizes are also available as per customer’s requirement.

All the impurities supplied by Pharmaffiliates are with complete structure elucidation and data interpretation with high-end analytical techniques like NMR, MASS and Chromatographic purity along with detailed Certificate of Analysis.

 

Simvastatin- A Statin drug

A class of drugs that helps in lowering the cholesterol levels in the blood are known as Statins. By lowering these levels they help in preventing heart attack, stroke and other related cardiovascular diseases.

One of the best-selling statin drugs is SIMVASTATIN, which is marketed under the trade name of Zocor and was developed by Merck. Simvastatin is a semi-synthetic derivative of fungus Aspergillus terreus and it is used for the treatment of dyslipidemia and to prevent atherosclerosis-related complications.

Simvastatin is a semi-synthetic drug and hence its synthesis involves several biocatalytic processes. This, in turn, results in numerous process related impurities of Simvastatin along with degradants and metabolites.

Pharmaffiliates Analytics and Synthetics have identified and synthesized these impurities, metabolites, derivatives and degradants of Simvastatin, which are classified below

1. Simvastatin-impurity A (Simvastatin acid sodium salt) – a sodium salt of Simvastatin metabolite i.e Simvastatin acid, the active form of the drug.
2. Simvastatin-impurity A (free base) - Simvastatin acid, an active form of Simvastatin.
3. Simvastatin-impurity B (4’-acetyl Simvastatin) - an acetate ester present as an impurity.
4. Simvastatin-impurity C (Anhydro Simvastatin) - an impurity formed in commercial preparation.
5. Simvastatin-impurity D - Simvastatin dimer present as an impurity.
6. Simvastatin-impurity E or Lovastatin - a fungal metabolite used in the synthesis of Simvastatin. Lovastatin also belongs to the family of HMG-CoA reductase inhibitors like Simvastatin and it is an antihypercholesterolemic agent.
7. Simvastatin-impurity F (epi Lovastatin) - an epimer of Lovastatin.
8. Simvastatin-impurity G (Simvastatin-3-en) - a 3-methylene Simvastatin impurity.
9. Simvastatin - impurity K (4α,5-dihydro Simvastatin) - an impurity formed in commercial preparation
10. Simvastatin methyl ester – A methyl ester present as an impurity
11. Simvastatin ethyl ester – An ethyl ester present as an impurity
12. Simvastatin glycerol ester – A glycerol ester present as an impurity
13. Simvastatin acid ammonium salt - An ammonium salt of Simvastatin metabolite i.e Simvastatin acid, the active form of the drug.
14. Anhydro Simvastatin acid sodium salt -An impurity formed in the synthesis.
15. (1S,3R,7S,8S,8AR)-8-(2-((2R,4R)-4-Hydroxy-6-oxotetrahydro-2h-pyran-2-yl)ethyl)-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl isobutyrate - An impurity of both Simvastatin and Lovastatin
16. (3S,5S)-Dihydroxy Simvastatin - An impurity formed in the synthesis.

Majority of the above mentioned impurities synthesized at Pharmaffiliates are 98% pure and are available in pack sizes as small as 50mg and 25mg. Customized pack sizes can also be made available as per the customer’s need.

Each of these standards synthesized at Pharmaffiliates are been identified through an elaborate structure elucidation data and certificate of analysis is provided for the same.

Gefitinib - An EGFR inhibitor

In early 90’s, lung cancer had become a common cause of death worldwide, as at the time of diagnosis the patients are in the advanced stages of the disease. Apart from several chemotherapy techniques, new and effective treatment options were urgently needed.

Gefitinib, an anti-cancer drug which was approved by US-FDA in the year 2003 for the treatment of advanced non-small-cell lung cancer.

Gefitinib is a synthetic anilinoquinazoline, which is orally available and acts as an inhibitor of tyrosine kinase activity of the epidermal growth factor receptor (EGFR).

Gefitinib which is sold under the trade name of ‘Iressa’ is a trademark of Astra Zeneca group of companies. It shows single-agent activity and mild toxicity profile in patients suffering from non-small-cell lung cancer for whom no other treatment exists.

Hence this drug has been observed as new and indispensable choice for the treatment of patients with advanced non-small-cell lung cancer (NSCLC). 

Various pharmaceutical companies have been manufacturing Gefitinib, keeping in view the necessity and advantage of this potent anti-cancer drug.

Pharmaffiliates Analytics and Synthetics P. Ltd, a world leading CRO located in North India, has been synthesizing the In house Reference standards of Gefitinib and the impurities related with Gefitinib.

Pharmaffiliates offers best quality (over 98%) reference standards which are synthesized In-house in a state-of-art facility by a professionally qualified and skilled team of scientists. Detailed Certificate of Analysis which is duly verified by the QA department is also provided with the Reference standard.

The Reference standards of the following impurities of Gefitinib are available in Pharmaffiliates:

Gefitinib Impurity A (7-METHOXY-6-(3-MORPHOLINOPROPOXY)QUINAZOLIN-4(3H)-ONE)- an intermediate in the synthesis of Gefitinib.

Gefitinib Impurity B (3-DESCHLORO-4-DESFLUORO-4-CHLORO-3-FLUORO GEFITINIB)- an impurity of Gefitinib.

3-Chloro-4-Fluorophenylamine – an important synthon used in the synthesis of Gefitinib.

Gefitinib 4-Desfluoro Hydrochloride Impurity - an impurity of Gefitinib.

Gefitinib N-Oxide - a degradation impurity of Gefitinib.

O-Des Morpholino propyl Gefitinib – a metabolite of Gefitinib.

Pack sizes of all the above mentioned In-house Reference standards are provided in 25mg and 50mg vials. Customized pack sizes as per the customer’s need are also obtainable at Pharmaffiliates.