Saturday, 28 April 2018

Canrenone- A bioactive metabolite of Spironolactone


Spironolactone, also known as a “water pill” is a drug used to remove excess fluid from the body build-up during congestive heart failure, cirrhosis of the liver, and kidney disease. Spironolactone is a prodrug with a short half-life and it is rapidly metabolized to its active form 7α-thiomethylspironolactone (7α-TMS). 7α-TMS is further converted to bioactive form Canrenone which is the major circulating metabolite.
Canrenone, which is a steroidal aldosterone antagonist is reportedly more potent as an antimineralocorticoid relative to its parent drug spironolactone. As an active metabolite Canrenone accounts for approximately 10 to 25% of the potassium-sparing effect (a diuretic which does not promote secretion of potassium in urine) of spironolactone and the other 80% is done by the other metabolite 7α-TMS.
Chemically, Canrenone is 10,13-Dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthrene-17,5'-oxolane]-2',3-dione, most commonly used diuretic and an important intermediate for the synthesis aldosterone receptor antagonist Spironolactone
Pharmaffiliates Analytics and Synthetics Pvt. Ltd. proudly introduce the reference standard of Canrenone, details of which are mentioned below:
 
                                                           
Product name- Canrenone/Spironolactone impurity F    Product name- Canrenone D6 (major)
Product Code - PA 19 18060                                           Product Code - PA D 17260
CAS No.- 976-71-6                                                         CAS No.- NA
Pack size – 25mg, 50mg                                                  Pack size – 1mg, 10mg


The above-mentioned reference standards are supplied with a Certificate of Analysis, MSDS, and all the required documentation to ensure statutory domestic and international requirements. Our standards are of high purity and are scientifically characterized.
For more details visit our website www.pharmaffiliates.com
The laboratory and quality systems of Pharmaffiliates have successfully passed major second and third party audits which include NABL accreditation, ISO Guide 34 and USFDA.


Pharmaffiliates Analytics and Synthetics P. Ltd. is an integrated Contract Research Organization (CRO) is a gigantic name in the global market, which offers services to Pharmaceutical industry, API manufacturers, Bulk drug suppliers, clinical CROs and other allied industries.



Wednesday, 11 April 2018

Sildenafil and Impurities by Pharmaffiliates


Pharmaffiliates Analytics and Synthetics Pvt. Ltd, a substantial and predominant name as manufacturer and supplier of impurity standards globally, proudly introduces a wide range of premium quality products at highly competitive prices.
Sildenafil is an eminent first-line therapy for erectile dysfunction and works by selectively inhibiting phosphodiesterase type 5, which allows corpus cavernosum smooth muscle to relax, potentiating erections during sexual stimulation. 
Pharmaffiliates offers a vast variety of Sildenafil impurity standards which includes both commercially available and unavailable standards. All the standards are provided in the pack size of 25mg of 50mg and these packs can be customized as per customer's requirement also.
Each standard is shipped with a Certificate of Analysis, MSDS, and all the required documentation to ensure statutory domestic and international reputations. Our standards are of high purity and are scientifically characterized.
Our laboratory and quality systems have successfully passed major second and third party audits which include NABL accreditation, ISO Guide 34 and USFDA.
Pharmaffiliates offers below listed impurity standards of Sildenafil:
Name of the impurity
Product Code
CAS No.
Application
PA 19 09010
1391053-95-4
An impurity (Isobutyl Sildenafil

Sildenafil - impurity B

PA 19 09020
1094598-75-0
A prodrug (Sildenafil N-oxide)

Sildenafil - impurity C


PA 19 09030
139755-91-2
A metabolite (Desethyl Sildenafil)
PA 19 09040
1357931-55-5
An impurity (Demethylpiperazinyl Sildenafil Sulfonic Acid)
PA 19 09050
288-32-4
By-product (Imidazole)
PA 19 09070
1346602-67-2
Dimer impurity

Sildenafil aldehyde

PA 19 09510
332374-42-2
Intermediate in synthesis

Sildenafil amino amide impurity 

PA 19 09520 (Freebase)/ PA 19 09530 (Hydrochloride salt)
139756-02-8/ 247584-10-7
Intermediate in synthesis

Sildenafil chloro impurity 

PA 19 09540
Important reactant for Sildenafil synthesis

Sildenafil carboxamide impurity 

PA 19 09550
An impurity

Sildenafil lactam impurity

PA 19 09560
An impurity

Sildenafil chlorosulfonyl impurity 

PA 19 09570
An impurity

N-Desmethyl Sildenafil

PA 19 09580
An active metabolite

4-Ethoxy-N,N-bis(2-hydroxyethyl)-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1h-pyrazolo[4,3-d]pyrimidin-5-yl)benzenesulfonamide

PA 19 09590
NA
An impurity

O-Desethyl-o-propyl methisosildenafil

PA 19 09600
An analog

Propoxyphenyl homohydroxy Sildenafil 

PA 19 09610
An analog of Homo Sildenafil

Propoxyphenyl Sildenafil

PA 19 09620
An impurity

Descarbon Sildenafil 

PA 19 09630
An analog

5-(5-Carboxy-2-ethoxyphenyl)-1-methyl-3-N-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 

PA 19 09640
A metabolite of Gendenafil, an analog of Sildenafil

4-Amino-1-methyl-5-propyl-1h-pyrazole-3-carboxamide

PA 19 09650
An intermediate

Sildenafil amide impurity

PA 19 09660
139756-01-7
An impurity

Sildenafil methyl sulfonate ester impurity 

PA 19 09670
NA
An impurity

1-Methyl-4-nitro-3-propyl-1h-pyrazole-5-carboxylic acid

PA 19 09680
An intermediate

Demethylpiperazinyl Iso Sildenafil sulfonyl chloride

PA 19 09690
501120-42-9
An intermediate of Sildenafil and Iso Sildenafil

(Z)-N'-(5-Chloro-4-methyl-2-propyl-1H-imidazol-1-yl)-2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)benzimidamide

PA 19 09700
NA
An impurity

(Z)-N'-(5-Chloro-4-methyl-2-propyl-1H-imidazol-1-yl)-2-ethoxybenzimidamide 

PA 19 09710
NA
An impurity


You can order the above-mentioned impurity standards here:
Or visit our website. www.pharmaffiliates.com




Diltiazem - A non-dihydropyridine calcium channel blocker


Hypertension or high blood pressure is a signification cause of Cardiovascular diseases like Coronary artery diseases, atrial fibrillation or hypertensive heart disease which are the leading causes of deaths worldwide. Calcium channel blockers are the first line treatment for hypertension.

Diltiazem, a non-dihydropyridine calcium channel blocker, is an effective and safe antihypertensive drug, which can be used alone or in combination with other agents. Diltiazem works by inhibiting calcium channels in the vessels resulting in the vasodilation and, consequently,  lowering of the blood pressure.

The reference standard of Diltiazem Hydrochloride (Product Code- PA 04 26000, CAS No. - 33286-22-5) and the impurities associated with it are available at Pharmaffiliates.
Diltiazem impurity D or N-DESMETHYL DILTIAZEM HYDROCHLORIDE (Product Code- PA 04 26040, CAS No. - 130606-60-9) which is the major metabolite of Diltiazem is also available at Pharmaffiliates

For other impurities of Diltiazem and further details, follow the link below


Pharmaffiliates Analytics and Synthetics P. Ltd. is already an established name, as a leading manufacturer and suppliers of Reference materials worldwide.

All the standards are shipped with a Certificate of Analysis, MSDS, and all the required documentation to ensure statutory domestic and international reputations. Our standards are of high purity and scientifically characterized. Our laboratory and quality systems have successfully passed major second and third party audits which include NABL accreditation, ISO Guide 34 and USFDA.

Started in the year 2005, Pharmaffiliates is one of the leading integrated Contract Research Organization located in North India which offers its expertise in Custom synthesis (Reference standards, Impurities, Metabolites, Deuterated compounds, Phyto standards, agrochemicals, pesticides, food standards etc.), Analytical research (PH Buffer Solutions, Method development, Validation), Stability studies, Formulation & Development (New Drug Delivery System), Quality assurance and Regulatory Services.




Cetirizine-Second generation antihistamine drug


Histamine H1 receptor antagonists or antihistamines are the class of drugs used in the treatment of allergic disorders. They are classified as first generation sedating and second-generation non-sedating antihistamine. The non-sedation antihistamines do not easily cross the blood-brain barrier causing lesser or no drowsiness and thereby improving the lives of the patients.

Cetirizine, which was approved as a second-generation non-sedating antihistamine by FDA in September 1996 is one of the most commonly prescribed drugs for all ages by the medical practitioners.

Cetirizine, available as dihydrochloride salt works by blocking one type of receptor for histamine (the H1 receptor) and thus preventing the activation of H1 receptor-containing cells by histamine (a chemical that is responsible for many of the signs and symptoms of allergic reactions). 
Chemically, Cetirizine Dihydrochloride is [2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic Acid Dihydrochloride and it is a bioactive carboxylated metabolite of hydroxyzine.Cetirizine is a racemic compound and its organic synthesis involves several stereochemical steps which result in a number of impurities along with the desired products.
Identification, isolation, and characterization of these impurities is an indispensable process for Pharmaceutical companies, as these impurities may change the effectiveness and efficacy of the drug product.

Pharmaffiliates Analytics and Synthetics P. Ltd. have successfully performed impurity profiling of Cetirizine impurities and reference standards of these impurities are readily available in pack sizes of 25 and 50mg vials at Pharmaffiliates.

Detailed of Cetirizine impurities are listed below

Name of the impurity
Product code
CAS No.
Description
Cetirizine Dihydrochloride
PA 03 36000
83881-52-1
Second generation antihistamine
PA 03 36010
303-26-4
Starting material used in the synthesis
PA 03 36020
113740-61-7
A Decarbomethoxy impurity formed during synthesis
PA 03 36030/ PA 03 36031 (Freebase form)
83881-59-8/NA
2-chloro impurity formed during synthesis
PA 03 36040
346451-15-8
Dimer impurity of Cetirizine
PA 03 36050/ PA 03 36051 (Freebase form)
83881-56-5/NA
Impurity formed during synthesis
PA 03 36060/ PA 03 36061 (Freebase form)
83881-54-3/ 83881-53-2
Deschloro impurity
PA 03 36070/ PA 03 36071 (Freebase form)
164726-80-1/ 109806-71-5
Important intermediate formed during synthesis
PA 03 36590
NA
A lactose adduct of Cetirizine

For more details and other impurities click on the link below


All the above-mentioned impurity standards are available along with a Certificate of Analysis along with the detailed chromatograms and spectroscopic data.

Pharmaffiliates is well-known name as an integrated CRO globally which specializes in the field of Custom synthesis of products which includes Reference standards, impurities, Iso-labeled compounds, Phyto standards, pesticides, agrochemicals, food, cosmetics and many more.