Asian Journal of Research in Chemistry

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Critical review: Significance of Force degradation study with respect to current Pharmaceutical Scenario


Affiliations
1 Parul Institute of Pharmacy, Waghodia, Limda, Gujarat, India
2 Institute of pharmacy, Nirma University, Ahmedabad, Gujarat
     

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Stress testing of the drug substance can help to identify the likely degradation products, which can in turn help to establish the degradation pathways and the intrinsic stability of the molecule. Quantitative estimation of degradation products and establishment of mass balance should be done by various hyphenated techniques. After quantitative estimation of degradation, isolation of the degradation products can be done with the help of different methods like TLC, flash chromatography (column chromatography) and preparative HPLC. After concurrent isolation, characterization of the degradation products should be done with the help of Ultraviolet spectroscopy, IR spectroscopy, NMR Spectroscopy, Mass Spectroscopy and HPLC. From the literature survey of antihypertensive drugs, it was found that major alkaline degradation products were found in angiotensin-II receptor antagonist (containing tetrazole moiety) for e.g. Losartan, Valsartan and Telmisartan etc. Dihydropyridine moiety containing calcium channel blocker drugs shows major photo degradation products for e.g. Amlodipine, Felodipine, Nilvadipine, Nimodipine etc. Due to amide group in anticancer taxanes (for e.g. Paclitaxel, Docetaxel), they shows major alkali degradation. Tetracycline antibiotics show major thermal degradation due to epimerization of tetracycline. Fluoroquinone antibiotics show photo degradation due to 8th position of Fluoroquinolone moiety containing halogen group. Deacetylation Causes acidic degradation of Cephalosporin antibiotics. Amide hydrolysis results in acidic degradation of -lactum antibiotics such as Dicloxacillin, Sultamicillin and Temocillin. Hydroxylation of cyclohexane group in Glipizide and Glimipride (antidiabetic drugs) causes both acidic and alkaline degradation. This paper discusses importance of force degradation study and degradation products with suitable examples of different categories of drugs.

Keywords

Degradation Products, Stability Study, Regulatory Guidelines, Characterization
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  • Critical review: Significance of Force degradation study with respect to current Pharmaceutical Scenario

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Authors

Nikita N. Patel
Parul Institute of Pharmacy, Waghodia, Limda, Gujarat, India
Charmy S. Kothari
Institute of pharmacy, Nirma University, Ahmedabad, Gujarat

Abstract


Stress testing of the drug substance can help to identify the likely degradation products, which can in turn help to establish the degradation pathways and the intrinsic stability of the molecule. Quantitative estimation of degradation products and establishment of mass balance should be done by various hyphenated techniques. After quantitative estimation of degradation, isolation of the degradation products can be done with the help of different methods like TLC, flash chromatography (column chromatography) and preparative HPLC. After concurrent isolation, characterization of the degradation products should be done with the help of Ultraviolet spectroscopy, IR spectroscopy, NMR Spectroscopy, Mass Spectroscopy and HPLC. From the literature survey of antihypertensive drugs, it was found that major alkaline degradation products were found in angiotensin-II receptor antagonist (containing tetrazole moiety) for e.g. Losartan, Valsartan and Telmisartan etc. Dihydropyridine moiety containing calcium channel blocker drugs shows major photo degradation products for e.g. Amlodipine, Felodipine, Nilvadipine, Nimodipine etc. Due to amide group in anticancer taxanes (for e.g. Paclitaxel, Docetaxel), they shows major alkali degradation. Tetracycline antibiotics show major thermal degradation due to epimerization of tetracycline. Fluoroquinone antibiotics show photo degradation due to 8th position of Fluoroquinolone moiety containing halogen group. Deacetylation Causes acidic degradation of Cephalosporin antibiotics. Amide hydrolysis results in acidic degradation of -lactum antibiotics such as Dicloxacillin, Sultamicillin and Temocillin. Hydroxylation of cyclohexane group in Glipizide and Glimipride (antidiabetic drugs) causes both acidic and alkaline degradation. This paper discusses importance of force degradation study and degradation products with suitable examples of different categories of drugs.

Keywords


Degradation Products, Stability Study, Regulatory Guidelines, Characterization

References