CHEMICAL HYDROLYSIS, INSILICOPHYSICOCHEMICAL PROPERTIESANDIN-VIVOPHARMACOLOGICAL EVALUATION OF ANTIDIABTIC AND ANTIHYPERTENSIVE CODRUGS
Journal Title: Asian Journal Of Pharmaceutical Research and Development - Year 2018, Vol 6, Issue 6
Abstract
n the present research work codrugs of Propranolol and Metoprolol with Metformin were synthesized with an aim of improving the biological activity and to check the effectiveness of release of the parent drugs in presence of spacer.Ester prodrugs of Propranolol and metoprolol were synthesized by using succinic, maleic, pthalic anhydride and substituted derivatives of them. The resulted prodrugs were converted into codrugs (CO1-6)by reacting with Metformin. The compounds were characterized by melting point, FT-IR, 1H-NMR and mass spectroscopy. The chemical hydrolysis of CO1-6 was carried out at the pH 1.2, 6.8 and 7.4. Almost all compounds showed encouraging chemical stability at pH 1.2 and 6.8 whereas showed the moderate hydrolysis at pH 7.4 but codrug CO4didn’t showed hydrolysis at any pH condition. Further codrugs were screened for antihypertensive and antidiabetic activity by simultaneous induction of two-kidney, one clip renal hypertension and STZ-induced diabetic model in wistarrats. The spacer containing dipropyl maleate codrugs (CO3 and CO6)showed longer duration of action. The current paper also describes about the molecular properties evaluation of the synthesized codrugs.
Authors and Affiliations
Ganesh S. Andhale, Giles D, Suresh Janadr, Basavraj Metikurki
Keywords
Related Articles
- EP ID EP516278
- DOI 10.22270/ajprd.v6i6.452
- Views 117
- Downloads 0
PATTERN OF ADVERSE DRUG REACTIONS AND ITS MANAGEMENT IN FEMALE CANCER PATIENTS IN A PRIVATE HOSPITAL IN TELANGANA, INDIA
Chemotherapy and radiation are one of the important components of treatment for many cancers. Anti-neoplastic agents are used with caution due to their high toxicity and narrow therapeutic window. Studies describing patt...
BIOLOGICAL EVALUATION OF SAUSSUREA LAPPAROOT EXTRACT FOR ANALGESIC AND ANTI-INFLAMMATORYACTIVITY
The present study was designed to evaluate the Phytochemical Screening for Analgesic and Anti-inflammatoryactivities of Ethonolic extract of Saussurea lappa. The collected plant root material were w...
CHEMICAL HYDROLYSIS, INSILICOPHYSICOCHEMICAL PROPERTIESANDIN-VIVOPHARMACOLOGICAL EVALUATION OF ANTIDIABTIC AND ANTIHYPERTENSIVE CODRUGS
n the present research work codrugs of Propranolol and Metoprolol with Metformin were synthesized with an aim of improving the biological activity and to check the effectiveness of release of the parent dru...
ANALYTICAL METHOD DEVELOPMENT, VALIDATION AND FORCED DEGRADATION STUDIES OF LANSOPRAZOLEBY RP-HPLC
The objective of this work is to develop a rapid, precise, accurate and sensitive revere phase liquid chromatographic method and Forced degradation studies for the estimation of Lansoprazole. Th...
NOVEL TOPICAL LIPOSOMAL GEL OF BENZOYL PEROXIDE AND RESVERATROL FOR TREATMENT OF ACNE
Liposomal formulations have been used in the treatmentof a number of dermatological diseases . Benzoyl peroxide is the drug of choiceused for the treatment of acne but suffers from side effects such as skin redness,...