Isfahan University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Enhancement of Anti-Diabetic Effects of Gliclazide Using Immediate Release Tablets in Streptozotocin-Induced Diabetic and Normal Rats



Varshosaz J1 ; Tavakoli N1 ; Enteshary S1
Authors
Show Affiliations
Authors Affiliations
  1. 1. Department of Pharmaceutics, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Farmacia Published:2013

Abstract

Gliclazide is widely used in the treatment of non-insulin dependent diabetes mellitus. Its major drawback is the hydrophobic nature, low dissolution rate and interindividual variation in bioavailability. The objective of the present study was to enhance dissolution rate and antidiabetic effect of gliclazide using immediate release tablets. Tablets containing wetting agents like: propylene glycol (PG), ethanol (Et) and Solutol H15 (S) in ratios of 1:1, 2:1, 4:1 to drug and mixed with ProSolv (A) as filler in concentrations of 10, 15, 20% were prepared. Sodium starch glycolate as disintegrating agent was added 5% w/w. The dissolution of gliclazide in tablets was investigated in HCl 0.1 N. The blood glucose lowering effect of tablets was studied in normal and streptozotocin-diabetic rats. The developed tablets caused significantly higher drug release rate than conventional tablets due to increased wetting properties and increased surface of drug available for dissolution. Increasing the ratio of ProSolv from 10 to 20% caused to increase drug dissolution rate. The area under the normalized blood glucose level vs. time curve up to 25 hr after administration of the optimized formulation (PG)4A20 showed significant decrease in blood glucose level in both normal and diabetic rats compared to conventional tablets. The developed tablets enhance water solubility of gliclazide and its efficacy.
Related Docs
View other Related Docs
1. Applying the Taguchi Design for Optimized Formulation of Sustained Release Gliclazide Chitosan Beads: An in Vitro/In Vivo Study, AAPS PharmSciTech (2009)
2. Gliclazide Microcrystals Prepared by Two Methods of in Situ Micronization: Pharmacokinetic Studies in Diabetic and Normal Rats, AAPS PharmSciTech (2010)
3. Dissolution Enhancement of Gliclazide Using in Situ Micronization by Solvent Change Method, Powder Technology (2008)
4. Dissolution Enhancement of Gliclazide Using Ph Change Approach in Presence of Twelve Stabilizers With Various Physico-Chemical Properties, Journal of Pharmacy and Pharmaceutical Sciences (2009)
5. Nanocrystalization of Pioglitazone by Precipitation Method, Drug Research (2018)
6. Enhancement of Solubility and Antidiabetic Effects of Repaglinide Using Spray Drying Technique in Stz-Induced Diabetic Rats, Pharmaceutical Development and Technology (2017)
7. Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques, Dissolution Technologies (2013)
8. Preparation and Characterization of Metoprolol Controlled-Release Solid Dispersions, Drug Delivery (2006)
Experts (# of related papers)
View all Related Experts
Jaleh Varshosaz (21)
Mohsen Minaiyan (11)
Other Related Docs
9. Development and Validation of a Novel Rp-Hplc Method for Pharmacokinetic Studies of Gliclazide in Rat, Farmacia (2011)
10. Preparation and Evaluation of a Controlled Drug Release of Repaglinide Through Matrix Pellets: In Vitro and in Vivo Studies, Journal of Microencapsulation (2014)
11. Crystal Engineering for Enhanced Solubility and Bioavailability of Poorly Soluble Drugs, Current Pharmaceutical Design (2018)
12. Effect of Hordeum Vulgare L. (Barley) on Blood Glucose Levels of Normal and Stz-Induced Diabetic Rats, Research in Pharmaceutical Sciences (2014)
13. Protective and Therapeutic Effects of Phoenix Dactylifera Leaf Extract on Pancreatic Β-Cells and Diabetic Parameters in Streptozotocin-Induced Diabetic Rats, Comparative Clinical Pathology (2020)
14. Anti-Diabetic Effects of Walnut Oil on Alloxan-Induced Diabetic Rats, African Journal of Pharmacy and Pharmacology (2011)
15. Design, Formulation, and Physicochemical Evaluation of Montelukast Orally Disintegrating Tablet, International Journal of Preventive Medicine (2016)
16. The Effects of Berberis Integerrima Fruit Extract on Glycemic Control Parameters in Patients With Type 2 Diabetes Mellitus: A Randomized Controlled Clinical Trial, Evidence-based Complementary and Alternative Medicine (2021)
17. The Nephroprotective Effect of Eryngium Caucasicum Extract Alone and in Combination With Metformin in Adult Male Diabetic Rats, Journal of Nephropharmacology (2023)
18. Effect of Fenugreek Seeds on Blood Glucose and Lipid Profiles in Type 2 Diabetic Patients, International Journal for Vitamin and Nutrition Research (2009)
19. Preparation and Characterization of a Hydroxypropyl Methylcellulose Based Wafer for Simultaneous Delivery of Phenytoin and Insulin As Wound Dressing Material, Pharmaceutical Development and Technology (2022)
20. Physicochemical, Pharmacodynamic and Pharmacokinetic Characterization of Soluplus Stabilized Nanosuspension of Tacrolimus, Current Drug Delivery (2017)
21. The Protective Effects of Ziziphus Vulgaris L. Fruits on Biochemical and Histological Abnormalities Induced by Diabetes in Rats, Journal of Complementary and Integrative Medicine (2014)
22. Effect of Oral Administration of Magnesium on Cisplatin-Induced Nephrotoxicity in Normal and Streptozocin-Induced Diabetic Rats, Nephro-Urology Monthly (2013)
23. The Inhibitory Effects of Pure Flavonoids on in Vitro Protein Glycosylation, Journal of Herbal Pharmacotherapy (2002)
24. Antidiabetic Effect of Hydroalcoholic Extract of Carthamus Tinctorius L. in Alloxan-Induced Diabetic Rats, Journal of Research in Medical Sciences (2012)
25. The Effect of Rosa Damascena Extract on Blood Glucose and Insulin Levels in Diabetic Rats, Journal of Isfahan Medical School (2020)
26. Enhancement of Dissolution Rate of Fenofibrate by Spray Drying Technique: Comparison of Eudragit E-100, Solutol® Hs15 and Hydroxypropyl Cellulose As Carriers, Farmacia (2015)
27. Nasal Delivery of Insulin Using Bioadhesive Chitosan Gels, Drug Delivery: Journal of Delivery and Targeting of Therapeutic Agents (2006)
28. Preparation and Characterisation of a New Form of Silymarin As a Potential Antidiabetic Agent in the Adult Male Rat, Archives of Physiology and Biochemistry (2023)
29. Development and Validation of a New Robust Rp-Hplc Method for Simultaneous Quantitation of Insulin and Pramlintide in Non-Invasive and Smart Glucose-Responsive Microparticles, Research in Pharmaceutical Sciences (2022)
30. Salsalate Efficacy in Blood Glucose Level Reduction in Diabetes, Journal of Isfahan Medical School (2009)
31. Exploring the Inhibitory Properties of Biflavonoids on Α-Glucosidase; Computational and Experimental Approaches, International Journal of Biological Macromolecules (2023)
32. Comparative Study of Anti-Diabetic Effects of Insulin, Epigenin and Salvia Mirzayanii Extract in Streptozotocin-Induced Diabetic Male Rats, Indian Journal of Biochemistry and Biophysics (2023)
33. Use of Natural Gums and Cellulose Derivatives in Production of Sustained Release Metoprolol Tablets, Drug Delivery: Journal of Delivery and Targeting of Therapeutic Agents (2006)
34. The Effect of Formulation Variables on the Characteristics of Insulin-Loaded Poly(Lactic-Co-Glycolic Acid) Microspheres Prepared by a Single Phase Oil in Oil Solvent Evaporation Method, Colloids and Surfaces B: Biointerfaces (2009)
35. The Effects of Aqueous Extract of Alfalfa on Blood Glucose and Lipids in Alloxan-Induced Diabetic Rats, Interventional Medicine and Applied Science (2015)
36. The Effect of Hydroalcoholic Saffron (Crocus Sativus L.) Extract on Fasting Plasma Glucose, Hba1c, Lipid Profile, Liver, and Renal Function Tests in Patients With Type 2 Diabetes Mellitus: A Randomized Double-Blind Clinical Trial, Phytotherapy Research (2019)
37. Influence of Different Solid-Dispersion Techniques Upon the Release of Dimenhydrinate From Chewing-Gum Formulations, Scientia Pharmaceutica (2002)
38. Development and Characterization of Floating Microballoons for Oral Delivery of Cinnarizine by a Factorial Design, Journal of Microencapsulation (2007)
39. Pharmacokinetics and Pharmacodynamics of Controlled Release Insulin Loaded Plga Microcapsules Using Dry Powder Inhaler in Diabetic Rats, Biopharmaceutics and Drug Disposition (2010)
40. Effect of Some High Consumption Spices on Hemoglobin Glycation, Indian Journal of Pharmaceutical Sciences (2014)
41. Salsalate Improves Glycemic Control in Patients With Newly Diagnosed Type 2 Diabetes, Acta Diabetologica (2013)
42. Use of Hydrophilic Natural Gums in Formulation of Sustained-Release Matrix Tablets of Tramadol Hydrochloride, AAPS PharmSciTech (2006)
43. Effects of Methanolic and Butanolic Fractions of Allium Elburzense Wendelbo Bulbs on Blood Glucose Level of Normal and Stz-Induced Diabetic Rats, Research in Pharmaceutical Sciences (2012)
44. A Randomized Controlled Study for Evaluation of Psyllium Effects on Kinetics of Carbohydrate Absorption, Journal of Research in Medical Sciences (2007)
45. Development and Characterization of Buccoadhesive Nifedipine Tablets, European Journal of Pharmaceutics and Biopharmaceutics (2002)
46. Antihyperlipidemic Effect of Peucedanum Pastinacifolium Extract in Streptozotocin-Induced Diabetic Rats, Clinics (2010)
47. Preparation and in Vitro Evaluation of Sustained-Release Matrix Tablets of Flutamide Using Synthetic and Naturally Occurring Polymers, Iranian Journal of Pharmaceutical Research (2008)
48. Effect of Hydroethanolic Extract of Nigella Sativa L. on Skin Wound Healing Process in Diabetic Male Rats, International Journal of Preventive Medicine (2019)
49. Crystal Engineering of Ibuprofen Using Starch Derivatives in Crystallization Medium to Produce Promising Ibuprofen With Improved Pharmaceutical Performance, RSC Advances (2015)
50. Effects of Hydroalcoholic Extract of Watercress (Nasturtium Officinale) Leaves on Serum Glucose and Lipid Levels in Diabetic Rats, Indian Journal of Physiology and Pharmacology (2015)