Solid dispersion a novel technique for solubility enhancement of poorly water soluble drug gliclazide

Shep, Santosh G.; Vinayak, Mundhe; Shep, Sachin G.; Chandewar, A. V.
March 2012
Journal of Pharmacy Research;2012, Vol. 5 Issue 3, p1706
Academic Journal
The aim of this study is to develop a novel sustained-release system for poorly water-soluble drugs by applying solid dispersion technique for improving the solubility. Solubility is an important determinant in drug liberation and absorption and hence plays a key role in its bioavailability. For a drug to be absorbed, it must be present in the form of an aqueous solution at the site of absorption. Solubility of a drug candidate is an important aspect for the formulation development. Thus poor aqueous solubility is a very challenging problem in drug formulation. "A dispersion of one or more active ingredients in an inert carrier or matrix at solid state prepared by the melting (fusion), solvent, or melting-solvent method is called as solid dispersion" Solid dispersion is one of the most promising approach for solubility enhancement. A combination of solid dispersion and sustained release technique is one of the attractive approaches since supersaturation of drugs can be achieved by solid dispersion. Gliclazide is an oral hypoglycemic (anti-diabetic drug) and is classified as a sulfonylurea. Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity-onset or adult type. It is used when diabetes cannot be controlled by proper dietary management and exercise or when insulin therapy is not appropriate. The principal action of sulfonylureas is on B-cells, stimulating insulin secretion and thus reducing plasma glucose. High affinity receptors for sulfonylureas are present on the K-ATP channels in B-cells plasma membranes and the binding of various sulfonylureas parallels their potency in stimulating insulin release. The drug reduce the k+ permeability of B-cells by blocking K-ATP channels, causing depolarization, ca2+ entry and insulin secretion.


Related Articles

  • LYOPHILIZED GLICLAZIDE-POLOXAMER SOLID DISPERSIONS FOR ENHANCEMENT OF IN-VITRO DISSOLUTION AND IN-VIVO BIOAVAILABILITY. Bandarkar, Farzana S.; Khattab, Ibrahim S. // International Journal of Pharmacy & Pharmaceutical Sciences;2011 Supplement 2, Vol. 3, p122 

    Gliclazide (GLC), an oral hypoglycemic agent, is characterized by low solubility in gastric fluid, low dissolution rate and inter-individual variability in bioavailability. The objective of this study was therefore to design optimized solid dispersions (SD) of GLC with a hydrophilic carrier...

  • Intra-individual variability of the metabolic effect of inhaled insulin together with an absorption enhancer. Heinemann, Lutz; Klappoth, W.; Rave, K.; Hompesch, B.; Linkeschowa, R.; Heise, T.; Heinemann, L // Diabetes Care;Sep2000, Vol. 23 Issue 9, p1343 

    Objective: To study the metabolic effect and the variability of the effect elicited by inhalation of 87.2 U insulin powder combined with an absorption enhancer. The metabolic effect was compared with that of 10.2 U regular insulin injected subcutaneously and of 5.5 U regular insulin...

  • Is Exubera Another GlucoWatch?  // Diabetes Health;Apr2006, Vol. 15 Issue 4, p42 

    Relates the opinions of endocrinologists on the potential of Exubera, the noninjectible insulin from Pfizer Inc., to succeed in the U.S. market in 2006. Cost consideration; Possible effect of the drug's absorption issues; Comparison with the Food and Drug Administration approved GlucoWatch...

  • Recovery Studies on Metformin Hydrochloride and Gliclazide Combined Dosage Form (Tablets) Using Rp-Hplc Techniques. Saha, Dibyajyoti; Paul, Swati // International Journal of Pharmacy Teaching & Practices (IJPTP);Dec2012, Vol. 3 Issue 4, p405 

    Metformin hydrochloride is 1, 1-dimethyl biguanide hydrochloride and is also a hypoglecaemic drug. Gliclazide, is a third generation sulphonyl urea class hypoglycaemic drug which acts via stimulating β- cells of the isleta of langerhans of pancreas to release insulin. Metformin HCL differs...

  • Sulfonylureas.  // Encyclopedic Reference of Molecular Pharmacology;2004, p891 

    A definition of the term "sulfonylureas" is presented. These referes to oral hypoglycemic drugs that are used in treating type 2 diabetes. Examples of the first generation of sulfonylureas are tolbutamide and chlorpropamide. While second generation includes gliclazide, glibenclamide and...

  • Pulmonary effects of inhaled insulin are small, reversible.  // Formulary;Aug2007, Vol. 42 Issue 8, p502 

    The article focuses on the pulmonary effects of inhaled insulin among patients with type 2 diabetes. Study demonstrated that patients who are using inhaled insulin as part of their basal-bolus insulin regimen experience a small decline in pulmonary function. It was found out that the decline is...

  • Comparison of continuous subcutaneous insulin infusion and multiple daily injection regimens using insulin lispro in type 1 diabetic patients on intensified treatment: a randomized study. The Study Group for the Development of Pump Therapy in Diabetes. Hanaire-Broutin, Helene; Melki, Vincent; Bessiees-Lacombe, Sylvie; Tauber, Jean-Pierre; Hanaire-Broutin, H; Melki, V; Bessières-Lacombe, S; Tauber, J P // Diabetes Care;Sep2000, Vol. 23 Issue 9, p1232 

    Objective: To compare the efficacy of 2 intensified insulin regimens, continuous subcutaneous insulin infusion (CSII) and multiple daily injections (MDI), by using the short-acting insulin analog lispro in type 1 diabetic patients.Research Design and Methods: A total of...

  • INITIATING INSULIN. Lasserson, Daniel // Pulse;11/16/2006, Vol. 66 Issue 43, p54 

    The article focuses on reducing vascular risk in diabetes patients on insulin in Great Britain. In a research of the United Kingdom Prospective Diabetes Study, it revealed that using glucose control of blood pressure resulted to 25% reduction in microwave events. The initial strategies used by...

  • Advances in Insulin Injection Research Influences Patient Adherence. Aronson, Ronnie; Bailey, Timothy; Hirsch, Laurence; Saltiel-Berzin, Rita // U.S. Endocrinology;Winter2013, Vol. 9 Issue 2, p114 

    Insulin formulations and injection devices have improved dramatically since the first insulin injection was given in 1922. Adherence to insulin therapy, however, is estimated at 62-64 % despite research indicating that good glycemic control improves patient outcomes. The challenge is to improve...


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics