REVIEW ARTICLE International Journal of Pharmaceutical Chemistry and Analysis; April-June 2015;2(2):51-58 51 SOLUBILITY AND DISSOLUTION ENHANCEMENT OF GLICLAZIDE BY SOLID DISPERSION TECHNIQUE More C.G * , Dabhade P.S, Jain N.P, Aher B.O Department of Quality Assurance, S.N.D. College of Pharmacy, Yeola. (MS) India. *Corresponding Author: Email: sushantmore166@gmail.com ABSTRSCT The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Most NCE are poorly water soluble drugs, not well-absorbed after oral administration. Solid dispersion is an increasingly important approach to enhance dissolution rate and solubility of poorly water soluble drug. Gliclazide is a second generation hypoglycemic sulfonylurea which is useful in the treatment of non-insulin dependent diabetes mellitus (NIDDM). It exhibits slow GI absorption rate and inter individual variations of its bioavailability. Oral bioavailability of drug is 59%. Half-life of drug is about 10hr. Thus solubility enhancement and dissolution enhancement of Gliclazide from its dosage form is an important issue for its in vivo bioavailability and therapeutic efficacy. Therefore it was planned in this investigation to improve the solubility and bioavailability of drug by using different hydrophilic polymers. Also, it was planned to evaluate such solid dispersion formulations for their various pre-compression and compression characteristics, in vitro drug release kinetics and stability of the dosage forms. Keywords: Non-insulin Dependent diabetes mellitus (NIDDM), New chemical Entities(NCE), Solid dispersion’s (SD’s) INTRODUCTION The poor aqueous solubility and dissolution rate of API is one of the biggest challenges in pharmaceutical development and is becoming more common among new drug candidates over the past two decades 1 . Because of the greater stability, smaller bulk, accurate dosage and easy production, solid oral dosages forms offers many advantages over other types of oral dosage forms. Therefore, most of the new chemical entities (NCE) under development these days are intended to be used as a solid dosage form originating an effective and reproducible in vivo plasma concentration profile after oral administration 2. The poor solubility and low dissolution rate of poorly water soluble drugs in the aqueous gastro-intestinal fluids often cause insufficient bioavailability rather than the limited permeation through the epithelia and the formulation of poorly soluble drugs for oral delivery now presents one of the major challenges to formulation scientists in the industries 3 .Moreover, most promising NCEs, instead of their high permeability, are usually only absorbed in the upper small intestine, absorption being reduced significantly after the ileum, showing, therefore, that there is a small absorption window. Consequently, the incomplete release of these drugs in the gastrointestinal area will show low bioavailability problems 4. Drug release is a crucial and rate limiting step for oral bioavailability, particularly for drugs with low solubility and high permeability i.e. BCS class II drugs. By improving the drug release profile of BCS class II drugs, it is possible to enhance their bioavailability and reduce side effects 3 . Solid dispersions are one of the most promising strategies to improve drug release of poorly soluble drugs. Solid dispersion’s (SD’s) can be defined as homogeneous molecular mixtures of poorly water soluble drugs in hydrophilic carriers, presenting a drug release profile driven by the polymer properties. Chemically Gliclazide is [1-(3-azabicyclo (3,3,0) oct- 3-yl)-3-p-tolylsulfonylurea]. It is a second generation hypoglycemic sulfonylurea which is useful in the treatment of non-insulin dependent diabetes mellitus (NIDDM). Gliclazide is a white crystalline powder, relatively insoluble in water. The pKa of Gliclazide is 5.8. It exhibits slow GI absorption rate and inter individual variations of its bioavailability. Oral bioavailability of drug in rang of 79 to 81 percent. Half-life of drug is about 10hr. Thus solubility enhancement and dissolution enhancement of Gliclazide from its dosage form is an important issue for its in vivo bioavailability and therapeutic efficacy. Materials and Equipments/Instruments: Materials: Table 1: List of Materials. Sr. No. Materials Manufacturer 1. Gliclazide Indoco, Mumbai. 2. Gelucire 50/13 Gattefosse, Mumbai. 3. Polyethylene glycol 6000 LobaCheme, Mumbai. 4. Glizid 40, Gliclazide tablet 40 mg. Panacea biotech ltd. Mumbai.