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M. Kranthi Kumar Reddy ¹, B. Narasimha Rao ¹, K. Ravindra Reddy ¹

Affiliations
1 Department of Pharmaceutics, P. Rami Reddy Memorial College of Pharmacy, Kadapa-516003 Andhra Pradesh, IN

Abstract

Nateglinide is a novel anti diabetic drug that lowers blood glucose levels by stimulating insulin secretion from the pancreas. This action is dependent upon functioning beta-cells in the pancreatic islets. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. Therefore, solid dispersions (SDs) of nateglinide were prepared using lactose, mannitol and urea to increase its aqueous solubility. Nateglinide SDS was prepared in 1:1, 1:2, and 1:3 ratios of the drug to polymer (by weight). In vitro release profiles of all SDs (F-1 to F-9) were comparatively evaluated and also studied against pure Nateglinide. Faster dissolution was exhibited by solid dispersion containing 1:3 ratio of drug: mannitol. The increase in dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and due to reduction in drug crystallinity. The prepared solid dispersion was subjected for % practical yield, drug content and infrared (IR) spectroscopic studies. Absence of significant drug-carrier interaction was confirmed by infrared spectroscopic (IR) data.

Keywords

Nateglinide, Solid Dispersions (SDs), Mannitol, Urea, Lactose, Kneading Method.

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B. Divya ¹, P. Sabitha ¹, Ravindra Reddy ¹, M. Kranthi Kumar Reddy ¹, B. Narasimha Rao ¹

Affiliations
1 Department of Pharmaceutics, P. Rami Reddy Memorial College of Pharmacy, Kadapa-516003 Andhra Pradesh, IN

Abstract

Bioavailability can be increased by changing in disintegration and dissolution the aqueous solubility is lesser than 1μg/ml will definitely create a bioavailability problem and thereby affecting the efficacy of the drug. There are number of methods through which aqueous solubility of the drug can be increased in which solid dispersions is one of the effective and accepted technique in the pharmaceutical industry. The solid dispersion was defined as the dispersion of one or more active ingredients in an inert carrier or matrix. The purpose of the study was to improve the physicochemical properties of gatifloxacin like solubility, dissolution properties and stability of poorly soluble drug by forming dispersion with mannitol as water soluble carrier. The solid dispersion of gatifloxacin by Physical triturating method, kneading and Solvent evaporation were prepared using 1:1, 1:2,1:3 and 1:4 ratios of drug and polymer (mannitol). The saturation solubility was carried using USP type XXIV (paddle) type dissolution apparatus. The prepared dispersion showed marked increase in the saturation solubility and dissolution rate of gatifloxacin than that of pure drug. The dispersion with mannitol (1:4) by kneading method showed faster dissolution rate (99.85%) as compared to other dispersions with urea (1:1,1:2 and 1:3) whichever prepared by physical mixture and solvent evaporation method. The FT-IR shows the complexation and there were no interactions. Finally solid dispersion of gatifloxacin: mannitol prepared as 1:4 ratio by kneading method showed excellent physicochemical characteristics and was found to be described by dissolution release kinetics and was selected as the best formulation in this study.

Keywords

Solid Dispersion, Water Soluble Carrier, Gatifloxacin and Mannitol.

Full Text

     

M. Kranthi Kumar Reddy ¹, B. Narasimha Rao ¹, K. Ravindra Reddy ¹

Affiliations
1 Department of Pharmaceutics, P. Rami Reddy Memorial College of Pharmacy, Kadapa-516003, Andhra Pradesh, IN

Abstract

Nateglinide is a novel anti diabetic drug that lowers blood glucose levels by stimulating insulin secretion from the pancreas. This action is dependent upon functioning beta-cells in the pancreatic islets. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. Therefore, solid dispersions (SDs) of nateglinide were prepared using lactose, mannitol and urea to increase its aqueous solubility. Nateglinide SDS was prepared in 1:1, 1:2, and 1:3 ratios of the drug to polymer (by weight). In vitro release profiles of all SDs (F-1 to F-9) were comparatively evaluated and also studied against pure Nateglinide. Faster dissolution was exhibited by solid dispersion containing 1:3 ratio of drug: mannitol. The increase in dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and due to reduction in drug crystallinity. The prepared solid dispersion was subjected for % practical yield, drug content and infrared (IR) spectroscopic studies. Absence of significant drug-carrier interaction was confirmed by infrared spectroscopic (IR) data.

Keywords

Nateglinide, Solid Dispersions (SDs), Mannitol, Urea, Lactose, Kneading Method.

Full Text