Research Journal of Pharmaceutical Dosage Form and Technology

Masheer Ahmed Khan ¹

Affiliations
1 School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshshila Campus, Khandwa Road, Indore-452001, IN

Abstract

Enhancement of solubility is one of the difficult tasks which become challenges in formulation development of orally administered drug with poor aqueous solubility. Poor water solubility of drugs often causes significant problems in producing formulations of sufficiently high bioavailability, preventing effective use of the drugs. 'Mixed-solvency ' concept is the phenomenon to increase the solubility of poorly water-soluble drugs in the aqueous solution containing blends of hydrotropic agents, co-solvents and water soluble solutes which may give synergistic enhancement effect on solubility of such drugs. In the present investigation, mixed solvency approach has been applied for the enhancement of aqueous solubility of a poorly water-soluble drugs diclofenec sodium (selected as a model drug), by making blends of randomly selected water-soluble substances from among the hydrotropic (urea, sodium acetate); water soluble solutes (PEG4000, PEG6000); and co-solvents (PEG200, PEG400). The aqueous solubility of diclofenac sodium was observed at room temperature in the randomly selected blends of solubilizers containing different combinations keeping total concentration 50%w/v constant. Diclofenec sodium have max 276 nm and obeys Beers Law in concentration range of 10-60 μg/ml. The results suggest that solubility of the diclofenac sodium containing blends of varying combinations was enhanced significantly using mixed solvency approach.

Keywords

Solubility, Mixed-solvency.

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Masheer Ahmed Khan ¹

Affiliations
1 School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshshila Campus, Khandwa Road, Indore, 452001, IN

Abstract

The present study was performed to illustrate the effect of pH on dissolution profile of atenolol sustained release matrix tablets. Atenolol is -1 cardio selective adrenergic receptor blocker, widely used in the treatment of hypertension. The drug is insoluble in water and has half-life of six to eight hours with oral bioavailability of 50% due to smaller dose of drug (less than 50 mg). Once daily Sustained release matrix tablets of Atenolol reduces the frequency of administration and improves the patient compliance. Atenolol matrices were prepared from combination of polymers HPMCK4M and HPMCK15M to sustain the release of the drug. Multimedia dissolution studies were performed to mimic the in-vivo condition by doing in-vitro test and pH/buffer selection is based on the exposure of drug from stomach to intestine/colon and to ensure the impact of pH changes on dissolution and release of drug substance for absorption. The study ensures the impact of pH changes on dissolution and release of drug substance for absorption.

Keywords

Atenolol, Dissolution Studies, Matrix.

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Masheer Ahmed Khan ¹

Affiliations
1 School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshshila Campus, Khandwa Road, Indore, 452001, IN

Abstract

Sustained release diclofenac sodium matrices are used to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose for analgesic, antipyretic and anti- inflammatory activities. The current study examines the relationship between swelling and drug release from the hydrophilic matrices of diclofenac sodium matrices prepared using combination of different grades of hydroxypropyl methylcellulose (HPMC), viz, HPMCK4M, HPMCK15M and HPMCK100M. The Degree of Swelling and Percent water uptake were determined for the matrices containing different concentrations and combinations. The results indicate that swelling and release profiles were affected by concentration and viscosity grade of the polymer. When the amount of HPMC in the matrix is high, wetting improves and water uptake into matrices is enhanced. The higher amount of HPMC causes a greater degree of swelling this in turn reduces the drug release, as the diffusional path length of drug is now longer. Conversely, reduction in the amount of HPMC reduces the degree of swelling and the thickness of gel layer, this enables faster drug release. Higher viscosity grades swells to greater extent and has greater intrinsic water uptake property than that of the lower viscosity grades. Swelling studies reveals an inverse relationship between swelling and drug release in the sustained release diclofenac sodium matrices.

Keywords

HPMC, Matrices, Swelling.

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