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Md Sarfaraz ¹, K. Arshad Ahmed Khan ¹, H. Doddayya ¹, S. R. Reddy ¹, R. H. Udupi ¹

Affiliations
1 Department of Pharmaceutics, N.E.T Pharmacy College, Raichur-584103, Karnataka, IN

Abstract

The purpose of present research was to obtain aceclofenac-disintegrant agglomerates with improved solubility, flow and compression characteristics by a novel crystallo-co-agglomeration (CCA) technique. Aceclofenac agglomerates were prepared by using a three solvent system comprising of acetone: DCM: water. Acetone-water containing PEG 6000, HPC and disintegrants like sodiumstarch glycolate (SSG), crospovidone (CP) and croscarmellose sodium (CCS) in different concentrations were used as the crystallization medium. The agglomerates were characterized by FTIR, DSC, PXRD, SEM studies and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that aceclofenac particles, crystallized in the presence of HPC, PEG 6000 and disintegrant did not undergo structural modifications. The dissolution rate of aceclofenac from the agglomerates could be controlled by the amount of included disintegrant, being enhanced as the latter was increased. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. Among all the formulations studied, F-9 prepared by incorporation of CP (18.43%) had shown short disintegration time (18.03 sec) and maximum drug release.

Keywords

Aceclofenac-Disintegrant Agglomerates, Crystallo-Co-Agglomeration, Direct Tableting, Disintegration Time, Dissolution.

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Md. Sarfaraz ¹, Y. Prasad ¹, S. R. Reddy ¹, H. Doddayya ¹, R. H. Udupi ¹

Affiliations
1 Department of Pharmaceutics, N.E.T Pharmacy College, Mantralayam Road, Raichur-584103, Karnataka, IN

Abstract

The aim of the study was to develop press coated time release tablets of nifedipine, from which the drug is released in a controlled manner to suite the Chronotherapeutics of the disease i.e., hypertension. The tablets, each consisting of a core and a coat, were prepared using compression coating technique. Core tablet was immediate-release formulation containing nifedipine soild dispersion of 1: 2 ratio with mannitol to enhance its solubility. The core tablet was then coated with a mixture of rate controlling polymers like polyethylene glycol (PEG6000) and hydroxyl propyl methyl cellulose (HPMC K100M) in different ratios to produce time release tablets of nifedipine. The core and press-coated tablets were evaluated for their physico-chemical properties, in-vitro release and stability studies. The in vitro drug release pattern indicated that type of polymer and its concentration had marked influence on the drug release from tablets. The drug release decreased with increasing amounts of HPMC K100M in the formulation. A lag time of 2 to 6 hrs was achieved with the polymers used. 2% sodium lauryl sulphate (SLS) was added as dissolution enhancer for dissolution study. The mechanism of drug release from all the press-coated tablets followed Higuchi model release kinetics with r² value 0.983 to 0.997. FT-IR and DSC studies revealed no chemical interaction between drug and polymers used.

Keywords

Chronopharmacotherapy, Nifedipine, Time-Release, Press-Coated Tablets, Lag Time.

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