OPTIMIZATION OF FORMULATION OF SOLID DISPERSION OF FUROSEMIDE BY FACTORIAL DESIGN

Objective: The present study aimed to improve the rate of dissolution of furosemide by solid dispersion technique. Methods: Solid dispersion of furosemide was prepared by using hydrogel isolated from the seeds of Lepidium sativum as a novel carrier by the solvent evaporation method. Solid dispersion was evaluated to study the improvement in the rate of dissolution. Molecular dispersion of furosemide in the novel carrier was studied by DSC and FTIR studies. Solid dispersion was filled in capsules after stability studies and the formulation was optimized by adopting factorial design. Results: Solid dispersion of furosemide exhibited dissolution improvement from 13.54 % (plain furosemide) to 69.12% (solid dispersion) in the first 60 min. Improvement in dissolution efficiency was found to be retained after stability studies. Capsules were filled with the formulation of solid dispersion using two different grades of lactose-α lactose monohydrate and anhydrous lactose and were found stable after stabilization studies. Conclusion: The dissolution improvement of furosemide was attributed to its molecular dispersion in the novel carrier selected for this study. The recrystallization of furosemide was prevented due to intermolecular interaction between the novel carrier and furosemide. This was confirmed by FTIR. Evaluation of the dissolution data of factorial batches was analyzed by ANOVA. Analysis of the data revealed that selected levels of α lactose monohydrate and anhydrous lactose would be useful to navigate design space

STUDY OF THE FUNCTIONALITY OF A NOVEL SOLUTION BINDER OBTAINED FROM OCIMUM BASILICUM SEEDS: A MECHANISTIC APPROACH

Objective: The aim of the present study was to investigate the functionality of the hydrogel isolated from the seeds of Ocimum basilicum (Gel) as a novel solution binder. Methods: Paracetamol is known to possess poor manufacturability. Therefore it was selected as a model drug to study the efficiency of Gel as a solution binder. Paracetamol tablets were prepared at gradually increasing compression pressure from the granules prepared by using Gel of various viscosities as a solution binder. Compactibility parameter was calculated to assess the utility of Gel as a novel tablet binder. Optimization of the formulation was done by adopting factorial design as an appropriate DOE. Tablets of factorial batches were evaluated for disintegration time and crushing strength. The effect of viscosity of binder solution used to prepare granulation and compression pressure applied on granulation on the performance of the tablets was confirmed by analyzing the data using ANOVA. Results: The addition of binder solution to prepare granulation with the viscosity ≥ 19.33 centipoises was found to be suitable to attain desired degree of agglomeration. The crushing strength of the tablets was found to be increased with an increase in compression pressure and an increase in viscosity of binder solution. Conclusion: The compatibility parameter was observed to be increased as the viscosity of the binder solution added in the formulation was gradually increased. The Gel as a binder material was found to deform plastically at compression pressures 34.48 to 75.85 MPa. This confirmed its functionality as a solution binder in Paracetamol tablet preparation

Formulation and Evaluation of Transdermal patches of Ropinirole HCl

ABSTRACT The conventional multidose antiparkinsons therapy leads to re-emergence of Parkinson's symptoms, due to fluctuations in serum levels of drug. The rational strategy to overcome this drawback is to minimize the fluctuations by fabricating sustained release formulations. Ropinirole HCl is a drug used to treat Parkinson's disorder and it is suitable drug candidate for transdermal delivery due to its small molecular size, optimum log P and low oral bioavailability due to first pass metabolism. Hence the present study was aimed at development of transdermal patch of Ropinirole HCl to show its prolonged release. The combination of HPMC K15 and Eudragit RL100 was tried as a porous matrix to control the release of Ropinirole HCl up to 12 hrs. The transdermal patches were prepared by solvent casting method. All the patches were evaluated for the permeation along with physical studies including appearance, thickness, folding endurance, drug content, percentage of moisture content and percentage of moisture uptake. The results of physical parameters ensured integrity, stability and applicability of the patches. The results of permeation studies clearly indicated that the release pattern of Ropinirole HCl can be controlled by maintaining appropriate proportion of HPMC K15 and Eudragit RL 100 in the matrix. No erythma was found within 12 hr after application of optimized transdermal patch when compared with standard irritant. Thus this formulation was suitable for transdermal application