Formulation and Evaluation of Lumefantrine Capsule Prepared by Using Liquisolid Technique

Abstract

Objective: The objective of present research work was to formulate and evaluate of Lumefantrine capsule by using novel liquisolid technique to give increased dissolution rate of poorly water-soluble drug Lumefantrine.Methods: Formulation of lumefantrine capsule using drug solution and suspension method was used. Different liquisolid formulations were prepared using a mathematical model for calculating required quantities of powder and liquid ingredients to produce an acceptably flowable and compressible admixture. Liquisolid capsule formulation F-1 to F-9 were prepared by using different type and different concentration of non-volatile solvent like PEG-400, Tween 80, propylene glycol and avicels, aerosil as carrier and coating material respectively. Results:The liquisolid formulation were within the acceptable limits and drug release rates of all prepared liquisolid were distinctly higher as compared to pure drug. Lumefantrine shows maximum solubility in tween 80 as a non-volatile solvent. All the preformulation parameters were evaluated such as organoleptic characterization of the drug sample, melting point, pH, identification of drug samples by using UV spectroscopy and FTIR analytical method, preparation of calibration curves, solubility studies of drug sample like qualitative, quantitative and pH-dependent solubility of the drug in a buffer solution of different pH. They were further processed for solid-state characterization such as, DSC and SEM and the results confirmed the transformation of native crystalline nature of drug to an amorphous state. FTIR analysis also confirmed no drug-excipient interaction. Liquisolid formulations showed improved in vitro dissolution behaviour of lumefantrine over that of pure drug. Conclusion:From this study, it was concluded that liquisolid method is a promising alternative for improvement of dissolution property of waterinsoluble drugs.

Formulation and Evaluation of Liquisolid Compacts of Lornoxicam

“…Pure lornoxicam was clearly in the crystalline state as it showed sharp distinct peaks notably at 2θ diffraction angles of 13.5 °, 24.3 °, 21.04 °, and 27.4 °. X-ray data supported the conclusion that the lornoxicam formed a solid solution within the carrier matrix [11]. Further, the photomicrographs of the liquisolid powder system signify the complete disappearance of lornoxicam crystals, a fact that indicates that the drug was totally solubilized in the liquisolid system [11].…”

“…The spectrum of pure lornoxicam shows a characteristic peak at 1733.2 due to C=O stretch, 3067.91 due to N-H stretch, 738.77 due to C-Cl stretch. Appearance of these peaks in the physical mixture and liquisolid formulation indicate the absence of chemical interaction between the drug and excipients [11]. FTIR spectral data is shown in fig.…”

“…3 for pure lornoxicam show a sharp exothermic peak at 218.5 °C corresponding to its melting temperature (Tm); such sharp exothermic peak signifies that lornoxicam was in the pure crystalline state. This characteristic sharp melting peak of lornoxicam completely disappeared in DSC thermograms of LS-4 liquisolid formulation and a broadened peak with markedly reduced intensity was observed at approximately 115.5 °C [11].…”

“…LS-4showed good flow properties therefore considered as a liquisolid system with acceptable flowability [11]. Result of the flow properties of lornoxicam liquisolid systems is given in table 3.…”

Liquisolid Compacts: An Innovative Approach for Dissolution Enhancement

“…This results in increased water solubility of such candidates. E. g.-Naproxen, Digitoxin, Prednisolone, Hydrocortisone, Ketoprofen [37].…”