Formulation and Evaluation of Furosemide Liquisolid Compact (original) (raw)
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Liquisolid: A Novel Technique for Dissolution Enhancement of Poorly Soluble Drugs
The poor dissolution characteristic of water insoluble drugs is a major challenge for formulation scientists. About 50% of orally administered drugs suffer from formulation difficulties related to their water insolubility. Thus it is rate limiting step for achieving optimum bioavailability of such drugs by pharmaceutical industry with developments of new pharmaceutical products.There are various methods but liquisolid technique is a new and promising method that can change the dissolution rate of water insoluble drugs. According to the new formulation method of liquisolid compacts, liquid medications such as solutions or suspensions of water insoluble drugs in suitable nonvolatile liquid vehicles can be converted into acceptably flowing and compressible powders by blending with selected powder excipients. In this case, even though the drug is in a solid dosage form, it is held within the powder substrate in solution or, in a solubilized, almost molecularly dispersed state, which contributes to the enhanced drug dissolution and release properties. Liquisolid system is characterized by flow behavior, wettability, powder bed hydrophilicity, saturation solubility, drug content, differential scanning calorimetry, Fourier transform infra red spectroscopy, powder X-ray diffraction, scanning electron microscopy, in-vitro release and in-vivo evaluation.
Formulation and Evaluation of Solid Dispersion Tablets of Furosemide Using Polyvinylpyrrolidone K-30
International Journal of Current Pharmaceutical Research, 2021
Objective: The objective of the present study was to improve the aqueous solubility and dissolution characteristics of the loop diuretic furosemide (FUR); a class IV drug in the Biopharmaceutical Classification System (BCS) using solid dispersion technique. Methods: Solvent evaporation and kneading methods were used to produce solid dispersions of FUR in different ratios with the hydrophilic carrier polyvinylpyrrolidone K-30 (PVP-K30). The prepared solid dispersions were evaluated in terms of solubility study, percentage yield, drug content and Fourier transform infrared spectroscopic study (FT-IR). Tablets containing the optimized formula of solid dispersions ( were formulated and their dissolution characteristics were compared with commercial furosemide tablets. Results: The prepared solid dispersions showed an increase in aqueous solubility, especially those formulated in a 1:2 drug: carrier ratio using solvent evaporation method ( it showed a four-fold increase in solubility com...
IntechOpen eBooks, 2022
Solubility plays a key role to achieve desired concentration of drug in systemic circulation and show its pharmacological action. An approach of liquisolid technique, developed by Spireas, was employed for the dissolution enhancement of poorly aqueous soluble drugs. Initially, liquid medication (liquid drug or drug solution or suspension in hydrophilic liquid vehicle) is transformed to free-flowing, non-sticky, compressible powder by the addition of suitable carrier material and coating materials for the development of liquisolid compacts. The postulated mechanism for enhanced solubility was improved wettability of drug and enhanced surface area of molecularly dispersed drug in the liquid environment. Pre-and post-the compression tests were performed for the developed liquisolid compacts to obtain optimized formulation. For the optimized compacts, FTIR and DSC studies were performed for determining drug-excipient compatibility; SEM and PXRD studies were performed to study the solid-state characterization. Furthermore, accelerated stability studies were performed for optimized liquisolid compacts for 6 months according to ICH guidelines and the results were compared with freshly prepared formulations. In conclusion, liquisolid compact formulation was proved to be safe, economic and alternative approach to formulate solid oral dosage forms of poorly aqueous soluble drugs.
Liquisolid Compact: A New Technique for Enhancement of Drug Dissolution
2011
The dissolution properties of a drug and its release from a dosage form have a basic impact on its bioavailability. Solving solubility problems is a major challenge for the pharmaceutical industry with developments of new pharmaceutical products. There are various methods but liquisolid technique is a new and promising method that can change the dissolution rate of water insoluble drugs. According to the new formulation method of liquisolid compacts, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non- volatile liquid vehicles can be converted into acceptably flowing and compressible powders by blending with selected powder excipients. It has been speculated that such systems exhibit enhanced release profiles. In this case, even though the drug is in a solid dosage form, it is held within the powder substrate in solution or, in a solubilized, almost molecularly dispersed state, which contributes to the enhanced drug dissolution properties.
ADMET and DMPK, 2020
Furosemide is a diuretic drug widely used in chronic renal failure. The drug has low solubility and permeability, which cause clinical problems. Studying the in vitro release performance elucidates the rate and extent of drug dissolved from dosage forms under different conditions. Furosemide reference tablets were tested using USP Apparatuses 1 and 2 as well as the flow-through cell method (USP Apparatus 4), a dissolution apparatus that simulates the human gastrointestinal tract better than the other methods. Dissolution profiles were created with USP Apparatuses 1 and 2 at 25, 50, and 75 rpm and 900 mL of 0.1 M hydrochloric acid, acetate buffer (pH 4.5), and phosphate buffer (pH 6.8). USP Apparatus 4 with a laminar flow of 16 mL/min and 22.6 mm cells was used. Drug dissolution was quantified at 274 nm for 60 min. Mean dissolution time, dissolution efficiency, time to 50 % dissolution, and time to 80 % dissolution data were used to compare dissolution profiles. Additionally, zero-or...
Liquisolids-A Technique for Dosage Formulation with Improved Solubility of Active Principle
2016
Liquisolid technique is a novel approach for the concept of dosage formulation to improve the bioavailability, dissolution rates and rapid disintegration of water insoluble drugs via oral route of administration. In this technique of formulation involves drugs dissolved in suitable non-volatile liquid vehicles, and converted in to powdered forms of liquid medications compact, they are compressible and acceptably industrial applicable by combination with selective powder excipients. The liquisolid technique allows the formulation transformation into solid drug delivery systems. With this technique as compare to commercial conventional tablet it shows confirmed increasing dissolution rates in addition to improved bioavailability. Approach has been successfully applied for poorly soluble drugs in release of low dose enhancement. However, for the high dose drugs one of the limitations for the formulation because of more liquid/vehicle required for the drug dissolution procedure as well ...
Liquisolid Technique for Dissolution and Bioavailability Enhancement of Poorly Soluble Drugs
Universal Journal of Pharmaceutical Research, 2017
Liquisolid formulations have attracted substantial interest as an efficient means of improving the dissolution and ultimately bioavailability. The technique is based upon the admixture of drug loaded solutions with appropriate carrier, coating materials and use of non-volatile solvent causes improved wettability. The inclusion complexes of drug with beta cyclodextrin (β CD) were formulated by kneading method and highest solubility complex was further used for preparation of liquisolid formulation to get synergistic effect. Also it raises drug incorporation with dissolution enhancement compared with conventional formulation. There are various techniques for bioavailability enhancement, such as altering the pharmacokinetic parameters, inhibition of enzyme etc. For this purpose some herbal inhibitors can be used; ex piperine. The prepared formulations were characterized by FTIR, DSC, PXRD and in vitro dissolution studies. Hence, this liquisolid technique with two way approach of solubility and bioavailability enhancement may found as key aspect in designing of formulations.
Effect of Dissolution Rate by Liquisolid Compact Approach: An Overview
2012
Liquisolid technique is a new and promising method that can change the dissolution rate of water insoluble drugs. According to the new formulation method of liquisolid compacts, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders by blending with selected powder excipients. It has been speculated that such systems exhibit enhanced release profiles. In this case, even though the drug is in a solid dosage form, it is held within the powder substratein solution or, in a solubilized, almost molecularly dispersed state, which contributes to the enhanced drug dissolution properties. Large scale production of fabricated drug on commercial level.succesful liquisolid tablet is a determination of optimal flowable liquid retention.
Liquisolid Technique: A Novel Approach to Enhance Solubility of Poorly Soluble Drugs
2019
Biovailability of any drug depends on the dissolution of the drug and its release from the dosage form. Solubility is the major challenge for pharmaceutical industries with the development of poorly soluble drugs. There are several approaches for solubility enhancement which includes micronisation, nanonisation, use of salt forms, surfactants, solid dispersions and supercritical fluid recrystallisation, etc. Liquisolid technique is a novel and efficient approach for solubility enhancement. According to this method the conversion of water insoluble drugs into dry looking, non-adherent, free flowing and acceptably compressible powder by incorporating into suitable nonvolatile solvents, carrier and coating materials (It is claimed that if hydrophobic carriers such as Eudragit RL and RS are used instead of hydrophillic carriers in liquisolid system, sustained release systems can be obtained). This free flowing powder is thus subjected to preformulation studies like differential scanning...
Liquisolid Dosage System : A Novel Approach for Dosage formulation
2015
In the drug development enhancement of oral bioavailability of poorly water soluble drugs is one of the most challenging aspects of drug. The pharmaceutical industry face the problem poor dissolution characteristics of water insoluble drug. these problem solve by applying recent techniques “powdered solution technology” or “liquisolid technology”, for prepare water-insoluble drugs into rapid-release solid dosage forms. Design and formulation of this approach is prescribed according to new mathematical model given by spires et al. the solubility is Increasing by using a non-volatile solvent which is suitable for drug, their by dissolving the drug in the non volatile solvent it is termed as liquid medicament. This case, the drug is in a solid dosage form, it is held within the powder substrate in solution or, in a solubilized, almost dispersed state, which contributes to the enhanced drug dissolution and release properties. Liquisolid system is characterized by flow behavior, wettabil...