Preparation and characterization of Furosemide-Eudragit controlled release systems

Aceves, J. M.; Cruz, Ricardo Machado; Hernández, Elena Pérez

doi:10.1016/s0378-5173(99)00303-8

Cited by 40 publications

(27 citation statements)

References 7 publications

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“…This implies that Eudragit L-100 provided protection for the microspheres in acidic conditions. Eudragit L-100 is a neutral copolymer of polyethylacrylate, methylmethacrylate and trimethylammoniumethylmethacrylate chloride [18]. It is inert to the content of digestive tract, thus does not adversely affect the mucosal lining and is commonly use for the development of oral drug delivery systems [19].…”

Section: Discussionmentioning

confidence: 99%

“…It is inert to the content of digestive tract, thus does not adversely affect the mucosal lining and is commonly use for the development of oral drug delivery systems [19]. Its degradation is pH dependent, being sparingly soluble in acidic medium due to the presence of acidic groups such as methacrylic acid [18], but soluble in solution medium of pH > 6.0. Therefore, it is widely used for targeted delivery of drugs to the colon [19].…”

Section: Discussionmentioning

confidence: 99%

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Formulation and Optimization of Celecoxib-Loaded Microspheres Using Response Surface Methodology

Shahzad¹,

Ubaid²,

Murtaza³

2013

Trop. J. Pharm Res

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Formulation and Optimization of Celecoxib-Loaded Microspheres Using Response Surface Methodology

Shahzad¹,

Ubaid²,

Murtaza³

2013

Trop. J. Pharm Res

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“…4, 5 and 6 respectively. Furosemide exhibits two characteristics, sharp endothermic peak at 218.16˚C and exothermic peak at 222.32˚C, which are associated with the decomposition and melting points of the drug and indicate the crystalline nature of the drug [41,42]. The physical mixture of liquisolid and liquisolid tablet showed the partial disappearance of the characteristic peak of furosemide, supporting the probable phenomena of getting molecularly dispersed into the liquisolid matrix system, which suggests conversion of the drug into an amorphous form.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

Formulation and Evaluation of Furosemide Liquisolid Compact

Jassim

2017

Int J App Pharm

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Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder xray diffraction (PXRD) studies. Results:The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion:The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

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“…The fourth generation of solid dispersions represents controlled release solid dispersion containing poorly water-soluble drugs with a short biological half-life, wherein two targets are to be achieved, i.e., solubility enhancement and extended release in a controlled manner (19). The controlled release systems of poorly water-soluble drugs having short half-life are highly desirable as these systems allow a reduction of pill burden, dosing frequency, and food restrictions while maintaining efficacy (20). However, there are very limited scientific literature and marketed products available having controlled release solid dispersion kind of system.…”

Section: Introductionmentioning

confidence: 99%

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

Verma

Rudraraju²

2014

AAPS PharmSciTech

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Abstract. The objective of this study was to develop a solid dispersion based controlled release system for drug substances that are poorly soluble in water. A wax-based disintegration mediated controlled release system was designed based on the fact that an amorphous drug can crystallize out from hydrophilic matrices. For this study, cilostazol (CIL) was selected as the model drug, as it exhibits poor aqueous solubility. An amorphous solid dispersion was prepared to assist the drug to attain a supersaturated state. Povidone was used as carrier for solid dispersion (spray drying technique), hydrogenated vegetable oil (HVO) as wax matrix former, and sodium carboxymethyl cellulose (NaCMC) as a disintegrant. The extreme vertices mixture design (EVMD) was applied to optimize the designed and developed composition. The optimized formulation provided a dissolution pattern which was equivalent to the predicted curve, ascertaining that the optimal formulation could be accomplished with EVMD. The release profile of CIL was described by the Higuchi's model better than zero-order, first-order, and Hixson-Crowell's model, which indicated that the supersaturation state of CIL dominated to allow drug release by diffusion rather than disintegration regulated release as is generally observed by Hixson-Crowell's model. The optimized composition was evaluated for disintegration, dissolution, XRD, and stability studies. It was found that the amorphous state as well as the dissolution profile of CIL was maintained under the accelerated conditions of 40°C/75% RH for 6 months.

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Preparation and characterization of Furosemide-Eudragit controlled release systems

Cited by 40 publications

References 7 publications

Formulation and Optimization of Celecoxib-Loaded Microspheres Using Response Surface Methodology

Formulation and Optimization of Celecoxib-Loaded Microspheres Using Response Surface Methodology

Formulation and Evaluation of Furosemide Liquisolid Compact

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

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