Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods

Sethia, Sundeep; Squillante, Emilio

doi:10.1016/j.ijpharm.2003.11.025

Cited by 387 publications

(205 citation statements)

References 21 publications

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“…The thermogram of PVP shows a broad endotherm peak at 80 -140°C due to the evaporation of absorbed water; this indicates the hygroscopic nature of this polymer (22). The melting point of the drug and polymer are observed in the thermogram of the physical mixture of loratadine and PVP powder, which shows that no physical change occurred in the drug and polymer powder mixture.…”

Section: Resultsmentioning

confidence: 95%

The Design and Evaluation of a Fast-Dissolving Drug Delivery System for Loratadine Using the Electrospinning Method

Akhgari

Dezfuli

Rezaei

et al. 2016

Jundishapur J Nat Pharm Prod

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Background: Due to their optimal mechanical and biological properties, nanofibers have numerous medical applications. Electrospinning is one of the widely used techniques for generating drug-containing nanofibers. Objectives: The aim of this study was to assess the use of the electrospinning method to prepare fast-dissolving loratadine nanofibers. Materials and Methods: Polyvinylpyrrolidone (PVP) nanofibers containing loratadine were produced using the electrospinning method. A full factorial design was employed to evaluate the formulations, including the four following variables: the concentration of PVP, the ratio of drug to polymer, the feed rate, and the voltage applied at two levels. After preparing the samples, assessments were carried out using scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, and differential scanning calorimetry (DSC). Dissolution tests and determination of the time of disappearance were also carried out. It was observed that reducing the concentration of polymer, reducing the feed rate, and increasing the voltage applied to the polymeric solution up to an adequate amount allowed the possibility of creating nanofibers with a smaller diameter and greater uniformity. Results:The results showed that the fiber diameter and the amount of loratadine affected the drug release and the disappearance time of nanofibers. The smaller the fiber diameter and drug amount, the faster the solubility and the release time of nanofibers. Conclusions: It was concluded that electrospinning can be a suitable method for preparing fast-dissolving loratadine nanofibers.

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Section: Resultsmentioning

confidence: 95%

The Design and Evaluation of a Fast-Dissolving Drug Delivery System for Loratadine Using the Electrospinning Method

Akhgari

Dezfuli

Rezaei

et al. 2016

Jundishapur J Nat Pharm Prod

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“…23 The drug and carriers; Eudragit E-100 and Eudragit L-100 were taken separately in different ratios (1:1, 1:1.5, 1:2) and transferred in a beaker containing appropriate amounts of ethanol (solvent). Subsequently, the solvent was removed by evaporation on magnetic stirrer with hot plate at temperature 40°C for 1 hr to get SD mass.…”

Section: Solvent Evaporation Methodsmentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

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“…Increasing the polymer fraction in the 1:1:2 ITSD improved the dissolution rate profile to almost double the profile of 1:2:2 ITSD. This can be explained by the phenomenon of the increasing solubility of a drug at the molecular level with an increasing amount of polymer (23). All internal systems dispersed uniformly in the media due to Syloid® 244FP, which may be the reason for the improved dissolution rate without precipitation of the drug.…”

Section: Dissolution Rate Studiesmentioning

confidence: 99%

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel¹,

Dave²

2013

AAPS PharmSciTech

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Abstract. Colloidal solid dispersion is an innovative breakthrough in the pharmaceutical industry that overcomes the solubility-related issue of poorly soluble drugs by using an amorphous approach and also the stability-related issue by means of a complex formation phenomenon using different carrier materials. In the present study, a newly developed adsorption method is introduced to incorporate a high-energy sulfathiazole-polyvinylpyrrolidone (Plasdone® K-29/32) solid dispersion on porous silicon dioxide (Syloid® 244FP). Different ternary systems of sulfathiazole-Plasdone® K-29/32-Syloid® 244FP were prepared (1:1:2, 1:1:3, and 1:2:2) and categorized depending on the mechanism by which Syloid® 244FP was incorporated. Modulated differential scanning calorimetry (MDSC), X-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were conducted to characterize the ternary systems. The X-ray diffraction and MDSC data showed a lack of crystallinity in all internal and external ternary systems, suggesting a loss of the crystallinity of sulfathiazole compared to the physical mixtures. USP apparatus II was used to measure the in vitro dissolution rate of the prepared systems at 75 rpm in different media. The dissolution rate of the optimum ratio (1:2:2) containing an internal ternary solid dispersion system was found to be three times higher than that of the external and physical systems. Thus, the porous silicon dioxide incorporated into the conventional binary solid dispersion acted as a carrier to disperse the complex and increase the dissolution rate.

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Solid dispersion of carbamazepine in PVP K30 by conventional solvent evaporation and supercritical methods

Cited by 387 publications

References 21 publications

The Design and Evaluation of a Fast-Dissolving Drug Delivery System for Loratadine Using the Electrospinning Method

The Design and Evaluation of a Fast-Dissolving Drug Delivery System for Loratadine Using the Electrospinning Method

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

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