Fabrication and Evaluation of Solid Dispersion Containing Glibenclamide

Sehgal, Nikita; N, Vishal Gupta; Dv, Gowda; Sivadasu, Praveen

doi:10.22159/ajpcr.2018.v11i8.26236

Cited by 6 publications

(6 citation statements)

References 7 publications

(9 reference statements)

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“…The solvent was then rapidly evaporated with the help of heat. The precipitate was crushed, sized, and stored in a desiccator, until further use 17,18 .…”

Section: Solvent Evaporation Methodmentioning

confidence: 99%

Untitled

2020

IJPSR

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The oral route of drug administration is the most common and preferred method of delivery due to convenience and ease of ingestion, but it is problematic if the drug is poorly soluble. Sufficient drug absorption, reproducible bioavailability and pharmacokinetic profile of orally administered drug substances are highly dependent on the solubility of that compound in an aqueous medium. Also, the therapeutic effectiveness of drugs depends upon bioavailability and, ultimately, upon the solubility of drug molecules. Solid dispersions have attracted considerable interest as an efficient means of improving the solubility and hence bioavailability of a range of hydrophobic drugs. These systems are one of the most promising approaches for solubility enhancement. They are referred to a group of solid products consisting of at least two different components, generally a hydrophilic matrix and a hydrophobic drug (1-4). The aim of the present study was to improve the solubility and dissolution rate of Lercanidipine Hydrochloride (L) by formulating a solid dispersion with Polyvinyl pyrollidone (PVP-K30) and Guar gum. Central composite design (CCD) was employed using Design-Expert software version 12 to prepare optimized fast disintegrating tablets of Lercanidipine Hydrochloride. INTRODUCTION: The most simple, easy, and convenient path of drug administration is through the oral route due to its better stability, dose accuracy, lesser bulk, and easy manufacturing 1, 2. Improvement in drug solubility and, in turn, the oral bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development.

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“…The solvent was then rapidly evaporated with the help of heat. The precipitate was crushed, sized, and stored in a desiccator, until further use 17,18 .…”

Section: Solvent Evaporation Methodmentioning

confidence: 99%

Untitled

2020

IJPSR

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“…On the other hand, due to their poor wetting ability, very thin powders of hydrophobic medicines are challenging to dissolve in water. Liquid drug loading into porous powder, often known as "powder solutions," encounters problems with flow properties and compressibility [8,9]. In this research article, solid dispersion (SD) of telmisartan (TLM) has been prepared as a combination of hydrophilic polymers and also studies the impact of various variables on drug release and entrapment efficiency [9].…”

Section: Introductionmentioning

confidence: 99%

“…Liquid drug loading into porous powder, often known as "powder solutions," encounters problems with flow properties and compressibility [8,9]. In this research article, solid dispersion (SD) of telmisartan (TLM) has been prepared as a combination of hydrophilic polymers and also studies the impact of various variables on drug release and entrapment efficiency [9]. SD is a technology for the formulation of a drug having low solubility.…”

Section: Introductionmentioning

confidence: 99%

Investigation of Solid Dispersion Approach for the Improvement of Pharmaceutical Characteristics of Telmisartan Using a Central Composite Design

KAUSHIK,

VERMA,

BUDHWAR

et al. 2023

Int J App Pharm

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Objective: The goal of this study was to use a solid dispersion approach to improve the aqueous solubility and dissolution rate of Telmisartan. Methods: Design of experiment trials was conducted following a central composite design with different combinations of polymers and stirrer rpm and the selected responses (drug release, entrapment efficiency) were determined. The selected optimized formulation was characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction, which reflected the changes that occurred in API and excipients after conversion in to the formulation. Results: In the design of experiments, central composite design was implemented and it was observed that polymers concentration (polyvinyl pyrrolidine K25, polyethylene glycol 4000) and stirrer rpm were having a significant impact on the responses (drug release, entrapment efficiency), and variables were having p-value<0.05 which reflected the significant impact. The results of stability study showed a significant no decrease in drug assay values, which reflected the stability behavior of the formulation. The results of comparative dissolution studies revealed that the optimized formulation have improved the drug solubility and dissolution rate. Conclusion: It can be concluded that optimized telmisartan-loaded solid dispersion improved the solubility and dissolution rate of Telmisartan. The optimized formulation was having release>85% release within 30 min. Further, the stability of the formulation was also assessed under the accelerated condition as per ICH which reflected their stability. So, this approach can be employed for improving dissolution rate of other BCS II class drugs.

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“…iii) drug is dispersed in the carrier amorph state by inhibiting crystallization in the solid state, and these systems can easily be dispersed and wetted in the medium by the dissolution of the carrier in the dissolution medium [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

Solubilization Effect of Anionic, Cationic and Nonionic Surfactants on Coenzyme Q10 Solid Dispersion

ERGİN¹

2023

jrp

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Coenzyme Q10 ( CoQ10) is an oil-soluble vitamin-like benzoquinone compound. Coenzyme Q10 plays a role in providing membrane stability, energy conversion and ATP production. It is also one of the important antioxidants in the body. The bioavailability of coenzyme Q10 is very low due to its low solubility in water and its large molecular mass. Among the solubility enhancement approaches, solid dispersions (SDs) are one of the most promising strategies. The use of suitable carrier and methodology plays a significant role in the biological response. In terms of a carrier, solid dispersions are classified broadly the third group. Surfactant-based SDs are called third-generation solid dispersions. To evaluate the surfactant effect on solubilization of CoQ10, three different surfactants of varying ratios between 1:1, 1:3 and 1:5 (w/w) were used namely sodium dodecylsulfate (SDS) (anionic), cetyl trimethyl ammonium bromide (CTAB) (cationic) and Pluronic F127 (non-ionic). CoQ10 solid dispersions were characterized in terms of particle size, polydispersity index, zeta potential, FTIR spectroscopy, DSC analysis, saturation solubility and in vitro dissolution studies. To compare dissolution rate, area under the dissolution curve (AUC), Mean Dissolution Time (MDT), mean residence time of the drug substance molecules in the dosage form (MRT), and dissolutio nefficiency % (DE%) were calculated. All the formulations showed improvement in the aqueous solubility, while the dissolution rate was increased only by Pluronic F127 (p<0.05). Among the surfactants, Pluronic F127-based SDs were found superior to other surfactants. The results revealed that surfactant-based SDs offered great success in improving the therapeutic efficacy of CoQ10.

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Fabrication and Evaluation of Solid Dispersion Containing Glibenclamide

Cited by 6 publications

References 7 publications

Untitled

Untitled

Investigation of Solid Dispersion Approach for the Improvement of Pharmaceutical Characteristics of Telmisartan Using a Central Composite Design

Solubilization Effect of Anionic, Cationic and Nonionic Surfactants on Coenzyme Q10 Solid Dispersion

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