Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Ali, Hezha Abdullah; Omer, Hunar Kamal

doi:10.1155/2022/7161660

Cited by 6 publications

(4 citation statements)

References 30 publications

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“…[10] A pharmaceutical substance is considered very permeable whenever the degree of absorption in humans is greater than 90% of an injected dose, as determined by mass balance or in comparison with an intravenous reference dose. [11] A medication product is considered to be swiftly dissolving when it dissolves more than 85% of its prescribed amount in thirty minutes or less employing USP apparatus I or II in the amount of lower than 900 ml containing buffer solutions. [12] [13] Factor Affecting Solubility…”

Section: Class Boundariesmentioning

confidence: 99%

A Systematic Review of Solubility Enhancement Techniques Used for BCS Class II & IV

Dhoble,

Tekade,

Bodke

et al. 2024

Int. J. Res. Pharm. Sci.

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Because of their low solubility, pharmaceutical researchers encounter tremendous difficulties in creating sustainable and more soluble drugs (BCS class II). About 40% of oral dosage forms have formulation and development problems due to water insolubility. The rate of dissolving, absorption, distribution, and excretion of an active medicinal substance is determined by its solubility parameters. Based on their solubility, drugs are divided into four kinds under the BCS categorization system. BCS Class II and Class IV drugs have problems with solubility. Increasing both the bioavailability and the solubility of poorly soluble medications can be accomplished in several ways. Some techniques—like solid dispersion, solid complexation, liquisolid, hydrotropy, sonocrystallization, and self-emulsifying techniques—are commonly used for solubility augmentation. Until an orally active medication dissolves in the lining of the stomach and/or intestinal fluids, it cannot pass through the GI tract membrane and enter the bloodstream. Therefore, a medication that is insoluble in water will typically exhibit limited absorption by dissolution, and a medication that is weakly permeabilized via membranes would typically exhibit limited absorption through permeation. Consequently, improving the oral bioavailability of active substances is the focus of two areas of pharmaceutical research: (i) accelerating the process of dissolution and solubility of drugs that are poorly soluble in water, and (ii) accelerating the permeability of poorly permeable drugs.

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Section: Class Boundariesmentioning

confidence: 99%

A Systematic Review of Solubility Enhancement Techniques Used for BCS Class II & IV

Dhoble,

Tekade,

Bodke

et al. 2024

Int. J. Res. Pharm. Sci.

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“…The entire experiment was carried out in duplicate and the value reported as mean of the two estimations. The solubility enhancement ratios were calculated as [11].…”

Section: Saturation Solubility Studiesmentioning

confidence: 99%

Development of Orodispersible Tablets of Loratadine Containing an Amorphous Solid Dispersion of the Drug in Soluplus® Using Design of Experiments

NAIR,

GADHIRAJU,

SUNNY

2023

Int J Pharm Pharm Sci

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Objective: The objective of the present work was to develop an orodispersible tablet of loratadine, an orally active, non-sedating anti-histaminic, belonging to BCS Class II. The drug was prepared as a solid dispersion using Soluplus® as carrier and formulated into an optimal tablet using Design of Experiments. Methods: Solid dispersions of loratadine with varying ratios of Soluplus® were prepared by solvent evaporation and subjected to solubility study in simulated salivary fluid. Selected composition was characterized by differential scanning calorimetry and X-ray diffraction and formulated into an orodispersible tablet by direct compression after addition of suitable excipients. DOE based on a full factorial design was used to optimize the product using a trial version of JMP software, so as to obtain a tablet with low friability, rapid disintegration and maximal drug dissolution within 5 min. The optimized tablet was prepared and evaluated for several attributes, including in vivo disintegration and palatability. Results: A solid dispersion prepared with a 1: 4 ratio of loratadine: Soluplus® was found to show a 130-fold increase in drug solubility in the simulated salivary fluid. X-ray diffraction revealed loratadine in amorphous form. The exercise using DOE for optimization of the orodispersible tablet formula served to balance the proportion of crospovidone as super disintegrant and PVP as dry binder and yielded a formulation with good mechanical strength, rapid in vitro disintegration (39 sec) and dissolution of 93.78% of the drug within 5 min. When evaluated in vivo, the tablets were found to disintegrate in about 60 secs and were reported to be palatable. Conclusion: A patient-friendly dosage form containing a highly soluble form of loratadine was prepared and could be of potential benefit in offering quick relief from allergic conditions.

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“…Glimepiride is a very poor water-soluble sulfonylurea with aqueous solubilities of less than 4 μg/mL at 310.15 K and 6.4 μg/mL at 298.15 K. This work aims to improve glimepiride's solubility, dissolution, and drug release by employing various highly water-soluble, non-toxic hydrotropic compounds [18].…”

Section: Introductionmentioning

confidence: 99%

Design and characterization of glimepiride hydrotropic solid dispersion to enhance the solubility and dissolution

Lakumalla,

Podichety,

Maddali

2024

JAPR

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Background: Glimepiride lowers blood sugar levels in the body, and treats type 2 diabetes mellitus. But the main problem with the drug is its low aqueous solubility. The primary purpose of this study is to increase its solubility in an aqueous medium by using amphiphilic hydrotropic agents instead of harmful, volatile organic solvents. Methodology: A solubility study of Glimepiride was carried out using various hydrotropic agents at 10%, 20%, 30%, and 40%. In mixed hydrography, 30% of the hydrotropic agents were chosen for making blends due to their highest solubility. The blend's solubility was raised more than 50 times at fixed concentrations of urea (20%) and sodium acetate (10%) in a mixed hydrotropic solution. The solubility of Glimepiride in distilled water is 0.0038 mg/ml; in 30% urea, 49.512 ug/ml; and in 30% sodium acetate, 40.43 ug/ml. The optimized blend prepared hydrotropic solid dispersions by physical mixing and solvent evaporation. It was evaluated for drug content, FTIR, SEM, X-ray diffraction, and in vitro drug release studies. Finally, the drug release profile of the prepared tablet is compared with an already available consumer product. Result: HSD-5 showed an in-vitro drug release of 84.77±0.44 at 90 min, which is higher than the remaining formulations, and no significant change was found in drug content or drug release after 15, 30, and 45 days of stability studies. Scanning electron microscopy (SEM) showed homogenous solid dispersion, crystallinity was determined using X-ray diffraction, and FTIR showed good drug compatibility with carriers. The drug release profile of the prepared tablet was higher than that of the available consumer product. Conclusion: This study revealed that hydrotropic agents can potentially increase glimepiride's solubility and drug release. This approach can effectively enhance the solubility of poorly water-soluble drugs.

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Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

Cited by 6 publications

References 30 publications

A Systematic Review of Solubility Enhancement Techniques Used for BCS Class II & IV

A Systematic Review of Solubility Enhancement Techniques Used for BCS Class II & IV

Development of Orodispersible Tablets of Loratadine Containing an Amorphous Solid Dispersion of the Drug in Soluplus® Using Design of Experiments

Design and characterization of glimepiride hydrotropic solid dispersion to enhance the solubility and dissolution

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