Solubility enhancementofcefixime trihydrate by solid dispersions using hydrotropic solubilization technique and their characterization

Agrawal, Gopal Prasad; Maheshwari, R. K.; Mishra, Pradeep

doi:10.1590/s2175-97902020000118553

Cited by 6 publications

(5 citation statements)

References 8 publications

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“…28 The increased wetting of ATV and good dispersibility in the presence of hydrotropic agents and better contact between the drug and the carrier, in addition to the change of one crystalline form to another, might be responsible for the better dissolving rate of ATV from hydrotropic solid dispersion. 43 Both formulations FTHS1 and FQHS1 required 30 minutes to attain their peak levels of drug release, which may have been linked with 95.34% and 82.31% of drug release, respectively. This might be due to the efficacy of the process utilized for the formulation of both solid dispersions since solvent evaporation resulted in homogeneous molecular dispersions of the medication in the hydrophilic carrier matrix.…”

Section: Discussionmentioning

confidence: 99%

The development of ternary and quaternary solid dispersion based hydrotropic blends of atorvastatin calcium

Ramadhan,

Omer

2024

Zanco J Med Sci

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Background and objective: Atorvastatin calcium (ATV) has a solubility in aqueous solutions of greater than 0.1 mg/ml to less than 1 mg/ml, which is very slightly soluble. When developing dosage forms for these medications, formulation scientists still face challenges. This study's goal was to use various hydrotropic agents in the formation of solid dispersion-based hydrotropic blends to improve the solubility properties of atorvastatin calcium. Methods: In this study, twenty-two distinct binary, ternary, and quaternary formulations of ATV were prepared by employing five different hydrotropic agents and combining at least two hydrotropic agents in concentrations of 10% and 20% (w/v). Moreover, solid dispersion by the solvent evaporation method and physical mixture-based hydrotropic blends in the ratio of (1:2) have been formulated. The produced formulations were characterized using an FTIR analysis. Results: According to the findings, binary formulations containing 20% (w/v) concentrations of sodium benzoate (SB), sodium salicylate (SS), and resorcinol (R) enhanced the solubility ratio of ATV by 439.31, 689.57, and 106.21 folds, respectively. Furthermore, ternary formulations (FT14) and quaternary formulations (FQ18) resulted in the enhancement of ATV solubility by 938.45 and 995.12 folds, respectively. Ternary solid dispersion demonstrated the highest enhancement in solubility ratio by 87.68 folds and resulted in a higher dissolution rate of ATV than pure samples of the drug. Finally, FTIR analyses excluded any interactions between medications and excipients by showing no noticeable shift in the peaks. Conclusion: Solid dispersion based hydrotropic blends can provide the production of the dosage forms of practically insoluble drugs with a favorable enhancement ratio in solubility.

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Section: Discussionmentioning

confidence: 99%

The development of ternary and quaternary solid dispersion based hydrotropic blends of atorvastatin calcium

Ramadhan,

Omer

2024

Zanco J Med Sci

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“…A portion of the sample was diluted with distilled water and examined at 242 nm using a UV-visibledouble-beam spectrophotometer against the respective solvent as a blank. The equilibrium solubility study was conducted in triplicate [ 14 , 15 ]. The following formula was used for the calculation of solubility enhancement ratios:

…”

Section: Methodsmentioning

confidence: 99%

“…Drug: hydrotropic agents' ratio of 1 : 4 was used. The components are combined in a glass mortar and pestle for 10 minutes to ensure homogeneity, then passed through a sieve of 250 μ m, and kept in a desiccator away from light and humidity until further examination [ 15 ].…”

Section: Methodsmentioning

confidence: 99%

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

Ali

Omer

2022

Advances in Pharmacological and Pharmaceutical Sciences

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Purpose. The biopharmaceutics classification system places rosuvastatin calcium in class II has a low and fluctuating oral bioavailability. The research focus is to maximize rosuvastatin calcium solubility in water and dissolution rate by employing and combining various hydrotropic agents to make a solid dispersion using solvent evaporation techniques. Methodology. The experimental study was conducted at Duhok University, College of Pharmacy. Initially, assess rosuvastatin’s solubility in hydrotropic agents including urea, mannitol, citric acid, sodium benzoate, and sodium salicylate at concentrations of 10, 20, 30, and 40% w/v. Then, various ratios of 2 and 3 hydrotropic agents were employed to reduce the concentration of each hydrotropic agent. By using a solvent evaporation procedure, solid dispersions were made. The solid dispersion powders underwent evaluation for their percentage drug content, percentage yield, solubility, dissolution test, XRD, DSC, SEM, and FTIR. For statistical analysis, GraphPad InStat Demo software was used to conduct a two-way analysis of variance (ANOVA). Results. In comparison to the pure drug, the solubility of hydrotropic solid dispersions and physical mixtures of rosuvastatin with a combination of hydrotropic agents (sodium salicylate, sodium benzoate, and urea) in the ratio of 13.33 for each increased in all formulations significantly, and all manufactured formulations’ drug release ranged from 98.83 to 104.78%, indicating a noticeably higher dissolution rate. Conclusion. The concept of mixed hydrotropic solid dispersion was shown to be an original, risk-free, and cost-effective method for enhancing the bioavailability of drugs that have a low degree of solubility in water.

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“…The aliquots after suitable dilution with water were analyzed under UV spectrophotometer at 228 nm. [20]…”

Section: Single Hydrotropymentioning

confidence: 99%

Untitled

2024

AJP

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Objectives: Drugs given by oral route will undergo dissolution followed by permeation then it reaches to blood. Low water solubility is the foremost issue that comes upon with the development of dosage forms for newly discovered drugs as well as old drugs. Telmisartan is a class II category drug under the biopharmaceutical classification system, which limits its bioavailability to about 40%. Hydrotropy method has several advantages compared to other methods such as cost-effectiveness, ease of process, compatibility, scalable, and flexibility to varieties of dosage forms. Henceforth, an attempt has been made to improve the solubility of telmisartan using the hydrotropy method. Materials and Methods: Three different hydrotropic agents (urea, mannitol, and lactose) in different concentrations (10-50%) were used to find the solubility of the drug. The design of an expert statistical tool was utilized to optimize the best concentration of hydrotropic agent for having maximum solubility of the drug. Results: In a 40% urea blend, the solubility was obtained approximately 25.87 times more than pure drug (0.003 mg/mL) which showed the potential of the hydrotropic agent. This obtained optimized batch was further characterized for drug release profile and other related parameters. The optimized concentration of urea showed 87.46 ± 0.17% of drug release in 8 h which is relatively higher than the plain drug release. Conclusion: Therefore, it can be concluded that the 40% concentration of urea as a hydrotropic agent showed to be a key factor for enhancement of solubility followed by dissolution of poorly soluble telmisartan drug.

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Solubility enhancementofcefixime trihydrate by solid dispersions using hydrotropic solubilization technique and their characterization

Cited by 6 publications

References 8 publications

The development of ternary and quaternary solid dispersion based hydrotropic blends of atorvastatin calcium

The development of ternary and quaternary solid dispersion based hydrotropic blends of atorvastatin calcium

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

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