Hydrotropy, mixed hydrotropy, and mixed solvency as trending concept for solubilization of lipophilic drugs

Padiyar, Anirudh; Agrawal, Om P.; Rajpoot, Kuldeep; Tekade, Rakesh K.

doi:10.1016/b978-0-12-814455-8.00005-0

Cited by 5 publications

(3 citation statements)

References 52 publications

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“…The mixed hydrotropic approach has a remarkable synergistic impact on the solubility of medications that are weakly water-soluble [ 5 ]. It lowers the concentration of each hydrotropic substance to reduce negative effects [ 25 ]. Salicylate is a very interesting ingredient because it can be used in small amounts as a preservative in cosmetics, drugs, and even food.…”

Section: Resultsmentioning

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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Section: Resultsmentioning

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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“…Many drugs that are poorly water-soluble have had their aqueous solubility improved by mixed hydrotropic solubilization. [4][5][6][7][8][9][10][11] Benefits of mixed hydrotropy…”

Section: Mixed Hydrotropymentioning

confidence: 99%

Untitled

2022

AJP

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Background:The primary goal of this research is to investigate the concept of mixed solvency in terms of developing a large number of safe solvent systems for aqueous intramuscular injections that include water-soluble additives. As a result, pharmaceutical industries can use these solvent systems to provide intramuscular injections of drugs that are poorly water-soluble. Safe solubilizers' solubilizing properties can be utilised to improve the solubility of poorly water-soluble drugs. Objective: The main purpose of this research is to provide pharmaceutical manufacturers with novel approaches for aqueous IM injections. Materials and Methods: In the present study, we employed sodium benzoate, sodium acetate, sodium citrate, valine, l-lysine, arginine, ethanol, Tween 80 and benzoic acid as solubilizers and ornidazole, paracetamol, aspirin, salicylic acid, gatifloxacin, naproxen, meloxicam, furosemide, piroxicam, acyclovir, fenofibrate, indomethacin, norfloxacin, and nimesulide. Furosemide was selected as the drug for the formulation of a typical aqueous IM injectable solution. For the drug identification, melting ranges were determined all the drugs using melting point apparatus (Analab Scientific). UV identification was also done for all drugs using UV-visible spectrophotometer (Shimadzu 1700). The pH of blend was estimated using pH meter (Cyber Scan). Drug and excipient interference studies were performed before formulation using UV-visible spectrophotometer. Drug and excipient interference studies also done before the formulation. The composition of formulation is L-lysine (3% w/v), sodium acetate (10% w/v), arginine (10% w/v), and Tween 80 (5% w/v). Results: By the solubility studies in different blends, the possibility of some IM injection solution can prepare such as furosemide (20 mg/2 ml), piroxicam (20 mg/2 ml), repaglinide (16 mg/3 ml), indomethacin (25 mg/ml), and acyclovir (20 mg/3 ml) can be produced. Furosemide: Chemical, physical, and freeze thaw studies were performed for the stability study of formulation. The formulation gives satisfactory results during physical and chemical stability studies. The pH of formulation was also performed and it was found similar to the pH of blend (pH-7). Conclusion: From this research work, it is clear that mixed solvency concept can be employed to develop a large numbers of expectedly safe aqueous IM injection solution type aqueous solvent systems for poorly water-soluble drugs. Thus, solubilizing power of safe additives can be employed to make marketable aqueous IM injections.

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“…The physiologically active natural polyphenol curcumin [1, 7-bis (4-hydroxy-3-methoxyphenyl)-1, 6-heptadiene-3, 5-Dione], also known as diferuloylmethane, is obtained from the rhizome of C. longa (Zingiberaceae family). [7] Mixed solvency concept [8][9][10][11] Any weak solvent (for a specific solute) can be made strong by choosing the right solubilizing agent. For instance, oil-soluble excipients such as polyvinylpyrrolidone (PVP), vanillin, butylated hydroxyanisole, butylated hydroxytoluene, propyl gallate, benzoic acid, methylparaben, and propylparaben, when used in the right concentrations, can improve the oil solubility.…”

Section: Medicinal Plantsmentioning

confidence: 99%

Untitled

2022

AJP

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Background: Since the beginning of time, humankind has employed herbal and medicinal plants as a source of food and medicine. Plant bioactive chemicals are currently of great research interest. However, extracting them as part of phytochemical and/or biological studies brings unique problems. Many techniques for the extraction of bioactive components have been devised by herbalists or scientists to indemnify the effectiveness and efficacy of the raw medications used to treat illness. The mode of extraction of active phytochemicals is receiving a lot of attention to reduce the costs associated with synthesis and separation. As a result, the extraction of active compounds from plants requires a proper procedure for extraction and techniques that provide extracts and fractions high in bioactive components, and also the solvents used in extraction do not harm humans as well as nature. As a result, they have a significant impact on yield, the nature of phytochemical content, and so on. Objectives: The purpose of this paper is to discuss and describe that solvents for extraction which shall be ecofriendly, safe, and also can be recovered easily by evaporation and preparation of the formulation using blends derived by idea of mixed solvency concept. Materials and Methods: Before extraction and formulation purity, tests were done on turmeric powder. Then, extraction was done using solvents prepared using mixed solvency such as camphor in ethanol (25% w/v and 50% w/v) and thymol in ethanol (25% w/v and 50% w/v). In addition, identification tests were done on the obtained extract. The comparative study was done on extraction yields, to establish a comparison between the yield obtained using conventional solvent and solvents prepared using the mixed solvency concept. In addition to that, a topical formulation was also prepared for the obtained extract. For formulation development solubility, studies of turmeric extract were done in various oils, ethanol, and blends (constituted in ethyl oleate with the combination of additives such as methyl paraben, propyl paraben, glyceryl monostearate, benzyl benzoate, and benzoic acid). The formulation so formed was a 0.9% curcumin oily solution and the evaluation tests such as viscosity, drug excipients interaction studies, and in vitro release studies were also done for the same. Results: In the extraction, it was discovered that adding camphor and thymol to ethanol improves the yield of turmeric extract, as compared to ethanol. Solubility studies were done for the preparation of topical solution and topical emulgel. The maximum solubility of turmeric extract was perceived in an oily blend which was formed by the purport of the mixed solvency concept). As a result, the oil base chosen for the formulation was an oily blend rather than a single oil or ethanol. In which the formulation produced positive outcomes. Evaluation studies such as freeze thaw, in vitro drug release, and antibacterial activity were performed for the formulation and it showed virtuous results.

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Hydrotropy, mixed hydrotropy, and mixed solvency as trending concept for solubilization of lipophilic drugs

Cited by 5 publications

References 52 publications

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

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

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