Solubility enhancement of some poorly soluble drugs by solid dispersion using Ziziphus spina-christi gum polymer

Alwossabi, Ameen M.; Elamin, Eltayeb S.; Ahmed, Elhadi M.; Abdelrahman, Mohammed

doi:10.1016/j.jsps.2022.04.002

Cited by 16 publications

(9 citation statements)

References 32 publications

(29 reference statements)

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“…[ 7 , 8 ]. Solid dispersion is the low cost and widely employed technique for improving the solubility of poorly aqueous soluble drugs [ 9 , 10 ]. The main advantages of solid dispersion include increased solubility and dissolution profile, reduction in particle size, improved porosity and wettability, and changing crystalline drugs to amorphous states.…”

Section: Introductionmentioning

confidence: 99%

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

et al. 2022

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The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, % yield, and entrapment efficiency), four formulations were selected for further detailed studies. Solid-state characterization of optimized formulations (S1, S6, S7, and S12) showed successful drug incorporation in the solid dispersion at the molecular state without any noticeable interactions. The in vitro solubility and release study showed an increase in solubility and 98–100% of drug release in 30–45 min. The in vivo gastro-protective effect of the optimized formulations containing flurbiprofen and silica (1:1) with 25% w/w gelucire (S6 and S12) showed a reduction in the gastric lesion index (GLI) after four days of treatment. Moreover, histological images of the stomach lining (S6 and S12) illustrated normal epithelial cells and a partially protected mucosal membrane. Thus, TSD exhibited a significant increase in solubility and the dissolution rate and reduced the gastric ulceration. Therefore, TSDs are dubbed as efficacious carriers to enhance the bioavailability of flurbiprofen while simultaneously reducing its side effects.

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Section: Introductionmentioning

confidence: 99%

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

et al. 2022

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“…Because of this, many different strategies were proposed to address this limitation. This includes amorphization [ 28 , 29 ], formation of monocrystals [ 30 , 31 ], micronization [ 32 ] and solid dispersion formation [ 33 ], complexation with cyclodextrins [ 34 , 35 ], salts [ 36 , 37 ] and cocrystals [ 38 , 39 ] formation. Another way of improving solubility involves cosolvation techniques in which a particular amount of a solvent is added to the primary solvent [ 40 , 41 , 42 ] resulting in elevated solubility.…”

Section: Introductionmentioning

confidence: 99%

Quantification of Caffeine Interactions in Choline Chloride Natural Deep Eutectic Solvents: Solubility Measurements and COSMO-RS-DARE Interpretation

Jeliński¹,

Cysewski²

2022

IJMS

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Solubility of active pharmaceutical ingredients is an important aspect of drug processing and formulation. Although caffeine was a subject of many studies aiming to quantify saturated solutions, many applied solvents suffer from not being environmentally friendly. This work fills this gap by presenting the results of solubility measurements in choline chloride natural deep eutectic solvents, ccNADES, comprising one of seven of the following polyalcohols: glycerol, sorbitol, xylitol, glucose, sucrose, maltose and fructose. The ratio of ccNADES components was optimized for maximizing caffeine solubility at room temperature. Additionally, temperature dependent solubility was measured for the first four systems exhibiting the highest solubility potential, both in their neat forms and in mixtures with water. Results were used for intermolecular interactions assessments using the COSMO-RS-DARE approach, which led to a perfect match between experimental and computed solubility values. An important methodological discussion was provided for an appropriate definition of the systems. Surprising linear trends were observed between the values of fitting parameters and water-ccNADES composition. In addition, comments on selection of the values of the fusion thermodynamic parameters were provided, which led to the conclusion that COSMO-RS-DARE solubility computations can effectively compensate for the inaccuracies of these important physicochemical properties.

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“…Preparation of SD using CMTG as a carrier VRZ loaded SD using CMTG was prepared by using kneading method at different drug: polymer ratio. [14] First, the required amount of VRZ was melted in an applicable quantity of methanol. Then, the necessary amount of CMTG (another substance) was added to this solution while continuously stirring it in a mortar for duration of 30 minutes.…”

Section: X-ray Diffraction Studymentioning

confidence: 99%

“…The yield was calculated using below formula. [14] % Yield = SD Wt/Wt of drug and polymer X 100 ------- (1) Drug content SD eq to 10 mg of VRZ was dissolved in a 100 mL methanol (25 mL). The resulting solution was then stirred in a centrifuge for duration of 60 minutes to ensure thorough mixing and dissolution.…”

Section: Percentage Yieldmentioning

confidence: 99%

Formulation and Development of Voriconazole Tablets Containing Solid Dispersion With Enhanced Solubility, Dissolution and Bioavailability

Velhal,

Salunkhe

2024

Int. J. Pharm. Sci. Drug Res.

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This research work enhances the solubility, dissolution and bioavailability of Voriconazole which belongs to BCS II class. Carboxymethyl tamarind gum was synthesized by using carboxymethylation of tamarind gum. Solid dispersion of Voriconazole was developed by kneading method followed by immediate release tablets. Solid dispersion characterised for solubility and instrumental analysis. Tablets were evaluated for dissolution study. Solid dispersions were confirmed by presence of distinctive peaks at 1745.58 cm-1 (C=O) and 1402 cm-1 (-COO-), using Infrared spectroscopy. The weight loss of 3.91% and 54.42 % at 100°C and in the rage of 235°C-425°C respectively was observed. 13C nuclear magnetic resonance spectrum of carboxymethyl tamarind gum displayed three distinct peaks of C1, -OH, and CH2O- group. X-ray diffraction analysis confirmed that ccarboxymethyl tamarind gum exhibits an amorphous structure. Soild dispersion of Voriconazole were developed using the kneading method, incorporating carboxymethyl tamarind gum. Compared to traditional methods, Solid dispersion formulated with carboxymethyl tamarind gum demonstrated a significant increase in solubility enhancement, ranging from 68.12 to 74.37-fold. Notably, the SD5 formulation exhibited complete release from the solid dispersion within 120 minutes. In rat models, Voriconazole levels in the bloodstream were markedly elevated with the administration of solid dispersion. Furthermore, dissolution profiles of all formulation batches showed considerable improvement. These findings shed light on effective strategies for enhancing the dissolution and bioavailability of poorly soluble drugs, thus contributing to the advancement of drug delivery systems.

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Solubility enhancement of some poorly soluble drugs by solid dispersion using Ziziphus spina-christi gum polymer

Cited by 16 publications

References 32 publications

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

Quantification of Caffeine Interactions in Choline Chloride Natural Deep Eutectic Solvents: Solubility Measurements and COSMO-RS-DARE Interpretation

Formulation and Development of Voriconazole Tablets Containing Solid Dispersion With Enhanced Solubility, Dissolution and Bioavailability

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