Efficacy of Combination Solid Dispersion Technology on Dissolution Performance of Nalidixic Acid and Cefdinir

Maraie, Nidhal K.; Alhamdany, Anas Tarik; Radhi, Ameera A

doi:10.22159/ajpcr.2017.v10i4.16913

Cited by 5 publications

(7 citation statements)

References 7 publications

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“…Dialysis bags (MWCO: 14 KDa) filled with samples were placed in to dissolution apparatus (100 rpm) containing phosphate buffer (300 ml, pH 7.4,) which was maintained at 37±2 °C [27]. Samples were taken at regular time intervals (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12) hrs) with replacement of dissolution medium for volume make up. Spectrophotometric analysis ( max 287 nm) of samples was conducted to evaluate percent drug release [28].…”

Section: In-vitro Dissolution Studymentioning

confidence: 99%

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Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

Kamran¹,

Khan²,

Rehman³

et al. 2019

Preprint

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Current study focused on resolution of poor oral bioavailability issues of cefixime through fabrication of its freeze dried binary solid lipid nano particles (SLNs). The nano formulation fabricated via hot melt encapsulation (HME) method was optimized using numerous formulation variables. Optimized nano formulation (CFX-4) showed particle size 206.6±2.3 nm, polydispersity index (PDI) 0.271±0.03, zeta potential (ZP) -30.7±3.1 mV, encapsulation efficiency (EE%) 88.2±2.3% along with drug loading capacity (DLC%) 4.83±0.16%. Micrograph of scanning electron microscopy (SEM) represented spherical shaped particles. Reduction in drug’s crystalline nature was acknowledged through differential scanning calorimetry (DSC) and x-ray powder diffraction (P-XRD) analysis. Drug-excepient compatibility was established through fourier transform infrared spectroscopic (FT-IR) analysis. During in-vitro studies; sustained drug release was favored by increased drug payload. Stability studies exposed that refrigerated temperature imparts maximum stability to binary SLNs. In-vivo pharmacokinetic studies revealed the desired enhancement in oral bioavailability compared to the marketed product (Cefiget®). Presented investigations established the dominance of binary SLNs for improvement of oral bioavailability with sustained drug release characteristics. Based on the reported outcomes, binary SLNs can be employed as an advanced drug delivery system for other hydrophobic drugs.

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Section: In-vitro Dissolution Studymentioning

confidence: 99%

“…Poor oral bioavailability of hydrophobic active pharmaceutical ingredients (APIs) is the foremost confront in drug deliverance [1,2]. Poor dissolution rate limited bioavailability of different drugs is a stumbling block in their commercialization.…”

Section: Introductionmentioning

confidence: 99%

Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

Kamran¹,

Khan²,

Rehman³

et al. 2019

Preprint

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“…In addition, as shown in table 2, the presence of poloxamer 188 could significantly improve the α-mangostin water solubility up to 727 times higher than MPE. This could be attributed to its high HLB value of 22 and surfactant property of poloxamer [13,14].…”

Section: Solubility Studymentioning

confidence: 99%

Development, Characterization and Skin Irritation of Mangosteen Peel Extract Solid Dispersion Containing Clay Facial Mask

et al. 2018

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Objective: To develop a clay facial mask containing mangosteen peel extract solid dispersion (MPESD) for enhancing α-mangostin bioavailability and to determine suitable clay-based facial mask.Methods: The MPESD were prepared by a melting-solvent method employing PVP K30 and poloxamer 188 as a carrier. The water solubility was determined by HPLC method. The in vitro skin permeability was examined using porcine ear epidermis. The effects of clay types on the physical stability of MPESD and α-mangostin adsorption capacity were evaluated. The skin irritation was determined by 4 h human patch test.Results: After dissolved optimal formulation of MPESD in water, the spherical micelle was observed with a mean size of ~150 nm and showed significantly α-mangostin water solubility enhancement of ~7 mg/ml, 700 times greater than MPE. Upon mixing the MPESD with clays, a dry powder was obtained. In vitro permeation studies of the MPESD mixed with titanium dioxide showed lowest α-mangostin permeation, while MPESD mixed with mica or talcum showed similar permeation profile as free MPESD solutions. No sign of skin irritation was observed in volunteers after application of the MPESD-based clay facial mask patch on the inner forearm skin for 4 h.Conclusion: MPESD demonstrates a promising technique for improving water solubility and permeation of α-mangostin which reducing the staining effect. In addition, it is safe for topical application and cosmetically acceptable.

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“…Several approaches have been investigated to improve the dissolution rate and bioavailability of Cefdinir, including nanosuspensions [8,9], amorphization [10], cyclodextrin complexation [7,11], self-emulsification [12], and solid dispersions (SDs) [13][14][15][16][17].…”

Section: Introductionmentioning

confidence: 99%

Cefdinir Inclusion in Mesoporous Silica as Effective Dissolution Enhancer with Improved Physical Stability

Nuss

Zein

2021

J. Pharm. Nutr. Sci.

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Objective: The objective of this research was to enhance the physical stability and the dissolution rate of cefdinir, a BCS class IV drug, characterized by low and variable bioavailability due to both its low solubility and low permeability. Methods: Cefdinir was loaded into the mesoporous silica (SBA-15), by using the solvent immersion method starting from different organic solvents. And then formula (F3), which exhibited the highest loading percentage, was selected to study its drug release in media with different pH (1.2, 4.5, and 6.8), and has been fully characterized by using: Fourier Transform Infrared Spectroscopy (FT-IR) Spectroscopy, Differential Scanning Calorimetry, Powder X-ray Diffraction, and has been subjected to accelerated stability tests using different temperatures and relative humidity. Drug release kinetics were studied by using the following models: Probit, Gompertz, Weibull, and Logistic. Results: The results showed a remarkable dissolution improvement of cefdinir from the loaded silica in comparison to the crystalline drug at the different studied media. Drug release behaviors were well simulated by the Weibull model for F3 in all studied media and for pure Cefdinir in phosphate buffer only, and by the Gompertz function for pure Cefdinir in HCl buffer and Acetate buffer. FTIR results showed hydrogen bonds formed between the drug and silica, DSC and PXRD results revealed the transformation of cefdinir into an amorphous form upon adsorption. Stability studies under different conditions revealed the ability of mesoporous silica to maintain the amorphous state of the drug, which has been formed upon adsorption, and to prevent re-organization in the crystal nucleus of the drug molecules. Conclusion: Thus, loading cefdinir onto mesoporous silica can be used as a promising method to enhance drug dissolution, and maintain the physical stability of its amorphous form.

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Efficacy of Combination Solid Dispersion Technology on Dissolution Performance of Nalidixic Acid and Cefdinir

Cited by 5 publications

References 7 publications

Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

Development, Characterization and Skin Irritation of Mangosteen Peel Extract Solid Dispersion Containing Clay Facial Mask

Cefdinir Inclusion in Mesoporous Silica as Effective Dissolution Enhancer with Improved Physical Stability

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