Development and Characterization of Self- Microemulsifying Drug Delivery System for Improvement of Bioavailability of Cefdinir

Chhayani, Rahul L.; Chhayani, Ravi B.; Patel, Dhaval; Borkhataria, Chetan

doi:10.21088/jpmc.2395.6615.2116.7

Cited by 2 publications

(3 citation statements)

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“…Dissolution studies were carried out using the USP paddle method at (37± 0.2)°C in a Pharma test PT-DT7 dissolution tester (Germany) at 50 rpm with 900 mL of HCl buffer (pH 1.2), acetate buffer (pH 4.5), and phosphate buffer (pH 6.8) fluids as dissolution media [15]. The pH M -SDs (equivalent to 300 mg of cefdinir) and pure drug were dispersed in the dissolution media, and at predefined intervals, 5-ml samples were withdrawn at (2,5,10,15,20,30,45, and 60) minutes, filtered through 0.45 µm syringe filter, and assayed via UV-VIS spectrophotometer (T80 PG, United Kingdom) for released drug at λ max (280, 286, and 287 nm) for HCl buffer pH=1.2, acetate buffer pH=4.5, and phosphate buffer pH=6.8, respectively. An equivalent amount of release medium was supplemented to keep the volume constant.…”

Section: Drug Release Studiesmentioning

confidence: 99%

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pH- Modified Solid Dispersions of Cefdinir for Dissolution Rate Enhancement: Formulation and Characterization

Nuss¹,

El-Zein²

2021

J. Pharm. Nutr. Sci.

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Objective: Cefdinir is a poorly- water-soluble drug, it belongs to Biopharmaceutical Classification System class IV, which shows that it may have limited therapeutic effects due to its low solubility and poor bioavailability. The aim of the present work was to design a pH-modified solid dispersion (pHM-SD) that can improve the dissolution rate of cefdinir and subsequently its bioavailability. Materials and Methods: pHM-SDs of cefdinir were prepared at different drug-to-carrier ratios by the spray-drying technique. The solid dispersions were investigated by dissolution studies at different pH media, drug release kinetics were studied, and their solid-state characterizations were performed by FTIR spectrophotometer, Scanning electron microscopy (SEM), Differential scanning calorimetry (DSC), and Powder X-ray diffraction (PXRD). Results: PVP- based and HPMC- based pHM-SDs exhibited a marked improvement in the dissolution behavior when compared with crystalline cefdinir powder, whereas Eudragit L100-based pHM-SDs showed lower dissolution at pH 1.2 and 4.5. FTIR results may indicate a formation of a salt between cefdinir and the alkalizer. Solid-state characterization may indicate a change in crystallinity of cefdinir into an amorphous state. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsmeyer–Peppas model and the drug release kinetics primarily as Fickian diffusion. Conclusion: According to these observations, pHM-SD in the presence of an alkalizer for a poorly water-soluble acidic drug, cefdinir, appeared to be efficacious for enhancing its dissolution rate.

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Section: Drug Release Studiesmentioning

confidence: 99%

“…Several approaches have been investigated to improve the dissolution rate and bioavailability of Cefdinir, including nanosuspensions [6,7], amorphization [8], cyclodextrin complexation [4,9], self-emulsification [10], and solid dispersions (SDs) [11][12][13][14][15][16].…”

Section: Introductionmentioning

confidence: 99%

pH- Modified Solid Dispersions of Cefdinir for Dissolution Rate Enhancement: Formulation and Characterization

Nuss¹,

El-Zein²

2021

J. Pharm. Nutr. Sci.

View full text Add to dashboard Cite

show abstract

“…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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Development and Characterization of Self- Microemulsifying Drug Delivery System for Improvement of Bioavailability of Cefdinir

Cited by 2 publications

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pH- Modified Solid Dispersions of Cefdinir for Dissolution Rate Enhancement: Formulation and Characterization

pH- Modified Solid Dispersions of Cefdinir for Dissolution Rate Enhancement: Formulation and Characterization

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

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