Development of a Discriminative Intrinsic Dissolution Method for Efavirenz

Pinto, Enrico; Cabral, Lúcio Mendes; Sousa, Valéria Pereira de

doi:10.14227/dt210214p31

Cited by 19 publications

(9 citation statements)

References 42 publications

(58 reference statements)

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“…The concentration of EFZ was determined at 248 nm using an ultraviolet (UV)-visible spectrophotometer (V-730; JASCO, New Delhi, India). 26…”

Section: Determination Of Efz Solubility In Various Mediamentioning

confidence: 99%

“…25 It has a pKa value of 10.2 and log p-value of 5.4 and with an intrinsic dissolution rate of 0.037 mg/cm 2 /min, which limits dissolution of its dosage forms. 26 Attempts have been made to improve the solubility of EFZ using high-energy grinding and preparing polymeric micelles approaches. 25,[27][28][29] The objective of this work is to explore the potential of mixed polymeric micelles in solubility enhancement of BCS class II drug.…”

Section: Introductionmentioning

confidence: 99%

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Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and In Vitro Characterization

Madan

Dere

Awasthi

et al. 2021

ASSAY and Drug Development Technologies

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Efavirenz (EFZ) is a biopharmaceutics classification system (BCS) Class-II, first-line antiretroviral (ARV) drug. However, its utility through the oral route is restricted by its poor solubility. The objective of this study was to formulate EFZ-loaded binary-mixed micelles as a potential carrier for oral administration of EFZ. Rubingh's regular solution theory was used to determine the interaction behavior of the two components (Cremophor RH 40 and Phospholipon 80H) and of the mixed micelles and synergistic behavior was confirmed. The mixed miceller system was formulated using solvent evaporation method and a 3 2 factorial design was used for the optimization of selected independent variables. Miceller systems were further characterized in terms of morphology, particle size, zeta potential, percent entrapment efficiency, and drug loading. Fourier transform infrared and differential scanning calorimetry measurements confirmed the entrapment of EFZ in the micelles. The optimized formulation presented desirable qualities viz., nanometric size (17.27 -0.079), high entrapment efficiency, and good colloidal stability. The prepared optimized micelles can be potential carriers for EFZ in ARV therapies.

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“…The concentration of EFZ was determined at 248 nm using an ultraviolet (UV)-visible spectrophotometer (V-730; JASCO, New Delhi, India). 26…”

Section: Determination Of Efz Solubility In Various Mediamentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and In Vitro Characterization

Madan

Dere

Awasthi

et al. 2021

ASSAY and Drug Development Technologies

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“…EFV belongs to class II of Biopharmaceutical Classification System (BCS); that is, it is poorly water-soluble and highly permeable [1]. Several approaches to improve efavirenz dissolution are reported, namely the manipulation of polymorphs [1], the use of superdisintegrants [2], solid dispersions [3,4], nano-sized polymeric micelles [5] and complexation with two chemically modified β-cyclodextrins, RAMEB and HPβCD [6].…”

Section: Introductionmentioning

confidence: 99%

Cyclodextrin-Efavirenz Complexes Investigated by Solid State and Solubility Studies

Braga

Lysenko

El-Saleh

et al. 2020

The 1st International Electronic Conference on Pharmaceutics

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This short paper investigates the solubilizing ability of various cyclodextrins with efavirenz as well as the formation of solid inclusion complexes of efavirenz with β-CD and γ-CD. (1) Background: Efavirenz is a non-nucleoside reverse transcriptase inhibitor used as first-line treatment for adult and pediatric human immunodeficiency virus type 1 infection (HIV-1). Belonging to class II of Biopharmaceutical Classification System (BCS), efavirenz is poorly water-soluble. Inclusion into cyclodextrins is a possible strategy for increasing its solubility. (2) Methods: Solubility modulation was investigated by the phase solubility method; inclusion of efavirenz with β- and γ-cyclodextrins was attempted by co-dissolution with co-precipitation; the precipitates were studied by DSC, FT-IR, powder X-ray diffraction and optical microscopy. (3) Results: Solid state analysis of the precipitates shows evidence of separate recrystallization of β-cyclodextrin and efavirenz, whereas in the case of γ-cyclodextrin, a single new phase was observed. (4) Conclusion: Results show that the cavity of β-cyclodextrin is too narrow to accommodate efavirenz and only γ-cyclodextrin, the largest of native cyclodextrins, is able to form a true inclusion complex with this bulky guest.

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“…10,11) During the development of a dissolution method, the in vitro parameters such as the presence of surfactants, pH, ionic strength and media volume should be evaluated. [12][13][14] The selection of dissolution apparatus also plays a key role for the establishment of discriminatory dissolution methodologies. 15,16) The United States Pharmacopeia (USP) Apparatus 3 (Reciprocating cylinder or BioDis) was specifically designed for dissolution evaluation of MR dosage forms because it can mimic physicochemical and mechanical changes experienced by a MR dosage form in the GIT.…”

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confidence: 99%

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

Bezerra

Pinto

Cabral

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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Gliclazide (GLZ) is a second generation hypoglycemic drug used for the treatment of Type 2 diabetes mellitus. The low solubility of GLZ has been described as the rate limiting step for drug dissolution and absorption, thus a prediction of its in vivo behavior based on a discriminative dissolution test should lead to a relevant in vitro-in vivo correlation (IVIVC). The aim of this study was to develop a dissolution method for GLZ modified-release (MR) tablets using an United States Pharmacopeia (USP) apparatus 3 through its evaluation by an IVIVC analysis. Various dissolution parameters were evaluated to establish an in vitro method for GLZ tablets. The final dissolution conditions, referred to as method 3, utilized a 400 µm mesh and 30 dips per minute over a total period of 10 h that included 1h in HCl media (pH 1.2), 2h in acetate buffer solution (pH 4.5), 1 h in phosphate buffer solution (PBS; pH 5.8), 5h in PBS (pH 6.8) and finally 1h in PBS (pH 7.2). The calculated point-to-point IVIVC (R 2 0.9970) was significantly greater than other methods. The robustness of method 3 suggests it could be applied to pharmaceutical equivalence studies and for quality control analyses of GLZ.

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Development of a Discriminative Intrinsic Dissolution Method for Efavirenz

Cited by 19 publications

References 42 publications

Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and In Vitro Characterization

Efavirenz Loaded Mixed Polymeric Micelles: Formulation, Optimization, and In Vitro Characterization

Cyclodextrin-Efavirenz Complexes Investigated by Solid State and Solubility Studies

Development of a Dissolution Method for Gliclazide Modified-Release Tablets Using USP Apparatus 3 with <i>in Vitro–in Vivo</i> Correlation

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