Preparation and characterizations of stable amorphous solid solution of azithromycin by hot melt extrusion

Jaiswar, Divakar R.; Jha, Durgesh K.; Amin, Purnima D.

doi:10.1007/s40005-016-0248-x

Cited by 23 publications

(19 citation statements)

References 30 publications

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“…Despite its wide therapeutic potential, NRG's clinical role has been hindered due to its its low solubility, hence poor bioavailability and a considerable pre-systemic metabolism. A promising approach to overcome this, is the preparation of Solid Dispersion (SD) to increase the aqueous solubility and dissolution rate and further, to enhance oral bioavailability [21,22]. In this work, solid dispersions of NRG with Poloxamer 188 and Gelucire® 48/16 were prepared by the simple melt fusion method.…”

Section: Introductionmentioning

confidence: 99%

Correlation of two validated methods for the quantification of naringenin in its solid dispersion: HPLC and UV spectrophotometric methods

et al. 2020

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A UV spectrophotometric and RP-HPLC method for the Naringenin quantification in the developed solid dispersions is described. Both the methods were validated according to ICH Q2 R (1) guidelines for linearity, accuracy, precision, limit of detection, limit of quantification, specificity and robustness. HPLC was run in isocratic mode on a reversed-phase C18 column (250 × 4.6 mm internal diameter and particle size of 5 μm) with methanol:water (70:30, v/v) as the mobile phase maintaining a flow rate of 1.0 ml/min. Naringenin showed an absorbance maximum (λ max) at 288 nm which was used for the UV spectrophotometric determinations. The calibration curve of Naringenin showed linearity in the required concentration range (R 2 > 0.999) by both the UV and HPLC methods. Both the methods were found to be precise and accurate with recovery range of 98-101% and relative standard deviation < 2%. Most importantly, the accuracy and precision achieved by the HPLC method, correlated closely with the UV method. Current study also involves detection and quantification of Naringenin released from its formulations by both the developed methods. This paper demonstrates the high correlation (R 2 ≥ 0.98) between the UV and HPLC methods when determining the release of Naringenin from various formulations. With this established correlation, we hereby suggest that, for routine analysis, UV spectroscopy can be an economic, simple, reliable and less time-consuming alternative for expensive and time-consuming chromatographic analysis.

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Section: Introductionmentioning

confidence: 99%

Correlation of two validated methods for the quantification of naringenin in its solid dispersion: HPLC and UV spectrophotometric methods

et al. 2020

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“…Materials can be thrown into the extruder, moved towards the die and homogeneously blended by rotating screws, and extruded from the die (or an orifice) [8][9][10][11]. During the HME process, the temperature of barrels is designed above the glass transition temperature (T g ) and sometimes over the melting temperature (T m ) of polymeric substances, and the drug can be molecularly dispersed in the polymer matrix [9,12,13].…”

Section: Introductionmentioning

confidence: 99%

Fabrication and Characterizations of Hot-Melt Extruded Nanocomposites Based on Zinc Sulfate Monohydrate and Soluplus

et al. 2017

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Zinc sulfate monohydrate (ZnSO 4 )-loaded nanocomposites (NCs) were fabricated by using a hot-melt extruder (HME) system. Soluplus (SP) was adopted as an amphiphilic polymer matrix for HME processing. The micro-size of ZnSO 4 dispersion was reduced to nano-size by HME processing with the use of SP. ZnSO 4 could be homogeneously dispersed in SP through HME processing. ZnSO 4 /SP NCs with a 75 nm mean diameter, a 0.1 polydispersity index, and a −1 mV zeta potential value were prepared. The physicochemical properties of ZnSO 4 /SP NCs and the existence of SP in ZnSO 4 /SP NCs were further investigated by solid-state studies. Nano-size range of ZnSO 4 /SP NC dispersion was maintained in the simulated gastrointestinal environments (pH 1.2 and 6.8 media). No severe toxicity in intestinal epithelium after oral administration of ZnSO 4 /SP NCs (at 100 mg/kg dose of ZnSO 4 , single dosing) was observed in rats. These results imply that developed ZnSO 4 /SP NC can be used as a promising nano-sized zinc supplement formulation. In addition, developed HME technology can be widely applied to fabricate nanoformulations of inorganic materials.

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“…The two spectral regions between 900 – 1900 cm −1 and 2600 – 4000 cm −1 were chosen for the analysis. The spray dried azithromycin showed distinguishable characteristic peaks at 3480, 1726 and 1050 cm −1 attributable to the O-H stretching, lactone carbonyl C=O stretching and asymmetric C-O-C stretching, respectively (45). FTIR spectra of colistin showed peaks at 3257 cm −1 and 3048 cm −1 corresponding to the characteristic of amide A and B, respectively, due to N–H stretch in resonance with amide II overtone.…”

Section: Resultsmentioning

confidence: 99%

Understanding the Impacts of Surface Compositions on the In-Vitro Dissolution and Aerosolization of Co-Spray-Dried Composite Powder Formulations for Inhalation

Mangal

Park

et al. 2018

Pharm Res

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Purpose: Dissolution behavior of dry powder inhaler (DPI) antibiotic formulations in the airways may affect their efficacy especially for poorly-soluble antibiotics such as azithromycin. The main objective of this study was to understand the effects of surface composition on the dissolution of spray dried azithromycin powders by itself and in combination with colistin. Methods: Composite formulations of azithromycin (a poorly water-soluble molecule) and colistin (a water-soluble molecule) were produced by spray drying. The resultant formulations were characterized for particle size, morphology, surface composition, solid-state properties, solubility and dissolution. Results: The results demonstrate that surfaces composition has critical impacts on the dissolution of composite formulations. Colistin was shown to increase the solubility of azithromycin. For composite formulations with no surface colistin, azithromycin released at a similar dissolution rate as the spray-dried azithromycin alone. An increase in surface colistin concentration was shown to accelerate the dissolution of azithromycin. The dissolution of colistin from the composite formulations was significantly slower than the spray-dried pure colistin. In addition, FTIR spectrum showed intermolecular interactions between azithromycin and colistin in the composite formulations, which could contribute to the enhanced solubility and dissolution of azithromycin. Conclusions: Our study provides fundamental understanding of the effects of surface concentration of colistin on azithromycin dissolution of co-spray-dried composite powder formulations.

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Preparation and characterizations of stable amorphous solid solution of azithromycin by hot melt extrusion

Cited by 23 publications

References 30 publications

Correlation of two validated methods for the quantification of naringenin in its solid dispersion: HPLC and UV spectrophotometric methods

Correlation of two validated methods for the quantification of naringenin in its solid dispersion: HPLC and UV spectrophotometric methods

Fabrication and Characterizations of Hot-Melt Extruded Nanocomposites Based on Zinc Sulfate Monohydrate and Soluplus

Understanding the Impacts of Surface Compositions on the In-Vitro Dissolution and Aerosolization of Co-Spray-Dried Composite Powder Formulations for Inhalation

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