Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach

Pawar, Jaywant; Tayade, Apurva; Gangurde, Avinash B.; Moravkar, Kailas K.; Amin, Purnima D.

doi:10.1016/j.ejps.2016.04.001

Cited by 63 publications

(30 citation statements)

References 51 publications

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“…Figure 8 shows the characteristic XRD peaks of pure forms of NRG, POX and GEL confirming their crystalline form which is in conjugation with the literature [28][29][30]. The diffractograms of SDs (NP1 and NG1) revealed a disappearance in NRG peaks, which denotes a transition from crystalline to an amorphous form; a behavior already observed for other drugs in solid dispersions [21,31]. From the above results, the values of NRG concentration given by both the methods; UV-spectroscopy and HPLC method are in the close agreement.…”

Section: Correlation Between the Hplc Methods And Uv Methods For Releassupporting

confidence: 79%

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: Correlation Between the Hplc Methods And Uv Methods For Releassupporting

confidence: 79%

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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“…The wave number of 2243 cm -1 corresponding to the -CN stretch, uniquely distinguishes in EFV in the SCS3 (Fig. 11C) was used to generate the FTIR chemical images (Pawar et al, 2016a). The peak range at 2186 cm -1 to 2289 cm -1 was selected as the chemical imaging reflectance spectrum for both analysis.…”

Section: Ftir Chemical Imaging Analysismentioning

confidence: 99%

“…AFM probes were employed to characterize and map the distribution of components within a SCSs prepared by HME. The distribution of drug inside polymer shows homogenous morphology (Pawar et al, 2016a). The two phases were mixed at molecular level as reflected by normal AFM image (nanoscale) and 3D image processed via AFM.…”

Section: Afm Analysismentioning

confidence: 99%

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Pawar

Fule

Maniruzzaman

et al. 2017

Materials Science and Engineering: C

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Poor aqueous solubility of drugs has emerged as a major issue for pharmaceutical scientists from many decades. The current study explores the manufacture and development of a thermodynamically stabilized solid crystal suspension (SCS) of poorly water soluble drug efavirenz via hot melt extrusion. Efavirenz is a non-nucleoside reverse transcriptase inhibitor and belongs to BCS class II. The SCS was prepared using pearlitol and xylitol as a crystalline carrier. The drug-excipient blend was processed by hot melt extrusion with up to 50% (w/w) drug loading. Physico-chemical characterization of the SCS conducted via a scanning electron microscopy, differential scanning calorimetry and hot stage microscopy confirmed that SCS are in crystalline state. Similarly, X-ray powder diffraction analysis revealed highly crystalline existence of pure drug, crystalline carriers and developed SCS. The FTIR chemical imaging analysis of SCS formulations showed a homogeneous drug distribution within respective crystalline carriers while an advanced chemical analysis via atomic force microscopy and Raman analysis complemented the foregoing findings. The developed SCS1 formulation showed up to 81 fold increase in the solubility and 4.1 fold increase in the dissolution rate of the drug compared to that of the bulk substance. Surprisingly, the developed SCS formulation remained stable for a period of more than one year at accelerated conditions inferred from dissolution studies. It can be concluded that the SCS approach can be used as an alternative contemporary technique to enhance the dissolution rates of many other poorly water-soluble drugs by means of thermal HME processing.

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“…The effect of independent variable, alone or in combination, on the process can be studied. Reduced process variability, higher percentage yields and less treatment time are additional advantages of RSM …”

Section: Introductionmentioning

confidence: 99%

“…Reduced process variability, higher percentage yields and less treatment time are additional advantages of RSM. [6] Mucoadhesive films are dosage forms that remain in intimate contact with the oral mucosa and release the drug for prolonged period either for local or systemic action. The release of drug can either be in the direction of oral mucosa or towards the oral cavity.…”

Section: Introductionmentioning

confidence: 99%

Effects of formulation composition on the characteristics of mucoadhesive films prepared by hot-melt extrusion technology

Bhagurkar

Darji

Lakhani

et al. 2018

Journal of Pharmacy and Pharmacology

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Objectives To investigate the effects of formulation composition on the physico‐chemical and drug release properties of mucoadhesive buccal films prepared by melt extrusion technology, using a response surface methodology. Methods Salbutamol sulphate, an antiasthmatic drug was used for this study. Klucel hydroxypropylcellulose (HPC) EF (film‐forming polymer), Benecel hydroxypropylmethylcellulose (HPMC) K‐15M (drug release retardant) and polyethylene glycol (PEG) 4500 (plasticiser) were the three independent factors utilised for the study. The responses were fitted to a full quadratic model and P‐values for each of the factors were used to determine their significance on the film characteristics. Key findings Films were successfully extruded using the corotating twin‐screw extruder. The torque during extrusion was found to be significantly affected by all the three factors and no interaction between factors was observed. A significant interaction was observed between HPC and PEG 4500 for stiffness of films. For disintegration time and swelling index, a significant interaction was found between HPC and HPMC. The in vitro % drug release was directly correlated with HPMC content and not with other factors and varied from 69–89% at 4 h. Conclusions The influence of extrusion process and formulation parameters on salbutamol sulphate films was elucidated, indicating the use of melt extrusion as a feasible method for film preparation.

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Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach

Cited by 63 publications

References 51 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

Solid crystal suspension of Efavirenz using hot melt extrusion: Exploring the role of crystalline polyols in improving solubility and dissolution rate

Effects of formulation composition on the characteristics of mucoadhesive films prepared by hot-melt extrusion technology

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