Statistical Considerations Concerning Dissimilar Regulatory Requirements for Dissolution Similarity Assessment. The Example of Immediate-Release Dosage Forms

Jasińska-Stroschein, Magdalena; Kurczewska, Urszula; Orszulak–Michalak, Daria

doi:10.1016/j.xphs.2017.01.003

Cited by 5 publications

(3 citation statements)

References 17 publications

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“…It is a unitless value that measures the closeness between the predicted and actual profiles. The FDA has set a public value of 50-100 to indicate similarity between two dissolution profiles (Jasińska-Stroschein et al, 2017). It was applied in this study as a quantitative measurement for model accuracy, where it was discovered that decision tree obtained a considerably greater accuracy than the other models.…”

Section: Predicting Dissolution Using Rheology and Machine Learningmentioning

confidence: 99%

3D printing tablets: Predicting printability and drug dissolution from rheological data

Elbadawi

Gustaffson

Gaisford

et al. 2020

International Journal of Pharmaceutics

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Rheology is an indispensable tool for formulation development, which when harnessed, can both predict a material's performance and provide valuable insight regarding the material's macrostructure. However, rheological characterizations are under-utilized in 3D printing of drug formulations. In this study, viscosity measurements were used to establish a mathematical model for predicting the printability of fused deposition modelling 3D printed tablets (Printlets). The formulations were composed of polycaprolactone (PCL) with different amounts of ciprofloxacin and polyethylene glycol (PEG), and different molecular weights of PEG. With all printing parameters kept constant, both binary and ternary blends were found to extrude at nozzle temperatures of 130, 150 and 170 C. In contrast PCL was unextrudable at 130 and 150 C. Three standard rheological models were applied to the experimental viscosity measurements, which revealed an operating viscosity window of between 100-1000 Pa.s at the apparent shear rate of the nozzle. The drug profile of the printlets were experimentally measured over seven days. As a proof-of-concept, machine learning models were developed to predict the dissolution behaviour from the viscosity measurements. The machine learning models were discovered to accurately predict the dissolution profile, with the highest f2 similarity score value of 90.9 recorded. Therefore, the study demonstrated that using only the viscosity measurements can be employed for the simultaneous high-throughput screening of formulations that are printable and with the desired release profile.

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Section: Predicting Dissolution Using Rheology and Machine Learningmentioning

confidence: 99%

3D printing tablets: Predicting printability and drug dissolution from rheological data

Elbadawi

Gustaffson

Gaisford

et al. 2020

International Journal of Pharmaceutics

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“…The characterization of dissolution profiles is compared by dissolution efficiency and the fit factor ( f 2 ) [ 44 ]. According to the guidelines of the FDA, the range of f 2 should be 50 to 100 [ 45 ]. The comparison of two test formulation dissolution profiles of Invega Sustenna ® is represented in Table 3 .…”

Section: Resultsmentioning

confidence: 99%

Comparison of Paliperidone Palmitate from Different Crystallization Processes and Effect on Formulations In Vitro and In Vivo

et al. 2022

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The quality of active pharmaceutical ingredients (APIs) is an important factor which can affect the safety and efficacy of pharmaceuticals. This study was designed to investigate the nature of paliperidone palmitate (PP) obtained by different crystallization processes, then compare the characteristics between test formulations which prepared PP of different crystallization and reference formulations (Invega Sustenna®) in vitro and in vivo. Two different PPs, namely PP-1 and PP-2, were prepared by different crystallization methods. Contact angle, morphology, and crystallinity of the PPs were characterized. Taking the particle sizes and distribution of Invega Sustenna® as reference, test formulations were prepared by the wet milling method using either a PP-1 or PP-2 sample. Their release behavior, stability in vitro, and pharmacokinetics in vivo were subsequently investigated. The results indicated that PP-2 had a higher surface free energy (SFE). More small particles were attached to the PP-1 surface under the influence of crystallization temperature. Different crystallization processes did not change the crystal of PP, but changed the crystallinity of PP. There was no obvious difference in in vitro releases between test formulations. However, the stability and state of formulation containing PP-2 were better compared to formulations containing PP-1, indicated by differences in crystallinity and SFE. Meanwhile, pharmacokinetic in vivo results demonstrated that the pharmacokinetic profiles and parameters of formulation containing PP-2 and Invega Sustenna® tended to be consistent, but those of formulations containing PP-1 were significantly different from those of formulations containing PP-2 or Invega Sustenna®, and there was burst release phenomenon of formulations containing PP-1 in rats. PP made by different crystallization processes could induce changes in appearance, SFE, and crystallinity, and further affect the stability, state, and pharmacokinetic in vivo formulation.

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“…Pure drug showed a poor dissolution profile (i.e., only 29.11% of drug was released at 45 min), whereas PMs revealed a slight improvement in dissolution profiles due to the presence of carrier in the respective mixtures. Immediate release dosage forms are those with at least 85% of the labelled amount which dissolves within 15, 20-30, or 45 min 41 . In vitro release studies revealed immediate release profiles of drug at all ratios of SDs prepared by both methods at 45 min as presented in Figure 8(i) and Figure 8(ii).…”

Section: In Vitro Dissolution Study Of Solid Dispersionsmentioning

confidence: 99%

The use of hydrophilic carrier derived from eggshell and novel gel forming technique in a solid dispersion system

Myint¹,

Lawanprasert²,

Puttipipatkhachorn³

et al. 2023

Pharm Sci Asia

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The study aimed to prepare calcium acetate (CaA) from the eggshell (ES) by the chemical reaction with aqueous acetic acid and to improve the dissolution properties of poorly soluble model drug, chloroxylenol (CXN), by solid dispersion (SD) system with CaA as a carrier. In the present study, SDs were prepared by two methods using various drug:carrier ratios. Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), thermal analysis and scanning electron microscope (SEM) studies were carried out to characterize the prepared SDs in comparison with pure drug and physical mixtures (PMs). FTIR analysis indicated that there was an intermolecular hydrogen bonding between the terminal hydroxyl group of drug and water molecules of CaA. Decrease in crystallinity of SDs was observed in PXRD and differential scanning calorimetry (DSC) studies. Moreover, thermogravimetric analysis (TGA) study showed the drug protected within SD. SEM images revealed the morphology of SDs prepared by the gel forming technique as a rod-like microstructure in which the drug was occupied. The rough surface of SD prepared by the wet granulation method was due to the adherence of drug particles on the surface of CaA. SDs prepared by the gel method exhibited superior performance for the dissolution of CXN with a release of 93-113% at 60 min compared to PMs and pure CXN, which could be due to its transformation from crystalline to amorphous form as well as the improved wettability. Therefore, CaA might be the potential candidate for the dissolution enhancement of poorly soluble drugs.

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Statistical Considerations Concerning Dissimilar Regulatory Requirements for Dissolution Similarity Assessment. The Example of Immediate-Release Dosage Forms

Cited by 5 publications

References 17 publications

3D printing tablets: Predicting printability and drug dissolution from rheological data

3D printing tablets: Predicting printability and drug dissolution from rheological data

Comparison of Paliperidone Palmitate from Different Crystallization Processes and Effect on Formulations In Vitro and In Vivo

The use of hydrophilic carrier derived from eggshell and novel gel forming technique in a solid dispersion system

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