Effect of API on Powder Flowability, Direct Compression and Properties of Orally Disintegrating Tablets: A Preformulation Study

Nachajski, Michał Jakub; Bazela, A.; Zarzycka, M.; Broszczyk, A.; Kolba, A.; Kołodziejczyk, Michał Krzysztof

doi:10.36468/pharmaceutical-sciences.534

Cited by 6 publications

(5 citation statements)

References 11 publications

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“…The disparity between the disintegration profiles arises from differences in the ingress of disintegration medium, which is the first step in the disintegration process for both formulations. Factors that affect the ingress of disintegration medium are the following: ( 1 ) polymer-drug interactions ( 34 ); ( 2 ) pore closure ( 35 ) and ( 3 ) the distribution of the formulation components within the tablet, for example, burst release happens if the drug or the disintegrating agent is close to the surface and thus accessible to disintegration media ( 36 ).…”

Section: Discussionmentioning

confidence: 99%

“…The distance between the camera and the 3D-printed disintegration vessel was adjusted to observe the tested formulations without zooming. A video for ( 1 ) disintegration media only (background); ( 2 ) tested tablet only and ( 3 ) tablet disintegration was recorded over 250 s. The video was converted to images, which was then analysed using a Java-based image processing program to measure the mean grey value (MGV) called ImageJ software.…”

Section: Methodsmentioning

confidence: 99%

“…Fast disintegrating tablets (FDTs) are dosage forms required to disintegrate or “melt” within a patient’s mouth without chewing or water intake ( 1 ). They have the advantages of simple administration, accurate dosing, rapid onset of action and avoidance of the first pass effect ( 2 ).…”

Section: Introductionmentioning

confidence: 99%

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Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Malallah

Rashid²,

et al. 2021

AAPS PharmSciTech

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Measuring tablet disintegration is essential for quality control purposes; however, no established method adequately accounts for the timeframe or small volumes of the medium associated with the dissipation process for fast disintegrating tablets (FDTs) in the mouth. We hypothesised that digital imaging to measure disintegration in a low volume of the medium might discriminate between different types of FTD formulation. A digital image disintegration analysis (DIDA) was designed to measure tablet disintegration in 0.05–0.7 mL of medium. A temperature-controlled black vessel was 3D-printed to match the dimensions of each tablet under investigation. An overhead camera recorded the mean grey value of the tablet as a measure of the percentage of the formulation which remained intact as a function of time. Imodium Instants, Nurofen Meltlets and a developmental freeze-dried pilocarpine formulation were investigated. The imaging approach proved effective in discriminating the disintegration of different tablets (p < 0.05). For example, 10 s after 0.7 mL of a saliva simulant was applied, 2.0 ± 0.3% of the new pilocarpine tablet remained, whereas at the same time point, 22 ± 9% of the Imodium Instants had not undergone disintegration (temperature within the vessel was 37 ± 0.5°C). Nurofen Meltlets were observed to swell and showed a percentage recovery of 120.7 ± 2.4% and 135.0 ± 6.1% when 0.05 mL and 0.7 mL volumes were used, respectively. Thus, the new digital image disintegration analysis, DIDA, reported here effectively evaluated fast disintegrating tablets and has the potential as a quality control method for such formulations.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Malallah

Rashid²,

et al. 2021

AAPS PharmSciTech

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“…Compressibility is the ability of drug powders to decrease in volume under pressure and compress into tablet dosage forms with specific tensile strength. It is calculated by the Hausner ratio and Carr's index (formula mentioned in Table 3) to determine the flow behaviour of powder-based drugs to calculate the density at the preformulation stages [45].…”

Section: Compressibilitymentioning

confidence: 99%

Preformulation Studies: A Versatile Tool in Formulation Design

Ahirwar¹,

Shukla²

2023

Drug Formulation Design

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The physicochemical properties of pharmacological molecules have a tremendous effect on safety and efficacy. Poor physicochemical properties can often make it hard to set up a reliable structure-activity relationship (SAR) with no prominent efficacy in preclinical and clinical models. This can lead to more variability in capability and higher drug development costs in the entire development process, and in the worst case, even to stop the clinical trials in the later period. Understanding the basic physicochemical properties makes it possible to separate and untangle investigational observations hence poor molecular properties can be changed or fixed during the design phase. This makes it more likely that the molecule will make it through the long and difficult development process. The decline in innovator pharmacotherapeutics number registrations decline each year and the industry is under even more pressure than in the past to speed up the drug development process. This reduces the length of time required for development and introduces innovative pharmaceutical products. To do this, it is imperative to proceed with an organised approach and act appropriately the first time. The current chapter aims to focus on the important physicochemical properties of the selected molecule, along with how those properties are evaluated and implicated in both discovery enablement and final dosage form development.

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“…Due to that, inclusion complexes obtained via these approaches can be used in the production of tablet dosage forms of gramicidin S applying direct compression technology, which is the most suitable for tablet production for buccal application [11]. The transition to this type of technology will significantly reduce costs by simplifying the technology and reducing the production time.…”

Section: фармацевтическая технология Pharmaceutical Technologymentioning

confidence: 99%

Investigation of the Influence of Formulation Method on Technological Parameters of Gramicidin S and β-cyclodextrin Inclusion Complexes

Drannikov

Vatlin

Trusova

et al. 2022

Razrabotka i registraciâ lekarstvennyh sredstv

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Introduction. Gramicidin S is a peptide antibiotic that has been widely used for more than 70 years. Gramicidin S is available in the form of tablets with a low dosage, which leads to possible deviations in the "Uniformity of dosage" parameter during manufacturing. Another limitation is the presence of lactose and sucrose in the formulation, which limits the drug application by patients demonstrating intolerance. As an alternative, we propose inclusion complexes of gramicidin S with β-cyclodextrin. Aim. The work aims to describe the influence of the methodology to prepare the inclusion complex on the characteristics and properties of the final product. Materials and methods. The gramicidin S -β-cyclodextrin inclusion complex has been prepared by dry mixing, paste complexation, coprecipitation and fluid-bed complexation. The complex formation has been confirmed by 1 H NMR spectroscopy, differential scanning calorimetry and thermogravimetry while the morphology and size by scanning electron microscopy for the solid and dynamic light scattering for the solution. The flowability, slope angle, bulk density of the obtained powders were estimated using the methods described in Russian Pharmacopoeia of the XIV edition. Results and discussion. In the present work, we prepared a set of gramicidin S and β-cyclodextrin inclusion complexes by various approaches. The thermal analysis demonstrated a significant change in the peak referring to phase transition of the substances, indicating the interaction between the components. The 1 H NMR spectroscopy reveals that the L-ornithine amino group is the part of gramicidin S involved in the complexation. Evaluating the technological properties of gramicidin S and β-cyclodextrin inclusion complexes significant variability, which is associated with the particle morphology. Complexes obtained using co-precipitation and fluid-bed complexation methods are more suitable for producing gramicidin S tablet production by direct compression technology. Conclusion. Herein, we demonstrate that the formation of the gramicidin S and β-cyclodextrin inclusion complex occurs through the L-ornithine amino group in the gramicidin S. In addition, depending on the method significant differences in the particle size and shape have been observed. The obtained results could provide valuable information for the development of new gramicidin S buccal formulations, which are more consistent in the "Uniformity of dosage" and allow to avoid the use of lactose and sucrose as excipients.

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Effect of API on Powder Flowability, Direct Compression and Properties of Orally Disintegrating Tablets: A Preformulation Study

Cited by 6 publications

References 11 publications

Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Digital Image Disintegration Analysis: a Novel Quality Control Method for Fast Disintegrating Tablets

Preformulation Studies: A Versatile Tool in Formulation Design

Investigation of the Influence of Formulation Method on Technological Parameters of Gramicidin S and β-cyclodextrin Inclusion Complexes

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