Formulation, Preparation, and Evaluation of Novel Orally Disintegrating Tablets Containing Taste-Masked Naproxen Sodium Granules and Naratriptan Hydrochloride

Stange, Ulrike; Führling, Christian; Gieseler, Henning

doi:10.1002/jps.23896

Cited by 23 publications

(7 citation statements)

References 62 publications

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“…Similar results are described in the existing literature; it was noticed that increasing the gelatine concentration, the disintegration time extended [14], respectively by increasing the gelatine concentration, the mechanical properties were enhanced but in the same time, the disintegration profile was prolonged to the unacceptable results [2]. On the contrary, the use of sodium alginate and xanthan gum determined a faster disintegration time of the OLs, down to 3.81 respectively 1.77 s. This behaviour was observed previously in similar studies and it is assigned to the porosity of the structures; a high porosity of the structure allows the water ingress and conducts to a rapid disintegration time [15]. Regarding the bio-adhesive agents, the use of polyox determined a longer disintegration time comparing with the use of PVP that shortened it.…”

Section: In Vitro Disintegration Time (Y1)supporting

confidence: 54%

QbD APPROACH IN THE DEVELOPMENT OF ORAL LYOPHILISATES WITH IBUPROFEN FOR PAEDIATRIC USE

Suciu¹

2018

FARMACIA

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Quality-by-Design (QbD) concept in drug formulation and development was introduced in order to achieve and ensure an adequate product quality through a good process understanding. By identifying the variability sources that influence the product features, the quality of the product can be built from the development phase. Applying the concept, in the current work it was intended to develop and characterize orodisperable lyophilisates (OLs) for paediatric use. The drug model used was ibuprofen and following risk assessment evaluation, twenty-five experimental formulations were prepared. With a Doptimal experimental design with six factors and two levels, the influence of the formulation factors on the desired quality target product profile was assessed (QTPP, the quality characteristics of a product that is intended to be achieved considering the aspects related to the safety and efficacy of the product): disintegration time, wetting time, mean dissolution time, texture and bio-adhesive features of the OLs were studied. During this experiment, it was observed that the type of the matrix forming and bio-adhesive agent influenced the disintegration time. All formulation factors influenced the wetting time, while no significant influence was observed for the bio-adhesive properties of the OLs. The hardness and rigidity of the OLs was increased by gelatine, while the methylcellulose and xanthan gum conducted to opposite results. The fracturability of the OLs was influenced only by the quantitative factors, respectively the percentage of the matrix forming agent and the bio-adhesive agent. The dissolution profile was slightly influenced by the type of bio-adhesive agent. The design space has been defined based on the obtained results. The QbD approach was successfully applied within this study and OLs with ibuprofen for paediatric use with desired pharmaceutical characteristics may be successfully obtained by lyophilisation. RezumatConceptul de calitate prin design (QbD) a fost introdus în formularea și dezvoltarea medicamentelor cu scopul de a obține și asigura o calitate adecvată a produsului, printr-o bună înțelegere a procesului. Prin identificarea surselor de variabilitate care influențează caracteristicile produsului, calitatea produsului poate fi construită din faza de dezvoltare a acestuia. Aplicând acest concept, în prezenta lucrare s-a urmărit dezvoltarea și caracterizarea liofilizatelor orale, concepute pentru uz pediatric. Ca și substanță model, s-a utilizat ibuprofenul, preparându-se douăzeci și cinci de formulări pe baza unui model experimental D-optimal, cu șase factori și două niveluri. S-a studiat influența factorilor de formulare asupra profilului de calitate dorit (QTPP -caracteristicile de calitate dorite ale produsului, ținând cont de siguranța și eficacitatea acestuia): timpul de dezintegrare, timpul de umectare, timpul mediu de dizolvare, textura și caracteristicile bio-adezive ale liofilizatelor. Principalele observații au fost: tipul formatorului de matrice și a agentului bio-adeziv care au inf...

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Section: In Vitro Disintegration Time (Y1)supporting

confidence: 54%

QbD APPROACH IN THE DEVELOPMENT OF ORAL LYOPHILISATES WITH IBUPROFEN FOR PAEDIATRIC USE

Suciu¹

2018

FARMACIA

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“…Additionally, the bitterness value of taste-masked particles was still below the threshold after freeze-drying and storage, indicating that the coating remained intact. On the other hand, the drug dissolution was not affected by the existence of coating film (63). Similar results were achieved in another study, demonstrating again that Eudragit E PO as drug particle coating agent in ODTs could achieve successful taste masking by the fluid-bed coating method (64).…”

Section: Formation Of Core-shell Structures Via Coatingsupporting

confidence: 83%

Engineering Size and Structure of Particles in Novel Modified-Release Delivery Systems

et al. 2019

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Particle engineering has become a hot topic in the field of modified-release delivery systems during last decades. It has a wide range of pharmaceutical applications and is a bridge linking between drugs and drug delivery systems. Particles are an important part of many dosage forms and viewed as a carrier of drugs. Their size, shape, crystalline form, and structure directly affect the stability and releasing pattern of drugs. Engineering size or modifying particles by forming porous, core-shell, or skeleton structures can realize the development and utilization of functionally modified release systems (including fast-release systems, sustained-release systems, and targeted-release systems). However, there are certain problems in the practical application, such as bitter taste and coating damage. Combining with some polymer or lipid materials to form core-shell or embedded structures is considered as the key to taste masking. And, using cushioning agents is proven to be effective in preserving the integrity of the functional coating film of multiparticulates during tableting. To sum up, this review, from a particle engineering point, expounds the influence of different factors on the functionality of particles and offers some useful comments and suggestions for industry personnel.

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“…psychiatric disorders, etc. ), or for chronic conditions that are characterized by random and rapid onset such as anxiety attacks or migraine headaches . Unfortunately, ODTs tend to be relatively fragile and suffer from increased friability which, in turn, leads to more expensive packaging requirements.…”

Section: Introductionmentioning

confidence: 99%

The Effects of Screw Configuration and Polymeric Carriers on Hot-Melt Extruded Taste-Masked Formulations Incorporated into Orally Disintegrating Tablets

Morott

Pimparade

Park

et al. 2015

Journal of Pharmaceutical Sciences

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The primary aim of this research was to produce successfully taste masked formulations of Sildenafil Citrate (SC) using hot-melt extrusion (HME) technology. Multiple screw configurations and polymeric carriers were evaluated for their effects on taste masking efficiency, which was assessed by both E-tongue analysis and in vitro dissolution in simulated salivary fluid (SSF, pH 6.8 artificial saliva). The screw configurations were further assessed for their effects on the morphology of the API using PXRD, FT-IR and mid-infrared chemical imaging. It was determined that the screw configuration had a profound effect on the taste masking efficiency of the formulations as a result of altering the physical state of the API. Selected extruded formulations using ethylcellulose (EC) with a pore former were further formulated into orally disintegrating tablets (ODTs), which were optimized by varying the grade and percentage of the superdisintegrant used. An optimized disintegration time of approximately 8 seconds was achieved. The final ODT formulation exhibited excellent taste masking properties with over 85% drug release in gastric media as well as physical tablet properties. Interestingly, friability, which tends to be a common concern when formulating ODTs, was well within the acceptable limits (<1%) for common tablets.

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Formulation, Preparation, and Evaluation of Novel Orally Disintegrating Tablets Containing Taste-Masked Naproxen Sodium Granules and Naratriptan Hydrochloride

Cited by 23 publications

References 62 publications

QbD APPROACH IN THE DEVELOPMENT OF ORAL LYOPHILISATES WITH IBUPROFEN FOR PAEDIATRIC USE

QbD APPROACH IN THE DEVELOPMENT OF ORAL LYOPHILISATES WITH IBUPROFEN FOR PAEDIATRIC USE

Engineering Size and Structure of Particles in Novel Modified-Release Delivery Systems

The Effects of Screw Configuration and Polymeric Carriers on Hot-Melt Extruded Taste-Masked Formulations Incorporated into Orally Disintegrating Tablets

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