Evaluation of two novel co-processed excipients for direct compression of orodispersible tablets and mini-tablets

Kokott, Marcel; Lura, Ard; Breitkreutz, Jörg; Wiedey, Raphael

doi:10.1016/j.ejpb.2021.08.016

Cited by 23 publications

(5 citation statements)

References 28 publications

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“…Mannitol-based co-processed excipients performed well in studies investigating their compressibility, mechanical resistance and disintegration profile, as well as regarding their taste-masking capabilities [15][16][17][18].…”

Section: Tablets (Odts)mentioning

confidence: 99%

“…Even though a plethora of tablet manufacturing methods have been developed over the years, compression has remained the most largely used, due to its efficiency, robustness and scale-up capabilities [17,[23][24][25][26][27]. Hence, the current research in the field of tablet manufacturing intends to optimise the compression process and exploit the potential of already existing excipients rather than developing entirely new methods.…”

Section: Tablets (Odts)mentioning

confidence: 99%

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Orally Dispersible Dosage Forms for Paediatric Use: Current Knowledge and Development of Nanostructure-Based Formulations

et al. 2022

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The paediatric population has always suffered from a lack of medicines tailored to their needs, especially in terms of accurate dosage, stability and acceptability. Orodispersible dosage forms have gone through a resurrection as an alternative to liquid formulations or fractioned solid formulations, although they are still subject to several inconveniences, among which the unpleasant taste and the low oral bioavailability of the API are the most significant hurdles in the way of achieving an optimal drug product. Nanostructures can address these inconveniences through their size and variety, owing to the plethora of materials that can be used in their manufacturing. Through the formation and functionalisation of nanostructures, followed by their inclusion in orodispersible dosage forms, safe, stable and acceptable medicines intended for paediatric use can be developed.

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Section: Tablets (Odts)mentioning

confidence: 99%

Section: Tablets (Odts)mentioning

confidence: 99%

Orally Dispersible Dosage Forms for Paediatric Use: Current Knowledge and Development of Nanostructure-Based Formulations

et al. 2022

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“…After rotation, tablets were collected and reweighed. The percentage of friabilator was calculated by deducting the weight of initial from final weight [31].…”

Section: Friabilitymentioning

confidence: 99%

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

KANUGO¹,

THANVI²

2023

jrp

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The therapeutic efficacy of an active ingredients are imperfect owing to the poor solubility and dissolution rate. Moreover, dissolution is the rate-limiting period towards the absorption and bioavailability of the active ingredients. Olmesartan medoxomil is an angiotensin II receptor blocker (ARB) recommended for the therapy of high blood pressure as well as minimizes the chances of stroke, heart attack and kidney problems. Olmesartan medoxomil is a BCS class II molecule with only 26 % bioavailability. Hence, the current research work was focused on cost-effective Liquisolid technology for the improvement of solubility, dissolution rate and thereby achieving higher therapeutic efficacy. Liquisolid Compact is one of the best technique for improvement of solubility of potent hydrophobic molecules by utilizing non-volatile solvent. The solubility of olmesartan was estimated in several non-volatile solvents and tween 80 (95 mg/ml) was found to be best. The formed liquid medicaments were converted into the free-flowing powder blends for direct compression by the addition of carrier (Dibasic anhydrous calcium phosphate) and coating agent (Neusilin US2). The drug-excipients compatibilities were confirmed with FTIR. QbD design (Box-Behnken) was applied which comprised of independent factors (X1: DCP, X2: Neusilin US2, X3: CCS) and dependable factors were (Y1: Disintegration time, Y2: Dissolution release). The Design of expert software (DOE, Statease, Version 11) showed 12 batches which were evaluated for their flowing characteristics. The optimized batch F12 showed excellent flowing characteristics (Carr's index: 14, Angle of repose: 24.42), rapid disintegration time (2.07 min), in-vitro drug release (99.45%) and qualify under accelerated stability testing with minimal drug loss.

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“…After rotation, tablets were collected and reweighed. The percentage of the friabilator was calculated by subtracting the weight of the initial from the final weight [27].…”

Section: Friabilitymentioning

confidence: 99%

pH-dependent pulsatile delivery of Ambrisentan for the treatment of hypertension

KANUGO¹,

DHAGE²

2023

jrp

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The greatest number of mortality in the world occurred due to hypertension. Several bodily functions are based on circadian rhythm including hypertension. The stimulation of the sympathetic nervous system in the early morning hours resulted in accelerating blood pressure which is a highly dangerous condition. This lead to cardiac failure and damage to the vital organs of the body. The current research focuses on pulsatile delivery of Ambrisentan for the treatment of high blood pressure which released the medicament at the right time and the right place. Primarily, core tablets were prepared with Ambrisentan. The compatibility of Ambrisentan with excipients was confirmed by FTIR analysis. The core tablets were evaluated for flowing characteristics which showed better flowing behavior and optimized core batch CT6 showed consolidation index 16.07±0.11 and angle of repose 27.02±0.14. Moreover, due to the least disintegration time (2.23±0.10) and greater dissolution release of 99.70 % ±0.49, CT6 was selected as an optimized core tablet for pulsatile delivery. Further, the combination of Eudragit L100 and ethyl cellulose were utilized for coating purposes in different proportion were utilized for achieving the desired lag time of 6 hrs. The optimized batch PC6 (Eudragit L100: EC 10) which comprised of 25:75 proportion showed a lag time of 6 hours, cumulative release of 99.25 % and content uniformity of 99.29±0.82. The dissolution release profile predicted zero-order release for Ambrisentan pulsatile tablets. The accelerated stability testing showed minimal loss of drug content when exposed at 40 0 C and 75 % relative humidity without altering lag time.

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Evaluation of two novel co-processed excipients for direct compression of orodispersible tablets and mini-tablets

Cited by 23 publications

References 28 publications

Orally Dispersible Dosage Forms for Paediatric Use: Current Knowledge and Development of Nanostructure-Based Formulations

Orally Dispersible Dosage Forms for Paediatric Use: Current Knowledge and Development of Nanostructure-Based Formulations

Neusilin US2 based Liquisolid Compact technique for the enhancement of solubility and dissolution rate of Olmesartan: Box-Behnken design approach

pH-dependent pulsatile delivery of Ambrisentan for the treatment of hypertension

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