Quality by design approach for optimization of repaglinide buccal tablets using Box-Behnken Design

Navamanisubramanian, Raja; Nerella, Raghunandan; Chamundeeswari, D.; Shanmuganathan, S

doi:10.1016/j.fjps.2018.10.002

Cited by 12 publications

(5 citation statements)

References 29 publications

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“…It was measured in grams which are required for the complete detachment of the tablet from the intestinal mucosa [24]. From a local slaughterhouse, the fatty acidfree freshly cut porcine intestine membrane was obtained and stored for 30 min in Krebb's buffer solution at pH 6.8 and temperature 37 ± 0.5 °C.…”

Section: Mucoadhesive Strengthmentioning

confidence: 99%

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

Jawed,

Satish

2023

Futur J Pharm Sci

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Background The current research aims to determine the pharmacokinetic parameters, mucoadhesive strength, and IVIVC correlation of the novel chronotherapeutic drug delivery system of montelukast sodium (MTS) loaded Parteck® SRP80 and hypromellose system. To accomplish this, an HPLC method was developed which is highly sensitive, precise, and rapid for quantifying pure MTS in rabbit plasma. Mucoadhesive strength and time-dependent mobility of developed formulation were established by ex-vivo study and X-ray radiography, respectively. Using a fraction of drug absorbed (FDA) and a fraction of drug released (FDR), Level-A in-vitro in-vivo correlation (IVIVC) was developed. According to ICH Q1A (R2) standards, stability experiments were conducted for 180 days. Result MTS retention time came as 3.971 min with a mobile phase of methanol: acetonitrile: 0.2 mM sodium acetate buffer (5:90:5). In-vitro dissolution showed pulsatile release of the drug up to 24 h with two lag phases. The in-vivo study showed a Cmax of 490.16 ± 33.95 ng/ml, Tmax of 9 h, and MRT of 14.08 ± 1.21 h. The correlation coefficient of 0.9899 confirmed the level-A IVIVC. Uncoated matrix tablet of Parteck® SRP 80 displayed mucoadhesive strength 1.25-fold higher than hypromellose. Stability experiments found no significant changes in drug content, physical appearance, and cumulative percentage release with a similarity factor of 87–90. Conclusion A single oral dose in-vivo study proved the sustained release of the drug for 24 h with satisfactory mucoadhesive strength. Moreover, X-ray radiography has confirmed the time-dependent presence of formulation at the needed spot. This study fulfilled all the requirements for chronotherapy of asthma and can be scaled up in the future. Graphical abstract

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Section: Mucoadhesive Strengthmentioning

confidence: 99%

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

Jawed,

Satish

2023

Futur J Pharm Sci

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“…7). [24] Where, k 0 is zero-order rate constant expressed in units of con centration/time and t is the time.…”

Section: Drug Permeation Studymentioning

confidence: 99%

Untitled

2022

AJP

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Aim:The main aim of this study was to Formulation and Characterization of Repaglinide Transdermal Patch Using Natural polymers. Materials and Methods: The Box-Behnken design was used, which has three levels and three factors to investigate the associate impact of significant attributes on tensile strength, In vitro drug release, and Ex vivo drug permeation. Fifteen formulations were developed that differed in the polymer ratio (9:1, 8:1, and 7:1). The permeation of repaglinide through hairless goat ear skin through Ex vivo was found to increase with the help of permeation enhancer d-limonene. Results: As per the experimental data, it is concluded that the R12 is the best formulation in ex vivo permeation, in which we have taken 30% propylene glycol as a plasticizer, 3% d-limonene as a permeation enhancer, and this formulation shown 301.825 µg/cm 2 permeation in 24 h. Conclusion: After optimizing all formulations, it concluded that the ratio of polymer in 9:1, 3% of a permeation enhancer, and 30% plasticize was the optimum quantity of different excipients used in the optimized formulation. These findings suggest that transdermal repaglinide delivery may have therapeutic promise, with benefits such as reduced dose frequency, better patient compliance, non-invasive properties, enhanced bioavailability, and ease of medication discontinuation.

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“…Accordingly, the development of novel formulations that can extend the effect of REP and improve patient compliance is extremely desirable. 20 , 21 To achieve this target, several approaches have been reported, including matrix pellets, 22 an osmotic pump system, 23 niosomal encapsulation, 15 biodegradable microspheres, 24 and transdermal microemulsion gels. 25 …”

Section: Introductionmentioning

confidence: 99%

Repaglinide–Solid Lipid Nanoparticles in Chitosan Patches for Transdermal Application: Box–Behnken Design, Characterization, and In Vivo Evaluation

Ali,

Namazi,

Elbadawy

et al. 2024

IJN

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Background Repaglinide (REP) is an antidiabetic drug with limited oral bioavailability attributable to its low solubility and considerable first-pass hepatic breakdown. This study aimed to develop a biodegradable chitosan-based system loaded with REP–solid lipid nanoparticles (REP-SLNs) for controlled release and bioavailability enhancement via transdermal delivery. Methods REP-SLNs were fabricated by ultrasonic hot-melt emulsification. A Box–Behnken design (BBD) was employed to explore and optimize the impacts of processing variables (lipid content, surfactant concentration, and sonication amplitude) on particle size (PS), and entrapment efficiency (EE). The optimized REP-SLN formulation was then incorporated within a chitosan solution to develop a transdermal delivery system (REP-SLN-TDDS) and evaluated for physicochemical properties, drug release, and ex vivo permeation profiles. Pharmacokinetic and pharmacodynamic characteristics were assessed using experimental rats. Results The optimized REP-SLNs had a PS of 249±9.8 nm and EE of 78%±2.3%. The developed REP-SLN-TDDS demonstrated acceptable characteristics without significant aggregation of REP-SLNs throughout the casting and drying processes. The REP-SLN-TDDS exhibited a biphasic release pattern, where around 36% of the drug load was released during the first 2 h, then the drug release was sustained at around 80% at 24 h. The computed flux across rat skin for the REP-SLN-TDDS was 2.481±0.22 μg/cm 2 /h in comparison to 0.696±0.07 μg/cm 2 /h for the unprocessed REP, with an enhancement ratio of 3.56. The REP-SLN-TDDS was capable of sustaining greater REP plasma levels over a 24 h period ( p <0.05). The REP-SLN-TDDS also reduced blood glucose levels compared to unprocessed REP and commercial tablets ( p <0.05) in experimental rats. Conclusion Our REP-SLN-TDDS can be considered an efficient therapeutic option for REP administration.

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Quality by design approach for optimization of repaglinide buccal tablets using Box-Behnken Design

Cited by 12 publications

References 29 publications

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

IVIVC assessment, pharmacokinetic evaluation, and X-ray radiography mapping of Novel Parteck® SRP 80 and hypromellose-loaded LTD4 receptor antagonist chronosystem

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Repaglinide–Solid Lipid Nanoparticles in Chitosan Patches for Transdermal Application: Box–Behnken Design, Characterization, and In Vivo Evaluation

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