Pulsatile Chronotherapeutic Drug Delivery for Controlling Early Morning Surge in Blood Pressure; Effect of Coating on Eplerenone In-vitro, In-vivo Release and Urinary Na/K Ratio

Marzouk, Maha A.; Darwish, Manal K.; Yassin, Ghada E.; El-Fattah, Marwa Adel Abd

doi:10.1590/s2175-97902022e19306

Cited by 2 publications

(1 citation statement)

References 19 publications

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“…Asthma is considered an early morning pathology where symptoms vary in the early morning and the entire day or night. Design and development of a time-dependent dosage form are the need of the hour [7][8][9][10].…”

Section: Introductionmentioning

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: Introductionmentioning

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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Gastroretentive Chronopharmaceutical Formulation of Lafutidine for Early Morning Acid Breakthrough

Parmar¹,

Yagneshwari²

2022

Pharmacophore

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The goal of the current study is to design a chronomodulated medicine delivery system for nocturnal acid situations. This strategy is based on a combination of floating and pulsatile principles. With this idea in mind, a floating-pulsatile drug delivery system of lafutidine was created to lengthen the time the dosage form, which has a lag phase followed by a burst release of the drug, stays in the stomach. Accordingly, floating pulsatile tablets were developed in three different steps viz. Preparation of drug-containing core tablets using a super disintegrant, pulsatile layer by compression coating using a mixture of hydrophilic erodible polymers like HPMC E5M and guar gum; and buoyant layer using gel-forming polymer like Carbopol 934P with sodium bicarbonate and citric acid. The effects of the independent variables-the weight ratio of HPMC E5M: Guar gum and the total weight of coating-on the dependent variables, the drug release lag time and cumulative percent drug release at 6 h, were studied using the response surface approach. Developed formulations were evaluated for buoyancy, dissolution, and stability studies. Results indicated the dependence of lag time on the ruptured nature of polymers used. Drug release lag time of optimized batch was found to be 6.20 ± 0.35 h with 98.45 ± 2.24 % of drug release at the end of 8 h. Accelerated stability studies suggested stability of dosage form for at least one month. In order to achieve the best treatment efficacy and increase patient compliance, a successful, stable, floating, pulsatile tablet was created. It can be administered after dinner at around 22:00 h.

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Pulsatile Chronotherapeutic Drug Delivery for Controlling Early Morning Surge in Blood Pressure; Effect of Coating on Eplerenone In-vitro, In-vivo Release and Urinary Na/K Ratio

Cited by 2 publications

References 19 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

Gastroretentive Chronopharmaceutical Formulation of Lafutidine for Early Morning Acid Breakthrough

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