Enhancement of Hypolipidemic Effect of Atorvastatin Calcium via Floating Microspheres

Ashmawy, Al Zahraa Al

doi:10.21608/zjps.2022.124307.1026

Cited by 2 publications

(1 citation statement)

References 15 publications

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“…The use of ES100 has been explored in oating and mucoadhesive systems like microparticles (repaglinide, meclizine HCl), microsphere (atorvastatin), capsule (propranolol HCl and o oxacin), pulsatile tablets (ivabradine), coating of nanoparticles (luteolin), etc. [16][17][18][19][20][21]. Carbopol934 is used as ller in pellet and that also work as an excellent bioadhesive in tablets [22][23][24][25].…”

mentioning

confidence: 99%

Design, development and optimization of itopride hydrochloride loaded floating pellets by spheronization after compression method: In vitro and in vivo evaluation

Dass

Verma

Kaushik

et al. 2023

Preprint

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Background Gastroesophageal reflux disease is the most common disorder with a considerably high global prevalence. It is known to manifest with wide range of symptoms. Prokinetic drugs are commonly recommended in treating gastric reflux in addition to antacids and antisecretory drugs. Itopride, a prokinetic agent, has found to improve symptoms of gastroesophageal reflux disease. It acts as D2 antagonist and acetylcholine esterase inhibitor. Objective This research aimed to develop a gastro retentive system using a dual approach of floating and mucoadhesion.The retention of the formulation was estimated by in vitro floating time and in vivo pharmacokinetic study. Methodology: Different batches of pellets were prepared using ethylcellulose, Eudragit S100 and Carbopol 934 with Itopride hydrochloride by compression and spheronization method. Central composite design (32) was applied to find the effect of independent variables (concentration of Eudragit S100 and ethylcellulose), on dependent variables (floating time and percent drug release). In vivo gastric retention and bioavailability were done on rabbits for optimized pellets formulation. Results All developed formulations passed general evaluations test for pellets (P1-P13). The optimized pellets resulted in the in vitro percent itopride hydrochloride release (97.84%) and (9.3hrs) floating time. In vivo residence was nearly 8hrs and bioavailability was 52.87 ± 0.15 µg/mL/h. Besides, pellets have showed the drug release by sustained action for 12hrs. Conclusion The experimental design of pellets formulation concluded that mucoadhesion with floating approach was suitable for gastric retention and sustained the release of the drug. So, this approach might be useful in controlling the reflux of stomachal fluid.

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confidence: 99%

Design, development and optimization of itopride hydrochloride loaded floating pellets by spheronization after compression method: In vitro and in vivo evaluation

Dass

Verma

Kaushik

et al. 2023

Preprint

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Preparation & Characterization of Sustained-release Floating Microsphere of Digestive Enzymes

Prajapati,

Bhagat,

Basu

2025

CDTH

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Introduction: Pepsin is a proteolytic enzyme which is widely used as a digestive aid. Its dose is 300 mg - 1 gm per day in divided doses. Its biological half-life is around 3.5 hrs. Pepsin is active only in the acidic pH of the stomach; its activity decreases tremendously in the basic pH. So, it is required to retain in the stomach for maximum proteolytic activity. The goal of the current effort is to develop and assess an oral controlled floating drug delivery system for pepsin that will shorten its stay in the stomach and result in a longer effect. Methods: The 12-hour sustained effect of pepsin floating microspheres was planned. This also improves the stability of the Pepsin by immobilizing them on the microsphere. Pepsin is widely used in chronic gastritis, so developing a floating drug delivery system is therefore necessary. In light of the aforementioned principles, a critical need for the creation of a dosage form to administer Pepsin in the stomach and boost the enzyme's effectiveness, enabling sustained action, was identified. The current study used a methodical strategy to create floating microspheres of Pepsin dosage forms. Results: Optimization was done for floating ability, yield, entrapment efficiency, and release study using different concentrations of ethylcellulose & HPMC E4M. For parameter optimization and to demonstrate the significant impact of variables, 32 full factorial designs were used. The manufactured microspheres had good encapsulation rates, excellent floating, & excellent micromeritic properties as single-unit dosage forms. Conclusion: It has been demonstrated that pepsin prepared as floating microspheres can be used to improve proteolytic activity and extend pepsin's gastric residence.

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Enhancement of Hypolipidemic Effect of Atorvastatin Calcium via Floating Microspheres

Cited by 2 publications

References 15 publications

Design, development and optimization of itopride hydrochloride loaded floating pellets by spheronization after compression method: In vitro and in vivo evaluation

Design, development and optimization of itopride hydrochloride loaded floating pellets by spheronization after compression method: In vitro and in vivo evaluation

Preparation & Characterization of Sustained-release Floating Microsphere of Digestive Enzymes

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