Development and Validation of &lt;i&gt;In Vitro&lt;/i&gt; Discriminatory Dissolution Testing Method for Fast Dispersible Tablets of BCS Class II Drug

The use of apex vessels may solve coning problems associated with dissolution testing. However, excessive dissolution acceleration can reduce the discriminatory power. This study aimed to clarify how different apex vessel sizes affect the dissolution behavior of cone-forming formulations. Five apex vessels with different heights, centralities, and compendial vessels were used. The paddle rotation speed at which the coning phenomenon resolved was measured using standard particles of different densities. Three model formulations—USP prednisone tablets, atorvastatin calcium hydrate tablets, and levofloxacin fine granules—were selected, and dissolution tests were conducted at 30–100 revolutions per minute (rpm). Compared to the compendial vessels, the disappearance of standard particles at the apex base at lower paddle speeds in apex vessels was observed. Standard particles tended to remain in the center of the apex vessels and disappear at rotational speeds comparable to those of the compendial vessels. Dissolution increased in an apex height-dependent manner in the model formulations, except for the atorvastatin calcium hydrate tablets at 50 rpm. For levofloxacin fine granules, dissolution was also improved by reducing the paddle agitation speed to 30 rpm in the compendial vessels. Differences in apex centrality by 3 mm did not affect the dissolution rate. Our results indicate that apex vessels with low apex heights have a mount-resolving effect, but the degree of dissolution improvement by avoiding the coning phenomenon depends on the formulation characteristics used in the dissolution tests. Graphical abstract

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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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Development and Validation of <i>In Vitro</i> Discriminatory Dissolution Testing Method for Fast Dispersible Tablets of BCS Class II Drug

Cited by 4 publications

References 10 publications

Development of In Vitro Dissolution Testing Methods to Simulate Fed Conditions for Immediate Release Solid Oral Dosage Forms

Development of In Vitro Dissolution Testing Methods to Simulate Fed Conditions for Immediate Release Solid Oral Dosage Forms

Effects of Apex Size on Dissolution Profiles in the USP II Paddle Apparatus

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

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