Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension

Maddiboyina, Balaji; Hanumanaik, Mudavath; Nakkala, Ramya Krishna; Jhawat, Vikas; Rawat, Pinki; Alam, Aftab; Foudah, Ahmed I.; Alrobaian, Majed; Shukla, Rahul; Singh, Sima; Kesharwani, Prashant

doi:10.1016/j.heliyon.2020.e05459

Cited by 36 publications

(13 citation statements)

References 16 publications

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“…Hausner's ratio was found to be in the range of 1.084-1.105 for both metoprolol succinate and amlodipine besylate. These values are below 1.25, confirming a good flow property [25,26].…”

Section: Evaluation Of Physical Properties Of Granulesmentioning

confidence: 74%

Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate

et al. 2021

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The development of new drugs that combine active ingredients for the treatment hypertension is critically essential owing to its offering advantages for both patients and manufacturers. In this study, for the first time, detailed development of a scalable process of film-coated bi-layer tablets containing sustained-release metoprolol succinate and immediate-release amlodipine besylate in a batch size of 10,000 tablets is reported. The processing parameters of the manufacturing process during dry mixing-, drying-, dry mixing- completion stages were systematically investigated, and the evaluation of the film-coated bi-layer tablet properties was well established. The optimal preparation conditions for metoprolol succinate layer were 6 min- dry mixing with a high-speed mixer (120 rpm and 1400 rpm), 30-min drying with a fluid bed dryer, and 5-min- mixing completion at 25 rpm. For the preparation of amlodipine besylate layer, the optimal dry-mixing time using a cube mixer (25 rpm) was found to be 5 min. The average weight of metoprolol succinate layers and bi-layer tablets were controlled at 240–260 mg and 384–416 mg, respectively. Shewhart R chart and X¯ charts of all three sampling lots were satisfactory, confirming that the present scalable process was stable and successful. This study confirms that the manufacturing process is reproducible, robust; and it yields a consistent product that meets specifications.

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“…Hausner's ratio was found to be in the range of 1.084-1.105 for both metoprolol succinate and amlodipine besylate. These values are below 1.25, confirming a good flow property [25,26].…”

Section: Evaluation Of Physical Properties Of Granulesmentioning

confidence: 74%

Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate

et al. 2021

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“…This preparation is intended to increase the duration of action of the drug and reduce toxicity. Several excipients have been developed: hydrophilic excipients and osmotic pore excipients [48][49][50]. The drug release profile is the typical quality parameter of this preparation because the objective of this excipient is to modify drug release.…”

Section: Modified Release Tabletmentioning

confidence: 99%

An Experimental Design in the Optimization of Various Tablet Excipient Formulations = a Concise Review

Sopyan

2022

Int J App Pharm

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The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

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“…After reacting with sodium bicarbonate, citric acid, and hydrochloride acid, carbon dioxide is produced, causing the tablets to float in the liquids for more than 12 hr in vitro. Due to the fact that cefdinir was primarily absorbed in the upper part of the GIT, the prolonged drug residence time in the stomach may result in enhanced absorption (17).…”

Section: Table (4): Disintegration Time Of Immediate Release Layermentioning

confidence: 99%

“…This suggests that the medicine is absorbed mostly in the upper gastrointestinal tract. Cefdinir had higher absorption in the proximal GI tract and poor absorption, as well as antibiotic-associated colitis, when a large amount of drug entered the colon, suggesting it is a perfect choice for a gastroretentive drug delivery system that will lengthen the dosage form's gastric residence time, allowing for continuous drug release in the upper GI tract, where cefdinir absorption is well restricted (17). Nanosuspension technology got the main attraction in the pharmaceutical industry for the last two decades.…”

Section: Introductionmentioning

confidence: 99%

Formulation and characterization of floating biphasic tablet consisting of cefdinir nanosuspension

Al-Mahmood

Alhammid

2022

ijhs

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Cefdinir (Cef) is a third-generation cephalosporin antibacterial agent with an extended spectrum and low solubility and permeability. In this study, cefdinir was prepared as nanosuspension and lyophilized to powder. The lyophilized cefdinir was further processed to develop a bilayer tablet. By utilizing the bilayer approach, the first therapeutic action is impacted by the immediate part's rapid disintegration and a prolonged release from the floating part is achieved. Floating system ensures a recognized extended-release in the gastric medium and avoids the numerous daily dosages. Different polymers were utilized with effervescent materials in different concentrations. The method employed in preparing tablets is direct compression. Every formulation undergoes through standard pre and post-compression floating tablet characteristics with unique results that allow for further comparison between various formulations and increase our understanding of the makeup of medications, polymers, additives, and preparation technique. The formula NFT8 was selected as the best formulation design. It contains (HPMC K4M 400 mg, Carbapol940 50 mg, sodium bicarbonate 100 mg, and citric acid 75 mg) and provided efficient floating characteristics for more than 24 hr as revealed by in vitro dissolution release.

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Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension

Cited by 36 publications

References 16 publications

Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate

Development of a Scalable Process of Film-Coated bi-Layer Tablet Containing Sustained-Release Metoprolol Succinate and Immediate-Release Amlodipine Besylate

An Experimental Design in the Optimization of Various Tablet Excipient Formulations = a Concise Review

Formulation and characterization of floating biphasic tablet consisting of cefdinir nanosuspension

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