A New Multiple-Unit Oral Floating Dosage System. I: Preparation and In Vitro Evaluation of Floating and Sustained-Release Characteristics

Ichikawa, Masaki; Watanabe, Sumio; Miyake, Yuichi

doi:10.1002/jps.2600801113

Cited by 112 publications

(62 citation statements)

References 11 publications

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“…Floating lag time of various batches was shown in table 4. 11,12,13 : In vitro dissolution has been recognized as an important element in drug development. Several kinetics models describe drug dissolution from immediate and modified release dosage form.…”

Section: Floating Time and Floating Lag Timementioning

confidence: 99%

FORMULATION & EVALUATION OF BILAYER FLOATING TABLETS OF METOPROLOL TARTRATE

Tagde¹,

Jain²,

Pathak³

2012

Int J of Biomed & Adv Res

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The objective of the present research was to develop a bi-layer tablet of Metoprolol tartrate using disintegrant starch for the fast release layer and HPMC K grade polymers for the sustaining layer. In vitro dissolution studies were carried out in an Indian Pharmacopoeia dissolution testing apparatus II (paddle method). The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 12 h from the sustaining layer of matrix embedded tablets. The Invitro release study of this tablet indicated sustained release for Metoprolol tartrate and followed zero order release and 95% drug in 24h in vitro and it follow Fickian diffusion.

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Section: Floating Time and Floating Lag Timementioning

confidence: 99%

FORMULATION & EVALUATION OF BILAYER FLOATING TABLETS OF METOPROLOL TARTRATE

Tagde¹,

Jain²,

Pathak³

2012

Int J of Biomed & Adv Res

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“…diazepam (Sheth and Tossounian, 1984) and verapamil hydrochloride (Streubel et al, 2002); thereby preventing solubility from being the rate-limiting step to the absorption of the drug by restricting the drug to the stomach drugs that have a narrow absorption window in the stomach or in the upper small intestine, e.g. levodopa (Erni and Held, 1987), para-amino benzoic acids (Ichikawa et al, 1991a, Ichikawa et al, 1991b and furosemide (Menon et al, 1994) drugs that are absorbed rapidly from the GI tract, e.g. amoxicillin drugs that degrade or are unstable in the colonic / intestinal environment, e.g.…”

Section: Gastroretentive Systemsmentioning

confidence: 99%

Gastroretentive microparticles for drug delivery applications

Adebisi

Conway

2011

Journal of Microencapsulation

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Many strategies have been proposed to explore the possibility of exploiting gastroretention for drug delivery. Such systems would be useful for local delivery, for drugs that are poorly soluble at higher pH or primarily absorbed from the proximal small intestine. Generally, the requirements of such strategies are that the vehicle maintains controlled drug release and exhibits prolonged residence time in the stomach. Despite widespread reporting of technologies, many have an inherent drawback of variability in transit times. Microparticulate systems, capable of distributing widely through the GI tract, can potentially minimize this variation. While being retained in the stomach, the drug content is released slowly at a desired rate,

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“…[3,4] However, the problems such as all or nothing emptying of single unit floating dosage forms made them unreliable and reproducible in prolonging gastric residence time that led to the development of multiple unit dosage forms. [5][6][7] Pyridoxine hydrochloride, i.e., vitamin B6 is having an absorption window in the upper part of GIT, i.e., jejunum. Therefore, it was considered as a good candidate for incorporating into a gastroretentive dosage form.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Kumar¹

2017

AJP

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Objective: The aim of this investigation was to prepare multiple unit floating mini matrix tablets of pyridoxine hydrochloride which is having an absorption window in the upper part of gastrointestinal tract, i.e., jejunum. Hence, this study was planned to formulate, characterize with in-vitro and in-vivo evaluation in human subjects. Materials and Methods: In this investigation, multiple unit floating mini matrix tablets of pyridoxine HCl were formulated using hydroxy propyl methyl cellulose K grade polymers along with ethyl cellulose by wet granulation method. The physicochemical characteristics of all the prepared batches were evaluated. The in-vitro buoyancy and in-vitro drug release studies were conducted in the study. Based on in-vitro buoyancy and in-vitro drug release, optimized formulation was selected and subjected to stability studies as per WHO and ICH guidelines for 6 months. The optimized formulation was further subjected to X-ray studies to establish the in-vivo gastric residence time in human volunteers by replacing the drug with X-ray grade barium sulfate. Results: The physicochemical characteristics of all the prepared batches were found to be satisfactory. All the prepared batches showed good in-vitro buoyancy and it was observed that the mini tablets remained buoyant for more than 12 h. The formulation FP8, which released complete drug release in 12 h with minimum floating lag time of 16 ± 2.54, was considered as optimized formulation. The stability studies indicated that the optimized formulation is stable during its stability period. The in-vivo radiographic studies revealed that the mini tablets remained in the stomach up to 6 h in human volunteers and altered its position without any adhesion to walls of stomach. Conclusion: Based on in-vitro characteristics and in-vivo radiographic studies, it can be concluded that the best formulation FP8 by choosing multiple unit floating matrix tablets could improve patient compliance and ensure better drug absorption.

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A New Multiple-Unit Oral Floating Dosage System. I: Preparation and In Vitro Evaluation of Floating and Sustained-Release Characteristics

Cited by 112 publications

References 11 publications

FORMULATION & EVALUATION OF BILAYER FLOATING TABLETS OF METOPROLOL TARTRATE

FORMULATION & EVALUATION OF BILAYER FLOATING TABLETS OF METOPROLOL TARTRATE

Gastroretentive microparticles for drug delivery applications

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