Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics

Kim, Seongkyu; Hwang, Kyu-Mok; Park, Yoong Sik; Nguyen, Thi-Tram; Park, Eun-Seok

doi:10.1016/j.ijpharm.2018.08.038

Cited by 55 publications

(49 citation statements)

References 38 publications

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“…The floating systems are categorized into non-effervescent systems and effervescent systems. In the case of non-effervescent systems, highly swellable cellulose derivatives or gel-forming polymers are used, which is preferable for potent drugs [ 13 , 14 , 15 ]. However, in effervescent systems, gas generating agents, such as sodium bicarbonate and calcium carbonate are used, which generate CO 2 gas upon contact with gastric fluid, and eventually reduce the bulk density of tablets [ 16 , 17 , 18 , 19 ].…”

Section: Introductionmentioning

confidence: 99%

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Thapa

Jeong

2018

Pharmaceutics

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To develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethylene oxide WSR 303 (PEO), sodium bicarbonate, and tablet compression force were used as independent variables. Various times required to release the drug, tablet tensile strength, floating lag time, tablet ejection force, and tablet porosity, were selected as the responses. Polymer screening showed that PEO had the highest gel strength among the various tested polymers. Sodium bicarbonate had the most significant effect on the release rate and floating lag time by retarding the rate from the hydrophilic matrices, whilst tablet compression force and PEO exerted the greatest influence on tablet properties (p < 0.0001). The design space was built in accordance with the drug release profiles, tensile strength, and floating lag time, following failure probability analysis using Monte Carlo simulations. The kinetic modeling revealed that the release mechanism was best described by the Korsmeyer-Peppas model. Overall, the current study provided a perspective on the systematic approach of gastro-retentive EFT, loaded with highly water-soluble drugs by applying quality by design concepts.

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Section: Introductionmentioning

confidence: 99%

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Thapa

Jeong

2018

Pharmaceutics

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“…The benefits of low density/floating systems are rooted on the buoyancy of the dosage in the gastrointestinal fluids. Its bulk density must be lower than that found in gastric fluids (1.004-1.010 g/mL) to ensure their floatability on the gastric fluid and hence to prolong their GRT [18] (4-24 h depending on the system) [26]. A low-density system requires high fluid levels in the stomach to float and work effectively and to avoid gastric irritation.…”

Section: Single-unit Low-density Systemsmentioning

confidence: 99%

“…Non effervescent systems incorporate a high level (20-75% w/w) of one or more such swellable matrix-forming polymers [16]. Generally the floatability can be improved by the incorporation of wicking agents or swelling enhancers [84] such as the hydrophilic polymeric excipients crospovidone (polyvinylpolypyrrolidone, PVPP) or microcrystalline cellulose (MCC) [26], sodium croscarmellose (cross-linked NaCMC) [46] and sodium carboxymethyl starch [46], which can increase the swelling rate to maintain the buoyancy of the tablets.…”

Section: Floating Tabletsmentioning

confidence: 99%

“…In this case, the latter may contain a disintegrating agent to facilitate its deconstruction [47] such as NaCMC, whose erosion properties are responsible for the disintegration of HPMC-Carbopol-based propranolol floating tablets [44]. Many of the swelling agents mentioned above can play this deconstruction role in floating tablets [26,47]. For example, the addition of the hygroscopic crosslinked crospovidone (Kollidon CL) is frequently used due to its excellent swelling characteristics that makes it useful as a disintegrant in pharmaceutical dosage forms [26].…”

Section: Floating Tabletsmentioning

confidence: 99%

“…Its use is usually linked to other widely used polymers such as sodium alginate and HPMC. For example, Kim et al [26] prepared new HPMC-based gastroretentive non-effervescent tablets with floating and swelling properties for once-daily administration of pregabalin in which the amount of HPC and crospovidone (cross-linked poly(vinyl pyrrolidone), PVP) were found to be critical factors affecting in vitro dissolution and floating properties of the prepared tablets. Qi et al [54] reported the development of ofloxacin floating tablets comprised of HPC as a compression coating agent, sodium alginate as a drug release modifier and sodium bicarbonate as an effervescent agent.…”

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confidence: 99%

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In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

et al. 2020

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The extensive use of oral dosage forms for the treatment of diseases may be linked to deficient pharmacokinetic properties. In some cases the drug is barely soluble; in others, the rapid transit of the formulation through the gastrointestinal tract (GIT) makes it difficult to achieve therapeutic levels in the organism; moreover, some drugs must act locally due to a gastric pathology, but the time they remain in the stomach is short. The use of formulations capable of improving all these parameters, as well as increasing the resident time in the stomach, has been the target of numerous research works, with low-density systems being the most promising and widely explored, however, there is further scope to improve these systems. There are a vast variety of polymeric materials used in low-density gastroretentive systems and a number of methods to improve the bioavailability of the drugs. This works aims to expedite the development of breakthrough approaches by providing an in-depth understanding of the polymeric materials currently used, both natural and synthetic, their properties, advantages, and drawbacks.

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Utilizing 4D Printing to Design Smart Gastroretentive, Esophageal, and Intravesical Drug Delivery Systems

Mahmoud

Schulz‐Siegmund

2023

Adv Healthcare Materials

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The breakthrough of 3D printing in biomedical research has paved the way for the next evolutionary step referred to as four dimensional (4D) printing. This new concept utilizes the time as the fourth dimension in addition to the x, y, and z axes with the idea to change the configuration of a printed construct with time usually in response to an external stimulus. This can be attained through the incorporation of smart materials or through a preset smart design. The 4D printed constructs may be designed to exhibit expandability, flexibility, self-folding, self-repair or deformability. This review focuses on 4D printed devices for gastroretentive, esophageal, and intravesical delivery. The currently unmet needs and challenges for these application sites are tried to be defined and reported on published solution concepts involving 4D printing. In addition, other promising application sites that may similarly benefit from 4D printing approaches such as tracheal and intrauterine drug delivery are proposed.

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Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics

Cited by 55 publications

References 38 publications

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

Utilizing 4D Printing to Design Smart Gastroretentive, Esophageal, and Intravesical Drug Delivery Systems

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