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

Thapa, P.; Jeong, Seong Hoon

doi:10.3390/pharmaceutics10030161

Cited by 62 publications

(45 citation statements)

References 65 publications

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“…Nonetheless, no systematic study has yet been carried out to investigate the effect of sodium bicarbonate on drug release kinetics, so it is important to investigate its impact in the effervescent process on drug release kinetics of higher water-soluble drugs.The gas entrapped membrane was usually observed during storage leading to failures in floating and sustained release these can be overcome by the using glyceryl monostearate and talc as an anti-tacking agent. [18,19] As shown in Figure 2. The effervescent reaction among carbonate/bicarbonate salts, citric/tartic acid, CO2 is released in presence of water when the formulation is put in the beaker it will sink with a production of gas it rises up and floats.…”

Section: )Effervescent Floating Drug Delivery Systemsmentioning

confidence: 91%

Current Approaches on Gastroretentive Drug Delivery systems

Pund

Shendge

Pote

2020

J. Drug Delivery Ther.

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Over recent years, there have been many efforts to develop the absorption rate of medications and the therapeutic efficacy of oral dosage types. GRDDS for strengthen the pharmacological effects of drugs with a small uptake site, are unbalanced at pH greater than 7, are dissolved under acidic region, and are effective local region in the stomach. The gastro retentive systems that have the different evaluation parameter that according to the dosage forms. There are many criteria for the choosing of the drug used in the gastro-retardant systems as the drug should be sparingly stable, it should be compatible with the gastric region, and narrow absorption. In this review, we have summarized the information related to the various approaches for enhancing and prolonging of the dosage forms in the stomach for their extended-release of action. Also talking about the many natural and synthetic polymers is used in the formulation with their different grade and their ratio that affects on the release action. The many scientist and inventors have increased their interest in developing the novel dosage forms and they staying in the stomach for showing the prolonged period action. We have also discussed the novel technology are involved in the gastric retention many companies has been developed the polymer grades for using it in the formulation for showing the retention action. Keywords: Introduction, Approaches, Novel technologies, Polymer used in floating systems.

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Section: )Effervescent Floating Drug Delivery Systemsmentioning

confidence: 91%

Current Approaches on Gastroretentive Drug Delivery systems

Pund

Shendge

Pote

2020

J. Drug Delivery Ther.

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“…Floating tablets are composed of swellable hydrophilic matrix forming polymers that swell in contact with gastric fluids, and the air entrapped in the hydrated polymers bestows the buoyancy [81]. Both for single-and bi-layered tablets, non-ionic hydrophilic polymers, such as HPMC, HPC and poly(ethylene oxide) (PEO), are commonly employed since they are not affected by pH [8]. HPMC is the most widely used material with low viscosity grades chosen for floating purpose [29].…”

Section: Floating Tabletsmentioning

confidence: 99%

“…Floating tablets are commonly chosen for the controlled release of hydrophobic active pharmaceutical ingredients (APIs) and are the formulation of choice for potent drugs [86] since it is challenging to maintain tablet buoyancy in high-dose tablets due to their high bulk density [8]. For promoting the dissolution of hydrophobic drugs, the incorporation of a surfactant to the hydrophilic polymeric matrix could be necessary in order to reduce the crystallinity of the drugs, thereby increasing the aqueous solubility and dissolution rate of the APIs [87].…”

Section: Floating Tabletsmentioning

confidence: 99%

“…Xanthan gum is an anionic material, soluble in warm or cold water, and is insoluble in ethanol and ether. Its solutions at low concentration are highly viscous and stable in a wide range of pH (3)(4)(5)(6)(7)(8)(9)(10)(11)(12) and temperatures (10-60 • C), as well as in the presence of enzymes and salts. Consequently, it can be used as a stabilizing agent, gelling agent, viscosity-increasing agent and thickening agent [76].…”

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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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“…For a long time, oral-controlled release (CR) formulations are popularly used for controlling the release of drugs. Short transit time of drug with the absorption window in the stomach causes the release of drug in the non-absorbing distal segment of GIT leading to poor bioavailability [1,2]. These features are responsible for the design of gastroretentive formulations [3,4].…”

Section: Introductionmentioning

confidence: 99%

Formulation and development of floating multiple-unit minitablets of Nimodipine without using a gas-generating agent: in vitro and in vivo characterization

et al. 2020

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Background: Floating drug delivery systems have been reported for different active pharmaceutical ingredients as single-unit tablets with gas-generating agents. In this present research, the formulation of floating multiple-unit minitablets of Nimodipine without using gas-generating agent was attempted with an objective of increased residence time, sustain-release and improved oral bioavailability. Solid dispersion with different ratios (1:0.5, 1:1, 1: 1.5, 1:2, 1:2.5) of drug with the lipophilic carrier such as Compritol ATO 888, Gelucire 43/01, G39/01 and Precirol ATO 05 was formulated using melt granulation technique. The adsorbent Sylysia 350 to lipophilic carrier is maintained at 1:1. The granules were compressed into minitablets weighing 15 mg and were filled into a '0' size capsule.Results: Differential scanning calorimetry study justified no interaction of the drug with excipients. The formulations which exhibited desirable flow property, floating lag time less than 1 min and floating time of 12 h were further characterized for various post-compression parameters. The optimized single-dose (capsule) of floating multiple-unit minitablets of Nimodipine consisting of 60 mg of drug, 120 mg of G43/01 and 120 mg of Sylysia 350 showed an average of floating lag time within 24.48 s, floating time of 14.32 h and sustained-release up to 12 h. Pharmacokinetic study of the optimized formulation (F9) showed nearly 2.5 times increase in area under the curve with increased residence time in comparison to aqueous suspension of Nimodipine. The stability study revealed no significant change in various parameters before and after storage.Conclusion: Hence, gelucire 43/01-based multiple-unit minitablets of Nimodipine can be considered a promising approach for sustaining the drug release with gastric retention for 12 h without using gas-generating agent.

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

Cited by 62 publications

References 65 publications

Current Approaches on Gastroretentive Drug Delivery systems

Current Approaches on Gastroretentive Drug Delivery systems

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

Formulation and development of floating multiple-unit minitablets of Nimodipine without using a gas-generating agent: in vitro and in vivo characterization

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