Gelucire: A versatile polymer for modified release drug delivery system

Panigrahi, Kahnu Charan; Patra, Chinam Niranjan; Jena, Goutam Kumar; Ghose, Debashish; Jena, Jayashree; Panda, Santosh Kumar; Sahu, Manoranjan

doi:10.1016/j.fjps.2017.11.001

Cited by 74 publications

(58 citation statements)

References 20 publications

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“…Non-ionic emulgents can also be used such as PPO-based triblock-copolymers (Poloxamer ® [37]) and glyceride-derivatives. Gelucire ® composites are examples of non-ionic emulgents, composed of mixtures of mono, di and triglycerides with PEG esters of fatty acids [38]. In addition, several glyceryl fatty acid esters have been chosen, such as glyceryl palmitostearate (Precirol ® ATO 5, equivalent to Gelucire ® 54/02) and glyceryl behenate (Compritol ® 888, equivalent to Gelucire ® 70/02).…”

Section: Single-unit Low-density Systemsmentioning

confidence: 99%

“…This highly effective spatial arrangement is facilitated by the β-1,4 linkages between glucopyranose units. Hydrogels prepared from unsubstituted cellulose have been scarcely reported because of its insolubility in aqueous solutions and in most organic solvents [38]. In order to solubilize cellulose, various substitutions have been incorporated along the glucopyranose backbone, which help break down its crystallinity.…”

Section: Cellulose Derivativesmentioning

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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Section: Single-unit Low-density Systemsmentioning

confidence: 99%

Section: Cellulose Derivativesmentioning

confidence: 99%

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

et al. 2020

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“…Hydrophobic polymer can be used in the preparation of sustained and floating formulations. Hydrophobicity of certain carriers such as Compritol ATO 888 (COM), Gelucire 43/01(G43/ 01), Gelucire 39/01 (G39/01) and precirol ATO 05 (PRE) is the reason for their release retarding ability [13]. Hydrophobic polymer retards the hydration rate of the matrix which results variability in release profile.…”

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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“…Extreme hydrophobicity (HLB 1) of Gelucire 43/01 is the reason for its release retarding ability. 17 Due to its low melting point (43°C), it can be used for the preparation of sustained released formulations by melt granulation method. Patel et al have reported that only gelucire 43/01 based granules could not achieve the desired sustainability and to sustain the release further release rate modifiers were used.…”

Section: Introductionmentioning

confidence: 99%

Systematic Development with Quality by Design Approach of Effervescent Floating Multiple Unit Minitablets of Metoprolol Succinate using Hydrophobic Grade of Gelucire

Panda¹,

Sahu²,

Panigrahi³

et al. 2019

IJPER

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Objective: The objective of this study was to systematically develop with Quality by Design (QbD) approach of Effervescent Floating Multiple unit Minitablets (EFMM) of metoprolol succinate (MS) for once-a-day dosing using hydrophobic grade of gelucire in order to increase gastric residence time. Methods: Risk assessment using Failure Mode Effect Analysis (FMEA) was conducted and further screened using taguchi design. A Box-Behnken Design (BBD) was adopted for the process of optimization. The dissolution profile of optimised formulation was compared with the marketed formulation. Drug compatibility study and stability study were also conducted. Results: After conducting risk assessment and screening amount of gelucire 43/01(G 43/01), HPMC K15 M (HM) and NaHCO 3 (SB) were found to be as significant factor. The process of optimisation results the single dose of EFMM MS consisting of 125 mg of G 43/01, 72 mg of HM and 28 mg of SB which shows an average of Floating Lag Time (FLT) within 3 min, Floating Time (FT) of 19 hr 36 min, time to release 50% of drug (t50) of 6 hr 38 min and time to release 90% of drug (t90) of 19 hr 12 min. The optimised formulation found to have better dissolution profile as compared to the marketed formulation. The stability study revealed no significant change in various parameters before and after storage. Conclusion: It can be concluded that an optimum combination of various excipient can be used to increase the gastric residence time, sustaining the drug release and ultimately achieve the desired objective of once-a-day dosing of MS.

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Gelucire: A versatile polymer for modified release drug delivery system

Cited by 74 publications

References 20 publications

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

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

Systematic Development with Quality by Design Approach of Effervescent Floating Multiple Unit Minitablets of Metoprolol Succinate using Hydrophobic Grade of Gelucire

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