Development and evaluation of new multiple-unit levodopa sustained-release floating dosage forms

Goole, Jonathan; Vanderbist, Francis; Amighi, Karim

doi:10.1016/j.ijpharm.2006.10.018

Cited by 67 publications

(50 citation statements)

References 16 publications

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“…The energy minimizations were found to be a collective phenomenon including nonbonding interactions in the form of van der Waals forces, H bonding and electrostatic interactions (Eqs. [7][8][9]. This contributed to a stress transduction requiring a large fraction of the surface to establish connectivity between chemically transformed regions.…”

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confidence: 99%

Design of an Interpolyelectrolyte Gastroretentive Matrix for the Site-Specific Zero-Order Delivery of Levodopa in Parkinson’s Disease

et al. 2013

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Abstract. This study focused on developing a gastroretentive drug delivery system employing a triplemechanism interpolyelectrolyte complex (IPEC) matrix comprising high density, swelling, and bioadhesiveness for the enhanced site-specific zero-order delivery of levodopa in Parkinson's disease. An IPEC was synthesized and directly compressed into a levodopa-loaded matrix employing pharmaceutical technology and evaluated with respect to its physicochemical and physicomechanical properties and in vitro drug release. The IPEC-based matrix displayed superior mechanical properties in terms of matrix hardness (34-39 N/mm) and matrix resilience (44-47%) when different normality's of solvent and blending ratios were employed. Fourier transform infrared spectroscopy confirmed the formation of the IPEC. The formulations exhibited pH and density dependence with desirable gastro-adhesion with Peak Force of Adhesion ranging between 0.15 and 0.21 N/mm, densities from 1.43 to 1.54 g/cm 3 and swellability values of 177-234%. The IPEC-based gastroretentive matrix was capable of providing site-specific levodopa release with zero-order kinetics corroborated by detailed mathematical and molecular modeling studies. Overall, results from this study have shown that the IPEC-based matrix has the potential to improve the absorption and subsequent bioavailability of narrow absorption window drugs, such as levodopa with constant and sustained drug delivery.

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confidence: 99%

Design of an Interpolyelectrolyte Gastroretentive Matrix for the Site-Specific Zero-Order Delivery of Levodopa in Parkinson’s Disease

et al. 2013

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“…Various gastro-retentive drug delivery approaches in practice include high density (sinking) 8 systems that are retained at the bottom of the stomach , low density (floating systems, that causes buoyancy in 9,10 gastric fluid) , mucoadhesive systems (causes bio- 11 adhesion to stomach mucosa) , unfoldable, extendible,…”

Section: Gastro-retentive Drug Deliverymentioning

confidence: 99%

Floating Microspheres - An Excellent Approach for Gastric Retention

Sudheer¹,

Kumar²,

Thomas³

et al. 2015

Journal of Pharmaceutical Research

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Background:The gastro-retentive system is one of the promising oral drug delivery system due to its ability to remain in the gastric region for a longer period. This helps in improving the bioavailability by increasing the solubility and reducing drug wastage. Approach: Various approaches have been put forward to achieve the gastro-retentive property. Among them, floating (hollow) microsphere is the most prominent approach. Findings: Hollow microspheres are spherical free flowing powders in the size range of 1-1000 m without core. It is prepared using proteins or synthetic polymers. This buoyant system improves gastric retention, sustains the drug release, and hence reduces the fluctuations in plasma drug concentration. Conclusion: This review presents an insight into recent advances in methods of fabrication, evaluation and applications of hollow microspheres as gastro-retentive drug delivery systems.

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“…As was shown in Figure 6, the release rate of the drug increased proportionally with the decrease in diameter. This could be attributed to the higher relative surface area of the dosage form when the diameter decreased, this result to a proportionately greater area of contact between the tablets and the solution (Goole et al, 2007). Photographs taken of different diameters of famotidine tablets were shown in Figure 7.…”

Section: Influence Of Tablet Diameter On the Drug Releasementioning

confidence: 99%

Preparation of multiple-unit floating-bioadhesive cooperative minitablets for improving the oral bioavailability of famotidine in rats

Zhu

et al. 2014

Drug Delivery

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The aims of this study were to prepare fine famotidine-containing floating-bioadhesive cooperative minitablets and to investigate the possibility of using those minitablets as a delivery system for promoting the oral bioavailability of famotidine. Nine minitablet formulations were designed using hydroxypropylmethylcellulose (HPMC K4M) as releaseretarding polymers, Carbopol 971P as bioadhesive materials and sodium bicarbonate (NaHCO 3 ) as gas formers. The prepared 3 ± 0.02 mm minitablets were evaluated in terms of their swelling ability, floating behavior, bioadhesion test and in vitro release. The optimized minitablets (F6) containing HPMC K4M (50.00%, w/w), Carbopol 971P (10.00%, w/w) and NaHCO 3 (10.00%, w/w) were found to float in 1 min and remain lastingly buoyant over a period of 8 h in vitro, with excellent bioadhesive properties (20.81 g) and sustained drug release characteristics (T 50% ¼ 46.54%) followed one-order model. In addition, plasma concentration-time profiles from pharmacokinetic studies in rats dosed with minitablets showed 1.62-fold (p50.05) increased absorption of famotidine, compared to the market tablets XinFaDing Õ . These studies demonstrated that the multiple-unit floating-bioadhesive cooperative minitablets may be a promising gastro-retentive delivery system for drugs that play a therapeutic role in the stomach.

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Development and evaluation of new multiple-unit levodopa sustained-release floating dosage forms

Cited by 67 publications

References 16 publications

Design of an Interpolyelectrolyte Gastroretentive Matrix for the Site-Specific Zero-Order Delivery of Levodopa in Parkinson’s Disease

Design of an Interpolyelectrolyte Gastroretentive Matrix for the Site-Specific Zero-Order Delivery of Levodopa in Parkinson’s Disease

Floating Microspheres - An Excellent Approach for Gastric Retention

Preparation of multiple-unit floating-bioadhesive cooperative minitablets for improving the oral bioavailability of famotidine in rats

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