Design and optimization of a stomach-specific drug delivery system of repaglinide: Application of simplex lattice design

Vaghani, Subhash S.; Patel, Sneha; Jivani, Rishad R.; Jivani, N. P.; Patel, Madhabhai M.; Borda, Rohit

doi:10.3109/10837450.2010.513988

Cited by 13 publications

(6 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…They should fulfil all the primary or basic requirements of the drug product without affecting the physical and therapeutic efficacy of the active pharmaceutical ingredient. The United States Food and Drug Administration (US FDA) provides a database of excipients that have been used in approved products 35 . This database comprises inactive ingredient guide (IIG) limits of the excipients which could be useful during initial development of the products.…”

Section: Drug and Excipients Selection For Grddsmentioning

confidence: 99%

“…The results of the optimization studies showed that dependent variables were greatly affected by the polymer concentration and volume of glutaraldehyde compared with other independent variables. Vaghani et al 35 developed oral bioadhesive hydrophilic matrices of repaglinide. Simplex lattice design was employed to optimize the independent variables.…”

Section: Optimization Studies In Grddsmentioning

confidence: 99%

See 1 more Smart Citation

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Chordiya¹,

Gangurde²,

Borkar³

2017

Current Science

View full text Add to dashboard Cite

Gastroretentive drug delivery systems (GRDDS) can overcome drawbacks associated with oral drug delivery, by defeating natural physiological principles. Various gastroretentive technologies have been developed in the past, but few of them achieved commercial success. Numerous mechanisms like floating, sinking, effervescence, swelling, bioadhesion, magnetic, etc. have been proposed over the years. At present, the polymeric swellings monolithic systems are popular. Dual working technology would be a possible way to overcome drawbacks associated with different GRDDS. Before development of a drug product, the principles of scale-up and process validation must be considered to improve the quality and market availability of GRDDS. Knowledge of all regulatory aspects will help deliver a product to the market within a reasonable time-frame and in a cost-effective manner.

show abstract

Section: Drug and Excipients Selection For Grddsmentioning

confidence: 99%

Section: Optimization Studies In Grddsmentioning

confidence: 99%

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Chordiya¹,

Gangurde²,

Borkar³

2017

Current Science

View full text Add to dashboard Cite

show abstract

“…Como se trata de um polímero insolúvel em água e nos solventes orgânicos, são, em geral, utilizados os seus derivados. Nestes derivados é possível incorporar um grande número de princípios ativos, tanto hidrofílicos, como niacina [38] , fenofibrato [39] , e hidrofóbicos como o meloxican [40] , clozapina [41] , repaglidina [42] e permitem ainda estabilizar algumas substâncias fotossensíveis [43] .…”

Section: Celulose E Derivadosunclassified

Polímeros usados como sistemas de transporte de princípios ativos

Severino¹,

Santana

Malmonge

et al. 2011

Polímeros

View full text Add to dashboard Cite

Resumo: Os diferentes sistemas de transporte têm evidenciado potencial terapêutico para uma grande variedade de princípios ativos, satisfazendo vários requisitos, como a prevenção da sua eliminação rápida do organismo, a redução da sua toxicidade sistêmica, a estabilização e a otimização do seu metabolismo, e o direcionamento específico ao local alvo e os mecanismos de defesa. No entanto, têm sido reconhecidos vários outros desafios associados à liberação específica do princípio ativo ao local alvo, pelo que, para ultrapassar os obstáculos químicos e biológicos, a seleção do polímero utilizado para a preparação do sistema de transporte é de importância crucial. O presente trabalho apresenta um relato sobre os principais polímeros naturais e sintéticos utilizados para a preparação de sistemas de transporte de princípios ativos in vivo. Palavras-chaves: Polímeros sintéticos, polímeros naturais, transporte de princípios ativos. Polymers for Drug Delivery Systems FormulationsAbstract: The different carrier systems have shown therapeutic potential for a wide variety of drugs, satisfying multiple requirements, such as prevention of rapid elimination, reducing toxicity, promoting stabilization, optimization of metabolism, drug delivery and defense mechanisms. However, it has been recognized several other challenges associated with the specific release of actives in drug delivery. Therefore, to overcome chemical and biological obstacles, the selection of the polymer used to prepare the transport system is crucial. This paper presents a report on the main natural and synthetic polymers used in the preparation of drug carrier systems in vivo. Keywords: Synthetic polymers, natural polymers, carrier of drugs. IntroduçãoA investigação científica de novos meios de veiculação de princípios ativos in vivo permitiu o desenvolvimento de vários tipos de sistemas de transporte dos quais se destacam os lipossomas [1] , conjugados de polímero e princípios ativos [2] , micelas de copolímeros anfipáticos [3] , micro e nanopartículas poliméricas [4] e, mais recentemente, as nanopartículas lipídicas sólidas [5] . Os diferentes sistemas de transporte têm evidenciado potencial terapêutico para uma grande variedade de princípios ativos, preenchendo assim vários requisitos, como a prevenção da sua eliminação rápida do organismo [6] , a redução da sua toxicidade sistêmica [7] , a estabilização e a otimização do seu metabolismo [8] , o direcionamento específico ao local alvo [9] e os mecanismos de defesa [10] . No entanto, têm sido reconhecidos vários outros desafios associados à liberação específica do princípio ativo ao local alvo, pelo que, para ultrapassar os obstáculos químicos e biológicos, a seleção do polímero utilizado para a preparação do sistema de transporte é de importância crucial.Para a preparação dos sistemas poliméricos de transporte, pode recorrer-se ao uso de polímeros naturais [11] , sintéticos [12] ou semi-sintéticos [13] . A seleção do polímero a ser empregado está condicionada, em grande medida pela natureza do princípio...

show abstract

“…Although repaglinide is completely absorbed from gastrointestinal tract, it is degraded in intestine and poorly absorbed from upper intestinal tract. [15] Moreover, it is reported that it is expected to enable control of both PBG (Post-Prandial Blood Glucose) and FBG (Fasting Blood Glucose) for moderate and severe diabetes patients with a controlled release formulation containing a short-acting type oral blood glucose regulator (repaglinide, meglitinide, etc.). [16,17] The physicochemical properties of repaglinide, its half life of 1 hour, and its low dose (2-16 mg), make it suitable candidate for administration by the buccal route.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of bioadhesive buccal drug delivery of repaglinide tablets

Patel¹,

Patel²,

Shah³

2012

Asian J Pharm

View full text Add to dashboard Cite

T he purpose of this research was to formulate and evaluate bioadhesive buccal tablets of repaglinide using HPMC K15M as a sustained release polymer, chitosan as a bioadhesive polymer and ethyl cellulose as an impermeable backing layer. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling index, in vitro drug release, ex vivo mucoadhesion time and ex vivo drug permeation. A 3 2 full factorial design was used in present study for optimization. Tablets containing HPMC K15M and chitosan in the ratio of 1:1 and lactose as a filler (F2) had the maximum percentage of in vitro drug release. The swelling index, friability and in vitro drug release was affected by type of filler as dicalcium phosphate (DCP) had good binding ability compared to lactose. The surface pH of all tablets was found to be satisfactory (between 6.26 and 7.01), close to neutral pH; hence buccal cavity irritation should not occur with these tablets. F2 batch was considered optimum based on good bioadhesive strength (17.83±0.51 gm) and maximum similarity factor (64.43). The drug release from optimum batch followed zero order kinetics with non-Fickian diffusion. Drugexcipients compatibility study showed no interaction between drug and excipients. Stability study of optimized formulation showed that tablets were stable at accelerated environment condition. Thus, buccal adhesive tablet of repaglinide could be an alternative route to bypass hepatic first pass metabolism and to improve bioavailability of repaglinide.

show abstract

Design and optimization of a stomach-specific drug delivery system of repaglinide: Application of simplex lattice design

Cited by 13 publications

References 32 publications

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Polímeros usados como sistemas de transporte de princípios ativos

Formulation and evaluation of bioadhesive buccal drug delivery of repaglinide tablets

Contact Info

Product

Resources

About