Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index

Sood, Anurag; Panchagnula, Ramesh

doi:10.1016/s0378-5173(03)00267-9

Cited by 48 publications

(25 citation statements)

References 11 publications

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“…The goal is to give a drug at a sufficient rate, frequency and dose so that the ratio C max /C min in plasma at steady state is always maintained at effective concentrations during the course of therapy, reducing side effects or improving physicochemical and biopharmaceutical properties. A number of controlled release drug delivery systems such as oral, transdermal, injectable and implantable drug delivery systems have been investigated (Sood, Panchagnula, 2003;Sun et al, 2003).…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Campos

Cassimiro

Crespi

et al. 2013

Braz. J. Pharm. Sci.

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A hydrogel was developed from 70 kDa dextran (DEX-70) and praziquantel (PZQ) incorporated as a model drug. Biopharmaceutical properties, such as solubility and dissolution rate, were analysed in the design of the hydrogel. Furthermore, the hydrogel was also characterized by IR spectroscopy and DSC. Tests of the swelling rate showed that the hydrogel swelled slowly, albeit faster than the rate for the free polymer. In dissolution tests, the hydrogel released the drug slowly and continuously. This slow release was similar to that observed in the swelling tests and resulted in controlled release of the drug. Thus, this dextran is a suitable polymer for the development of hydrogels as vehicles for the controlled release of drugs.Uniterms: Hydrogel/development. Hydrogel/biopharmaceutical properties. Dextran/hydrogel development. Praziquantel/controlled release. Hydrogel/swelling test.Um hidrogel foi desenvolvido a partir de dextrano 70 kDa (DEX-70) e praziquantel incorporado (PZQ) como fármaco modelo. Propriedades biofarmacêuticas, como solubilidade e velocidade de dissolução, foram analisadas no desenvolvimento do hidrogel. Além disso, o hidrogel também foi caracterizado por espectroscopia na região do infravermelho e calorimetria diferencial exploratória (DSC). Testes da taxa de intumescimento mostraram que o hidrogel intumesce lentamente, embora tenha sido mais rápido do que a taxa do polímero livre. Nos testes de dissolução, o hidrogel liberou o fármaco lenta e continuamente. Esta liberação lenta foi semelhante a observada nos testes de intumescimento e resultou em uma liberação controlada do fármaco. Assim, o dextrano 70 kDa é um polímero adequado para o desenvolvimento de hidrogéis como veículos para a liberação controlada de fármacos.Unitermos: Hidrogel/desenvolvimento. Hidrogel/propriedades biofarmacêuticas. Dextrano/ desenvolvimento de hidrogel. Praziquantel/liberação controlada. Hidrogel/teste de intumescimento.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Campos

Cassimiro

Crespi

et al. 2013

Braz. J. Pharm. Sci.

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“…While an effective drug against more than 80% of MDR-TB clinical strains, ETH has a low therapeutic index, or margin of safety, characterized by a narrow therapeutic effective concentration range (Sood & Panchagnula, 2003, Zimmerman et al, 1984. In other words, it is more difficult to prescribe ETH treatment doses that ensure effective treatment outcomes and yet avoid toxic side effects (Burns, 1999).…”

Section: Ethionamidementioning

confidence: 99%

Potentiation of Available Antibiotics by Targeting Resistance – An Emerging Trend in Tuberculosis Drug Development

Wolff¹,

Sherman²,

Nguyen³

2011

Drug Development - A Case Study Based Insight Into Modern Strategies

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“…Oral controlled drug delivery system is useful to maintain therapeutically effective plasma drug concentration levels for a longer duration thereby reducing the dosing frequency and to minimize fluctuations in the plasma drug concentration at the steady state by delivering the drug in a controlled and reproducible manner [1]. Moreover, it is easy for administration, no patient compliances, and flexibility in the formulation.…”

Section: Introductionmentioning

confidence: 99%

Design and Evaluation of Intragastric Buoyant Tablets of Venlafaxine Hydrochloride

Radhika¹,

Nishala²,

Kiruthika³

et al. 2017

Asian J Pharm Clin Res

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Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate the intragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulations were formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration of drug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent. Methods:The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitro buoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion. Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimized formulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMC K100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studies and was found to be stable as no significant change was observed in various evaluated parameters of the formulation. Conclusion:It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach to increase gastric residence time, thereby improving its bioavailability.

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Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index

Cited by 48 publications

References 11 publications

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Preparation and characterisation of Dextran-70 hydrogel for controlled release of praziquantel

Potentiation of Available Antibiotics by Targeting Resistance – An Emerging Trend in Tuberculosis Drug Development

Design and Evaluation of Intragastric Buoyant Tablets of Venlafaxine Hydrochloride

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