Formulation and evaluation of a pulsatile drug delivery system using time- and pH-dependant polymers

Kadam, Vinayak D.; Gattani, Surendra G.

doi:10.1080/10837450902980254

Cited by 3 publications

(3 citation statements)

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“…For tablets, simulation of gastrointestinal transit conditions was achieved by using different dissolution media. Thus, drug release studies were conducted in simulated gastric fluid without pepsin (SGF, pH 1.2) for the first 2 h as the average gastric emptying time is about 2 h. Then, the dissolution medium was replaced with enzyme-free simulated intestinal fluid (SIF, pH 6.8) and tested for drug release for 3 h, as the average small intestinal transit time is about 3 h, and finally enzyme-free simulated colonic fluid (SCF, pH 7.4) was used for 2 h to mimic colonic pH conditions [12]. Drug release was measured from coated tablets, added to 900 mL of dissolution medium.…”

Section: Drug Release Studies Of Coated Tabletsmentioning

confidence: 99%

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

et al. 2017

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Rheumatoid arthritis is an auto immune disease which requires chronotherapy as it occurs during early morning. Tramadol hydrochloride (TH) is an analgesic drug, used to treat rheumatoid arthritis. The aim of the present investigation was to develop chronomodulated drug delivery system of tramadol hydrochloride such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of TH, initially core tablets of TH were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit S100 was optimized and coating tablets of TH was prepared. The prepared coated tablets were evaluated for weight variation, hardness, drug content and in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 7.5% of coating solution (ES2) had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. DSC studies revealed that no interaction between core and coated materials with drug was observed. Thus, chronomodulated drug delivery system of TH was formulated and assuming that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am.

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Section: Drug Release Studies Of Coated Tabletsmentioning

confidence: 99%

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

et al. 2017

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“…The amount of surfactant required depends on the CMC and the degree to which the compound partitions into the surfactant micelles 48 . 55 .…”

Section: Surfactantsmentioning

confidence: 99%

Solubility and Dissolution Enhancement: Technologies and Research Emerged

Kataria¹,

Bhandari²

2013

J Biol Sci Opin

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Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system.Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. About 40 % drugs from newly developed chemical entities are lipophilic and fail to reach market due to their poor water solubility. The solubility behavior of drugs remains one of the most challenging aspects in formulation development. The bioavailability of an orally administration drug depends on its solubility in aqueous media over different pH ranges. The insufficient dissolution rate of the drug is the limiting factor in the oral bioavailability of poorly water soluble compounds. Most of drugs are weakly acidic and weakly basic with poor aqueous solubility.Various techniques are used for the improvement of aqueous solubility, dissolution rate and bioavailability of poorly water soluble drugs include micronization, chemical modification, pH adjustment, solid dispersion, nanosuspension, superdisintegrant, liquisolid technique, complexation, co-solvency, micellar solubilization, hydrotrophy etc. The purpose of this review article is to describe the techniques of solubilizaton and research materialized for the attainment of effective absorption and improved bioavailability.

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“…Принцип сочетания противоположно заряжённых типов эудрагитов оказался наиболее востребованным при конструировании систем доставки ЛВ в толстый отдел кишечника [2,13,14,23]. Идея заключается в том, что наружное покрытие из кишечнорастворимых марок Eudragit ® L100/S100 обеспечивает целенаправленную доставку, а рН-независимый внутренний слой из RL100/RS100 контролирует равномерность выхода ЛВ в оптимальном месте его всасывания.…”

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Intermacromolecular interactions with Eudragit® copolymers as a new principle of the microparticulate oral drug delivery systems development

Moustafine

2016

Kazan Med J

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The main trends of combining the chemically complementary types of (meth)acrylic copolymers of pharmaceutical-grade - Eudragit® in oral microparticulate systems with modified release (spheres, granules, capsules, etc.) - and the technological methods used in their manufacture, including various types of coating (single-layer, multi-layered, combined) are considered. It is noted that the processes that control the drugs release are based on pH-dependent intermacromolecular interaction of reactive groups between a pair of opposite charged Eudragit® copolymers both inside of spherical micro-matrix and inside the multilayer and combined coatings, allowing regulating both the degree and time of active pharmaceutical ingredients (API) release from pharmaceutical form. Using this principle allows to develop time-sensitive and pH-sensitive systems with a targeted API delivery to predetermined parts of the gastrointestinal tract, preferably to the colon, which is not only the optimal zone for absorption of many API, but also often requires treatment of inflammatory diseases of different origin. Analysis of these processes is of key importance to a better understanding of the mechanisms underlying the API transport from considered systems types, methods of their correction, modification of macromolecular parameters (such as the copolymer units charge density, the stoichiometry of the produced composition, the hydrophilic and hydrophobic fragments ratio in the polycomplexes structure affecting the swelling and resulting permeability of the system), as well as perspectives of (meth)acrylate polycomplexes use as a new class of carriers in the design of modern self-regulating, depending on the gastrointestinal tract physiological fluids pH, microparticulate oral API delivery systems.

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Formulation and evaluation of a pulsatile drug delivery system using time- and pH-dependant polymers

Cited by 3 publications

References 0 publications

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride

Solubility and Dissolution Enhancement: Technologies and Research Emerged

Intermacromolecular interactions with Eudragit® copolymers as a new principle of the microparticulate oral drug delivery systems development

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