Formulation and evaluation of multiple tablets as a biphasic gastroretentive floating drug delivery system for fenoverine

Bandari, Suresh; Eaga, Chandra Mohan; Thadishetty, Ashok; Yamsani, Madhusudan Rao

doi:10.2478/v10007-010-0001-3

Cited by 21 publications

(9 citation statements)

References 9 publications

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“…Biphasic release (Table 3) can offer effective, safe and convenient delivery of many APIs including non-steroidal anti-inflammatory drugs, antihypertensive, antihistaminic and anti-allergic agents [127,204]. Many different types of dosage forms providing biphasic release have been reported in the literature [89,201,[293][294][295]. Biphasic release is different from the simple occurrence of an uncontrolled initial burst of release; the latter is a negative phenomenon frequently seen with sustained release profiles [239], particularly in monolithic electrospun medicated nanofibers composed of a drug encapsulated in a water insoluble polymer [156].…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

244

156

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The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This method uses electrical energy to induce changes from liquid to solid. Through the direct applications of electrical energy, electrospinning can generate nanofiber-based ASDs from drug-loaded solutions, melts and melt-solutions. The technique can also be combined with other approaches using the application of mechanical, thermal or other energy sources. Electrospinning has numerous advantages over other approaches to produce ASDs. These advantages include extremely rapid drying speeds, ease of implentation, compatibility with a wide range of active ingredients (including those which are thermally labile), and the generation of products with large surface areas and high porosity. Furthermore, this technique exhibits the potential to create so-called 'fifth-generation' ASDs with nanostructured architectures, such as core/shell or Janus systems and their combinations. These advanced systems can improve dissolution behaviour and provide programmable drug release profiles. Additionally, the fiber components and their spatial distributions can be precisely controlled. Electrospun fiber-based ASDs can maintain an incorporated active ingredient in the amorphous physical form for prolonged periods of time because of their homogeneous drug distribution within the polymer matrix (typically they comprise solid solutions), and ability to inhibit molecular motion. These ASDs can be utilised to generate oral dosage forms for poorly water-soluble drugs, resulting in linear or multiple-phase release of one or more APIs. Electrospun ASDs can also be exploited as templates for manipulating molecular self-assembly, offering a bridge between ASDs and other types of dosage forms. This review addresses the development, advantages and pharmaceutical applications of electrospinning for producing polymeric ASDs. Material preparation and analysis procedures are considered. The mechanisms through which performance has been improved are also discussed.

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Section: Accepted Manuscriptmentioning

confidence: 99%

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Williams

et al. 2018

Journal of Controlled Release

244

156

View full text Add to dashboard Cite

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“…For some active pharmaceutical ingredients (API) such as non-steroidal anti-inflammatory drugs (NSAIDs), as well as antihypertensive, antihistaminic and anti-allergic agents, an initial fast release of a fraction of the dose in the shortest time after administration is in favor of relieving the symptoms of the disease [17]. Meanwhile, a sustained release of the remaining dose over a defined period can optimize the therapy and avoid repeated administration for the patients’ convenience [18,19]. …”

Section: Introductionmentioning

confidence: 99%

Dual Drug Release Electrospun Core-Shell Nanofibers with Tunable Dose in the Second Phase

Qian

et al. 2014

IJMS

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This study reports a new type of drug-loaded core-shell nanofibers capable of providing dual controlled release with tunable dose in the second phase. The core-shell nanofibers were fabricated through a modified coaxial electrospinning using a Teflon-coated concentric spinneret. Poly(vinyl pyrrolidone) and ethyl cellulose were used as the shell and core polymer matrices respectively, and the content of active ingredient acetaminophen (APAP) in the core was programmed. The Teflon-coated concentric spinneret may facilitate the efficacious and stable preparation of core-shell nanofibers through the modified coaxial electrospinning, where the core fluids were electrospinnable and the shell fluid had no electrospinnability. The resultant nanofibers had linear morphologies and clear core-shell structures, as observed by the scanning and transmission electron microscopic images. APAP was amorphously distributed in the shell and core polymer matrices due to the favorite second-order interactions, as indicated by the X-ray diffraction and FTIR spectroscopic tests. The results from the in vitro dissolution tests demonstrated that the core-shell nanofibers were able to furnish the desired dual drug controlled-release profiles with a tunable drug release amount in the second phase. The modified coaxial electrospinning is a useful tool to generate nanostructures with a tailored components and compositions in their different parts, and thus to realize the desired functional performances.

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“…The density of the SR minitablets (in g cm À3 ) was calculated from tablet height, diameter and mass using the equation (Bandari et al, 2010)…”

Section: Characterization Of Granules and Minitabletsmentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

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Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

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Formulation and evaluation of multiple tablets as a biphasic gastroretentive floating drug delivery system for fenoverine

Cited by 21 publications

References 9 publications

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review

Dual Drug Release Electrospun Core-Shell Nanofibers with Tunable Dose in the Second Phase

Design and characterization of cefuroxime axetil biphasic floating minitablets

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