Oral solid gentamicin preparation using emulsifier and adsorbent

Ito, Yoshiaki; Kusawake, Tomohiro; Ishida, M.; Tawa, Riichi; Shibata, Nobuhito; Takada, Kanji

doi:10.1016/j.jconrel.2005.03.017

Cited by 103 publications

(58 citation statements)

References 19 publications

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“…The solid carriers used include microcrystalline cellulose and colloidal silicon dioxide. The carrier's chosen can adsorb at high levels up to 70% (w/w) (13)…”

Section: Conversion To Solid Intermediates Of Self-microemulsifying Fmentioning

confidence: 99%

Solid Self-Microemulsifying Formulation for Candesartan Cilexetil

et al. 2009

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Abstract. Sparingly, water-soluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability. The objective of the present study was to develop and characterize self-microemulsifying drug delivery system (SMEDDS) of candesartan cilexetil for filling into hard gelatin capsules. Solubility of candesartan cilexetil was evaluated in various nonaqueous careers that included oils, surfactants, and cosurfactants. Pseudoternary phase diagrams were constructed to identify the self-microemulsification region. Four self-microemulsifying formulations were prepared using mixtures of oils, surfactants, and cosurfactants in various proportions. The self-microemulsification properties, droplet size, and zeta potential of these formulations were studied upon dilution with water. The optimized liquid SMEDDS formulation was converted into free flowing powder by adsorbing onto a solid carrier for encapsulation. The dissolution characteristics of solid intermediates of SMEDDS filled into hard gelatin capsules was investigated and compared with liquid formulation and commercial formulation to ascertain the impact on self-emulsifying properties following conversion. The results indicated that solid intermediates showed comparable rate and extent of drug dissolution in a discriminating dissolution medium as liquid SMEDDS indicating that the self-emulsifying properties of SMEDDS were unaffected following conversion. Also, the rate and extent of drug dissolution for solid intermediates was significantly higher than commercial tablet formulation. The results from this study demonstrate the potential use of SMEDDS as a means of improving solubility, dissolution, and concomitantly the bioavailability.

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“…The solid carriers used include microcrystalline cellulose and colloidal silicon dioxide. The carrier's chosen can adsorb at high levels up to 70% (w/w) (13)…”

Section: Conversion To Solid Intermediates Of Self-microemulsifying Fmentioning

confidence: 99%

Solid Self-Microemulsifying Formulation for Candesartan Cilexetil

et al. 2009

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“…The well known poor gastrointestinal membrane permeability and the consequent low bioavailability (class III of the biopharmaceutical classification system) are likely connected to the high polarity of this cationic compound. Various approaches have been investigated in order to increase GM oral bioavailability, including the co-administration of absorption-enhancing agents such as surfactants (Hu et al, 2001;Ito et al, 2005), bile salts and glucosteroids (Axelrod et al, 1998), and liposaccharides (Ross et al, 2004). Although good gastrointestinal absorptionenhancing effects were demonstrated, cytotoxicity and damage to the mucosa have been reported (Swenson et al, 1994;Aungst, 2000;Ross et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Microparticulate polyelectrolyte complexes for gentamicin transport across intestinal epithelia

et al. 2010

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“…This solid mixture is filled into capsule or added to more excipient before compression into tablets. 18 The above mixture was solidified to powder forms using three kinds of adsorbents: microporous calcium silicate (FloriteTM RE); magnesium aluminum silicate (NeusilinTMUS2) and silicon dioxide (SylysiaTM 320).…”

Section: Solid Carriersmentioning

confidence: 99%

Self-Emulsifying Drug Delivery Systems: A Review

Reza

2013

Int. J. Pharma Life Sci.

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Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble or lipophilic drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro-or nanoemulsions containing the solubilized drug. Owing to its miniscule globule size, the micro/nanoemulsified drug can easily be absorbed through lymphatic pathways, bypassing the hepatic first-pass effect. But it has drawbacks as formulation development, quality control, stability etc. These liquid SEDDS can be converted into solid dosage form without affecting drug release property. After administering the drug gets released and self emulsify in the GI tract. Generally solid SEDDS are formed with mono, di or triglycrides of fatty acid, non ionic surfactants and solidifying agents with diluents such as microcrystalline cellulose, lactose etc.

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Oral solid gentamicin preparation using emulsifier and adsorbent

Cited by 103 publications

References 19 publications

Solid Self-Microemulsifying Formulation for Candesartan Cilexetil

Solid Self-Microemulsifying Formulation for Candesartan Cilexetil

Microparticulate polyelectrolyte complexes for gentamicin transport across intestinal epithelia

Self-Emulsifying Drug Delivery Systems: A Review

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