Redispersible Dry Emulsion System as Novel Oral Dosage Form of Oily Drugs: In Vivo Studies in Beagle Dogs.

Takeuchi, Hirofumi; Sasaki, Hideto; Niwa, Toshiyuki; Hino, Tomoaki; Kawashima, Yasunaru; Uesugi, Kentaro; Ozawa, Hiroshi

doi:10.1248/cpb.39.3362

Cited by 37 publications

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“…In recent years, dry forms of emulsions have been developed as improved formulations for pharmaceuticals [Takeuchi et al, 1991;Vyas et al, 1992;Sastre et al, 2004;Harris et al, 2004;Steckel and Brandes, 2004;Hansen et al, 2005;Jang et al, 2006;Cui et al, 2007]. They are based on lipids from which an oil-inwater (o/w) emulsion easily reconstitutes upon aqueous dilution [Farah et al, 1987] or after in vivo adminis-tration [Takeuchi et al, 1991, Jang et al, 2006Ahmed and Aboul-Einein, 2007].…”

Section: Introductionmentioning

confidence: 99%

“…They are based on lipids from which an oil-inwater (o/w) emulsion easily reconstitutes upon aqueous dilution [Farah et al, 1987] or after in vivo adminis-tration [Takeuchi et al, 1991, Jang et al, 2006Ahmed and Aboul-Einein, 2007]. Unlike liquid emulsions, dry emulsions are far less subject to physical destabilisation (i.e., flocculation, coalescence, creaming, or sedimentation) or microbiological contamination [Shively and Myers, 1993;Floyd, 1999;Welin-Berger and BergenstÅ hl, 2000].…”

Section: Introductionmentioning

confidence: 99%

“…Unlike liquid emulsions, dry emulsions are far less subject to physical destabilisation (i.e., flocculation, coalescence, creaming, or sedimentation) or microbiological contamination [Shively and Myers, 1993;Floyd, 1999;Welin-Berger and BergenstÅ hl, 2000]. In dry emulsion-based pharmaceuticals, the active substance is also better protected against light degradation or oxidation [Takeuchi et al, 1991;Heinzelmann and Franke, 1999;Jang et al, 2006] and show improved bioavailability or control of drug release [Steckel and Brandes, 2004;Hansen et al, 2005;Jang et al, 2006].…”

Section: Introductionmentioning

confidence: 99%

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Development of spray‐ and freeze‐dried high‐concentration sesamol emulsions and antioxidant evaluation in fibroblasts and UV‐exposed rat skin slices

Alencar¹,

Gosset²,

Rahmouni³

et al. 2008

Drug Development Research

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Dry sesamol emulsions were synthesized from several combinations of saccharose with hydroxypropylmethylcellulose (HPMC) or sodium caseinate (SC) using spray-drying techniques at 1201 to 1801C, or freeze-drying. On the basis of physical characteristics such as droplet size distribution, residual moisture, and microscopic structure, the best material was obtained when spray-drying was applied at either 1501 or 1801C with SC or HPMC as excipients, respectively. The extent to which the antioxidant properties of free sesamol towards a set of free radicals (galvinoxyl, diphenylpicrylhydrazyl, superoxide, and hydroxyl) were altered in the starting and reconstituted liquid emulsions submitted to normal storage or pre-exposed to a flux hydroxyl radicals was investigated. Emulsions were further evaluated for their antioxidant properties in cultured 3T3 murine fibroblasts and in an ex vivo model of ultraviolet irradiated rat skin. It was found that, in the material having the best physical properties, encapsulation was decisive in: (1) improving the overall antioxidant behavior of reconstituted versus starting liquid emulsions: (2) sparing sesamol consumption due to free radical attack; and (3) significantly protecting cells and skin against free radical-or irradiation-induced enzymatic release and/or lipid peroxidation. Demonstrating a high activity at high dilutions where interactions of excipient become negligible, the new emulsions could be of great interest in sesamol-based pharmacology or topical applications. Drug Dev Res 69: 251-266, 2008.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development of spray‐ and freeze‐dried high‐concentration sesamol emulsions and antioxidant evaluation in fibroblasts and UV‐exposed rat skin slices

Alencar¹,

Gosset²,

Rahmouni³

et al. 2008

Drug Development Research

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“…A tablet preparation of oily drugs can be expected to improve the compliance and utility of the medicine for patients. 13,14) In particular, from the viewpoint of many geriatric and pediatric patients who may have difficulty swallowing, the use of ODTs to deliver fat-soluble drugs is favorable among the various dosage forms. However, during the preparation of tablets containing fat-soluble drugs, there is often adhesion to manufacturing equipment due to heat generation in the manufacturing process; therefore, advanced formulation development is required for tablet preparation.…”

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confidence: 99%

Preparation and Evaluation of Orally Disintegrating Tablets Containing Vitamin E as a Model Fat-Soluble Drug

Ikematsu

Uchida

Namiki

2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to develop orally disintegrating tablets (ODTs) containing fatsoluble drugs that disintegrate rapidly while having appropriate tablet strength. We chose vitamin E (VE) as a model drug; d-α-tocopheryl acetate, as the oily VE (VE-OI), and d-α-tocopheryl acid succinate, as the powder VE (VE-PO), were used. The oily VE was added directly to ODTs (VE-OI ODTs) and also used for the preparation of two types of VE granule, i.e., granules prepared using adsorption to calcium silicate (VE-FL granules) and granules prepared using spray-drying with gelatin (VE-SD granules); each type of granule was added to ODTs (VE-FL ODTs and VE-SD ODTs). Powder VE was added directly to ODTs (VE-PO ODTs). Various VE ODTs were prepared using these four additional methods with varying amounts of VE per tablet and were evaluated with respect to their manufacturability, physicochemical characteristics, and stability. It was demonstrated that a tablet porosity of 30% to 35% and tensile strength of 7 kg/cm 2 or greater are required to provide VE ODTs with rapid disintegration and appropriate tablet strength, and that VE-SD granules and powder VE are suitable forms of VE to be added. When stability tests of VE-SD ODTs and VE-PO ODTs were performed, VE-PO ODTs exhibited prolongation of disintegration time and increased tensile strength, whereas VE-SD ODTs showed none of these changes. These changes were thought to be attributable to a decrease in the pore size of VE-PO ODTs resulting from the softening and migration of powder VE under hot storage conditions. Key words orally disintegrating tablet; fat-soluble drug; vitamin E; disintegration; tensile strength; porosity Most pharmaceutical dosage forms for oral administration are developed for drug delivery after swallowing. In particular, tablets and capsules are the most common oral solid dosage forms, because they are convenient to carry, the duration of action of the contained drugs can be controlled, 1) and their taste or smell can be improved. 2)However, many geriatric and pediatric patients often have difficulties swallowing conventional tablets or capsules.3) It is estimated that 50% of the population experiences this problem, which results in a high prevalence of non-compliance and ineffective therapy. 4,5) To overcome this issue, a variety of pharmaceutical studies have been conducted to develop new dosage forms. Among the dosage forms developed to facilitate ease of medication, the orally disintegrating tablet (ODT) is one of the most widely employed in commercial products. 6)Numerous studies have therefore been performed on the various compositions of and manufacturing methods for ODTs. For example, ODTs can be prepared by several manufacturing methods, e.g., lyophilization, 7) granulation, 8) the cotton candy process, 9) and phase transition of sugar alcohols by direct compression. 10,11) The oily type of fat-soluble drugs have generally been produced and marketed commercially in soft capsule form, 12) though some prescription and over-the-counter d...

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“…[13][14][15] It is worth noting the many studies done on microencapsulating of emulsions using spray-drying. [16][17][18][19][20][21][22] However, the objectives and scope of these published works are restricted to the drying of oily or fatty species, and do not deal with the conservation of the structure (eg, size) of the dispersed system or emulsified forms. That is precisely why these studies only concern conventional "macro emulsions" (ie, with a mean diameter of over 1 µm).…”

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confidence: 99%

Microencapsulation of nanoemulsions: novel Trojan particles for bioactive lipid molecule delivery

Li¹,

Anton²,

Ta³

et al. 2011

IJN

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Background Nanoemulsions consist of very stable nanodroplets of oil dispersed in an aqueous phase, typically below 300 nm in size. They can be used to obtain a very fine, homogeneous dispersion of lipophilic compounds in water, thus facilitating their handling and use in nanomedicine. However, the drawback is that they are suspended in an aqueous media. This study proposes a novel technique for drying lipid nanoemulsion suspensions to create so-called Trojan particles, ie, polymer microparticles (around 2 μm) which very homogeneously “entrap” the nano-oil droplets (around 150 nm) in their core. Methods Microencapsulation of the nanoemulsions was performed using a spray-drying process and resulted in a dried powder of microparticles. By using a low-energy nanoemulsification method and relatively gentle spray-drying, the process was well suited to sensitive molecules. The model lipophilic molecule tested was vitamin E acetate, encapsulated at around 20% in dried powder. Results We showed that the presence of nanoemulsions in solution before spray-drying had a significant impact on microparticle size, distribution, and morphology. However, the process itself did not destroy the oil nanodroplets, which could easily be redispersed when the powder was put back in contact with water. High-performance liquid chromatography follow-up of the integrity of the vitamin E acetate showed that the molecules were intact throughout the process, as well as when conserved in their dried form. Conclusion This study proposes a novel technique using a spray-drying process to microencapsulate nanoemulsions. The multiscale object formed, so-called Trojan microparticles, were shown to successfully encapsulate, protect, and release the lipid nanodroplets.

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Redispersible Dry Emulsion System as Novel Oral Dosage Form of Oily Drugs: In Vivo Studies in Beagle Dogs.

Cited by 37 publications

References 0 publications

Development of spray‐ and freeze‐dried high‐concentration sesamol emulsions and antioxidant evaluation in fibroblasts and UV‐exposed rat skin slices

Development of spray‐ and freeze‐dried high‐concentration sesamol emulsions and antioxidant evaluation in fibroblasts and UV‐exposed rat skin slices

Preparation and Evaluation of Orally Disintegrating Tablets Containing Vitamin E as a Model Fat-Soluble Drug

Microencapsulation of nanoemulsions: novel Trojan particles for bioactive lipid molecule delivery

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