Development of novel ibuprofen-loaded solid dispersion with improved bioavailability using aqueous solution

Park, Young-Joon; Kwon, Ram; Quan, Qi Zhe; Oh, Dong Hoon; Kim, Jong Oh; Hwang, Ma Ro; Koo, Yoon Bon; Woo, Jong Soo; Yong, Chul Soon; Choi, Han‐Gon

doi:10.1007/s12272-009-1516-3

Cited by 26 publications

(17 citation statements)

References 25 publications

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“…To disperse a drug in an excipient, several methods can be used, including the solvent method (Ford, 1986), the fusion method (Sharma, Joshi, 2007;Yi et al, 2008), the solvent-melting method, as well as freeze-and spraydrying technology (Park et al, 2009).…”

Section: Solid Dispersionsmentioning

confidence: 99%

Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Almeida

Amaral

Lobão

2012

Braz. J. Pharm. Sci.

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Ibuprofen is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory diseases. In its pure state, ibuprofen presents poor physical and mechanical characteristics and its use in solid dosage forms needs the addition of excipients that improve these properties. The selection of the best excipients and the most suitable pharmaceutical dosage form to carry ibuprofen is very important for the industrial success of this drug. Given these factors, lipid microparticles and solid dispersions of ibuprofen with cetyl alcohol, stearic acid, and hydrogenated castor oil were prepared. These formulations were intended to improve the physical and mechanical characteristics and to sustain the release of this drug. Physical mixtures were also prepared with the same ingredients in similar proportions. The solid dispersions of ibuprofen/stearic acid and ibuprofen/hydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Further, gelatin capsules filled with lipid microparticles and solid dispersions were submitted to dissolution tests in order to study the influence of the prepared systems in the release profiles of ibuprofen. Prolonged release of ibuprofen was achieved with the lipid microparticles and solid dispersions prepared with the different types of excipients. O ibuprofeno é um dos antiinflamatórios não esteróides mais utilizados no tratamento de patologias associadas a processos inflamatórios. Este fármaco, quando no seu estado puro, apresenta características físicas e mecânicas pouco satisfatórias e a sua utilização em formas sólidas só é possível se forem adicionados excipientes que permitam melhorar estas propriedades. A seleção dos excipientes ideais e da forma farmacêutica mais adequada para veicular o ibuprofeno é fundamental para o sucesso industrial deste fármaco. Tendo em conta estes fatores, prepararam-se micropartículas lipídicas e dispersões sólidas de ibuprofeno com cada um dos seguintes excipientes: álcool cetílico, ácido esteárico e óleo de rícino hidrogenado. Estas formulações tinham por finalidade melhorar as características físicas e mecânicas e prolongar a liberação deste fármaco. Foram, também, preparadas misturas físicas do ibuprofeno com os mesmos excipientes e nas mesmas proporções. As dispersões sólidas de ibuprofeno/ácido esteárico e as dispersões sólidas de ibuprofeno/óleo de rícino hidrogenado foram aquelas que apresentaram melhores características de escoamento comparativamente com o ibuprofeno puro. Por outro lado, foram preparadas cápsulas de gelatina com as diferentes micropartículas lipídicas e dispersões sólidas e submetidas a ensaios de dissolução com o objetivo de estudar a influência dos sistemas preparados nos perfis de liberação do ibuprofeno. A liberação prolongada do ibuprofeno foi conseguida nas diferentes micropartículas lipídicas e dispersões sólidas preparadas com os diferentes excipientes.Unitermos: Ibuprofeno/dispersões sólidas/perfil de liberação. Ibuprofeno/micropartículas lipídicas/perfil de libe...

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Section: Solid Dispersionsmentioning

confidence: 99%

Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Almeida

Amaral

Lobão

2012

Braz. J. Pharm. Sci.

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“…Solid dispersion technology is used to increase the solubility of hydrophobic compounds. Consequently, BAs of the drugs were increased considerably after oral administration (48)(49)(50)(51)(52). In the case of dissolving microneedles, solid dispersion technology was not intended to increase the solubility of the formulated drug, because both rhGH and DDAVP were water-soluble protein and peptide drugs.…”

Section: Design Of Two-layered Dissolving Microneedlesmentioning

confidence: 99%

Two-Layered Dissolving Microneedles for Percutaneous Delivery of Peptide/Protein Drugs in Rats

et al. 2010

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“…Solid dispersion technology has been used to increase the solubility of hydrophobic compounds and as a result bioavailability of those drugs were significantly increased after oral administration. [44][45][46][47][48] In the case of SDMP array tip, we did not intend to use solid dispersion technology to increase the solubility of AA, because both AA and base polymer, sodium chondroitin sulfate, were highly watersoluble compounds. AA dissolved in accordance with the dissolution of SDMP base polymer.…”

Section: )mentioning

confidence: 99%

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Ito¹,

Maeda²,

Fukushima³

et al. 2010

Chem. Pharm. Bull.

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Ascorbic acid (AA, vitamin C) is a hydrophilic vitamin that cannot be produced endogenously in rats and primates including human and is widely used for the protection of the aging of the skin due to the exposure to the UV light and for the acceleration of the synthesis of collagen in the skin. [1][2][3][4] AA was shown to be absorbed from the gastrointestinal tract by an active transport system, though limited amount of AA was transported by this system. 5) In addition, after AA was absorbed, AA was rapidly eliminated from the body by the oxidative metabolism through both enzymatic and nonenzymatic processes.2) Therefore, even if we intake excess amount of AA, sufficient amount of AA is not absorbed into the systemic circulation and is not delivered to its target tissue, skin.2) To conquer this problem, percutaneous delivery of AA has been challenged. The advantage of percutaneous delivery of AA is (1) to obtain high concentration of AA in the skin and (2) to escape the hepatic first-pass effect before reaching to the systemic circulation. However, when AA is percutaneously administered, the penetration of AA to the dermal tissue is difficult because of the high barrier function of the skin. To increase the permeability of AA, derivatives such asascorbic acid 2-sulfate 8) and disodium isostearyl 2-o-L-ascorbyl phosphate, 9,10) has been developed. Also Gopinath et al. designed ascorbyl palmitate vesicles (Aspasomes) for the transdermal delivery of ascorbic acid.11) Furthermore, recent advances in pharmaceutical technology have promoted the research on the permeability enhancement of AA using physical absorption enhancing method like iontophoresis 12) and microemulsion technologies.11,13) Iontophoresis uses an electric field to drive ionized molecules across the skin by electrophoresis and non-ionized molecules by electro osmosis. 14)Despite concerns about skin irritation, iontophoresis may be useful to deliver some peptides and small proteins.15) On the other hand, microneedles are also one of the physical methods for the percutaneous absorption of drugs. With microneedles, small microconduits are formed on the skin. Recent advance in microfabrication technology has made it possible to prepare microneedles that have a possibility of novel transdermal drug delivery system (TDDS). Since the first publication by Henry et al.,16) microfabrication techniques for the production of silicon, metal, glass and polymer microneedle arrays with micrometer dimensions have been developed. 17-20) The microneedles are either solid or hollow and posses a geometrical shape. Microneedle TDDS is roughly defined by a micron size needle preparation for percutaneous administration. Microneedle TDDSs are classified as follows; (1) extremely small needle through which drug solution can be injected into the skin, (2) metallic and/or silastic microneedles on which surface drug is coated, and (3) metallic and/or silastic microneedles by which microconduits are made on the skin and drug solution is applied after removing the microneedles. H...

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Development of novel ibuprofen-loaded solid dispersion with improved bioavailability using aqueous solution

Cited by 26 publications

References 25 publications

Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Two-Layered Dissolving Microneedles for Percutaneous Delivery of Peptide/Protein Drugs in Rats

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

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