Aspectos biofarmacêuticos da formulação de medicamentos para neonatos: fundamentos da complexação de indometacina com hidroxipropil-beta-ciclodextrina para tratamento oral do fechamento do canal arterial

Rama, Ana Cristina Ribeiro; Veiga, Francisco; Figueiredo, Isabel V.; Sousa, Andreia F.; Caramona, Margarida

doi:10.1590/s1516-93322005000300002

Cited by 7 publications

(5 citation statements)

References 81 publications

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“…In this case, the heating and consequent reduction of medium viscosity was not performed, and thus, the high viscosity of medium complexation resulted in a reduction in mobility of hindering the formation of DAP/CDs systems due to the presence of polymers. According to Rama et al [18], only complexes with K c between 100 and 1,000 mol L -1 have biological applications, because complexes with K c lower than 100 mol L -1 constitute unstable drug/CD systems, whereas complexes with a K c higher than 1,000 mol L -1 could adversely affect the absorption of the drug. The K c values found in all the systems investigated (Table 3) indicate the formation of inclusion complexes with a suitable stability.…”

Section: Resultsmentioning

confidence: 99%

Binary and ternary inclusion complexes of dapsone in cyclodextrins and polymers: preparation, characterization and evaluation

Grebogi

Tibola

Barison

et al. 2011

J Incl Phenom Macrocycl Chem

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Dapsone (DAP) is a synthetic sulfone drug with bacteriostatic activity, mainly against Mycobacterium leprae. In this study we have investigated the interactions of DAP with cyclodextrins, 2-hydroxypropyl-b-cyclodextrin (HPbCD) and b-cyclodextrin (bCD), in the presence and absence of water-soluble polymers, in order to improve its solubility and bioavailability. Solid systems DAP/HPbCD and DAP/bCD, in the presence or absence of polyvinylpyrrolidone (PVP K30) or hydroxypropyl methylcellulose (HPMC), were prepared. The binary and ternary systems were evaluated and characterized by SEM, DSC, XRD and NMR analysis as well as phase solubility assays, in order to investigate the interactions between DAP and the excipients in aqueous solution. This study revealed that inclusion complexes of DAP and cyclodextrins (HPbCD and bCD) can be produced in order to improve DAP solubility and bioavailability in the presence or absence of polymers (PVP K30 and HPMC). The more stable inclusion complex was obtained with HPbCD, and consequently HPbCD was more efficient in improving DAP solubility than bCD, and the addition of polymers had no influence on DAP solubility or on the stability of the DAP/CDs complexes.

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Section: Resultsmentioning

confidence: 99%

Binary and ternary inclusion complexes of dapsone in cyclodextrins and polymers: preparation, characterization and evaluation

Grebogi

Tibola

Barison

et al. 2011

J Incl Phenom Macrocycl Chem

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“…Persistence of this foetal structure beyond 10 days of life is considered abnormal. IM is a drug of choice for closure of the ductus administered by intravenous route [22,23]. The overall idea of our work is to investigate the possibility of using an inclusion complex form of IM to treat PDA by oral administration, with the aim of overcoming, on one hand, the problems of administering intravenous medications to newborns, and on the other hand, the impossibility of using the oral route due to the hydrolysis of IM that occurs at gastric basic pH of newborns of 6-8, and also due to gastrointestinal toxicity.…”

mentioning

confidence: 99%

Evaluation of gastric toxicity of indomethacin acid, salt form and complexed forms with hydroxypropyl‐β‐cyclodextrin on Wistar rats: histopathologic analysis

Ribeiro-Rama

Figueiredo

Veiga

et al. 2009

Fundamemntal Clinical Pharma

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Indomethacin (IM) is a non-steroidal anti-inflammatory drug which inhibits prostaglandin biosynthesis. It is practically insoluble in water and has the capacity to induce gastric injury. Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) is an alkylated derivative of beta-CD with the capacity to form inclusion complexes with suitable molecules. IM is considered to form partial inclusion complexes with HP-beta-CD by enclosure of the p-chlorobenzoic part of the molecule in the cyclodextrin channel, reducing the adverse effects. The aim of this paper is to evaluate the gastric damage induced by the IM inclusion complex prepared by freeze-drying and spray-drying. A total of 135 Wistar rats weighing 224.4 +/- 62.5 g were put into 10 groups. They were allowed free access to water but were maintained fasted for 18 h before the first administration until the end of the experiment. IM acid-form, IM trihydrated-sodium-salt and IM-HP-beta-CD spray and freeze-dried, at normal and toxic doses, were administered through gastric cannula once/day for 3 days. Seventy-two hours after the first administration, the animals were sacrificed and the stomachs collected and prepared for morphological study by using the haematoxylin-eosin technique. Lesion indexes (rated 0/4) were developed and the type of injury was scored according to the severity of damage and the incidence of microscopic evidence of harm. Microscopic assessment demonstrated levels of injury with index one on 10-25%. The type of complexation method had different incidence but the same degree. The results show that IM inclusion complexation protects against gastric injury, reducing the incidence and the maximum degree of severity from 4 to 1, with a better performance of the spray-dried complex.

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“…É valido ressaltar que A administração oral das ciclodextrinas naturais não demonstra a indução de toxicidade aguda e, mesmo quando administradas em doses substancialmente elevadas a animais, não resulta em mortalidade. Em testes com ratos, o DL50 (dose letal para 50% dos animais) para administração oral é relatado como superior a 12,5 g/kg para a α-CD, 18,8 g/ kg para a β-CD e 8 g/kg para a γ-CD (Rama et al, 2005).…”

Section: Utilização Das Ciclodextrinas Em Formulações Farmacêuticasunclassified

Polissacarídeos Naturais: Anacardium Occidentale L. E Suas Aplicações Na Obtenção De Scaffolds Para Liberação De Fármacos

Marques,

Soares,

Barud

et al. 2023

Biotecnologia E Farmacologia: Abordagens Interdisciplinares Na Terapêutica Com Recursos Naturais

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Aspectos biofarmacêuticos da formulação de medicamentos para neonatos: fundamentos da complexação de indometacina com hidroxipropil-beta-ciclodextrina para tratamento oral do fechamento do canal arterial

Cited by 7 publications

References 81 publications

Binary and ternary inclusion complexes of dapsone in cyclodextrins and polymers: preparation, characterization and evaluation

Binary and ternary inclusion complexes of dapsone in cyclodextrins and polymers: preparation, characterization and evaluation

Evaluation of gastric toxicity of indomethacin acid, salt form and complexed forms with hydroxypropyl‐β‐cyclodextrin on Wistar rats: histopathologic analysis

Polissacarídeos Naturais: Anacardium Occidentale L. E Suas Aplicações Na Obtenção De Scaffolds Para Liberação De Fármacos

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