Study of a complexation process between naltrexone and Eudragit® L as an oral controlled release system

Álvarez-Fuentes, Josefa; Caraballo, Isidoro; Boza, Ana Senent; Llera, J. M.; Holgado, M.A.; Fernández‐Arévalo, M.

doi:10.1016/s0378-5173(96)04849-1

Cited by 9 publications

(5 citation statements)

References 11 publications

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“…Release pro®le of naltrexone±Eudragit L An in-vitro dissolution study (USP XXIII basket apparatus, Turu Grau, mod. D-6) using a pH gradient technique showed that the release of half of the drug charge was assured between the ®rst 2 h, and the rest of the drug charge was gradually released during the following 6 h. This release pro®le was adequate for our objectives: to obtain an immediate and effective antagonism of opiate effects and to maintain this action over a long period of time (Alvarez-Fuentes et al 1997b).…”

Section: Naltrexone±eudragit L Complexmentioning

confidence: 98%

“…The analysis of 13 C chemical shifts showed that the spectroscopic behaviour of naltrexone carbons in the complex was closer to naltrexone base (Dd i 0±1Á7 ppm) than to naltrexone hydrochloride (Dd i 0± 3Á5 ppm). It can be deduced that naltrexone was present in the complex as free base and not as ammonium salt; so, naltrexone interacted with the polar groups of the polymer by means of hydrogen bonds (Alvarez-Fuentes et al 1997b).…”

Section: Naltrexone±eudragit L Complexmentioning

confidence: 99%

“…Considering the optimal pharmacokinetic and physicochemical characteristics of naltrexone, it was introduced into the polymeric structure Eudragit L30D (anionic copolymer based on polymethacrylic acid and ethylacrylate). Alvarez-Fuentes et al (1997b) have evaluated the physicochemical properties and the in-vitro behaviour of naltrexone Eudragit L.…”

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confidence: 99%

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Preclinical Study of an Oral Controlled Release Naltrexone Complex in Mice

Álvarez-Fuentes

Rojas-Corrales

Holgado

et al. 2000

Journal of Pharmacy and Pharmacology

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Naltrexone, a long-acting, orally effective, opioid antagonist which blocks opioid effects as well as the development of physical dependence, would appear to be a drug ideally suited to addiction treatment. An optimal dosage regimen is critical for the treatment patient compliance in ambulatory opiate detoxification programs. The ideal dosage regimen would be an oral controlled-release system of naltrexone that allowed once-a-day administration providing stable plasma levels. A naltrexone-Eudragit L complex was produced in aqueous medium from naltrexone hydrochloride solution and Eudragit L30D (30% w/v) previously diluted (6% w/v) and partially neutralized. The antagonistic activity of naltrexone-Eudragit L on morphine-induced thermal antinociception, in comparison with conventional naltrexone, was evaluated, using the mouse hot-plate model. Mice were administered 10 mg kg(-1) morphine subcutaneously, 10 min before test, and the antagonist products, either naltrexone-Eudragit L or naltrexone hydrochloride, were administered orally at 0.5, 1, 2, 4, 6, 8, 10, 12, 14 and 16h before the test. The results showed that the antagonism induced by naltrexone-Eudragit L was effective until 12 h after drug administration, while that induced by naltrexone hydrochloride disappeared 10 h after its administration. A 23.47% increase of the area under curve was obtained when naltrexone-Eudragit L was administered, compared with that induced by conventional naltrexone. The time taken to decrease the inhibition of analgesic activity to 50% was delayed by 51.80%. This complexation technique can be considered as a useful tool in the design of oral controlled-release systems capable of inducing a long-lasting effect in-vivo.

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Section: Naltrexone±eudragit L Complexmentioning

confidence: 98%

Section: Naltrexone±eudragit L Complexmentioning

confidence: 99%

See 1 more Smart Citation

Preclinical Study of an Oral Controlled Release Naltrexone Complex in Mice

Álvarez-Fuentes

Rojas-Corrales

Holgado

et al. 2000

Journal of Pharmacy and Pharmacology

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show abstract

“…However, when MD was granulated using 5 or 10% ELNa (MD#11 or MD#12), or using 5 or 10% ESNa (MD#13 or MD#14), significant retardations in MD release in all dissolution media were observed (p ≤0.05). An interaction between a cationic drug containing an amino group and a polymer with anionic pending groups, that is, carboxylic group, electrostatically [42][43][44][45][46] or by hydrogen bonding [47][48][49][50][51] has been reported frequently. However, it seemed that such interaction was insignificant in case of MD with EL or with ES since drug release retardation was experienced in tablets containing the salt forms of the polymers.…”

Section: Insert Figure 4 Herementioning

confidence: 99%

“…In addition, hydrogen bonding which implies a weaker interaction than electrostatic bond, might have taken place. For example, a complex between Naltrexone hydrochloride and Eudragit L was successfully obtained by hydrogen bond occurring among polar group of both molecules [48]. Also, hydrogen bond was used to prepare interpolymer complexes for pharmaceutical applications [49,51,52].…”

Section: Insert Figures 7 and 8 Herementioning

confidence: 99%