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Titolo:
In vivo evaluation of submicron emulsions with pilocarpine: the effect of pH and chemical form of the drug
Autore:
Sznitowska, M; Janicki, S; Zurowska-Pryczkowska, K; Mackiewicz, J;
Indirizzi:
Med Univ Gdansk, Dept Pharmaceut Technol, PL-80416 Gdansk, Poland Med UnivGdansk Gdansk Poland PL-80416 Technol, PL-80416 Gdansk, Poland
Titolo Testata:
JOURNAL OF MICROENCAPSULATION
fascicolo: 2, volume: 18, anno: 2001,
pagine: 173 - 181
SICI:
0265-2048(200103)18:2<173:IVEOSE>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
ENHANCED TRANSDERMAL DELIVERY; VEHICLE; STABILITY; CARRIERS; DIAZEPAM;
Keywords:
submicron emulsion; pilocarpine; miotic effect; encapsulation;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Sznitowska, M Med Univ Gdansk, Dept Pharmaceut Technol, Ul J Hallera 107, PL-80416 Gdansk, Poland Med Univ Gdansk Ul J Hallera 107 Gdansk Poland PL-80416 and
Citazione:
M. Sznitowska et al., "In vivo evaluation of submicron emulsions with pilocarpine: the effect of pH and chemical form of the drug", J MICROENC, 18(2), 2001, pp. 173-181

Abstract

Submicron emulsions containing 2.0% w/v pilocarpine as pilocarpine HCl, soybean oil (10% w/v) and egg lecithin (1.2% w/v) were formulated. Emulsions at pH 5.0, 6.5 and 8.5 were applied to the rabbit's eye, and the reduction in pupil diameter was measured for 6 h. The miotic effect was compared withthat obtained with aqueous solutions at the same pH. A prolonged miotic effect was observed when the submicron emulsion was used as a vehicle. After application of emulsions at pH 5.0, 6.5 or 8.5, the time when 20% reductionof pupil diameter was still observed was 3.9 +/- 1.1 h, 4.3 +/- 1.3 h and 5.3 +/- 0.8 h, respectively, while, after application of a solution, this parameter was shorter by 30-40%. AUC(0-6h) values were larger after application of the submicron emulsions in comparison to aqueous solutions; however,statistically significant differences were only observed for emulsions at pH 6.5. Although the bioavailability of the drug is pH dependent, emulsionsat higher pH cannot be considered for clinical use because of pilocarpine degradation which occurs with a similar rate as in aqueous solutions. Introduction of pilocarpine into the oily phase in the form of pilocarpine base or its oleate did not improve either the physicochemical or the pharmacological properties of the formulations. Irrespective of the pH and chemical form of pilocarpine used for emulsion preparation, practically all drug was found in the aqueous phase of the emulsion; thus, partitioning to the oily phase was negligible.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 19:13:26