369) The concentrations of OP and oseltamivir carboxylate (OSCA) in rats plasma using LC-MS have been determined and performed via pharmacokinetic software DAS 2.0 package. |
PMID:24299495 DOI:10.3109/10717544.2013.863526 |
2015 Drug delivery |
* Development and evaluation of a dry powder formulation of liposome-encapsulated oseltamivir phosphate for inhalation. |
- This study aims to develop oseltamivir phosphate (OP) liposomes as inhalation powders by spray-drying based on the single factor investigation, which was mainly composed of lactose, L-leucine and mannitol. It was found that the ratio of OP and liposomes (1:10), inlet temperature (110 °C) and airflow rate (2.3 mL/min) showed optimized physical properties of OP liposomes. Deposition was evaluated after the aerosolization of powders at 600 L/h via the Aerolizer® into a twin-stage impinger. The concentrations of OP and oseltamivir carboxylate (OSCA) in rats plasma using LC-MS have been determined and performed via pharmacokinetic software DAS 2.0 package. The liposomal OP dry powders displayed an average particle size around 3.5 µm with fine particle fraction (FPF = 35.40%). In vitro evaluation demonstrated a sustained release pattern accounting for 20% drug release compared to that of OP solution up to 90% drug release in 2 h. And the cumulative release percentage was up to 50% in 20 h. Atrioventricular fitting results indicated that all preparations were best fitted with a two-compartment model. There was a significant difference in MRT, Cmax and Tmax (p < 0.01) between the two groups of liposomal OP dry powders and OP solution with t-test, which indicated that the drug released slowly from liposomal OP dry powders in the lung. To sum up, dry powders formulation of liposome-encapsulated OP for inhalation was suitable for pulmonary administration, which offering the opportunity to reduce dosing frequency. |
(1)60 in | (10)15 for | (19)3 based | (28)2 equally |
(2)58 *null* | (11)13 at | (20)3 of | (29)2 normally |
(3)45 to | (12)6 as | (21)3 this | (30)2 procedures |
(4)35 using | (13)5 the | (22)2 3 | (31)2 successfully |
(5)33 on | (14)5 under | (23)2 6 | (32)2 three |
(6)30 with | (15)5 via | (24)2 better | (33)2 through |
(7)23 by | (16)4 an | (25)2 both | (34)2 twice |
(8)22 a | (17)4 before | (26)2 but | |
(9)16 and | (18)3 after | (27)2 daily |
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