van Asselt D Z, Merkus F W, Russel F G, Hoefnagels W H
Department of Geriatric Medicine, University Hospital Nijmegen, The Netherlands.
Br J Clin Pharmacol. 1998 Jan;45(1):83-6. doi: 10.1046/j.1365-2125.1998.00642.x.
To investigate the nasal absorption of hydroxocobalamin in 10 healthy elderly adults.
In a cross-over study, blood samples were collected before administration of the drug and after 10, 20, 30, 40, 60, 120, 180 and 240 min. The plasma cobalamin concentration was determined by competitive radioisotope binding technique.
The maximal plasma cobalamin concentration (Cmax) after nasal administration of 750 microg hydroxocobalamin was 1900 +/- 900 pmol l(-1) (mean +/- s.d.). The maximal plasma cobalamin concentration was reached in 35 +/- 13 min (t[max]). The Cmax after nasal administration of 1500 microg hydroxocobalamin was 3500 +/- 2500 pmol l(-1) with a t(max) of 28 +/- 16 min. Both the AUC(0,240 min) and AUC(0,00) increased significantly with an increase of the dose from 750 microg to 1500 microg (P = 0.037 and P = 0.028, respectively). The nasal spray was well tolerated. No signs of irritation or local sensitivity were noted.
The nasal absorption of hydroxocobalamin in healthy elderly adults is rapid, high and well tolerated.
研究10名健康老年成年人中羟钴胺素的鼻腔吸收情况。
在一项交叉研究中，于给药前以及给药后10、20、30、40、60、120、180和240分钟采集血样。采用竞争性放射性同位素结合技术测定血浆钴胺素浓度。
鼻腔给予750微克羟钴胺素后，血浆钴胺素最大浓度（Cmax）为1900±900皮摩尔/升（均值±标准差）。在35±13分钟（t[max]）时达到血浆钴胺素最大浓度。鼻腔给予1500微克羟钴胺素后的Cmax为3500±2500皮摩尔/升，t(max)为28±16分钟。随着剂量从750微克增加到1500微克，AUC(0,240分钟)和AUC(0,∞)均显著增加（分别为P = 0.037和P = 0.028）。鼻腔喷雾剂耐受性良好。未观察到刺激或局部敏感迹象。
健康老年成年人中羟钴胺素的鼻腔吸收迅速、高效且耐受性良好。
