Human insulin microcrystals with lactose carriers for pulmonary delivery.
Dry powder formulations for pulmonary delivery are attractive because many issues of solubility and stability can be minimized. Human insulin microcrystals with lactose carriers were produced for pulmonary delivery. The average particle diameter was 2.3 microm, with a narrow, monodispersed size distribution. The percentages of high molecular weight proteins (%HMWPs), other insulin-related compounds (%OIRCs), and A-21 desamido insulin (%D(es)) were very low throughout the microcrystal preparation process. Administration of the microcrystal powder by intratracheal insufflation significantly reduced the blood glucose levels of Sprague-Dawley rats. The percent minimum reductions of the blood glucose concentration (%MRBG) produced by the insulin microcrystal powder and by an insulin solution reached 40.4% and 33.4% of the initial glucose levels respectively, and their bioavailability relative to subcutaneous injection (F) was 15% and 10% respectively. These results confirm that the insulin microcrystal powder prepared is suitable for pulmonary delivery in an effective dosage form.
Lim
Se-Hwan
SH
School of Life Sciences and Biotechnology, Korea University, Seoul.
Park
Hye Won
HW
Shin
Chang-Hoon
CH
Kwon
Jai-Hyun
JH
Kim
Chan-Wha
CW
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D004333:Drug Administration Routes; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D007003:Hypoglycemia / Q000097:blood / Q000139:chemically induced; D007328:Insulin / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology; D007785:Lactose / Q000737:chemistry*; D008168:Lung / Q000378:metabolism*; D008297:Male; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D014132:Trachea
D001786:Blood Glucose; D004337:Drug Carriers; D007328:Insulin; D007785:Lactose