1. Author : brajgaurav@indiatimes.com
Development and characterization of Budesonide pressurized metered dose inhaler (pMDI) using gamma scintigraphy
Sharma BG, Kumar N, Soni S, Rawat HS, Nishad DK, Kumar A, Mittal G and Bhatnagar A
Institute of Nuclear Medicine and Allied Sciences, Brig. SK Mazumdar Marg, Delhi-54, India
Author :
Defence R&D Organisation
Institute of Nuclear Medicine & Allied Sciences
INTRODUCTION
4. In-vitro aerodynamic particle size distribution using Anderson Cascade Impactor (ACI)
3.In-vitro aerodynamic particle size distribution using Anderson Cascade Impactor (n=6)
Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies). Additionally, it is used for inflammatory bowel disease.
A metered-dose inhaler (MDI) is a device that delivers a specific amount of medication to the lungs, in the form of a short burst of aerosolized medicine that is inhaled by the patient
Aerodynamic particle size distribution and dose proportionality of budesonide was quantified using ACI using radiometry as well as spectroscopy techniques. The flow rate was maintained at 28.3 L/min
5.Gamma scintigraphy study of 99mTc-labeled budesonide in healthy human volunteers
Human volunteers were inhaled radiolabeled budesonide by pMDI to quantify pulmonary deposition of the drug. Each volunteer inhaled 2 puffs in single dose. Scintigraphy was used to estimate inhaled drug in lungs, trachea, oesophagus, mouth and GIT.
OBJECTIVE
MMAD (mass median aerodynamic diameter): 4.75µm
GSD (geometric standard deviation):1.59 µm
RF (respiratory fraction): %
Radiolabeling of Budesonide (steroid)
Serum stability studies of radiolabeled drug
Preparation of MDI canister
In-vitro aerodynamic particle size distribution studies using Anderson Cascade Impactor (ACI)
Lung deposition studies of drug in healthy volunteers using scintigraphy
4.Gamma scintigraphy study of radiolabeled budesonide in healthy human volunteers (n=6)
5 min
120 min
180 min
EXPERIMENTAL
RESULTS AND DISCUSSION
1.Radiolabelling of Budesonide: The drug was successfully radiolabeled with 99mTc-pertechnetate using stannous salt as reducing agent
2.Labeling efficiency: Labeling efficiency was ascertained by ITLC-SG chromatography using 100 % acetone as mobile phase
1. Radiolabeling efficiency of Budesonide
Time
5 Mins
2 Hrs
3 Hrs
Left Lung
12%
10% 6%
Right Lung
11% 9%
R.F..
23%
19%
99mTcO4
Reducing agent
Budesonide
99mTc-Budesonide
Reducing agent
Radiolabeling efficiency was consistently > 97% as ascertained by ITLC using 100 % acetone as mobile phase
CONCLUSION
2. Serum stability studies at 370C
3.pMDI preparation: Budesonide pMDI was prepared by filling hydrofluoroalkanes and 99mTc-Budesonide in an aluminum canister under sterilized environment
Budesonide pressurized meter dose inhaler was developed and characterized using pharmacoscintigraphy techniques
Budesonide was radiolabeled with 99mTc with good labeling efficiency & stability
Respiratory fraction & MMAD of the drug using pMDI was found to be 22% & 4.8µm respectively, as estimated by ACI studies.
Scintigraphy studies in human volunteers have shown significant deposition of the drug in lungs using pMDI, thereby highlighting its usefulness in asthma & other pulmonary disease conditions.
Tc99M –Budesonide +
HFA propellant
-200C
seelar
99mTc-budesonide was found to be fairly stable in vitro as well as in vivo and the stability in serum indicated that 99mTc labeled drug remained bound to the chelate up to 24 hrs
Final test product
42ND Annual conference of Society of Nuclear Medicine (India)
Chandigarh, 11TH – 14TH November, 2010
REFERENCES