Extended Release Tablet stable Formulation of Albuterol Sulphate using wet granulation process
Albuterol Sulphate is indicated for bronchospasm and reversible obstructive air way disease. The objective of the research was to formulate and evaluate Extended-Release (ER) tablets of Albuterol Sulphate which will be simple in design, stable and cost effective to the patients.
ER matrix tablets of albuterol sulphate were made by aqueous wet granulation process utilizing Methocel K100M CR as a rate controlling polymer. The prepared ER matrix tablets were 2% seal coated with Opadry Clear YS-1-7006 followed by 4% ER coating with ethyl cellulose as polymer and Hypromellose 3 cps as pore former in the ratio of 8:2.
This coating was done to prevent the initial burst release from the core matrix tablets. Over the ER coating, 4% aesthetic coating was given for appeal, appearance and finish with Opadry II White 85F18422. The drug release rate and dissolution profile of prepared ER tablets were comparable to the marketed product VOSPIRE.
The drug release mechanism of both the prepared ER tablets and the marketed product follows Higuchi?s model of drug release kinetics indicating fickian diffusion.
The finalized ER tablets of Albuterol Sulphate were stable at accelerated temperature and humidity.
1. ER tablets of Albuterol Sulphate were made by aqueous wet granulation process with API to Methocel K100M CR ratio of about 1:3.
2. The process was optimized with respect to granulation in which the amount of granulating fluid was fixed at 15% of the total intragranular ingredients.
3. Total addition time of granulating fluid was fixed for 5 minutes; kneading time was optimized and finalized for 3 minutes.
4. Impeller and Chopper operation was also finalized at high speed throughout the granulation process; drying time will be based on LOD of NMT 3%.
5. Blending and lubrication time was optimized based on blend uniformity and was finalized for 10 minutes and 5 minutes respectively.
6. Compression process was characterized based on turret speed which was optimized by content uniformity and finalized the range of 20-30 RPM and hardness of tablets was optimized by dissolution and was finalized for 4-8 kP range.
From the blend to tablet stage, the process was characterized with respect to
- LOD
- Repose Angle
- Bulk / Tapped Density
- Hausner Ratio
- PSD
- Weight
- Thickness
- Hardness
- Friability
Prepared ER core tablets were 2% seal coated with 10% w/w aqueous solution of Opadry Clear YS-1-7006 and the seal coated tablets were ER coated upto 4% with 20% w/w aqueous dispersion of Ethyl Cellulose with Hypromellose 3cps as pore former in the ratio of 8:2. Finally, the ER coated tablets were aesthetic coated upto 4% with 20% w/w aqueous solution of Opadry II White 85F18422.
The finalized ER tablets of Albuterol Sulphate were characterized with respect to drug release rate & mechanism and linearity - Correlation coefficient.
Dissolution profile and similarity & difference factor of prepared ER tablets of Albuterol Sulphate was comparable to the marketed product VOSPIRE.
Both the marketed product and the test product have comparable drug release rate, linearity (based on Correlation coefficient) and follows Higuchi?s model of drug release kinetics indicating fickian diffusion.
The finalized ER tablets of Albuterol Sulphate were stable at accelerated temperature and humidity.