Development of a melting tablet containing promethazine HCl against motion sickness.

Abstract

The purpose of this study was to design a 'Traveller Friendly Drug Delivery System' for PM-HCl. Conventional promethazine (PM-HCl) tablets are bitter, need to be taken 1 h before symptoms and water is also needed. Taste-masked granules were produced with Eudragit E100 by extrusion, and analyzed with FTIR, DSC, and XRD. Tablets formulated from granules by direct compression using Ac-Di-Sol, Polyplasdone-XL, Primojel and ion-exchanger Tulsion339 and evaluated for mass uniformity, friability, tensile strength, drug content uniformity, water absorption ratio, in-vitro and in-vivo disintegration time and in-vitro dissolution studies. The observed drug-polymer interactions and reduced crystallinity may be reasons for increased dissolution rates. The formulated tablets were disintegrated within 15 s. Tablets (25 mg PM-HCl) with Ac-Di-Sol (4%) showed complete release within 1 min, while marketed conventional tablets (Phenergan; Rhone-Poulec) release 25% during the same period. A preliminary stability studies for the prepared tablets carried at 30 +/- 2 degrees C/60 +/- 5% RH, and 40 +/- 2 degrees C/75 +/- 5%RH for 3 months showed no significant changes in the tablets quality at 30 +/- 2 degrees C/60 +/- 5% RH. However, at 40 +/- 2 degrees C/75 +/- 5%RH marked increase in in-vitro disintegration time, tensile strength and decrease in friability and water absorption ratio was found. The present studies indicate the abilities of Eudragit E 100 for taste masking and improving the dissolution profile of PM-HCl after complexation. In addition, by employing cost effective direct compression method, fast-dissolving tablets of 400 mg total weight with an acceptable quality could be prepared.

• Authors: Rahul V Haware, P D Chaudhari, S R Parakh, A Bauer-Brandl
• Journal: AAPS PharmSciTech (AAPS PharmSciTech) Vol. 9 Issue 3 Pg. 1006-15 ( 2008) ISSN: 1530-9932 [Electronic] United States
• PMID: 18770049 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Powders
• Tablets
• Promethazine

Topics

• Administration, Oral
• Calorimetry, Differential Scanning
• Chemistry, Pharmaceutical
• Drug Design
• Drug Stability
• Hardness (drug effects, physiology)
• Humans
• Motion Sickness (metabolism, prevention & control)
• Powders
• Promethazine (administration & dosage, chemical synthesis, pharmacokinetics)
• Solubility (drug effects)
• Tablets (administration & dosage, chemical synthesis, pharmacokinetics)
• Taste Perception (drug effects, physiology)