FLOATING RANITIDINE MICROPARTICULATES: DEVELOPMENT AND IN VITRO EVALUATION


Mohamed E. Etman, Engy H. Mahmoud, Sally Galal, Aly H. Nada

Abstract


Objective: Rapid and inconsistent gastrointestinal tract (GIT) transit could result in reduced drug efficiency and the need for frequent dose administration, which usually result in patients’ incompliance. Ranitidine hydrochloride (RH), as a model drug is freely soluble, moisture sensitive drug with a short biological half-life (~2.5-3 h) and narrow absorption window in the initial part of the small intestine. The present study aimed to develop ranitidine floating multi-particulates (RFM) using melt granulation technique and investigation of the effect of lipids and additives on the physicochemical properties.

Methods: RFM were prepared using Compritol® 888 ATO, glyceryl behenate, Cutina® HR, Cutina® GMS, hydrogenated castor oil, glyceryl monostearate, and beeswax as lipids and ethyl cellulose, Povidone® K 90 and Aerosil® 200 as release modifiers. The effect of the preparation method and additives, as well as storage for 6 mo at 40 °C, on floating and release characteristics were evaluated.

Results: Size distribution indicated that the prepared formulations exhibited reasonably small floating micro particulates; more than 90% of the prepared microparticles were less than 710 µm. Hausner ratios and Carr’s compressibility indices ranged from 1.17 to 1.29% and 14.54 to 22.4 %, respectively, and the angle of repose values was ≤40 °, indicating good flow properties. RFM containing Compritol® showed a relatively higher release properties compared to hydrogenated castor oil. Increasing the proportion of the fatty component was accompanied by retardation in RH release. The tested additives (PVP, ethyl cellulose, Aerosil®) resulted in different degrees of retardation of drug release. The percent-floating of RFM was almost 100% in all formulations with the exception of formulations prepared using glyceryl monostearate. FT-IR and DSC studies indicated the compatibility of the excipients with RH. Stability results revealed an insignificant change in RFM properties over 6 mo.

Conclusion: The prepared microparticles exhibited optimum particle size, good compressibility, and flow properties. RFM containing Compritol® showed a relatively higher release properties compared to hydrogenated castor oil. Increasing the proportion of the fatty component was accompanied by retardation in RH release. The percent-floating of RFM was almost 100% in most formulations. FT-IR and DSC indicated good compatibility of the excipients with RH and insignificant change in RFM properties over 6 mo’s storage.


Keywords


Floating Ranitidine Micro-particulates (RFM), Melt granulation technique

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About this article

Title

FLOATING RANITIDINE MICROPARTICULATES: DEVELOPMENT AND IN VITRO EVALUATION

Keywords

Floating Ranitidine Micro-particulates (RFM), Melt granulation technique

Date

01-10-2016

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 8, Issue 4, 2016 Page: 1-9

Online ISSN

0975-7058

Statistics

143 Views | 565 Downloads

Authors & Affiliations

Mohamed E. Etman
Faculty of Pharmacy, Alexandria University, Egypt
Egypt

Engy H. Mahmoud
Faculty of Pharmacy, Alexandria University, Egypt
Egypt

Sally Galal
Faculty of Pharmacy, Alexandria University, Egypt
Egypt

Aly H. Nada
Faculty of Pharmacy, Alexandria University, Egypt
Kuwait


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