Formulation Development of Taste-Masked Rapidly Dissolving Films of Cetirizine Hydrochloride - Pharmaceutical Technology

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Formulation Development of Taste-Masked Rapidly Dissolving Films of Cetirizine Hydrochloride
The authors formulated and developed taste-masked RDFs of cetirizine hydrochloride for patients who experience difficultly in swallowing the tablet dosage form of the drug.


Pharmaceutical Technology
Volume 33, Issue 2, pp. 48-56


Figure 1: Comparative in-vitro dissolution profile of batch T3. (FIGURE IS COURTESY OF THE AUTHORS.)
Table III indicates that the subsequent addition of citric acid and passion fruit flavor (batches T1 and T3) resulted in completely taste-masked films. The in vitro disintegration time was 50 s and the in vivo disintegration time of batch T3 was 20 s. The addition of lemon flavor (batches T2 and T4) resulted in highly acidic taste of the film, which was unacceptable. Batch T3 showed good elasticity and taste masking properties. Figure 1 indicates the comparative in vitro dissolution profile of batch T3 in different dissolution media. Figure 1 shows that in 2 min batch T3 showed 100% drug release in distilled water, 95% in 0.1 N HCl, and 80% in simulated saliva.


Table IV : Comparative mechanical properties.
Study of mechanical properties. A suitable RDF requires moderate tensile strength, good percentage elongation, and low elastic modulus. Table IV shows the comparative mechanical properties of various formulations prepared during the study. RDFs containing 2% and 4% HPMC E3 LV without drug (i.e., batches 2E and 4E) showed extremely high tensile strength, poor percent elongation, and very high elastic modulus. The same formulation in the presence of drug and plasticizer (i.e., batch E9) demonstrated lower tensile strength compared with batch 2E and 4E. The percent elongation values increased and elastic modulus values decreased. The taste-masked batches S4 and T3 had acceptable mechanical properties. The tensile strength was in a moderate range (4–9 N/m2 ). The percent elongation (21–28) and elastic modulus (35–165) were also satisfactory. These changes in the mechanical properties can be attributed to the presence of plasticizer in batches E9, S4, and T3. Batch T3 showed the most acceptable mechanical properties along with complete taste masking, which might be attributed to the presence of suitable plasticizers and flavors. The stability study of the optimized batch T3 was carried out at 25 ?C for a one-year period. The batch was found be acceptable visually, mechanically, with a slight increase in the in vitro and in vivo disintegration time of 55 s and 22 s, respectively.

Conclusion

RDFs containing taste-masked CTZ showed acceptable properties such as tensile strength, elasticity, percentage elongation, in vitro disintegration, and in vitro dissolution characteristics. The RDFs were transparent, without any air entrapment. The drug-release profiles indicated that it could be used for the oral delivery of CTZ in chronic and acute urticaria as well as perennial rhinitis. Taste masking could be achieved using suitable sweeteners, flavors, and sour ingredients. The various grades of HPMC E LV highly affected the in vitro disintegration time and in vitro dissolution profiles. HPMC E3 LV was the most suitable grade for the manufacture of RDF containing CTZ.

Renuka Mishra is a lecturer in the department of pharmaceutical technology, and Avani Amin, PhD,* is principal and I/C director, both at the Institute of Pharmacy, Nirma University of Science and Technology, Sarkhej-Gandhinagar Highway, Ahmedabad, Gujarat, India, tel. 91 02717 241900 to 04, fax 91 02717 241916,

*To whom all correspondence should be addressed.

Submitted: May 1, 2008. Accepted: May 9, 2008.




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