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Drug Development & Delivery July/August 2012 Vol 12 No 6 22 evaluation of the ability to fit to the model, and response surface methodology (RSM) were performed by employing Design-Expert ® software (Version 7.1.2, Stat-Ease Inc., Minneapolis, MN). RSM is a collection of mathematical and statistical techniques useful for the modeling and analysis of problems in which a response of interest is influenced by several variables and the objective is to optimize this response. The most extensive applications of RSM are in the industrial world, particularly in situations where several input variables potentially influence some performance measure or quality characteristic of the product or process. This performance measure or quality characteristic is called the response. A. B. Factors (Independent Variables) Chewing time (mins.) Amount of gum powder (%) Table 3 summarizes the independent and dependent variables along with their coded and actual levels. A total of four experimental testing runs were conducted. It was illustrated from the surface response graph that as chewing time (A) increases, percent of drug release increases as well, but an increasing amount of gum powder (B) has very little drop-off effect on T A B L E 3 Results of official product quality assessment tests. Levels Used -1 0 +1 5 70 10 75 T A B L E 4 Experimental Variable Factors in Coded tTerms (Actual Terms) Test Run Chewing Time Amt. of Gum (mins.) Powder (%) 1 -1(05) -1(70) 2 0(10) -1(70) 3 +1(15) -1(70) 4 - 1(05) 0(75) 5 0(10) 0(75) 6 +1(15) 0(75) 7 -1(05) +1(80) 8 0(10) +1(80) 9 +1(15) +1(80) Experimental testing runs with values of variable factors. 15 80 Response (Dependent Variables) % Drug Release percent of caffeine release. Specifically: % Drug Release = + 88.33 + 5.67 A - 1.50 B + 0.25 AB - 2.00 A²- 0.50 B². The quadratic models generated by regression analysis were used to construct a two-dimensional contour plot and threedimensional response surface plot in which response parameter DR was represented by a curvature surface as a function of A and B. Figure 1 shows the effect of chewing time and amount of gum powder in contour plot as well as response surface plot. A numerical optimization technique using the desirability approach was employed to develop a new formulation with the desired responses. In this study, optimization was performed with constraints for DR (90% < DR < 95%) set as goals to locate the optimum settings of the independent variables in the new formulation. The optimal parameters to achieve predicted CFN release of 92% (90% to 95%) as calculated from the predicted equation of drug release (A: chewing time = 15 minutes, and B: amount of gum powder = 75%). CONCLUSION Optimized formulation of directly compressed CFN-MCG has achieved the following: • Has passed all official MCG quality tests, including uniformity of mass, assay for uniformity of content, and friability testing as per compliance criteria mentioned in the official monograph of MCG in BP. • Released an average 92% of CFN (n=6) within 15 minutes of chewing, which is half of the normal average chewing time, in an in vivo chew out study. • Interindividual variability in percent CFN-release was observed in only up to 1 to 3 minutes, afterward, much less interindividual variability was observed in percent CFN release. Thus, the present study demonstrated that CFN could be successfully delivered by MCG into systemic circulation via direct intraoral buccal absorption. Concerning statistical analysis, it was shown that a 32 full factorial experimental design (FFED) and optimization technique can be successfully used in the development of an optimized formulation of MCG and for deciding appropriate chewing time for sufficient drug release. The optimized formulation exhibited drug release profiles that were close to the predicted responses, which was confirmed by high significant r2 = 0.988 (> 0.9) value. Based on the overall results, it was concluded that the developed formulation of directly compressible taste-masked MCG of caffeine presents a better alternative to any other dosage form, including tea or coffee, because it is a synergistic delivery option for
staying alert. Moreover, CFN-MCG can be taken anywhere and anytime without preventing the consumer from living an active life, which promotes higher acceptance and compliance. Moreover today, it is known that chewing gum has other benefits: it promotes oral health, it is a mild stress relief, and it reduces the appetite sensation, all of which are added positive characteristics that increase the value of a caffeine drug delivery system in the form of chewing gum.This eventually can lead to the development of a new attractive market directed to energy and sports products, which is already flourishing in occidental countries. Other potential applications for MCG include areas like allergy, cough and cold, digestive, and oral care, added to the consolidated available nicotine and motion sickness gums. u REFERENCES 1. European Pharmacopoeia, 2.9.5., 2.9.6, 2.9.7, 2.9.25, 2.9.36, 6th edition. 2. Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry. 11th ed. New York, NY: Lippincott Williams & Wilkins Publishing; 2004:511- 512. 3. Adopted from www.chewinggumfacts.com/chewing-gumbenefits/health-benefits-of-gum-chewing. 4. Jacobsen, Christrup-LL. Medicated chewing Ggum: Ppros and cons. Am J Drug Del. 2004;2(4):75-88. B I O G R A P H I E S Shivang Chaudhary is a Formulation Scientist with a BPharm from Nirma University of Science & Technology, India, and an MSPharm in Pharmaceutics from the National Institute of Pharmaceutical Education & Research (NIPER), Ahmedabad. During his Masters he felt a necessity of reformulating existing drugs into Novel Drug Delivery Systems (NDDS) to extend or protect product patents thereby delaying, reducing, or avoiding generic erosion at patent expiry. Apart from this chewing gum containing Caffeine (Alllert®) for staying alert, he has also developed medicated chewing gum containing different drugs for various other diseases, such as MCG for Erectile Dysfunction (EreX®) in vanilla, chocolate, strawberry, wild cherry, pineapple, and butterscotch flavors; MCG for motion sickness (Gaglet®) in cardamom, orange, lemon(lime), and ginger flavors; MCG for Vit-B12 deficiency (Smirk®) in banana flavor; and MCG for acidity (Relaaax®) in peppermint and spearmint flavors. He strongly believed that by formulating the drugs in MCG composition, revitalization of old products and reformulation of new patented products is possible to distinguish from future generics competition in the global market. Dr. Aliasgar Shahiwala is currently working as an Associate Professor in Dubai Pharmacy College. Before joining Dubai Pharmacy College, he was associated with the National Institute of Pharmaceutical Education and Research-Ahmedabad, India. Dr. Shahiwala has earned Masters and Doctorate degrees in Pharmaceutics and Pharmaceutical Technology from The Maharaja Sayajirao University of Baroda, India, and has completed 1-year of post-doctoral research experience at Northeastern University, USA. He has more than 3 years of rich research experience in the formulation and development division of large-scale manufacturers of pharmaceuticals in India and more than 7 years of teaching experience at both the graduate and post-graduate level. His research credentials have established him a reviewer, a member of editorial board, a speaker, and an invited author for various pharmaceutical scientific journals and conferences. Dr. Shahiwala’s key strength is diversity of work experience in different settings. Dr. Manju Misra is currently serving as Assistant Professor at NIPER Ahmedabad. She has prior experience working as part of an ANDA formulation development team at Macleods Pharmaceuticals, Mumbai, and Cadila Pharmaceuticals, Ahmedabad. She earned her PhD from BIT Mesra, Ranchi, India, and her MPharm from Nagpur University, India. Drug Development & Delivery July/August 2012 Vol 12 No 6 23
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