STUDY ON CAUSE-EFFECT RELATIONS AND OPTIMIZATION OF TABLETS CONTAINING AQUILARIA CRASSNA SPRAY-DRIED EXTRACT
Objective: The aim of this study was to develop and optimize the formulation of tablets containing Aquilaria crassna extract using the direct compression method.
Methods: D-optimal design based on three independent variables was applied to evaluate the cause-effect relations and optimize the A. crassna tablet formulation. The weight variation (Y1), disintegration time (Y2), hardness (Y3) and friability (Y4) were investigated with respect to three independent variables including % dicalcium phosphate anhydrous (DCPA) in filler (X1), % filler (X2) and % croscarmellose sodium (CCNa) (X3). The dissolution study of the optimized A. crassna tablets were investigated in simulated gastric fluid (SGF) (pH 1.2) using a validated high-performance liquid chromatography (HPLC) method for mangiferin analysis.
Results: All investigation factors were found to have significant effects on the physical properties of A. crassna tablet. The tablet hardness and the disintegration time increased in positive relations with the ratios of DCPA. The results exhibited the negative relations between disintegration time and the percentages of CCNa. The optimized A. crassna tablet formulation which included 35 % (w/w) DCPA in filler, 60 % (w/w) filler and 7% (w/w) CCNa possessed the weight variation of 1.38 % (w/w), the disintegration time of 6.29 min, the hardness of 85.63 N and the friability of 0.41 % (w/w). The optimized A. crassna tablet formulation was experimentally examined which demonstrated a good agreement between the experimental and predicted values. Mangiferin was found to release completely from the optimized A. crassna tablets within 30 min.
Conclusion: The cause-effect relations and optimization of A. crassna tablet formulation were investigated and reported for the first time. The A. crassna spray-dried extract could be formulated into tablet by direct compression method with good mechanical properties and acceptable release profile.
2. Pranakhon R, Pannangpetch P, Aromdee C. Antihyperglycemic activity of agarwood leaf extracts in STZ-induced diabetic rats and glucose uptake enhancement activity in rat adipocytes. Songklanakarin J Sci Technol 2011;33:405-10.
3. Ito T, Kakino M, Tazawa S, Oyama M, Maruyama H, Araki Y, et al. Identification of phenolic compounds in Aquilaria crassna leaves via liquid chromatography-electrospray ionization mass spectroscopy. Food Sci Technol Res 2012;18:259-62.
4. Kakino M, Izuta H, Ito T, Tsuruma K, Araki Y, Shimazawa M, et al. Agarwood induced laxative effects via acetylcholine receptors on loperamide-induced constipation in mice. Biosci Biotechnol Biochem 2010;74:1550-5.
5. Telang M, Dhulap S, Mandhare A, Hirwani R. Therapeutic and cosmetic applications of mangiferin: a patent review. Expert Opin Ther Pat 2013;23:1561-80.
6. Yoshimi N, Matsunaga K, Katayama M, Yamada Y, Kuno T, Qiao Z, et al. The inhibitory effects of mangiferin, a naturally occurring glucosylxanthone, in bowel carcinogenesis of male F344 rats. Cancer Lett 2001;163:163-70.
7. Kumare MM, Marathe RP, Kawade RM, Ghante MH, Shendarkar GR. Design of fast dissolving tablet of atenolol using novel co-processed superdisintegrant. Asian J Pharm Clin Res 2013;3:81-5.
8. Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment-a review. Int J Pharm 2014;473:64-72.
9. Peck GE, Anderson NR, Banker GS. Principles of improved tablet production system design. In: Liebermann HA, Lachman L, Schwartz JB. editors. Pharmaceutical Dosage Forms: Tablets. Lea and Febiger; 1990. p. 1-76.
10. Hentzschel CM, Sakmann A, Leopold CS. Comparison of traditional and novel tableting excipients: physical and compaction properties. Pharm Dev Technol 2012;17:649-53.
11. Ilic I, Govedarica B, Sibanc R, Dreu R, Srcic S. Deformation properties of pharmaceutical excipients determined using an in-die and out-die method. Int J Pharm 2013;446:6-15.
12. Utami D, Nugrahani I, Ibrahim S. Mefenamic acid-nicotinamide co-crystal synthesized by using melt crystallization method and its solubility study. Asian J Pharm Clin Res 2017;10:135-9.
13. British Pharmacopoeia. London, United Kingdom: The General Council of Medical education and Registration of the United Kingdom 2013.
14. Jallo LJ, Dave RN. Explaining electrostatic charging and flow of surface-modified acetaminophen powders as a function of relative humidity through surface energetics. J Pharm Sci 2015;104:2225-32.
15. Bushra R, Shoaib MH, Ali H, Zafar F, Naeem MI, Aslam N, et al. Formulation design and optimization of aceclofenac tablets (100 mg) using central composite design with response surface methodology. Latt Am J Pharm 2014;33:1009-18.
16. Rojas J, Guisao S, Ruge V. Functional assessment of four types of disintegrants and their effect on the spironolactone release properties. AAPS PharmSciTech 2012;13:1054-62.
17. Autamashih M, Isah AB, Allagh TS, Ibrahim MA. Use of anhydrous calcium phosphate and selected binders in the tablet formulation of a deliquescent crude plant extract: Vernonia galamensis (Asteraceae). J Appl Pharm Sci 2011;1:118-22.
18. Tibalinda P, Sempombe J, Shedafa R, Masota N, Pius D, Temu M, et al. Formulation development and optimization of lamivudine 300 mg and tenofovir disopropxil fumarate (TDF) 300 mg FDC tablets by D-optimal mixture design. Heliyon 2016;2:e00207.
19. Tye CK, Sun CC, Amidon GE. Evaluation of the effects of tableting speed on the relationships between compaction pressure, tablet tensile strength, and tablet solid fraction. J Pharm Sci 2005;94:465-72.
20. Vithani K, Maniruzzaman M, Slipper IJ, Mostafa S, Miolane C, Cuppok Y, et al. Sustained release solid lipid matrices processed by hot-melt extrusion (HME). Colloids Surf B 2013;110:403-10.
21. Thoorens G, Krier F, Leclercq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environmentâ€“a review. Int J Pharm 2014;473:64-72.
22. Solaiman A, Suliman AS, Shinde S, Naz S, Elkordy AA. Application of general multilevel factorial design with formulation of fast disintegrating tablets containing croscarmellose sodium and Disintequick MCC-25. Int J Pharm 2016;501:87-95.
23. Agrawal A, Dudhedia M, Deng W, Shepard K, Zhong L, Povilaitis E, et al. Development of tablet formulation of amorphous solid dispersions prepared by hot melt extrusion using quality by design approach. AAPS PharmSciTech 2016;17:214-32.
24. Akhtar MS, Malik A, Bashir S, Baig MF, Irshad N. Pharmaceutical evaluation of different brands of levofloxacin tablets (500 mg) available in Pakistan. Int J Curr Pharm Res 2013;5:42-5.
25. Oza NA, Sahu AR, Tripathi SN, Patel PU, Patel LD, Ramkishan A. Formulation development and optimization of fast orodispersible tablets of naratriptan hydrochloride by using factorial design. Int J Res Med 2013;2:48-53.