APPLICATION OF LIQUISOLID TECHNOLOGY TO ENHANCE THE DISSOLUTION OF CEFIXIME FROM ITS ORAL CAPSULES
Keywords:Cefixime trihydrate, liquisolid, microcrystalline cellulose
Objective: Oral drug delivery is the most desired route for drug administration for its well-known features. Therefore, many attempts were implemented to improve the poor solubility of many active ingredients in order to enhance their dissolution and absorption via the oral route. From these, the liquisolid system is a very promising technology for enhancing solubility and bioavailability of poorly soluble drugs.
Methods: In this research, oral capsules of cefixime were prepared by liquisolid technique after mixing different concentrations of the drug with propylene glycol (non-volatile solvent), followed by their addition to different proportions of microcrystalline cellulose and aerosil i.e. different carrier: coating (R-value). The liquisolid capsules were evaluated for In vitro disintegration and dissolution in addition to content uniformity and weight variations. Furthermore, solubility studies, scanning electron microscope (SEM) were performed to the optimum formula. Finally, the release profile of the optimum formula was compared with the marketed cefixime capsules.
Results: Liquisolid formula (F3) with 70% cefixime and R-value equals 10 was selected as the optimum formula having higher % release in 45 min (99.5%Â±0.53) compared to other formulas with faster release rate in the first 20 min than marketed capsules. It had an acceptable disintegration time (25 minÂ±0.76), content uniformity (197.6Â±0.92) and weight variation (698.04Â±0.16). Results of solubility study, SEM assured enhancement in solubility and dispersibility of the drug.
Conclusion: This research proved that liquisolid system is a promising technology in improving the solubility and dissolution of cefixime from its capsules and hence it may improve its absorption and oral bioavailability.
Soujanya BS, Srujan MK, Subrahmanyam KV, Shubhrajit M. Enhancement of solubility of efavirenz by liquisolid compact technique. Int J Innov Pharm Sci Res 2013;1:347-59.
Rajkumar G, Kalla M, Swathi RT, Anilkumar V, Indarapu RP. Enhancement of solubility and dissolution rate of ezetimibe through liquisolid technique. Int J Pharm Sci Res 2013;4:3229-38.
Mokale V, Naik J, Patil K, Chaudhari R, Khairnar G. Enhancement of solubility with the formulation and in vitro evaluation of oral nateglinide compacts by liquisolid technique. Adv Diabetes Metab 2013;1:57-64.
Pavan RK, Karimunnisa SS, Pravin DC. Application of liquisolid technology for enhancing solubility and dissolution of rosuvastatin. Adv Pharm Bull 2014;4:197-204.
Shailendra SS, Pritesh P, Sachin J, Praveen S, Biresh S. Formulation and evaluation of curcumin liquisolid tablets. Curr Res Pharm Sci 2012;4:210-4.
Ngiik T, Amal AE. Effects of liquisolid formulations on the dissolution of naproxen. Eur J Pharm Biopharm 2009;73:373â€“84.
Indrajeet DG, Amrit BK, Avinash HH. Evaluation of in vitro dissolution profile comparison methods of sustained release tramadol hydrochloride liquisolid compact formulations with marketed sustained-release tablets. Dig J Nanomater Biostruct 2009;4:651â€“61.
Spireas S, Bolton M. Liquisolid systems and methods of preparing same. United States Patent Application Publication 5,968,550A; 1999.
Sai SR, Shamili K, Sathesh PR, Subrahmanyam VS. Formulation and in vitro evaluation of efavirenz liquisolid compacts. Int J Pharm Pharm Sci 2016;8:137-43.
Suryakant S, Chinam NP, Bhanoji ME. Pharmaceutical drug delivery systems and vehicles. In: Chinam NP, Suryakanta S, Kahnu CP, Muddana EB. editors. An overview of liquisolid technology. India: Woodhead Publishing; 2016. p. 146-60.
Satyajit P, Varaprasad R, Priyanka K, Ranjit P. Liquisolid technique: a novel approach for dosage form design. Int J Appl Pharm 2017;9:8-14.
Maraie NK, Emad A. Comparative study between liquisolid compacts, liquisolid microsystem and solid dispersion technology for the preparation of immediate release nicardipine tablets. Int J Pharm Sci Rev Res 2017;43:116-26.
Sweetman SC. editor. Martindale the complete drug reference. China: Pharmaceutical Press publishing; 2009.
Anthony CM, David MO, Brian W. Clarke's analysis of drugs and poisons. London: Pharmaceutical Press; 2005.
Patel N. Liquisolid dosage system: a novel approach for dosage formulation. J Pharm Sci Bio-Sci Res 2014;4:125-30.
Shrikant M. Liquisolid technique for dissolution and bioavailability enhancement of poorly soluble drugs. Univers J Pharm Res 2017;2:46-53.
Spireas S. Liquisolid systems and methods of preparing same, United States Patent Application Publication 5,800,834; 1998.
Gilbert SB, Neil RA. The theory and practice of industrial pharmacy. In: Lachman L, Lieberman HA. editors. Tablets. India: CBS Publishing; 2009. p. 293-4.
Reecha M, Rajni B, Tejeswini V, Ritima S, Shivali G. Formulation and characterization of matrix tablets using mucilage of tinosporacordifolia as a natural binder. Int J Pharm Pharm Sci 2018;10:22-7.
Mogal P, Derle D. Optimization and formulation development of cefixime complex using a spray drying technique: doe approach. J Appl Pharm 2017;9:1-8.
Pawar JD, Jagtap RS, Doijad RC, Desai JR, Pol SV, Jadhav VV, et al. Dissolution enhancement of Itraconazole by liquisolid compacts techniques and its in vitro evaluation. Asian J Sci Technol 2017;8:5894-9.
Rajesh A, Alpesh Y, Isha S, Sangeeta A, Shailendra B. The liquisolid technique: a review. Int J Pharm Res Bio-Sci 2013;2:464-73.
Silverstein RM, Webster FX, Kiemle D. editors. Infrared spectrometry. New York: Wiley publishing; 2005.
Allen LV, Popovich NG, Ansel HC. editors. Capsule. Philadilphia: Lippincott Williams and Wilkins Publishing; 2011.
Mogal P, Deeliprao D. Cefixime, in general, class 4 drug but individually class 2 drug. J Med Physiol Ther 2017;1:1-10.
Remeth JD, Kailas KM, Vishwajeet SG, Vijay DH, Vishal RM. Formulation and evaluation of carbamazepine liquisolid compacts using novel carriers. Indian J Pharm Edu 2017;51:69-78.
Rania HF, Mohammed AK. Enhancement of famotidine dissolution rate through liquisolid tablets formulation: in vitro and in vivo evaluation. Eur J Pharm Biopharm 2008;69:993â€“1003.
Janakidevi S, Ramanamurthy KV. Formulation and evaluation of cefixime trihydrate matrix tablets using hpmc, sodium cmc, ethyl cellulose. Indian J Pharm Sci 2015;77:321-7.
Evangelos K, Georgios K, Aristotelis X, Emmanouel G. Effect of hydrogen bonding interactions on the release mechanisim of felodipine from nanodispersions with polyvinylpyrrolidone. Eur J Pharm Biopharm 2006;63:1-12.
Remeth JD, Shashi R, Kailas KM, Vishwajeet SG, Vijay DH. Liquisolid compacts of meloxicam: in vitro and in vivo evaluation. Egypt Pharm J 2017;16:112-20.