PREPARATION AND IN VITRO EVALUATION OF CYCLODEXTRIN BASED EFFERVESCENT AND DISPERSIBLE GRANULES OF CARBAMAZEPINE


Hussain Ali M. Hussain, Eman B.h. Al-khedairy

Abstract


Objective: Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. One of the major problems with this drug is its low solubility in water; therefore the objective of this study was to enhance the solubility of carbamazepine by complexation with cyclodextrin to be formulated as effervescent and dispersible granules.

Methods: Solvent evaporation method was used to prepare, binary (Carbamazepine/β-cyclodextrin) complex and ternary (Carbamazepine/β-cyclodextrin/hydroxypropyl methyl cellulose (HPMC E5). The more soluble complex will be further formulated as unit dose effervescent and dispersible granules. The complexes were evaluated for their solubility, drug content, percentage practical yield and differential scanning calorimetery (DSC) to confirm the formation of the complex.

Results: The ratio of effervescent components, amount of effervescent base, amount of croscarmellose sodium (superdisintegrant) within the formula were found to play a role in the percentage of drug dissolved. Among the all prepared formulas, the effervescent granules containing ternary complex equivalent to 200 or 100 carbamazepine with effervescent base of 1:2:3.4 citric acid: tartaric acid: sodium bicarbonate not less than 48% w/w and 3% w/w croscarmellose sodium within the formula may be considered as a promising formulas regarding the amount of drug dissolved within 5 min.

Conclusion: The solubility of carbamazepine was enhanced by complexation with β-cyclodextrin and HPMC E5 as a ternary complex. Hence effervescent and dispersible granules of carbamazepine with good flow properties can be successfully prepared by using this complex.


Keywords


Carbamazepine, β-cyclodextrin, HPMCE5, Effervescent granules, Effervescent base

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References


Aulton ME. Pharmaceutics: the science of dosage form design. 2nd ed. New York: Churchill Livingstone; 2002.

Palanisamy P, Abhishekh R, Kumar KD. Formulation and evaluation of effervescent tablet of aceclofenac. Int Res J Pharm 2011;2:185-90.

Cherukuri PC, Palanisamy P, Krishna VA, Aparna S, Ali S S, Rakesh P, et al. Formulation and evaluation of effervescent tablets of paracetamol. Int J Pharm Res Dev 2011;3:76-104.

British Pharmacopoeia. Vol. III. Formulated preparations: General Monographs; 2009.

Rogawski MA, Loscher W, Rho JM. Mechanisms of action of antiseizure drugs and the ketogenic diet. Cold Spring Harb Perspect Med 2016;6:1-28.

Shahira F El-Menshawe, Essam E, Adel A Ali, Ahmed A Abderhman. Enhancement of lornoxicam solubility by inclusion complexation with cyclodextrin: preparation and characterization. Int J Pharm Pharm Sci 2017;9:132-8.

Jouyban A. Hand book of solubility data for pharmaceuticals. 1st ed. Taylor and Francis Group USA; 2010.

Higuchi T, Connors KA. Phase solubility techniques. ADV Anal Chem Instrum 1965;4:117–212.

Jagdale SC, Gawali VU, 10-Kuchekar BS, Chabukswar AR. Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride. Braz J Pharm Sci 2011;47:908-16.

Kuchekar BS, Narkhede M. The effect of water soluble polymers on felodipine aqueous solubility and complexing abilities with natural and modified β-cyclodextrin. Indian J Pharm Sci 2007;2:197-202.

Shirser P, Rao KS, Iqbal MM. Formulation and evaluation of cyclodextrin inclusion complex tablets of water insoluble drug-glimepiride. Int J Res Pharm Chem 2012;2:222-30.

Shekhr I, Gupta V, Jain A, Gupta N. Preparation and characterization of β cyclodextrin aspirin inclusion complex. Int J Pharm Life Sci 2011;2:704-10.

Parmar GR, Gandhi KS, Sailor GU, Chauhan SP, Seth AK. Influence of ethylcellulose on dissolution profile of carbamazepine cyclodextrin complex. Iran J Pharm Res 2014;6:43-7.

Doile MM, Fortunato KA, Schmücker IC, Schucko SK, Silva MAS, Patrik O Rodrigues. Physicochemical properties and dissolution studies of dexamethasone acetate-β-. cyclodextrin inclusion complexes produced by different methods. AAPS PharmSciTech 2008;9:314-21.

Ashok T, Veeravalli SK, Pavan KM, Roshitha B. Effect of effervescence in combination with superdisintegrants in the formulation of propranolol HCl oral disintegrating tablets. Asian J Pharm Clin Res 2017;10:227-34.

Bhattacharyya S, Swetha G. Formulation and evaluation of effervescent granules of fexofenadine hydrochloride. Pharma Innovation J 2014;3:1-8.

Shanbhag P PS, Bhalerao S. Development and evaluation of antipyretic pediatric formulation. Int J Pharm Tech Res 2009;1:1373-5.

Sagar TB, Yogesh SP, Swati RS, Satish NL. Formulation development and evaluation of effervescent tablet of alendronate sodium with vitamin D3. J Drug Delivery Ther 2013;3:65-74.

Pandey A, Rath B. Improved physicochemical characteristics of amorphous drug solid dispersions. Res J Pharm Biol Chem Sci 2012;3:844-9.

Ashok RP, Pradeep RV. Preparation and evaluation of taste masked famotidine formulation using drug/β-cyclodextrin/polymer ternary complexation approach. AAPS PharmSciTech 2008;9:544-50.

Gabriel OKL, Fung Tan YT, Khiang Peh K. Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin. Afr J Plant Sci 2016;11:536-46.

Stella VJ, Rao VM, Zannou EA, Zia V. Mechanisms of drug release from cyclodextrin complexes. Adv Drug Delivery Rev 1999;36:3–16.

Neito N, Sanchez SE, Amoza G, Espinar O. Competitive displacement of drugs from cyclodextrin inclusion complex by polypseudorotaxane formation with poloxamer: implications in drug solubilization and delivery. Eur J Pharm Biopharm 2012;80:585-95.

Jones D. Pharmaceutics–dosage form and design 1st ed. Pharmaceutical Press: London; 2008.

USP30 NF25 2007.

Om M Bagade, Priyanka P Kharat, Rohini R Pujari, VS Raskar, Amruta M Shete, Maduhri D Vanve. Design and statistical optimization of antacid analgesic effervescent tablets by using factorial design. Int J Pharm Pharm Sci 2014;6:453-9.




About this article

Title

PREPARATION AND IN VITRO EVALUATION OF CYCLODEXTRIN BASED EFFERVESCENT AND DISPERSIBLE GRANULES OF CARBAMAZEPINE

Keywords

Carbamazepine, β-cyclodextrin, HPMCE5, Effervescent granules, Effervescent base

DOI

10.22159/ijap.2018v10i6.28276

Date

15-10-2018

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Articles In Press [Scheduled in Nov-Dec 2018] Page: 290-297

Online ISSN

0975-7058

Authors & Affiliations

Hussain Ali M. Hussain
Ministry of Health and Environment, Baghdad, Iraq
Iraq

Eman B.h. Al-khedairy
Department of Pharmaceutics, College of Pharmacy/University of Baghdad, Baghdad, Iraq
Iraq


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