FORMULATION AND EVALUATION OF SYNTHESIZED QUINAZOLINONE DERIVATIVE FOR COLON SPECIFIC DRUG DELIVERY


Vidya Viswanad, Shammika P, Aneesh Tp

Abstract


ABSTRACT
Objective: The current research deals with the formulation and evaluation of synthesized quinazolinone derivative for colon site specific delivery.
Methods: The synthesized quinazolinone derivative was enteric coated 5% Eudragit L-100 with by wet granulation method using guar gum, pectin,
and guar gum pectin combination as hydrophilic polymer. The prepared matrix tablet was characterized by differential scanning calorimetry and
evaluated for different pre-compression and post-compression studies and drug release profiles.
Results: All the matrix tablets were within the range of pharmacopeial limits with better flow properties. All the six formulations of matrix tablets had
disintegrated within 5-6 minutes. The optimized formulation selected was F6 formulation combination of guar gum and pectin with 95.79% of drug
release than compared to the remaining formulation. The optimized matrix tablets followed zero order kinetics with Fickian diffusion.
Conclusion: The results proposed that the combination of guar gum and pectin coated tablet with 5% Eudragit L-100 of synthesized quinazolinone
derivative is a promising colon site specific delivery.
Keywords: Quinazolinone derivative, In vitro drug release, Disintegration time, Guar gum, Pectin, 5% Eudragit L-100, Colon site-specific delivery, Wet
granulation, Compression.


| PDF |

References


REFERENCES

Sinha VR, Kumria R. Colonic drug delivery: Prodrug approach. Pharm Res 2001;224(5):557-64.

Grover G, Kini SG. Synthesis and evaluation of new quinazolinone derivative of nalidixic acid as potential anticancer and antifungal agent. Eur J Chem 2007;42:1234-8.

Giri RS, Thaker HM. Design, synthesis and characterization of novel 2-(2,4-disubstututed-thiazole-5-yl)-3-aryl-3H-quinazoline-4-one derivatives as inhibitors of NF-kappa B and AP-1mediated transcription activation and as potential anti-inflammatory agents. Eur J Med Chem 2009;44:2184-9.

Kohli D, Hashim SR, Vishal S, Sharma M, Singh A. Synthesis and antibacterial activity of quinazolinone derivatives. Int J Pharm Pharm Sci 2009;1(1):163-9.

Nagwa MA, Hanan HG, Riham MY, Nehad AE. Synthesis and antitumor activity of some 2, 3-disubstituted quinazolin-4(3H)-ones and 4,6-disubstituted-1,2,3,4-tetrahydroquinazolin-2H-ones. Eur J Med Chem 2010;45:6058-67.

Ye C, You J, Li XF, You R, Weng Y, Li J, et al. Design, synthesis and anticoccidial activity of a series of 3-(2-(2-methoxyphenyl)-2-oxoethyl) quinazolinone derivatives. Pesticide Biochem Physiol 2010;97:194-8.

Aly MM, Mohamed YA, El-Bayouki KA. Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities. Eur J Med Chem 2010;45(8):3365-73.

Anjana MN, Joseph J, Nair SC. Solubility enhancement methods - Apromising technology for poorly water soluble drugs. Int J Pharm Sci Res 2013;20(2):127-34.

Ramprasad YV, Krishnaiah YS, Satyanarayana S. In vitro evaluation of guar gum as a carrier for colon-specific drug delivery. J Controlled Release 1998;59:281-7.

Kothawade PD, Gangurde HH. Conventional and novel approaches for colon specific drug delivery: A review. E-JST J Controlled Release 2011;6(2):33-56.

Sinha VR, Kumria R. Microbially triggered drug delivery to the colon. Eur J Pharm Sci 2003;18:3.

Khan MZ, Prebeg Z, Kurjakovic N. A pH dependent colon targeted oral drug delivery system using methacrylic acid copolymers: Manipulation of drug release using Eudragit L100-55 and Eudragit S 100 combinations. J Controll Release 2014;58:215-22.

Wajid S. Formulation and evaluation of colon targeted drug delivery system for antineoplastic drug. Int J Res Pharm Chem 2013;3(3):697-707.

Yang L, Chu JS, Fix JA. Colon-specific drug delivery: New approaches and in vitro/in vivo evaluation. Int J Pharm 2002;235(1-2):1-15.

Ashford M, Fell JT, Attwood D, Sharma H, Woodhead P. An evaluation of pectin as a carrier for drug targeting to colon. J Controlled Release 1993;26:213-220.

Aswar PB, Khadabadi SS, Kuchekar BS, Wane TP, Matake N. Development and evaluation of colon specific formulations for orally administered diclofenac sodium. Arch Pharm Sci Res 2009;1(7):48-53.

Ashutosh M, Parikh RK, Parikh MC. Formulation, development and evaluate; on of patient friendly dosage forms of metformin. Asian J Pharm 2008;2:177-81.

Singh BN. Modified-release solid formulations for colonic delivery. Recent Pat Drug Deliv Formul 2007;1(1):53-64.

Randall J. The colon as a site for drug delivery. J Controlled Release 1992;22:15-34.

Krishnaiah YS, Reddy PR, Satyanarayana V, Karthikeyan RS. Studies on the development of oral colon targeted drug delivery systems for metronidazole in the treatment of amoebiasis. Int J Pharm

Fig. 4: (a) Zero order kinetics, (b) First order kinetics, (c) Higuchi model, (d) Koresmeyer–Peppas model

a

b

c

d

Asian J Pharm Clin Res, Vol 10, Issue 3, 2017, 207-212

Shammika et al.

;236(2):43-55.

Wu B, Chen Z, Wei X, Sun N, Lu Y, Wu W. Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: I. Characterization and mechanistic study. Eur J Pharm Biopharm 2007;67(3):707-14.

Liu X, Sun Q, Wang H, Zhang L, Wang JY. Microspheres of corn protein, zein, for an ivermectin drug delivery system. Biomaterials 2005;26(1):109-115.

Florey K, David WF. Analytical Profiles of Drug Substances-Ivermectin. New Delhi: Academic Press-Elsevier; 2005. p. 156-84.

Fatima L, Asghar A, Chandran S. Multiparticulate formulation approach to colon specific drug delivery: Current perspectives. J Pharm Pharm Sci 2006;9(3):327-38.

Jain HN, Patel KR, Kanzariya VR, Shah HN, Upadhyay UM. Formulation and evaluation of colon targeted matrix tablet of naproxen. Int J Pharm Pharm Sci 2014;6(8):183-6.

Vivekanandan K, Gunasekaran V, Jayabalan G. Design and evaluation of colon specific drug delivery of budenoside. Int J Pharm Pharm Sci 2015;7(1):261-3.

Takashi I. Design and evaluation of a new capsule-type dosage form for colon-targeted delivery of drugs. Int J Pharm 1998;87(5):31-40.

Dorozynski P, Jachowicz R, Jasinski A, Kulinowski P, Kwiecinski S, Skorka T, et al. The polymers for the preparation of hydrodynamically balanced systems: Methods of evaluation. Drug Dev Ind Pharm 2004;9(9):947-57.

Prasad YV, Krishnaiah YS, Satyanarayana S. In vitro evaluation of guar gum as a carrier for colon-specific drug delivery. J Controlled Release 1998;51(2-3):281-7.

Kotwal A. Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulfate. AAPS Pharm Sci Technol 2007;8(4):88.

Umamaheswari RB, Jain S, Tripathi PK, Agrawal GP, Jain NK. Floating-bioadhesive microspheres containing acetohydroxamic acid for clearance of Helicobacter pylori. Drug Deliv 2002;9(4):223-31.

Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: Design and release kinetics. Drug Dev Ind Pharm 2000;26(9):965-9.

Sruthy PN, Anoop KR. Formulation and evaluation of olmesartan medoxomil floating tablets. Int J Pharm Pharm Sci 2013;5(3):0975-1491.




About this article

Title

FORMULATION AND EVALUATION OF SYNTHESIZED QUINAZOLINONE DERIVATIVE FOR COLON SPECIFIC DRUG DELIVERY

DOI

10.22159/ajpcr.2017.v10i3.16024

Date

01-03-2017

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 10 Issue 3 March 2017 Page: 207-212

Print ISSN

0974-2441

Online ISSN

2455-3891

Statistics

126 Views | 189 Downloads

Authors & Affiliations

Vidya Viswanad

Shammika P

Aneesh Tp


Article Tools


Email this article (Login required)
Email the author (Login required)

Refbacks

  • There are currently no refbacks.