The Mechanical and In vitro Release Properties of Diazepam from Tablets Containing Fluid Bed Dried and Lyophilized Cocos nucifera Microcrystalline Cellulose

Main Article Content

Nkemakolam Nwachukwu
Sabinus Ifeanyi Ofoefule

Abstract

Aim: This study aimed to evaluate the mechanical and in vitro release properties of diazepam from tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from the matured fruit husks of Cocos nucifera (CN).


Study Design: Method of experiment.


Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from March 2015 to September, 2016


Methods:  Dried CN fruit husks were digested in sodium hydroxide to obtain alpha (α) cellulose which on hydrolysis with mineral acid (Hydrochloric acid) solution gave CN-MCC. The dry MCC obtained by either fluid bed or lyophilized drying of the wet CN-MCC were coded MCCF-Cocos and MCCL-Cocos respectively. Both MCCs were used in the formulation of diazepam tablets at 20, 30 and 40% w/w. Avicel PH 102 (AVC-102), was used as comparing standard. The tablets were evaluated for physical and dissolution properties using standard methods.


Results: Results show the tablets passed the British Pharmacopoeia specifications for weight uniformity, crushing strength, disintegration time, friability and dissolution. Diazepam tablets containing MCCL-Cocos (coded DCL) were mechanically stronger than those containing MCCF-Cocos (coded DCF). Disintegration time was in the order of DCF > DCL tablets while friability was in the order of DCL < DCF tablets. Diazepam tablets containing AVC-102 (coded DAV) were mechanically stronger than DCL and DCF tablets. The dilution potential was in the order DAV > DCL > DCF. More than 80% of the diazepam content was released from DAV, DCL and DCF tablets.


Conclusion: Generally, DAV, DCL and DCF tablets met the British Pharmacopoeia limits for mechanical properties and in vitro drug release with DCL tablets showing significantly (P = .05) superior mechanical properties while DCF showed faster drug release.

Keywords:
Tablets, mechanical, diazepam, Cocos nucifera, microcrystalline cellulose, dissolution

Article Details

How to Cite
Nwachukwu, N., & Ofoefule, S. (2019). The Mechanical and In vitro Release Properties of Diazepam from Tablets Containing Fluid Bed Dried and Lyophilized Cocos nucifera Microcrystalline Cellulose. Asian Journal of Research in Medical and Pharmaceutical Sciences, 7(3), 1-14. https://doi.org/10.9734/ajrimps/2019/v7i330120
Section
Original Research Article

References

Gibson LI. The hierarchical structure and mechanics of plant materials. J. R. Soc. Interface. 2012;9:2749–2766.

Gaitán A, Gacitúa W. Morphological and mechanical characterization of electrospun polylactic acid and microcrystalline cellulose. BioRes. 2018;13(2):3659-3673.

Thoorens G, Krier F, Leclerq B, Carlin B, Evrard B. Microcrystalline cellulose, a direct compression binder in a quality by design environment- a review. Int. Journal of Pharmaceutics. 2014;473:64-72.

Azubuike CP, Odulaja JO, Okhamafe AO. Physicotechnical, spectroscopic and thermogravimetric properties of powdered cellulose and microcrystalline cellulose derived from groundnut shells. J. Excipients and Food Chem. 2012;3(3): 106-115.

Klemm D, Hublein B, Fink HPC, Bohn A. Cellulose: Fascinating biopolymer and sustainable raw material, Anewandie Chemie-International Edition. 2005;44: 3358-3393.

Kong Y, Hay JN. The enthalpy of fusion and degree of crystallinity of polymers as measured by DSC. European Polymer Journal. 2003;39:1721-1727.

Ejikeme PM. Investigation of the physicochemical properties of microcrystalline cellulose from agricultural wastes I: Orange Mesocarp, Cellulose. 2008;15(1):141-147.

Nwachukwu N, Ofoefule SI. Effect of drying methods on the powder and tableting properties of microcrystalline cellulose obtained from Cocos nucifera. Journal of Pharmaceutical Research International. 2017;20(2):1-15.

Dennis V. Johnson. Enhancement of date palm as a source of multiple products: Examples from other industrialized palms. Emir. J. Food Agric. 2012;24(5): 408-414.

Hahn WJ. Arecanae: The palms. Retrieved April 4, 2016 from the Tree of Life Web Project; 1997.
Available:http://tolweb.org/Arecanae/21337

Milhorn HT. Sedative-hypnotic depen-dence. In substance use disorders. Springer, Cham. 2018;59-76.

British National Formulary (BNF 73), Diazepam. 2017;36.
Available:www. bnf.org

British Pharmacopoiea. Her Majesty Stationary Office, University Press, Cambridge. 2012;2:A326-327.

Armstrong NA. “Tableting” In: Aulton M.E. (Ed.), Pharmaceutics: The science of dosage form design. ELBS, Churchill Livingstone, London. 1990;663.

Evans WC. Trease and evans pharmacognosy. 13th Ed., Bailliere Tindall. 1989;339-377.

Lahdenpää E, Niskanen M, Yliruusi J. Crushing strength, disintegration time and weight variation of tablets compressed from three Avicelä PH grades and their mixtures. Eur. J. Pharm. Biopharm. 1997; 43:315–322.

USP 32. The U.S. Pharmacopioeal Convention, Rockville. 2009;2:2113- 2116.

Ghori MU, Conway BR. Powder compaction: Compression Properties of Cellulose Ethers, British Journal of Pharmacy. 2016;1:19-29.

Ingram JT, Lowenthal W. Mechanism of action of starch as a tablet disintegrant III: Factors Affecting Starch grain damage and their effect on swelling of starch grains and disintegration of tablets at 37°C. J Pharm Sci. 1968;57:393–8.

Zamostny P, Jetru P, Majerova D. Effect of maize starch excipient properties on drug release rate. Procedia Engineering. 2012; 42:482-488.

Hartesi B, Sriwododo, Abdassah M, Chaerunisaa AY. Starch as pharmaceutical excipient. Int. J. Pharm. Sci. Rev. Res. 2016;41(2):59-64.

Ahlneck, Zografi G. The molecular basis of moisture effects on the physical and chemical stability of drugs in the solid state. International Journal of Pharmacy. 2004;62:87-95.

Monika T, Kumar SA, Raj SA. Effect of moisture content of exicipient (microcrystalline cellulose) on direct compressible solid dosage forms. Int J Pharm Sci Res. 2017;8(1):282-88.
DOI: 10.13040/IJPSR.0975-8232.8(1).282-88

Gerhardt Armin. Moisture effects on solid dosage forms –formulation, processing and stability. Journal of GXP Compliance. 2009;1:58-66.