scholarly journals Evaluation of Chitosan-Microcrystalline Cellulose Blends as Direct Compression Excipients

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Emmanuel O. Olorunsola ◽  
Grace A. Akpan ◽  
Michael U. Adikwu

This study was aimed at evaluating chitosan-microcrystalline cellulose blends as direct compression excipients. Crab shell chitosan, α-lactose monohydrate, and microcrystalline cellulose powders were characterized. Blends of the microcrystalline cellulose and chitosan in ratios 9 : 1, 4 : 1, 2 : 1, and 1 : 1 as direct compression excipients were made to constitute 60% of metronidazole tablets. Similar tablets containing blends of the microcrystalline cellulose and α-lactose monohydrate as well as those containing pure microcrystalline cellulose were also produced. The compact density, tensile strength, porosity, disintegration time, and dissolution rate of tablets were determined. Chitosan had higher moisture content (7.66%) and higher moisture sorption capacity (1.33%) compared to microcrystalline cellulose and lactose. It also showed better flow properties (Carr’s index of 18.9% and Hausner’s ratio of 1.23). Compact density of tablets increased but tensile strength decreased with increase in the proportion of chitosan in the binary mixtures. In contrast to lactose, the disintegration time increased and the dissolution rate decreased with increase in the proportion of chitosan. This study has shown that chitosan promotes flowability of powder mix and rapid disintegration of tablet. However, incorporation of equal proportions of microcrystalline cellulose and chitosan leads to production of extended-release tablet. Therefore, chitosan promotes tablet disintegration at low concentration and enables extended-release at higher concentration.

2020 ◽  
Vol 19 (8) ◽  
pp. 1569-1576
Author(s):  
Hamad S. Alyami ◽  
Samer S. Abu-Alrub ◽  
Mater H. Mahnashi ◽  
Mohammad H. Alyami ◽  
Osaid T. Al Meanazel

Purpose: To investigate the influence of two often-used excipients (starch and microcrystalline cellulose) on the physical properties of powder blends and tablets that contain mannitol as diluent.Methods: Powder and powder mixtures of three commonly used excipients (starch, mannitol and microcrystalline cellulose) were thoroughly examined using the angle of repose for flowability, particle size analyzer to determine the diameter of the particles, scanning electron microscopy (SEM) for morphological assessment, and x-ray diffraction to determine crystalline/amorphous characteristics. Tablets were prepared by direct compression technique and were evaluated for mechanical strength and disintegration behavior as part of quality control test.Results: The results showed that increase in MCC concentration of the mixture leads to significantly enhanced flowability (p < 0.05) when compared to starch. The angle of repose for mannitol/MCC powder mixture with 70 % w/w MCC was approximately 29°, indicating good flow properties of thepowder mix. Moreover, starch tablets containing MCC exhibited better mechanical strength and longer disintegration time, while, at 1:1 ratio of MCC and mannitol, tablet disintegration was faster (33.0 ± 5.2s)Conclusion: MCC (at 30 %w/w in the blend) produces optimal flow of the powder blend and superior mechanical strength, Keywords: Tablet disintegration, Flowability, Starch, Hardness, Mechanical strength


2021 ◽  
Vol 2 (3) ◽  
Author(s):  
Nagina Gulab Belali ◽  
Anis Y. Chaerunisaa ◽  
Taofik Rusdiana

Microcrystalline cellulose was isolated from rami (Boehmeria Nivea L. Gaud), and applied as disintegrant in tablets of dimenhydrinate, made by direct compression and wet granulation. The aim of this study is to produce dimenhydrinate tablets with Microcrystalline Cellulose Rami (MCC Rami) isolated from Rami (Boehmeria Nivea L. Gaud), as a disintegrant and assess the effect of MCC Rami and Granulation technique on physical properties of drug such as, disintegration time, drug release and dissolution. Formulations of dimenhydrinate 100mg tablets were prepared with a combination of mannitol and lactose as a filler and MCC Rami as disintegrant in a concentration of 10-20%. The formulas were directly compressed or were compressed into tablets after wet granulation. The mechanical properties, drug release, physical properties and effects of process parameters, methods of applying disintegrant in tablet formulas were examined. A significant difference in disintegration time of tablets that were produced by direct compression and wet granulation was seen, that can be attributed to the porous structure of granules that enhanced fast disintegration, which had eventually improved dissolution and drug release. F1 and F2 with MCC Rami and physical mixture of MCC Rami with crosspovidone as a disintegrant that were directly compressed disintegrated in 79 and 72 seconds respectively thats not a significant difference, however when MCC was applied in an intragranular way its disintegration time is 67 seconds. The results showed that the method of disintegrant application and press of tableting has a significant effect on drug release and dissolution.Keywords : Microcrystalline Cellulose, wet granulation, disintegrant, Boehmeria Nivea L. Gaud.


Food Research ◽  
2021 ◽  
Vol 5 (S1) ◽  
pp. 182-187
Author(s):  
A.K. Mukri ◽  
J.H. Tan ◽  
S.M. Tahir ◽  
M.S. Anuar ◽  
S.M. Yusoff

Cocoa powder is an important ingredient in the confectionery industry and, mannitol is an alternative sugar alcohol. In this work, mannitol powder was mixed with cocoa powder and compacted into tablet form via the uniaxial die compaction process. The frictional, compaction, tablet mechanical and disintegration properties were studied due to their importance in characterizing the behaviour of the tablets during processing and its final product characteristics at varying mannitol contents. The composition of mannitol in the mannitol-cocoa tablet varied at 95% w/w, 50% w/w and 5% w/w, while pure 100% w/w mannitol and cocoa tablets were set as controls. The compaction pressures used in making the tablets varied at 37.67 MPa, 75.34 MPa, 113.01 MPa, 150.68 MPa and 188.35 MPa. The compaction behaviour of the powder during the compaction process was evaluated using the plastic work and the maximum ejection stress values. The tablet strength was determined using the tensile strength method and tablet disintegration study was also conducted. The results showed that the increase in the compaction pressures increased the plastic work, maximum ejection pressure, tablet strength and also its disintegration time. The tablet formed having 95% w/w mannitol composition exhibited the highest plastic work value of 10.32±0.01 J, highest maximum ejection pressure value of 4.4±0.06 MPa, highest tensile strength value of 1.06±0.04 MPa and shortest disintegration time of 171±51 s amongst the three different mannitol compositions studied. Meanwhile, the effects of mannitol composition in the tablet on these observed responses were also dependent upon the compaction pressures used during tablet formation. In conclusion, the addition of mannitol improved the tablet strength and shorten the disintegration time in the experimental range employed in this study.


2015 ◽  
Vol 13 (2) ◽  
pp. 187-192 ◽  
Author(s):  
Md Nurul Islam Setu ◽  
Md Yeunus Mia ◽  
Nur Jaharat Lubna ◽  
Abu Asad Chowdhury

Microcrystalline cellulose (MCC) was prepared by acid hydrolysis from the cellulose purified from the cotton. Chemical assay, determination of degree of polymerization (DP) and FT-IR confirm the identification of prepared microcrystalline cellulose. The FT-IR spectrum of synthesized MCC is very similar to that of Avicel® PH- 102, a commercial direct compression excipient, at consideration of both band position and intensity. The degree of polymerization (DP) of prepared MCC and Avicel PH102, determined from the value of intrinsic viscosity, were 210 and 240, respectively. The tableting properties of prepared MCC was excellent while formulating naproxen tablet. The hardness and friability of the tablets prepared from MCC was 5.33 ± 0.45 kg and 0.077%, respectively which were comparable to the tablets prepared from marketed Avicel PH102 having hardness and friability 7.35 ± 0.41 kg and 0.063%, respectively. The disintegration time of tablet prepared from MCC and Avicel PH102 was 8.25 ± 0.41 min and 4.50 ±0.28 min, respectively. Again, the tablets prepared from MCC and Avicel PH102 showed more than 90% and 98% dissolution, respectively as per the USP specified medium. All these data indicate that the hardness, friability, disintegration and dissolution properties of tablets prepared by using our MCC comply with the USP specifications. This makes the prepared MCC as a promising candidate for direct compressible excipient of tablet. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21899 Dhaka Univ. J. Pharm. Sci. 13(2): 187-192, 2014 (December)


2017 ◽  
Vol 16 (10) ◽  
pp. 2341-2347
Author(s):  
Emmanuel O. Olorunsola ◽  
Stephen O. Majekodunmi

Purpose: To develop an extended-release formulation of domperidone using a blend of Raphia hookeri gum and hydroxypropyl methylcellulose as tablet matrix.Methods: Tablets (400 mg) containing 30 mg domperidone (DPD) were formulated using binary mixtures of hydroxypropyl methylcellulose (HPMC) and Raphia hookeri gum (RHG) as matrix former; and microcrystalline cellulose (MCC) as direct compression excipient. The proportions of the matrix formers (40 % of tablet weight) was varied as 100:0, 75:25, 50:50, 25:75 and 0:100. The composition of the matrix former was also kept constant (50:50) while MCC was varied as 40, 30, 20 and 10 %. The tablets were evaluated for compact density, tensile strength, friability and drug release over 24 h.Results: The tensile strength of tablets decreased while their friability increased with increase in the proportion of RHG. A similar trend was observed with decrease in the concentration of MCC. Tablets containing RHG alone as matrix former and 40 % MCC as direct compression excipient had tensile strength of 0.95 MNm-2, friability of 1.07 % and cumulative drug release of 83.2 % over a period of 24 h. Tablets containing equal proportions of HPMC and RHG as matrix former had the best release properties of 95.0 % over a period of 24 h.Conclusion: RHG is comparable with HPMC in terms of extending the release of  domperidone for a once daily administration. A suitable combination of the two  polymers for use as a matrix former is superior to either of the individual polymers.Keywords: Domperidone, Extended drug release, Hydroxypropyl methylcellulose, Raphia hookeri gum, Tablet properties


Author(s):  
Rocío González ◽  
Mª Ángeles Peña ◽  
Norma Sofía Torres ◽  
Guillermo Torrado

This work proposes a methodology for the design, development, optimisation, and evaluation of amorphous rosuvastatin calcium tablets (BCS class II drug). The main goal was to ensure rapid disintegration and high dissolution rate of the active ingredient, thus enhancing its bioavailability. The design started from a careful selection of excipients, which due to their characteristics and proportions within the formulation allowed the use of their properties such as fluidity or granulometric distribution. The formulation was characterised using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetry (TGA), Fourier transform infrared spectroscopy (FT-IR) and powder X-ray diffraction (PXRD) methods. The galenic SeDeM methodology was used to establish the profile of the active ingredient-excipient mixture and guarantee its suitability for producing tablets by the direct compression method. The results demonstrate that the amorphous rosuvastatin calcium tablets formulation developed made it possible to obtain cost-effective tablets by direct compression with optimal pharmacotechnical characteristics that showed a remarkable disintegration and dissolution rate. The manufactured tablets complied with the pharmacopoeia guidelines regarding uniformity of weight, tablet hardness, thickness, friability, in vitro disintegration time and dissolution profile.


2012 ◽  
Vol 1 (10) ◽  
pp. 311-316 ◽  
Author(s):  
Devendra Revanand Rane ◽  
Hemant Narhar Gulve ◽  
Vikas Vasant Patil ◽  
Vinod Madhaorao Thakare ◽  
Vijay Raghunath Patil

Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism.  In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different concentration and evaluated for the pre-compression parameters. The prepared tablets were evaluated for post compressional evaluation. Among all, the formulation F3 containing 5%w/w superdisintegrant Crospovidone and 20%w/w Microcrystalline Cellulose was considered to be best formulation, which release up to 99.097% in 40 min.DOI: http://dx.doi.org/10.3329/icpj.v1i10.11848 International Current Pharmaceutical Journal 2012, 1(10): 311-316 


2020 ◽  
Vol 16 (1) ◽  
pp. 31-37
Author(s):  
S.O. Eraga ◽  
D.N. Elue ◽  
M.A. Iwuagwu

Background: Natural materials have gained a lot of significance in the field of drug delivery because of their cost effectiveness and ready availability.Purpose: The study aimed at evaluating the direct compression property of microcrystalline cellulose from cassava fermentation waste in directly compressed paracetamol tablet formulations.Methods: Alkali delignification of the dried cassava fermentation fibres, followed by bleaching and acid depolymerisation was employed in the extraction of α-cellulose and conversion to microcrystalline cellulose (MCC). The MCC obtained and Avicel® were used at different concentrations (5.0-15 %w/w) to formulate batches of paracetamol tablets by directed compression. A comparative evaluation of the formulated paracetamol granules and tablets properties were undertaken.Results: The paracetamol granules formulated showed good flowability with Hausner’s ratios of 1.15-1.25, Carr’s indices of 13.10-20.00 % and angles of repose ≤ 34.41°. The formulated tablets showed good hardness (> 5.0 kgf) and disintegration time within 10 min. Only tablets containing 5.0 and 7.5 %w/w of the test MCC failed the BP dissolution test specification for tablets which stipulates that at least 70 % of the drug should be in solution after 30 min.Conclusion: This study has shown that the extracted MCC has direct compression ability evidenced in the mechanical strength of the formulated paracetamol tablets. The tablet properties of the formulated paracetamol tablets revealed pharmaceutically acceptable tablets though they were not comparable with Avicel® at all concentrations and the MCC may serve as an alternative local source for direct compression excipient. Keywords: Cassava, microcrystalline cellulose, direct compression, paracetamol, tablets


Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2165
Author(s):  
Djordje Medarević ◽  
Jelena Djuriš ◽  
Mirjana Krkobabić ◽  
Svetlana Ibrić

Co-processing is commonly used approach to improve functional characteristics of pharmaceutical excipients to become suitable for tablet production by direct compression. This study aimed to improve tableting characteristics of lactose monohydrate (LMH) by co-processing by fluid-bed melt granulation with addition of hydrophilic (PEG 4000 and poloxamer 188) and lipophilic (glyceryl palmitostearate) meltable binders. In addition to binding purpose, hydrophilic and lipophilic excipients were added to achieve self-lubricating properties of mixture. Co-processed mixtures exhibit superior flow properties compared to pure LMH and comparable or better flowability relative to commercial excipient Ludipress®. Compaction of mixtures co-processed with 20% PEG 4000 and 20% poloxamer 188 resulted in tablets with acceptable tensile strength (>2 MPa) and good lubricating properties (ejection and detachment stress values below 5 MPa) in a wide range of compression pressures. While the best lubricating properties were observed when glyceryl palmitostearate was used as meltable binder, obtained tablets failed to fulfil required mechanical characteristics. Although addition of meltable binder improves interparticle bonding, disintegration time was not prolonged compared to commercial excipient Ludipress®. Co-processed mixtures containing 20% of either PEG 4000 or poloxamer 188 showed superior tabletability and lubricant properties relative to LMH and Ludipress® and can be good candidates for tablet production by direct compression.


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