Studies on Microcrystalline Cellulose Obtained from Saccharum Officinarum 2: Flow and Compaction Properties (original) (raw)
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The degree of deformation and densification of pellets during compression have been quantified. The relationship between the degree of deformation of the pellets and their compactability were also studied. Two sets of pellets of microcrystalline cellulose, showing a marked difference in intragranular porosity, were prepared by extrusionspheronization. The pellets were mixed with a lubricant and compacted at a series of applied pressures. The individual pellets were retrieved after compression by tablet deaggregation and the porosity (densification behaviour) and dimensions (deformation behaviour) of the retrieved pellets were determined. Tensile strength of compacts prepared of unlubricated pellets was also determined. The incidence of pellet fragmentation was almost non-existent during the compression for both sets of pellets. The low porosity pellets showed only limited local permanent deformation during compression and the pellet porosity was unaffected by the compression. The high porosity pellets showed both a high compression-induced change in shape and a marked decrease in pellet porosity. Tensile strength values of tablets of unlubricated pellets indicated that a marked bulk structure deformation of the pellets was necessary for the formation of intergranular contacts of a high bonding force in the compact.
Revista De Ciencias Farmaceuticas Basica E Aplicada, 2013
Excipients are widely used to formulate solid drug forms by direct compression. However, the powderforming and tableting properties of these excipients are affected by the presence of lubricants and active ingredients. In this study, a screening methodology was employed to test the performance of an excipient for direct compression. The effects of three lubricants (magnesium stearate, stearic acid and talc) on the compressibility and compaction of these excipients were assessed by the compressibility index and lubricant sensitivity ratio, respectively. Likewise, the dilution potential in blends with a poorly compactible drug such as acetaminophen was also assessed. Finally, the elastic recovery of tablets was evaluated five days after production. All lubricants increased the compressibility of these excipients and improved their flowability. However, hydrophobic lubricants such as magnesium stearate had a marked negative effect on compactibility, especially in plastic-deforming and more regularlyshaped materials with a smooth surface such as Starch 1500. Alginic acid, rice and cassava starches had the largest elastic recovery (>5%), indicating a tendency to cap. Moreover, highly plastic deforming materials such as sorbitol and polyvinylpyrrolidone (PVP-K30) exhibited the best dilution potential (~10%), whereas alginic acid showed a very high value (~70%). In terms of performance, sorbitol, PVP-K30, Avicel PH-101, sodium alginate and pregelatinized starch were the most appropriate excipients for the direct compression of drugs.
Advances in Pharmacological and Pharmaceutical Sciences, 2020
Taro Boloso-I (TB1), a newly improved Colocasia esculenta variety, is a potential source of starch with high yield. However, to improve some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch modifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the NS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic anhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072 (SA1) and 0.695 (SA2) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder flow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the swelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA1 (41.40) and SA2 (63.43 Kg/cm2), was significantly higher than tablets made of the NS (31.96) and Starch 1500® (15.12 Kg/cm2). The SAs also showed lower sensitivity towards lubrication than the NS and Starch 1500® as lower lubricant sensitivity ratios were recorded. In addition, tablets comprising the SAs satisfactorily accommodated at least up to 50 % w/w paracetamol—compared to 30 % w/w by Starch 1500®—upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications for disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in tablet formulations.
CHEMICAL & PHARMACEUTICAL BULLETIN, 2004
In a previous study 1) we performed a comparative analysis of the properties of Cellactose, a coprocessed excipient for direct compression, and of two cellulose-lactose excipients (prepared by dry granulation and extrusion-spheronization respectively) of similar composition and particle size. We found major differences among the three excipients in particle structure and rheological properties, and in the mechanical properties and disintegration behaviour of the corresponding tablets. In the present study, as a follow-up to our previous study, 1) we evaluate the drug-loading capacities of these three excipients, since drug loading is one of the major limitations of excipients of this type. 2) The model drugs used were acetaminophen (which is problematic at the compression stage 3,4)) and furosemide (which is highly cohesive 5)). Drug-loading capacity was evaluated in terms of the flow and compression properties of different drug-excipient mixtures, and the mechanical, microstructural and drug release properties of tablets prepared from these mixtures. Experimental Materials Cellactose, from Meggle, was supplied by Fher, S.A. (lot 919), and was used as supplied. Alpha-lactose monohydrate Ph. Eur. was from Merck (lot 2444543). Avicel PH-101 (FMC Corp.) was supplied by C. Barcia, S.A. (lot 5648). Magnesium stearate B.P. was likewise supplied by C. Barcia, S.A. (lot 548). Acetaminophen (lot 841) and furosemide (lot 97) were supplied by UTEFSA. The cellulose-lactose excipients were prepared by us by dry granulation (excipient B) and extrusion-spheronization (excipient C). 1) Characterization of the Drugs Particle Size: Particle size distribution was evaluated in triplicate in a Coulter LS100 laser diffraction apparatus, using water as dispersal medium. For both drugs, mean diameter and standard deviation were estimated after fitting a log-normal distribution. Flow Properties: Bulk density was determined over 20 min in a Hosokawa PT-E Powder Tester operating at 50 taps/min. Compressibility was calculated from the initial and final bulk densities. 6) Compression Properties: 99.5 : 0.5 (w/w) mixtures of drug and magnesium stearate were prepared over 5 min in a Turbula T2C mixer operating at 30 rpm, and samples were tabletted in a Bonals B/MT eccentric apparatus equipped with 9-mm flat punches and a compression data acquisition system. 7) Mean yield pressures (Py) were estimated from Heckel plots of the upper punch force-displacement data for three punch cycles. 8) Preparation of Drug-Excipient Mixtures Mixtures (Turbula T2C,
International Journal of Pharmacy and Pharmaceutical Sciences
Objectives: The aim of this study was to investigate crystallinity and compatibility transformation of two binary mixtures of analgesic substance with excipient due to mixing and compression. Methods: Analgesic substances used in this study were mefenamic acid (MA) and acetaminophen (AC). Each substance was mixed with microcrystalline selolusa as excipient with drug-excipient ratio of 70:30, 80:20 and 90:10 %w/w then compressed with pressure of 29.4 kN. Characterization was done by Powder X-Ray Diffraction (PXRD), thermal analysis (DTA), FTIR spectrometer and a Scanning Electron Microscope (SEM). Mechanical properties was also evaluated by calculating its tensile strength Results: Evaluation of crystallites size of MA and MA-MCC mixture showed that the value of MA crystallite size is relatively fixed in all the peaks observed. Crystallite size of the AC and AC-MCC mixture also showed similar results with MA. From the elastic modulus curve, it was recognized that the tensile strength...
Bayero Journal of Pure and Applied Sciences, 2021
Spherical crystallization and crystal agglomeration have been used to optimize compact crystals and functional properties of powders. The aim of this work is to evaluate the effect of spherical crystallization of acetylsalicylic acid crystals and crystal agglomeration of Manihotesculenta starch on direct compression tablet. Typical spherical crystallization using three solvent system of water–ethanol-carbon tetrachloride was used to produce spherical acetylsalicylic acid. Salting-out agglomeration of gelling in water and salting in ethanol was used to produce starch-xerogel from Manihotesculenta starch. The modified products were qualified using FT-IR analysis. The analysis results showed that modification did not alter chemical nature of the products. Acetylsalicylic acid tablets were formulated using spherical-crystallizedacetylsalicylic acid with 5 and 10% w/w starch-xerogel respectively, and using acetylsalicylic acid with 5 and 10% w/w of starch, and microcrystalline cellulose ...
Microcrystalline Cellulose: The Inexhaustible Treasure for Pharmaceutical Industry
2017
Microcrystalline cellulose (MCC) is pure partially depolymerized cellulose synthesized from α-cellulose precursor. The MCC can be synthesized by different processes such as reactive extrusion, enzyme mediated, steam explosion and acid hydrolysis. The later process can be done using mineral acids such as H2SO4, HCl and HBr as well as ionic liquids. The role of these reagents is to destroy the amorphous regions remaining the crystalline domains. The MCC is a valuable additive in pharmaceutical, food, cosmetic and other industries. The MCC is one of the most important tableting excipients due to its outstanding dry binding properties of tablets for direct compression. Different properties of MCC are measured to qualify its suitability for such utilization, namely particle size, density, compressibility index, angle of repose, powder porosity, hydration swelling capacity, moisture sorption capacity, moisture content, crystallinity index, crystallite size and mechanical properties such a...
Purpose: To comparatively evaluate the tableting properties of binary mixtures and bi-layer tablets containing plastic deformation and brittle fracture excipients. Methods: Binary mixture and bi-layer tablets of microcrystalline cellulose (MCC), ethyl cellulose, anhydrous lactose and dextrate were prepared by direct compression and the effect of compaction pressure on the materials was investigated by scanning electron microscopy (SEM). True, bulk and tap densities of excipients were determined. Furthermore, Heckel equation and Carr’s index were used to analyze the compression behavior of the tablets. Results: The flowability of dextrate, based on Heckel and Carr’s Index data, was superior to that of other powder excipients tested. No significant difference was observed between the tensile strength of binary and bi-layer tablets of the same composition. However, the tensile strength of binary and bi-layer tablets of different compositions varied significantly (p < 0.001), e.g., the tensile strength of microcrystalline cellulose (MCC)/ethyl cellulose (EC) tablets (50/50) was 1.77 MPa while that of MCC/dextrate at 50/50 composition was 1.47 MPa. Conclusion: Binary mixture and bi-layer tablets show similar behavior when formulated using excipients of similar deformation properties. However, their behavior changes when excipients with different deformation properties are blended together. Keywords: Binary mixture, Bi-layer tablet, Brittle fracture, Plastic deformation, Tensile strength.
Journal of Applied Pharmaceutical Science
Microcrystalline cellulose (MCC) is a popular pharmaceutical excipient, used as a filler or binder in directly compressible tablets, and is the most economical form of all available tablets. In the present research work, we pretreated waste paper with a chelating agent followed by pulping, bleaching, and subsequent hydrothermal degradation with hydrochloric acid at a concentration of 0.5 mol/l and at a 150°C temperature for 120 minutes to produce MCC. The derived MCC was dried at 60°C for 3 hours, ground, and graded into two types based on the particle size. Grade 1 had a particle size of ≤75 microns, while grade 2 had a particle size of 75-125 microns. The derived MCC was chemically identified by an iodinated ZnCl 2 solution. Evaluation of the degree of polymerization (DP) and Fourier transforminfrared spectroscopy spectrum further confirmed the identity of the MCC. From the value of intrinsic viscosity of the MCC in cuene, the DP was found to be 126 and 191 for Avicel PH101 and the derived MCC, respectively. The morphological study of derived MCC types by the scanning electron microscopy method suggested that their shapes were very similar to that of Avicel PH101, while the size of MCC grade 1 was very similar to the marketed Avicel PH101. Moreover, the derived MCC types were comparable to the commercial Avicel PH101 based on different physicochemical parameters associated with flow property such as bulk density, tapped density, Hausner's ratio, Carr's index, angle of repose, and ash value. The applicability of the derived MCC as a directly compressible excipient was further investigated through the formulation of an uncoated aceclofenac immediate-release tablet. The various tablet parameters like hardness, friability, disintegration, and dissolution time all complied with standard specifications.