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1.
Chinese Journal of Biotechnology ; (12): 1994-2002, 2022.
Article in Chinese | WPRIM | ID: wpr-927833

ABSTRACT

Avicel is made of a mixture of microcrystalline cellulose (MCC) and carboxymethyl cellulose (CMC), and used for virus plaque assay. The avicel in common use is produced by FMC Biopolymer. Due to the relatively fixed proportion of MCC and CMC, avicel in common use is not suitable for plaque determination experiment of all types of viruses. In this study, we evaluated the effect of avicel made of different proportions of MCC and CMC on virus plaque assay, and developed an improved avicel virus plaque assay featured with simple and convenient operation, good practicability and high stability. To generate avicel overlays with different proportions of MCC and CMC, twelve different 2×avicel solutions were prepared. Their overall viscosity and bottom viscosity were measured to evaluate the ease of operation. The results showed that most of the 2×avicel solutions (except the 4.8% MCC+1.4% CMC and 4.8% MCC+1.0% CMC group) were easy to absorb and prepare nutrient overlap than 2×CMC solution. In order to find the best scheme to detect the titer of porcine epidemic diarrhea virus (PEDV), these avicel overlay solutions with different proportion of MCC and CMC were used as a replacement in the standard plaque assay. By comparing the size, clarity, stability and titer accuracy of virus plaque, we identified that 0.6% MCC and 0.7% CMC was the most preferable composition of avicel overlay for PEDV plaque assay. In conclusion, we developed an improved virus plaque assay based on avicel, which may facilitate the research of virus etiology, antiviral drugs and vaccines.


Subject(s)
Animals , Carboxymethylcellulose Sodium/chemistry , Cellulose/chemistry , Swine
2.
China Journal of Chinese Materia Medica ; (24): 4978-4985, 2021.
Article in Chinese | WPRIM | ID: wpr-921635

ABSTRACT

In this paper, co-processed lactose SuperTab 40 LL was selected as fillers to study the preparation of musk sustained-release mini-tablets in the Xihuang multiple-unit drug release system. Musk sustained-release tablets containing different proportions of SuperTab 40 LL and MCC were prepared under various pressures, and then the compressibility and compactibility of these prescriptions were evaluated by Walker, Heckel and Ryshkewitch-Duckworth equations. In addition, the fluidity of the prescriptions was evaluated by parameters of Kawakita equation. There was a comprehensive analysis of the effect of SuperTab 40 LL on musk sustained-release mini-tablets combined with the appearance of SuperTab 40 LL and their tensile strength. The results shown that SuperTab 40 LL had better compression process through the Heckel equation, and the direct compression process of drug powders with excipients can be analyzed by the Kawakita and Ryshkewitch-Duckworth equations. As a new type of co-processed lactose, SuperTab 40 LL had a good fluidity and compactibility. SuperTab 40 LL may undergo particle crushing and plastic deformation during the compression process, which increased the contact area and bonding sites between the particles, and aggregated and shaped the mixed powder easy. Moreover, MCC showed a synergistic effect, and the combined application with SuperTab 40 ll could effectively improve the fluidity and compressibility of the musk sustained-release powder. When the ratio of SuperTab 40 LL and MCC was 2∶1, musk sustained-release mini-tablets had a high drug loading capacity and good compactibility in line with the design objectives.


Subject(s)
Delayed-Action Preparations , Drug Compounding , Excipients , Fatty Acids, Monounsaturated , Models, Theoretical , Powders , Tablets
3.
Int J Pharm Pharm Sci ; 2020 Mar; 12(3): 7-14
Article | IMSEAR | ID: sea-206056

ABSTRACT

Objective: This study aimed to increase the yield of microcrystalline cellulose (MCC) from kapok pericarpium alpha-cellulose produced by enzymatic hydrolysis using purified cellulase from Termites (Macrotermes gilvus) and to compare the characteristics with the reference product. Methods: In this research, MCC was prepared from kapok pericarpium powder through the chemical isolation process of alpha-cellulose, followed by enzymatic hydrolysis with purified cellulase from Macrotermes gilvus. The yield was improved by using purified cellulase in optimized temperature, pH, and hydrolysis time. Identification was carried out by using ZnCl and infrared spectrophotometry, followed by characterization of MCC include particle size analysis (PSA) and diffracto­gram pattern (X-Ray Diffraction). The results were compared with Avicel PH 101 as the reference product. Results: Purified cellulase from Macrotermes gilvus showed high cellulose activity. Cellulose in the concentration of 11.743 U/ml formed 49 mm clear zone area with cellulolytic index 7.16 that similar to the formed clear zone area of Trichoderma reesei (50 mm), the optimum hydrolysis condition was achieved at 50 °C, pH 6.0, in 2 h, which produced 80% yield of MCC. Produced MCC was analyzed with ZnCl and FTIR spectrum resulting in positive results, similar to reference. The results of the organoleptic test, particle size analysis, and diffracto­gram pattern (X-Ray Diffraction) showed crystalline characteristics of MCC is similar to the reference (Avicel PH 101). Conclusion: Cellulase Macrotermes gilvus yielded 80% MCC and higher enzymatic activity than Trichoderma reesei. Based on the organoleptic test, particle size analysis, and diffracto­gram pattern observation, MCC from kapok pericarpium has shown similar characteristics to reference (Avicel pH 101) and might be potential to be further developed.

4.
Braz. J. Pharm. Sci. (Online) ; 56: e18660, 2020. tab, graf
Article in English | LILACS | ID: biblio-1132061

ABSTRACT

The effect of drying method, a process variable, on the powder and compaction properties of microcrystalline cellulose (MCC) obtained from the partial acid hydrolysis of bleached alpha (α) cellulose content of matured linters of Gossypium herbaceum (GH) was investigated. A portion of the wet MCC obtained was fluid bed dried at 60 ± 1 ºC, inlet air of 30 m3 min-1 for 3 h (coded MCC-GossF). The second portion was lyophilized at - 45 ± 2 ºC for 6 h (coded MCC-GossL). The physicochemical, scanning electron micrographs, X ray diffraction patterns and micromeritic properties of the derived MCCs were determined using standard methods. The cohesiveness and compactibility of the powders were investigated using Kawakita model while the deformation and compressibility pattern were determined using Heckel model. Avicel® PH 102 (AV-102) was used as comparing standard. Ash values of < 2%, pH (6.54 ± 0.23 to 6.58 ± 0.08), degree of polymerization, DP (231.50) was obtained. MCC-GossF had higher moisture content, swellability, better flow indices, and lesser porosity than MCC-GossL. Kawakita model demonstrated good consolidation and compactibility for both powders. Compacts of MCC-GossL were significantly (p < 0.05) harder than those of MCC-GossF. Heckel analysis demonstrated good compressibility and deformation pattern that was comparable with AV-102. Compacts of MCC-GossL had better mechanical and tablet compression properties than MCC-GossF


Subject(s)
Powders , Ash/adverse effects , Cellulose/classification , Gossypium herbaceum/analysis , Bays/analysis , Air , Hydrogen-Ion Concentration , Hydrolysis , Methods
5.
Chinese Traditional and Herbal Drugs ; (24): 4041-4050, 2019.
Article in Chinese | WPRIM | ID: wpr-850873

ABSTRACT

Objective: To study the influence of microcrystalline cellulose (MCC) on the direct pressure properties of powder extracted from Shufeng Jiedu formula (SFJDE), and discuss the correlation between the basic physical properties and its functional properties of the powder before compression. Methods: SFJDE and MCC was mixed in different proportions, the physical properties of the mixed powder and the compression parameters under different pressures were determined. The basic physical properties and functional parameters of the powder were processed and analyzed by linear regression and partial least squares (PLS). Results: The addition of MCC in SFJDE showed a good linear relationship with the moisture content (MC), bulk density (ρb), and porosity ratio (ε) of the powder (r2 ≥ 0.991 9), and showed a good positive correlation with Hausner ratio (HR) and Carr’s index (CI) of the powder flow index (r2 ≥ 0.834 2). The parameters of powder compressibility compaction ratio (CR) and yield pressure (Py) gradually decreased, Unit effective work (Esp) and paramter a gradually increased; The powder compaction parameter kA was gradually increased, and kB was gradually decreased. The basic physical properties of MC, ρb, tap density (ρt), true density (ρtrue), and particle size (D0.5) of the powder had the obvious impact on these parameters by PLS analysis, while size distribution (span), HR, CI had little effect on it. However, span, HR, and CI had the obvious influence on the parameters ab and f, which characterized powder breakage and rearrangement. Conclusion: The increase of MCC reduces the fluidity of SFJDE, improves the compressibility and compactibility of the powder, therefore, we should pay attention to the influence of fluidity and pressure sensitivity during the process of use.

6.
Acta Pharmaceutica Sinica ; (12): 806-811, 2018.
Article in Chinese | WPRIM | ID: wpr-779940

ABSTRACT

In this study, multivariate statistical analysis was applied to characterize the flowability of different types of microcrystalline cellulose (MCC), and the visualization of R language was used to explore the intrinsic correlation on its performances. To verify the operability of multivariate statistical analysis, we compared the results of the conventional methods such as repose angle method, Hausner ratio method, Carr's index method and the parameter a of Kawakita equation to determine whether there are significant differences between the conventional ones and multivariate statistical analysis. Moreover, the fillibility and compressibility were characterized by parameters 1/b of Kawakita equation and the means of pressure-tensile strength and compressibility curve method, respectively. The data was analyzed through R language for visualizing the correlation among the performance parameters of MCC. The flowability of the series of microcrystalline cellulose PH (MCCPH) were superior to the series of microcrystalline cellulose WJ (MCCWJ), the compressibility of MCCPH-302 was optimum, and the flowability and fallibility of MCCPH-102 were better than others. The results of conventional methods were consistent with multivariate statistical analysis. The fillibility was positively correlated with flowability, both negatively correlated with compressibility by analyzing correlation coefficient diagram, which was statistically significant (P<0.01). It is reasonable that adopting multivariate statistical analysis to character the flowability of powders, which is more objective than the traditional approach. The correlation visualization of performance parameters of powders provides convenience for screening preparation material via the visualization of R language.

7.
Braz. J. Pharm. Sci. (Online) ; 54(4): e17222, 2018. tab, graf, ilus
Article in English | LILACS | ID: biblio-1001590

ABSTRACT

Colonic carcinoma is one of the most common internal malignancies and is the second leading cause of deaths in United States. Methotrexate (MTX) is a drug of choice in the treatment of colon cancer. The aim of the present research work was to develop and characterize colon targeted pellets of MTX for treatment of colonic carcinoma. The product and process parameters were optimized by screening methods. Pellets were prepared by extrusion spheronization using microcrystalline cellulose (MCC) as spheronizing aid and ethyl cellulose (EC) as release retardant in different ratio. Based on the physical appearance, sphericity and % in vitro drug release, batch P17 containing EC: MCC (3:7) was optimized for core pellets. The site specificity was obtained by screening the coating polymers and by coating the core pellets with EudragitS100. The 32 full factorial design was applied in which airflow rate (X1) and coating time (X2) were the independent parameters and physical appearance (Y1) and time taken for 100% drug release (Y2) were selected as the dependent variables. From the results obtained, 6min of coating time and 60cm3/min airflow rate was optimized. The batch B5 showed appropriate physical appearance and % in vitro drug release upto 17hr indicating sustained release property. The ex-vivo studies performed on rat colon indicated a significant relation with the in vitro drug release. The drug release followed Higuchi's model indicating the diffusion pattern of drug release from the matrix of pellets. Thus, the coated pellets can be a good candidate for site specific delivery of MTX to colon by decreasing the gastric irritation and thus to improve bioavailability.


Subject(s)
Methotrexate/administration & dosage , Methotrexate/analysis , Colonic Neoplasms/drug therapy , In Vitro Techniques/instrumentation , Pharmaceutical Preparations/analysis , Colon/abnormalities
8.
Electron. j. biotechnol ; 27: 70-79, May. 2017. tab, ilus, graf
Article in English | LILACS | ID: biblio-1010399

ABSTRACT

Background: Endoglucanase plays a major role in initiating cellulose hydrolysis. Various wild-type strains were searched to produce this enzyme, but mostly low extracellular enzyme activities were obtained. To improve extracellular enzyme production for potential industrial applications, the endoglucanase gene of Bacillus subtilis M015, isolated from Thai higher termite, was expressed in a periplasmic-leaky Escherichia coli. Then, the crude recombinant endoglucanase (EglS) along with a commercial cellulase (Cel) was used for hydrolyzing celluloses and microbial hydrolysis using whole bacterial cells. Results: E. coli Glu5 expressing endoglucanase at high levels was successfully constructed. It produced EglS (55 kDa) with extracellular activity of 18.56 U/mg total protein at optimal hydrolytic conditions (pH 4.8 and 50°C). EglS was highly stable (over 80% activity retained) at 40­50°C after 100 h. The addition of EglS significantly improved the initial sugar production rates of Cel on the hydrolysis of carboxymethyl cellulose (CMC), microcrystalline cellulose, and corncob about 5.2-, 1.7-, and 4.0-folds, respectively, compared to those with Cel alone. E. coli Glu5 could secrete EglS with high activity in the presence of glucose (1% w/v) and Tween 80 (5% w/v) with low glucose consumption. Microbial hydrolysis of CMC using E. coli Glu5 yielded 26 mg reducing sugar/g CMC at pH 7.0 and 37°C after 48 h. Conclusions: The recombinant endoglucanase activity improved by 17 times compared with that of the native strain and could greatly enhance the enzymatic hydrolysis of all studied celluloses when combined with a commercial cellulase.


Subject(s)
Bacillus subtilis/enzymology , Cellulase/metabolism , Isoptera/microbiology , Thailand , Recombinant Proteins/metabolism , Cellulase/genetics , Cellulose , Gene Amplification , Agriculture , Escherichia coli/metabolism , Hydrolysis
9.
Chinese Pharmaceutical Journal ; (24): 2098-2103, 2017.
Article in Chinese | WPRIM | ID: wpr-858496

ABSTRACT

OBJECTIVE: To evaluate microcrystalline cellulose(MCC) and stearic acid(SA) on extrusion-spheronisation(E-S) for aspirin sustained release pellets. METHODS: Mixtures with varying drug concentration and SA/MCC ratios were processed via non-aqueous E-S. Multi-index evaluation method were assessed by rheological behavious, drug stability and release in vitro compared with aqueous E-S. RESULTS: The extrusion was easier when SA/MCC was > 35%. When the ratio of SA/MCC was about 1, the roll effect was the best. The drug content was 65%. Compared with aqueous E-S, non-aqueous E-S was small and homogeneous pellets, better apparent characteristics, stability. There were no obvious different in drug release in vitro. CONCLUSION: These prove to be superior aids for water sensitive aspirin when exposed to non-aqueous solvent by E-S.

10.
Article in English | IMSEAR | ID: sea-174300

ABSTRACT

The present work was carried out to study the disintegrant property of plantago ovata mucilage. The objective of the work was to formulate fast disintegrating tablets of Domperidon with a view to enhance patient compliances and dissolution rate by direct compression method using 3² full factorial design. Plantago ovata mucilage (2-10% w/w) was used as natural superdisintegrant and microcrystalline cellulose (0-30% w/w) was used as diluent, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 10s); the formulation containing 10% w/w Plantago ovata mucilage and 30%w/w microcrystalline cellulose was found to be promising and tested for in vitro drug release pattern (in 0.1 N HCl), short-term stability (at 40º/75% RH for 3 month) and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables (concentrations of Plantago ovata mucilage and microcrystalline cellulose) on the in vitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design check point formulations. The optimized tablet formulation was compared with conventional commercial tablet formulation for drug release profiles. This formulation showed nearly four-fold faster drug release (t50% 2.85 min) compared to the conventional commercial tablet formulation (t50% 7.85 min). Short-term stability studies on the formulation indicated that there are no significant changes in drug content and in vitro dispersion time (p < 0.05).

11.
Article in English | IMSEAR | ID: sea-168002

ABSTRACT

The present work was carried out to study the disintegrant property of plantago ovata mucilage. The objective of the work was to formulate Fast disintegrating tablets of Domperidon with a view to enhance patient compliances and dissolution rate by direct compression method using 3² full factorial design. Plantago ovata mucilage (2-10% w/w) was used as natural superdisintegrant and microcrystalline cellulose (0-30% w/w) was used as diluent, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 10s); the formulation containing 10% w/w Plantago ovata mucilage and 30%w/w microcrystalline cellulose was found to be promising and tested for in vitro drug release pattern (in 0.1 N HCl), short-term stability (at 40º/75% RH for 3 month) and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables (concentrations of Plantago ovata mucilage and microcrystalline cellulose) on the in vitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design check point formula-tions. The optimized tablet formulation was compared with conventional commercial tablet formulation for drug release profiles. This formulation showed nearly four-fold faster drug release (t50% 2.85 min) compared to the conventional commercial tablet formulation (t50% 7.85 min). Short-term stability studies on the formulation indicated that there are no significant changes in drug content and in vitro dispersion time (p < 0.05).

12.
Article in English | IMSEAR | ID: sea-159013

ABSTRACT

Microcrystalline cellulose (MCC) was prepared by hydrochloric acid hydrolysis from Muli bamboo (Melocanna baccifera) fibers to tap its potential as a green source of MCC. The cellulose and α-cellulose yield from the original material were 62.5 and 54.8 % respectively. The physicochemical properties of the prepared MCC were investigated using Avicel PH101 as a comparator. Micromeritic properties of the powder MCC samples were analyzed by determining its average particle size, flow properties, particle porosity and density. The total ash and moisture content along with the swelling index were also determined. The prepared MCC was also characterized by fourier transformed infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and x-ray diffraction spectroscopy (XRD). Results from these analyses indicate that the Muli bamboo can be used as a green source of MCC.

13.
Article in English | IMSEAR | ID: sea-151983

ABSTRACT

The work was aimed to investigate the suitability of acid modified alpha cellulose obtained from the back of the fruit of Lageriana siceraria (water gourd) in production of pharmaceuticals, particularly solid dosage forms. Cellulose is the commonest Filler/Binder or disintegrant used in tablet formulation. Cellulose was extracted from the fruit of Lageriana siceraria and subjected to modification by controlled acid micronisation to produce microcrystalline cellulose (LS-MCC) using 2.5N hydrochloric acid and Avicel pH 101 was used as the basis for comparison. The powder and flow properties of the microcrystalline cellulose was investigated and the result of both the LS-MCC and Avicel pH 101compared. Microcrystalline cellulose (LS-MCC) displayed superior swelling and hydration capacities as compared to Avicel PH101 but lesser flow properties in view of its higher angle of repose, Carr’s and Hausner’s index.

14.
Chinese Traditional and Herbal Drugs ; (24): 1072-1077, 2014.
Article in Chinese | WPRIM | ID: wpr-854604

ABSTRACT

Objective: To study the effect of microcrystalline cellulose (MCC) on compressibility and moldability of Galla chinensis extract (GCE). Methods: Four types of MCC were chosen and mixed with GCE respectively in different proportions. The powder was tabletted by Korsch XP-1 Intelligent Induction Tablet Machine, and the compressibility and moldability were evaluated using plasticity constant, elastic recovery, compression ratio, yield pressure, tensile strength, and their change rules as indexes. Results: The compressibility and moldability of GCE were poor. CeolusKG802 was the best at improving elastic recovery and compression ratio among the four kinds of MCC. AvicelDG improved the plasticity constant and tensile strength most when the adding amount was low, and CeolusKG802 improved them most when the adding amount was high. To yield pressure, CeolusKG802 exhibited greater reduction than the other MCC when added in a low amount. As for a high amount, the result was opposite. Conclusion: MCC has good compressibility and moldability in the compression process; Different types of MCC have different advantages. The change law of compression parameters is obtained by investigating the compression of mixed powders of MCC with different proportions on GCE.

15.
Chinese Traditional and Herbal Drugs ; (24): 1245-1251, 2014.
Article in Chinese | WPRIM | ID: wpr-854582

ABSTRACT

Objective: The co-processd excipient containing microcrystalline cellulose (MCC) and glycerol monostearate (GMS) was prepared. The humidity resistance of MCC used in Chinese materia medica (CMM) was improved and the possibility of this co-processd excipient used in the preparation of CMM tablet was explored. Methods: The co-processd excipient containing MCC and GMS was prepared by applying spray drying method. The moisture absorption, flow ability, compressibility, and disintegration were as the indexes to optimize the best preparation of co-processd excipient through uniform design methodology. The powder characteristic of co-processd excipient was investigated and the microstructures were studied by scanning electron microscope (SEM), differential scanning calorimeter (DSC), X-ray diffraction (XRD), and Flourier transform infra-red (FTIR) spectroscopy. The effect of co-processd excipient on the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts was investigated. The in vitro dissolution of hyperside and ferulic acid in Xinyueshu Tablet was studied. Results: The results showed that the optimal conditions of the preparation consisted of 1 portion of GMS, 12 portions of MCC, and 200 portions of water, emulsionzing temperature of 66°C, and mixing time of 1 h. It was confirmed that the chemical constituents in co-processd excipient were not changed after spray drying with smaller particle size and better fluidity. The co-processd excipient can improve the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts without affecting the disintegration of MCC. Conclusion: The co-processd excipient prepared has good humidity resistance and it is confirmed to have application prospect.

16.
Chinese Traditional and Herbal Drugs ; (24): 1998-2004, 2014.
Article in Chinese | WPRIM | ID: wpr-854452

ABSTRACT

Objective: To investigate the correlations between micromeritic primary properties and compactibility of granules produced by wet granulation of Sarcandrae Herba with soluble starch and microcrystalline cellulose (MCC). Methods: Micromeritic primary properties and compactibility of granules produced by wet granulation which was obtained by different prescriptions and processes were determined. Particle size (D90), specific surface area (SSA), pore volume (PV), moisture content (MC), bulk density (BD), tap density (TD), tap index (TI), angle of repose (AOR), and Kawakita equation parameters a and b were used as evaluation indexs to study the micromeritic primary properties of granulation. The tensile strengths of granules at 5, 10, 15, 20, 25, and 30 kN pressure were used as the indexs to evaluate the compactibility of granules produced. Multivariate analysis was applied to evaluating the correlations between micromeritic primary properties and compactibility of granules produced. Results: The micromeritic primary properties of granules could be extracted as two principal components, morphology parameter and compressibility parameter. The significant effects on the tablet compactibility are the compressibility, moisture, and surface morphology of granules produced. Conclusion: Multivariate data analysis could make the quick and easy classification of Sarcandrae Herba Granule. The correlation between granules micromeritic primary properties and tablet compactibility is given. By controlling compressibility, moisture, and surface morphology of granules produced, the tablets with good compactibility can be obtained.

17.
Rev. bras. farmacogn ; 23(1): 186-193, Jan.-Feb. 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-666182

ABSTRACT

This study evaluated the technological feasibility of producing a semipurified extract of guaraná (Paullinia cupana Kunth, Sapindaceae) in tablet form, using a direct-compression process. Maltodextrin and gum arabic were used to produce the extract microparticles, in order to protect the microparticles against such factors as temperature, oxidation, and humidity. Using pharmacopoeial methodologies, technological and physicochemistry tests (determination of residual moisture, of bulk and tapped density, Hausner ratio, compressibility and compactibility index, appearance, mean weight, hardness, friability, disintegration time, determination of EPA amount in tablets and in vitro release profile) were conducted. The formulation containing 200 mg of microparticles, 170 mg microcrystalline cellulose, and 10 mg lactose gave the best results in terms of hardness (116 N), friabilility (0.28%), mean weight (0.3821 g), and disintegration time (25 min) for a tablet designed for oral administration. The results met pharmacopoeial specifications, and the tablets are suitable for oral administration.

18.
Chinese Pharmaceutical Journal ; (24): 116-122, 2013.
Article in Chinese | WPRIM | ID: wpr-860500

ABSTRACT

OBJECTIVE: To study correlation between physical properties and compressibility and compactablility of Microcrystalline cellulose. METHODS: After determining the physical properties such as particle size distribution, moisture capacity, angle of repose, bulk density, tapped density, the powder was tableted by the Korsch XP1 at the same filling height, and data derived from heckle model, plasticity constant, cumulative elastic recovery, tensile strength and it's changes with time were evaluated. RESULTS: The physical properties of microcrystalline cellulose had great effect on its compactablility as well as cumulative elastic recovery out of die, but not on compressibility. And pressure applied correlated closely with changes of tensile strength in storage, which was intensified by the influence of water in powder on the particle size. CONCLUSION: Microcrystalline cellulose shows excellent compressibility, however, particle size reduction is able to decrease the compactability. Since the water in powder can increase particle size by changing internal structure of particles and plays a prerequisite role in lubrication and adherence, the variation of water content may weaken the compatability of microcrystalline cellulose and worsen the mechanical strength stability of tablets in storage.

19.
Article in English | IMSEAR | ID: sea-152857

ABSTRACT

Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.

20.
Article in English | IMSEAR | ID: sea-151182

ABSTRACT

The specific aim of this study was to prepare sustained release matrix tablets containing indapamide as a low dose and low water solubility model drug. The matrix formers were composed of blends of hydroxypropyl methylcellulose as a swellable polymer and methyl cellulose as an erodible polymer. The matrix tablets were prepared by the direct compression technique and they have shown robust and acceptable physical properties with a content uniformity within the acceptable limits. Lactose and microcrystalline cellulose were investigated as additives to these matrices in order to adjust and modulate the release of the drug from the matrices to achieve a release profile similar to that obtained from the reference commercial product, Natrilix®. All matrix tablets prepared with these two additives have gave a release profile that is close to zero order kinetics, however, the matrix tablets prepared with lactose gave a release profile with closer resemblance to that of the reference product with a similarity factor (F2) of 86. This is attributed to the rapid water solubility of lactose which enhanced higher erosion of the tablets, and thus, higher dissolution and diffusion of the drug. Microcrystalline cellulose is a swellable polymer where it has resulted in delayed release of the drug with time as compared to the reference product. Investigation of the mechanism of release of the drug from the matrices indicated that erosion is the dominant mechanism of drug release from these matrices.

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