scholarly journals Comparative evaluation of the use of dry binders in a physical mixture or as a coprocessed dry binder in matrix tablets with extended drug release

2018 ◽  
Vol 68 (3) ◽  
pp. 295-311 ◽  
Author(s):  
Jitka Mužíková ◽  
Alena Komersová ◽  
Václav Lochař ◽  
Lucie Vildová ◽  
Bára Vošoustová ◽  
...  
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Polyvinyl Alcohol ◽  
Total Energy ◽  
Linear Regression Analysis ◽  
Physical Mixture ◽  
Matrix Tablets ◽  
Compression Process ◽  
Drug Release Rate ◽  
Dissolution Behaviour

Abstract This paper evaluates and compares the properties of directly compressible tabletting materials and matrix tablets containing a combination of α-lactose monohydrate and microcrystalline cellulose in the 3:1 ratio in a physical mixture and in a coprocessed dry binder. Tested parameters include flow properties, compressibility, compactibility and the rate of drug release from tablets. Compressibility is evaluated by means of the energy profile of the compression process. Compactibility is evaluated by means of the tensile strength of the tablets. Dissolution testing is done using the rotating basket method. Dissolution profiles are evaluated by non-linear regression analysis. Total energy of compression and plasticity values were higher in tabletting materials with the coprocessed dry binder. Increasing additions of polyvinyl alcohol decreased the values of total energy of compression, plasticity, tensile strength of tablets and drug release rate. Dissolution behaviour of tablets, which contained the physical mixture or coprocessed dry binder and the same amount of polyvinyl alcohol, was comparable.

scholarly journals A study of compressibility and compactibility of directly compressible tableting materials containing tramadol hydrochloride

2016 ◽  
Vol 66 (3) ◽  
pp. 433-441 ◽  
Author(s):  
Jitka Mužíková ◽  
Alena Kubíčková
Keyword(s):  
Tensile Strength ◽  
Total Energy ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Energy Profile ◽  
Compression Process ◽  
Tramadol Hydrochloride ◽  
Hydrophilic Gel

Abstract The paper evaluates and compares the compressibility and compactibility of directly compressible tableting materials for the preparation of hydrophilic gel matrix tablets containing tramadol hydrochloride and the coprocessed dry binders Prosolv® SMCC 90 and Disintequik™ MCC 25. The selected types of hypromellose are Methocel™ Premium K4M and Methocel™ Premium K100M in 30 and 50 % concentrations, the lubricant being magnesium stearate in a 1 % concentration. Compressibility is evaluated by means of the energy profile of compression process and compactibility by the tensile strength of tablets. The values of total energy of compression and plasticity were higher in the tableting materials containing Prosolv® SMCC 90 than in those containing Disintequik™ MCC 25. Tramadol slightly decreased the values of total energy of compression and plasticity. Tableting materials containing Prosolv® SMCC 90 yielded stronger tablets. Tramadol decreased the strength of tablets from both coprocessed dry binders.

scholarly journals Effect of Channeling Agents on the Release Profile of Theophylline from METHOCEL K4M Based Matrix tablets

1970 ◽  
Vol 7 (1) ◽  
pp. 27-32 ◽  
Author(s):  
Md Shaikhul Millat Ibn Razzak ◽  
Ferdous Khan ◽  
Md Ziaur Rahman Khan ◽  
Kanij Fatema ◽  
Muhammed Shahidul Islam ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Release Profile ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
Compression Process ◽  
Low Viscosity ◽  
Time Required

The present study was undertaken to investigate the effect of channeling agents on the release profile of Theophylline from METHOCEL K4M based matrix systems. Matrix tablets of Theophylline using METHOCEL K4M were prepared by direct compression process. METHOCEL K4M polymer is hydrophilic in nature. NaCl and PEG 1500 were used as channeling agents. Drug release study was evaluated for eight hours using USP 22 paddletype dissolution apparatus using distilled water as the dissolution medium. The release mechanisms were explored and explained with zero order, Higuchi and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by channeling agent type and content. Higher channeling agent content (42.49%) in the matrix increased the rate and extent of the drug release because of increased porosity in the tablet matrices, at lower channeling agent (19.76%) level, the rate and extent of drug release was decreased and in absence of channeling agents these were least. NaCl ensures maximum release of drug from low viscosity grade METHOCEL K4M than PEG 1500 when other parameters were kept constant. It was found that type and amount of channeling agent significantly affect the time required for 50% of drug release (T50%), percentage drug release at 8 hours, release rate constant (K) and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was mainly dependent on the presence of type and amount of channeling agent. These studies indicate that the proper balance between a matrix forming agent and a channeling agent can produce a drug dissolution profile similar to a theoretical dissolution profile.Key words: Channeling agent, Theophylline, Release Profile, Methocel K4MDOI = 10.3329/dujps.v7i1.1214Dhaka Univ. J. Pharm. Sci. 7(1): 27-32, 2008 (June)

Study of formulation variables influencing the drug release rate from matrix tablets by experimental design

2006 ◽  
Vol 62 (1) ◽  
pp. 77-84 ◽  
Author(s):  
S FURLANETTO ◽  
M CIRRI ◽  
F MAESTRELLI ◽  
G CORTI ◽  
P MURA
Keyword(s):  
Experimental Design ◽  
Drug Release ◽  
Release Rate ◽  
Matrix Tablets ◽  
Drug Release Rate ◽  
Formulation Variables

Effect of Freezing and Thawing Process on Betamethasone Acetate Release from Polyvinyl Alcohol Nanospheres

2009 ◽  
Vol 151 ◽  
pp. 159-165 ◽  
Author(s):  
Shahin Bonakdar ◽  
Seyed Ali Poursamar ◽  
Mohammad Rafienia ◽  
Mohammad A. Shokrgozar ◽  
Afshin Farhadi ◽  
...  
Keyword(s):  
Drug Release ◽  
Polyvinyl Alcohol ◽  
Freezing And Thawing ◽  
Drug Release Rate ◽  
Water Emulsion ◽  
Transmission Electron ◽  
Oil In Water ◽  
Thawing Process ◽  
Freezing Cycle ◽  
Oil In Water Emulsion

Betamethasone acetate (BA) is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties which can be used in treatment of asthma and itching. In this research, polyvinyl alcohol nanospheres loaded by betamethasone acetate were prepared by oil in water emulsion method after which they were exposed to 1, 2 and 4 cycles of freeze-thawing (F-T) process including 24 hours freezing cycle at -25 °C and 24 hours thawing at ambient temperature. Nanospheres fabrication was confirmed by transmission electron microscopy and betamethasone release was analyzed by UV spectrophotometer at 245 nm. The results revealed that by increasing the number of F-T cycles the rate of drug release decreased. The effect of BA concentration was also investigated on human chondrosarcoma (sw 1353). The MTT assay was utilized to assess the cell proliferation. The results showed that these biocompatible nanospheres can be used for sustained release of such drugs for more than four months and drug release rate can be effectively controlled by implementing F-T cycles.

scholarly journals A PROMISING APPROACH TO PROVIDE APPROPRIATE COLON TARGET DRUG DELIVERY SYSTEMS OF METRONIDAZOLE: DEVELOPMENT AND EVALUATION

2020 ◽  
Vol 9 (3) ◽  
Author(s):  
Bijay Kumar Sahoo ◽  
Sidheswar Prasad Pattajoshi ◽  
Sandhyarani Pattajoshi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Natural Polymers ◽  
Drug Release Rate ◽  
Hydroxypropyl Methyl Cellulose ◽  
Enteric Coated ◽  
Synthetic And Natural Polymers

The aim of present study was to develop colon targeted system for Metronidazole using guar gum and xanthan gum. Tablet matrices containing 10–60% of tablet weight of guar gum (F1–F6) were prepared by direct compression and subjected to in vitro release studies to explore their sustained release in the colon. Various release retarding synthetic and natural polymers, namely, hydrogenated castor oil, hydroxypropyl methyl cellulose, xanthan gum, and ethyl cellulose, Eudragit RL 100, were incorporated to modify the drug release rate from the guar gum matrix tablets. Matrix tablets were enteric coated with hydroxypropyl methyl cellulose phthalate as an enteric polymer. Various synthetic and natural polymers were incorporated to F6 to modify the drug release rate. Different 15 matrix tablet formulations (F6–F20) were enteric coated with hydroxypropyl methyl cellulose phthalate. The in-vitro drug release study was undertaken at 37±0.5°C in 0.1N HCl for 2 h; followed by pH 7.4 phosphate buffer (3h) finally in, simulated colonic fluid pH 6.8 phosphate buffer 20 h. The formulation F6, F13 and F20 showed promising sustained release results having median dissolution time (MDT) values: 8.25, 7.97, and 7.64, respectively. When studies were continued in colonic fluids, matrix tablets released almost 100% drug. whereas, Metronidazole enteric  formulations did not release drug in stomach and small intestine, but delivered drug to the colon resulting in slow absorption of the drug and making drug available for local action in the colon. Keywords:  Colon Target Delivery, Guar gum, Metronidazole, Enteric coated, Tablet Matrices

scholarly journals Achieving High Excipient Efficiency with Elastic Thermoplastic Polyurethane by Ultrasound Assisted Direct Compression

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 157 ◽  
Author(s):  
Eduardo Galdón ◽  
Marta Casas ◽  
Isidoro Caraballo
Keyword(s):  
Drug Release ◽  
Mechanical Energy ◽  
Thermoplastic Polyurethane ◽  
Matrix Tablets ◽  
Special Focus ◽  
Direct Compression ◽  
Sustained Drug Release ◽  
Compression Process ◽  
Thermoplastic Polyurethanes ◽  
Ultrasound Assisted

Ultrasound assisted compression (USAC) is a manufacturing technique which applies thermal and mechanical energy to the powder bed, producing tablets with improved characteristics compared to the direct compression process. This technology is ideal for thermoplastic materials, as polyurethanes, whose particles usually undergo a sintering process. Thermoplastic polyurethanes are widely used in sustained drug release systems but rarely seen in tablets due to their elastic properties. The aim of this work is to investigate the ability of USAC to manufacture sustained release matrix tablets based on elastic thermoplastic polyurethanes (TPU), overcoming the limitations of direct compression. The technological and biopharmaceutical characteristics of the TPU matrices have been evaluated, with special focus on the porous structure due to the implications on drug release. For the first time, USAC has been successfully employed for manufacturing elastic thermoplastic polyurethanes-based matrices. TPU tablets show an inert character with a sustained drug release governed by a diffusional mechanism. Initial porosity of matrices was similar in all batches studied, with no influence of drug particle size, and a fractal nature of the pore network has been observed. SEM microphotographs show the continuum medium created by the sintering of the polymer, responsible for the high excipient efficiency.

scholarly journals Comparative Evaluation of HPMC, PVA and Gelatin as Matrices for Controlled Release Drug Delivery

1970 ◽  
Vol 2 (1) ◽  
pp. 51-55
Author(s):  
Mohammad Anwarul Basher ◽  
Abul Kalam Lutful Kabir ◽  
Mohammad Musarraf Hussain ◽  
Mir Mohammad Abdullah Al Mamun
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Pharmaceutical Sciences ◽  
Drug Release Profile ◽  
Compression Process ◽  
Model Drug

The present study was undertaken to compare three different polymeric gums- HPMC, PVA and gelatin as controlled release matrices. Diclofenac sodium, a potent analgesic, was used as the model drug. Different ratio of HPMC, PVA and gelatin were incorporated into the lactose loaded Diclofenac tablet to explore their impact on drug release. Matrix tablets of Diclofenac were prepared by using individual polymer with magnesium stearate and aerosil by direct compression process at 5 ton pressure. The release of drug from these matrices was studied over 2 hrs in acidic media where insignificant release was observed. Then, the same formulations were studied over 8 hours in buffer media of pH 6.8 at a temperature of 37± 0.5°C. Statistically significant differences in drug release profile was found among the tablets prepared from different matrices. The study revealed that the average % release of drug from different types of polymer loaded matrix tablet varied with the ratio of different polymers. Among the three polymers, PVA showed best dissolution pattern. A comparison of Higuchi curve and bi-exponential curve was also performed. Key words: HPMC; PVA; Gelatin; Controlled release; Diclofenac DOI: 10.3329/sjps.v2i1.5816Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 51-55

scholarly journals A Study of Compressibility, Compactability and Mucoadhesivity of Tableting Materials for Matrix Systems Based on Chitosan

Polymers ◽  
2021 ◽  
Vol 13 (21) ◽  
pp. 3636
Author(s):  
Jitka Muzikova ◽  
Eva Snejdrova ◽  
Juraj Martiska ◽  
Bara Doubkova ◽  
Andrea Veris
Keyword(s):  
Tensile Strength ◽  
Sodium Alginate ◽  
Matrix Tablets ◽  
Energy Profile ◽  
Compression Process ◽  
Gel Layer ◽  
Sensitivity Ratio ◽  
The Matrix ◽  
Negative Effect ◽  
Targeted Drug

The objective of the present research is to evaluate directly compressible chitosan-based tableting materials for the formulation of mucoadhesive matrix tablets intended for targeted drug release to distal segments of the GIT. The influence of sodium alginate, hypromellose, and silicified microcrystalline cellulose (P90) on compressibility, compactability and lubricant sensitivity ratio was tested. Furthermore, the rheological properties of the hydrated surface layer of the matrix tablets and the mucoadhesion to a mucin substrate were analysed. Compressibility was evaluated using the energy profile of the compression process, compactability by means of the tensile strength of tablets, and lubricant sensitivity ratio was calculated to assess the sensitivity to lubricant. Addition of P90 to chitosan improved compressibility, which is demonstrated by the increase in the energy of plastic deformation and the higher tensile strength of tablets. P90 also significantly reduced the high lubricant sensitivity of chitosan. Presence of retarding components led to a decrease in Emax. All tested matrix tablets revealed a good mucoadhesion without a negative effect of P90 content. The viscosity of a gel layer on the surface of matrix tablets containing hypromellose was higher compared to those with sodium alginate. This was not reflected in the adhesive strength of the tablets. The formulated tableting materials combining chitosan and P90 are a suitable matrix for incorporation of an active ingredient, whose delayed release in the intestine can be achieved by the functionality of the chitosan-sodium alginate complex.

Fabrication of Shellac-Zein Based Matrix Tablet as a Carrier for Controlling of Drug Release

2014 ◽  
Vol 1060 ◽  
pp. 50-53
Author(s):  
Noppadol Chongcherdsak ◽  
Direk Aekthammarat ◽  
Teerayuth Prathumchat ◽  
Chutima Limmatvapirat ◽  
Sontaya Limmatvapirat
Keyword(s):  
Drug Release ◽  
Acid Resistance ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Composite Polymer ◽  
Drug Release Profile ◽  
Compression Process ◽  
Model Drug ◽  
Release Data ◽  
Kinetics Of

The aim of research was to fabricate shellac-zein composite polymer-based matrix tablets by using theophylline as a model drug. The tablets were prepared by direct compression process. The initial weight and hardness of tablets were controlled within the range of 300±5 mg and 60±10 N, respectively. The tablets were annealed at 80 °C for 24 h and kept in the ambient temperature before evaluation. Drug release profile and kinetics of drug release in 0.1 N HCl and buffer pH 6.8 were investigated. The result showed that the annealing process and shellac:zein ratio, affected drug release characteristic in both media.The delayed released in acid medium of formulation containg shellac-zein composite polymer at the ratio from 30:70 was extended to over 120 min. In addition, the more sustained drug released in buffer was observed after increasing shellac:zein ratio. The good acid resistance of shellac and the swollen characteristic of zein in buffer might be a good explanation for the specific release. For the analysis of drug release data, drug release profiles were fitted into Higuchi model suggesting that the main mechanism of drug release from matrix tablets was super case II transport.

FORMULATION AND EVALUATION OF DRUG RELEASE PROFILE OF HYDROPHILIC POLYMER BASED INDOMETHACIN PROLONG RELEASE MATRIX TABLETS

2021 ◽  
pp. 30-33
Author(s):  
Jayashree B. Gaja ◽  
Jesindha Beyatricks ◽  
Monisha R
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Drug Release Rate ◽  
Weight Variation

An oral modied release dosage forms have always been more effective therapeutic alternative to conventional dosage forms. The present invention is directed to a modied release pharmaceutical composition of indomethacin by using hydrophilic release retardant polymers like HPMC K15M, Na CMC alone or in combination. Matrix embedded prolong release tablet formulations of Indomethacin were prepared by wet granulation technique and evaluated for tablet properties such as the thickness, hardness, friability, weight variation, drug content, drug release kinetics and in vitro release studies. The inuence of drug polymer ratio on drug release was studied by dissolution test. The FTIR studies showed no interactions among drug and polymers. The tablets formulation (F7 and F8) containing combined polymers of HPMC K15M and Na CMC resulted in slower drug release rate form the matrix. So, it can be concluded that Indomethacin prolong release tablets using HPMC K15M and Na CMC as the retardant has successfully extended the release of indomethacin from its formulations. The mixing of two cellulose polymers, ionic and non-ionic, for the formulation of hydrophilic matrices, resulted in a valuable decrease in drug release rate. All the formulations showed KorsmeyerPeppa’s model as a best t.

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