scholarly journals Disintegrant Properties of Microcrystalline Cellulose isolated from Rami (Boehmeria nivea L. Gaud) in Dimenhydrinate tablets by Wet Granulation and Direct compression

2021 ◽  
Vol 2 (3) ◽  
Author(s):  
Nagina Gulab Belali ◽  
Anis Y. Chaerunisaa ◽  
Taofik Rusdiana
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Physical Properties ◽  
Process Parameters ◽  
Microcrystalline Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Disintegration Time ◽  
Boehmeria Nivea ◽  
Significant Difference

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.

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

2019 ◽  
pp. 1-14
Author(s):  
Nkemakolam Nwachukwu ◽  
Sabinus Ifeanyi Ofoefule
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Microcrystalline Cellulose ◽  
Cocos Nucifera ◽  
In Vitro Release ◽  
Disintegration Time ◽  
British Pharmacopoeia ◽  
Fluid Bed ◽  
Vitro Release

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.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

scholarly journals FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Rapid Release ◽  
Weight Variation ◽  
Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 

scholarly journals Effect of Polymers on the Pharmaco-mechanical Properties of Direct Compressed Tablets with Ketoprofen

2019 ◽  
Vol 56 (1) ◽  
pp. 239-244
Author(s):  
Monica Iliuta Stamate ◽  
Ciprian Stamate ◽  
Daniel Timofte ◽  
Bogdan Ciuntu ◽  
Carmen Gafitanu ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Direct Compression ◽  
Mechanical Parameters ◽  
Compression Method ◽  
Drug Substances ◽  
Polymeric Binders ◽  
Made In

In this study, the effect of polymers on the mechanical properties of ketoprofen extended drug release systems were studied. Many polymers are added in formulation of compressed tablets in order to improve the physicochemical characteristics of the drug release system. The samples were made in the form of cylindrical tablet about 9 mm in diameter, containing different mixtures of drug substances and excipients acording to seven formulations. Cylindrical tablets containing mixtures of ketoprofen and various types of polymers are made by direct compression method. Among the binders used were a series of different polymers like Kollidon va 64, hydroxypropyl methyl cellulose and sodium carboxyl methyl cellulose. Mechanical parameters such as hardness, mechanical strenght, friability and roughness were studied in order to determine how they are influenced by polymeric binders.

scholarly journals Effect of a co-processed excipient on the disintegration and drug release profile of ibuprofen tablets

Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Angle Of Repose ◽  
Oral Dosage ◽  
Direct Compression ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
Crushing Strength ◽  
Tablet Properties ◽  
Spray Dried

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.  

scholarly journals Effect of nonionic surfactants on the release of paracetamol from suppositories

2015 ◽  
Vol 26 (1) ◽  
pp. 40-44
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Phosphate Buffer ◽  
Nonionic Surfactants ◽  
Tween 80 ◽  
Content Uniformity ◽  
Fusion Method ◽  
Disintegration Time ◽  
Span 60

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.

scholarly journals Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Rajni Bala ◽  
Sushil Khanna ◽  
Pravin Pawar
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Content Uniformity ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
Significant Difference ◽  
Film Formulation ◽  
Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

scholarly journals Spherical crystallization of drugs

2012 ◽  
Vol 62 (1) ◽  
pp. 1-14 ◽  
Author(s):  
Borut Kovačič ◽  
Franc Vrečer ◽  
Odon Planinšek
Keyword(s):  
Mechanical Properties ◽  
Process Parameters ◽  
Physical And Mechanical Properties ◽  
Spherical Particles ◽  
Direct Compression ◽  
Solvent Diffusion ◽  
Spherical Crystallization ◽  
Stirring Rate ◽  
Diffusion Systems ◽  
Rate Type

Spherical crystallization of drugs Spherical crystallization of drugs is the process of obtaining larger particles by agglomeration during crystallization. The most common techniques used to obtain such particles are spherical agglomeration and quasi-emulsion solvent diffusion. Ammonia diffusion systems and crystallo-co-agglomeration are extensions of these techniques. By controlling process parameters during crystallization, such as temperature, stirring rate, type and amount of solvents, or excipient selection, it is possible to control the formation of agglomerates and obtain spherical particles of the desired size, porosity, or hardness. Researchers have reported that the particles produced have improved micromeritic, physical, and mechanical properties, which make them suitable for direct compression. In some cases, when additional excipients are incorporated during spherical crystallization, biopharmaceutical parameters including the bioavailability of drugs can also be tailored.

scholarly journals Development and Evaluation of Alprazolam Controlled Release tablets

2014 ◽  
Vol 1 (1) ◽  
pp. 8-23 ◽  
Author(s):  
Sarmila Shrestha ◽  
Dharma Prasad Khanal ◽  
Panna Thapa
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Drug Formulation ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Significant Difference ◽  
Model Independent ◽  
Tablet Formulations

Twenty three different tablet formulations of alprazolam were prepared using Polymer like hydroxypropylmethyl cellulose (HPMC K4M, HPMC K15M and HPMC K100M) in the concentration of 5 – 50 % of total weight of tablets and combination of HPMC K15M and HPMC K100M with ethyl cellulose (EC) was formulated by using wet granulation method. Drug formulation containing 1.0 mg, 1.5 mg, 5 mg, 10 mg and 15 mg alprazolam per tablet maintaining constant HPMC K15M concentration was also developed.The in-vitro dissolution studies of the formulated and marketed product in USP type II apparatus showed that the drug release is dependent upon the drug: polymer ratio; also molecular weight of the polymer and solubility of loaded drug. With increasing concentration and molecular weight of polymer, drug release was found to be decreased. When formulating the tablets the method used whether direct compression or wet granulations also affect the release of the drug from matrix. Wet granulation method by using 40 % HPMC K15M in combination with 5 % EC was found to be most suitable controlled release alprazolam tablet as drug release was found to be appreciable in this formulation. When loading dose of alprazolam was increased, drug release was found to be tremendously decreased because of the poor solubility of alprazolam in water. When one-way ANOVA was applied for various formulated and marketed tablets it was found that there is no significant difference (p > 0.05) in drug release rate among formulation similarly model independent methods was also applied such as similarity and dissimilarity factor and found that there is no significant difference between these formulations.DOI: http://dx.doi.org/10.3126/jmmihs.v1i1.9896 Journal of Manmohan Memorial Institute of Health Sciences Vol.1(1) 2011; 8-23

scholarly journals Tablet Formula Optimization From Helminthostachys Zaylanica Extract Using A Simplex Lattice Design

2021 ◽  
Vol 6 (3) ◽  
pp. 131-136
Author(s):  
Fitrya Fitrya ◽  
Najma Annuria Fithri ◽  
Budi Untari ◽  
Aprililianti
Keyword(s):  
Physical Properties ◽  
Toxicity Tests ◽  
Dissolution Time ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Lattice Design ◽  
Simplex Lattice Design ◽  
Weight Variation ◽  
Simplex Lattice ◽  
Helminthostachys Zeylanica

Helminthostachys zeylanica extract has pharmacological activities such as antioxidant, antiinflamatory, and antihyerucemia. This extract is nontoxic substance from the acute and subchronic toxicity tests. This extract has a potency to be formulated into tablet dosage forms. This study aims to optimize a tablet formula from Helminthostachys zeylanica extract. Disintegrant and binder concentrations were independent variables, while physical properties and dissolution time of the tablets were dependent variables. The tablet was prepared by a wet granulation method. Formula was optimized by Simplex Lattice Design. Physicochemical propertiesof granule, physical properties and dissolution of tablet were then analyzed with One Way ANOVA (p = 0.05). Based on granule analysis, specification of physicochemical parameters, such as hausner’s ratio, compressibility index, flowability, repose angle, and water content, met standard British Pharmacopeia. In addition, the starch and PVA concentrations influenced thickness, weight variation, hardness, friability, disintegration time and dissolution of the tablets (p <0.05), except for friability (p> 0.05). Based on this study, the starch and PVA concentrations for the optimum tablet formula were 19.5% and 1.05%, respectively.

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