scholarly journals Improving Tableting Performance of Lactose Monohydrate by Fluid-Bed Melt Granulation Co-Processing

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2165
Author(s):  
Djordje Medarević ◽  
Jelena Djuriš ◽  
Mirjana Krkobabić ◽  
Svetlana Ibrić
Keyword(s):  
Direct Compression ◽  
Disintegration Time ◽  
Poloxamer 188 ◽  
Lactose Monohydrate ◽  
Peg 4000 ◽  
Wide Range ◽  
Fluid Bed ◽  
Interparticle Bonding ◽  
Melt Granulation ◽  
Lubricating Properties

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.

scholarly journals Fluidized Hot Melt Granulation Technique: An Approach to Improve Micromeritics Properties and Dissolution Rate of Efavirenz

2020 ◽  
pp. 554-560
Author(s):  
Deval J. Modi ◽  
Pragna K. Shelat ◽  
Divyesh H. Shastri
Keyword(s):  
Dissolution Rate ◽  
Primary Objective ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
Content Uniformity ◽  
Peg 4000 ◽  
Fluid Bed ◽  
Hot Melt Granulation ◽  
Hot Melt ◽  
Melt Granulation

The Fluidized hot melt granulation technique is a process by which pharmaceutical powders are efficiently agglomerated using a low melting binder. The effect of the binder properties and concentrations on agglomerate growth mechanisms were studied in this research paper using this technique with the primary objective of improvement in the solubility and dissolution rate of efavirenz by melt-dispersion granulation employing meltable hydrophilic carrier and then to convert the melt dispersion into flowable and compressible dispersion granules to yield a rapidly dissolving tablet formulation. The Optimized concentrations of co-polymers like PEG 6000, PEG 4000, Gelucire 50/13, Gelucire 44/14, Poloxamer 188 and Poloxamer 407 in different ratios (i.e., 1:1, 1:2, 1:3 and 1:4) as meltable binder along with the drug were sprayed dropwise over lactose as diluent loaded into fluid bed chamber for the preparation of the granules of efavirenz and characterized for its micromeritical properties, DSC, XRD etc. The tablets prepared from the granules were evaluated for drug dissolution rate. The prepared granules were found to have excellent flow properties indicated by mean diameter D50:138µm, Carr’s index 13.92% and the drug content uniformity of 98.10%. XRD data exhibited partial loss of crystallinity as indicated by significantly less intensity of efavirenz peak in sample than pure efavirenz. Drug release from tablet was fast found 99.12% w/v within 30 minutes. Absence of Efavirenz endothermic peak at higher proportions of meltable binder reported by DSC data exhibited amorphous form of efavirenz led to complete solubilization and thus faster dissolution rate of efavirenz.

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
Keyword(s):  
Tensile Strength ◽  
Dissolution Rate ◽  
Microcrystalline Cellulose ◽  
Extended Release ◽  
Moisture Sorption ◽  
Direct Compression ◽  
Disintegration Time ◽  
Lactose Monohydrate ◽  
Compact Density ◽  
Tablet Disintegration

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.

Design, Optimization and Evaluation of Fast-Dissolving Oral Films of Ropinirole

2018 ◽  
Vol 11 (1) ◽  
pp. 3958-3967
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 4000 ◽  
Oral Films

The main objective of this study was to develop fast dissolving oral films of ropinirole HCl to attain quick onset of action for the better management of Parkinson’s disease. Twenty-seven formulations (F1-F27) of ropinirole oral dissolving films by solvent-casting method using 33 response surface method by using HPMC E15, Maltodextrin PEG 4000 by using Design of experiment software. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F4 showed minimum disintegration time 11 sec, maximum drug was released i.e. 99.68 ± 1.52% of drug within 10 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 92.77 ± 1.52 after 50 min. Therefore, it can be a good alternative to conventional ropinirole for immediate action. In vitro evaluation of the ropinirole fast dissolving films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of ropinirole. The oral dissolving film is considered to be potentially useful for the treatment of Parkinson’s disease where quick onset of action is desired

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. 

Synthesis of high viscosity index base stock and study on the lubricating properties

2016 ◽  
Vol 68 (1) ◽  
pp. 52-56 ◽  
Author(s):  
Weiwei Wang ◽  
Shan Jiang ◽  
Yan Shen ◽  
Shunba Xia ◽  
Jiujun Xu
Keyword(s):  
Ionic Liquid ◽  
Reaction Time ◽  
Viscosity Index ◽  
Content Type ◽  
Group I ◽  
Film Forming ◽  
Wide Range ◽  
Catalyst Dosage ◽  
Group Ii ◽  
Lubricating Properties

Purpose – This paper aims to address the polymerization of 1-decene by [Emim]Cl/AlCl3 ionic liquid and the film-forming properties of the product compared with commercially available base stocks. Design/methodology/approach – Experiments were carried out to investigate the influence of [Emim]Cl/AlCl3 mole ratio, catalyst dosage, reaction temperature, reaction time and water on the polyreaction. Poly alpha-olefin (PAO) is prepared under optimal reaction condition. Film-forming properties of PAO have been compared with those of Group I, Group II and Group III base stocks, which are selected with approximately the same viscosity. Findings – Experimental results show that after a 4-h reaction time, yield of PAO can be higher than 85 per cent and viscosity index can be up to 160 with [Emim] Cl/AlCl3 mole ratio of 2:1, catalyst dosage of 3 per cent wt. and water content of 20 ppm. A strong influence of water on reaction is observed. With approximately the same viscosity, PAO shows the superiority in film thickness at low-sliding speeds compared with Group I and Group II base stocks. At high temperature, PAO provides a thicker film than other base stocks. Originality/value – In recent years, there has been considerable interest in ionic liquids. As a novel catalyst, it has so many advantages including low corrosion, low toxicity, low cost and a potentially wide range of properties compared with traditional catalysts. This paper reports the polymerization of 1-decene by [Emim]Cl/AlCl3 ionic liquid and the study on lubricating properties of PAO compared with mineral base stocks.

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 Formulation and evaluation of taste masked oral disintegrating tablets of lornoxicam

2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar
Keyword(s):  
Cation Exchange Resin ◽  
The Elderly ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Weight Variation ◽  
Croscarmellose Sodium

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders.  The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.

Effect of Modified Hydroxypropyl Tapioca Starch and Percentage of Drug Loading on Physical Property of Paracetamol Tablet

2020 ◽  
Vol 859 ◽  
pp. 3-8
Author(s):  
Vipaluk Patomchaiviwat ◽  
Sontaya Limmatvapirat ◽  
Chaisai Sirisapaya ◽  
Rohanee Kolae ◽  
Kulmanee Anantakul ◽  
...  
Keyword(s):  
Drug Loading ◽  
Physical Property ◽  
High Hardness ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Tapioca Starch ◽  
Drug Concentrations ◽  
Model Drug ◽  
Better Than

The objective of this study was to investigate the effect of modified hydroxypropyl tapioca starch (HPTS) and % drug loading on physical property of tablet. Paracetamol was used as model drug because of its poor compressibility. The filler ability of modified HPTS such as hydroxyl propyl oxidized tapioca starch (HPOTS), hydroxyl propyl crosslinked tapioca starch (HPCTS) and pregelatinized tapioca starch (PTS) were evaluated and compared with the commercial starch (Starch 1500®). Tablets were prepared by direct compression method and the percent drug loading were 15, 30, 45, 60, 75%. For modified HPTS, the hardness of the tablets tended to decrease when the concentration of paracetamol increased. At drug concentrations of 15-30%, HPOTS exhibited good performance of tablet as indicated by the high hardness, low friability and acceptable disintegration time. The obtained results were better than HPTS and comparable to Starch 1500®. Moreover, the results revealed that tablet containing PTS provided the highest hardness and prolonged disintegration time (>30 min) while tablet containing HPCTS showed rapid disintegration time (<2 min). Therefore, modified HPTS disclosed promising properties for application as tablet filler

scholarly journals PREFORMULATION STUDIES USING LACTOSE IN DEVELOPMENT OF SOLID ORAL DOSAGE FORM: A GRAPHICAL REPRESENTATION USING SeDeM METHOD

2017 ◽  
pp. 168-172
Author(s):  
Imran Tadwee ◽  
Sadhana Shahi ◽  
Zahed Zaheer
Keyword(s):  
Dosage Form ◽  
Graphical Representation ◽  
Oral Dosage ◽  
Direct Compression ◽  
Compression Index ◽  
Compression Process ◽  
Lactose Monohydrate ◽  
Anhydrous Lactose ◽  
Good Compression ◽  
Parameter Profile

Objective: The objective of the study is to evaluate and present lactose scientifically as an excipient of choice in formulation development of solid orals dosage form for direct compression method. Present work will establish the ability of lactose as an excipient to be the choice of candidate while developing formulation having poor flow API using direct compression process. In addition to this different type of lactose is processed using secure development method (SeDeM) in order to evaluate best suitable type of lactose amongst its different type.Methods: Lactose anhydrous, lactose monohydrate and Lactose spray dried (SD) were employed for evaluation using SeDeM method, twelve different selected pharmacotechnical parameters were determined experimentally and were treated mathematically and expressed in the graphical representation as SeDeM diagram. Parameter index, parameter profile index and good compression index values were calculated.Results: Good compression index was found to be 6.06,5.72,6.83 parameter index was 0.25, 0.42, 0.17 and parameter profile index found to be 6.36,6.01,7.18 for lactose anhydrous, lactose monohydrate and Lactose SD respectively.Conclusion: This research work reveals that data obtained will be useful for the pharmaceutical industries while formulating the drug product and will reflect the scientific characteristics of this excipient as well. This will enable the availability of values obtained after performing SeDeM studies on lactose to scientific society based on the results researchers can use establised data and statistics in their pre-formulation studies to incorporate lactose with confidence and can be justified scientifically in the development formulation of the direct compression process and API having poor flow. Results indicating good direct compression characteristics of the all 3 type of lactose, and Lactose SD can be preferred amongs these 3 types. 

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