scholarly journals The Comparison of Two Challenging Low Dose APIs in a Continuous Direct Compression Process

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 279 ◽  
Author(s):  
Tuomas Ervasti ◽  
Hannes Niinikoski ◽  
Eero Mäki-Lohiluoma ◽  
Heidi Leppinen ◽  
Jarkko Ketolainen ◽  
...  
Keyword(s):  
Process Parameters ◽  
Powder Mixture ◽  
Significant Influence ◽  
Low Dose ◽  
Quality Parameters ◽  
Direct Compression ◽  
Compression Process ◽  
Viable Solution ◽  
Powder Analysis ◽  
Dose Tablet

Segregation is a common problem in batch-based direct compression (BDC) processes, especially with low-dose tablet products, as is the preparation of a homogenous mixture. The scope of the current work was to explore if a continuous direct compression (CDC) process could serve as a solution for these challenges. Furthermore, the principle of a platform formulation was demonstrated for low dose tablets. The combination of filler excipients and the API in the formulation used was suitable for direct compression, but also prone to induce segregation in BDC process. The CDC process was found to be very promising; it was shown that tablets with the desired quality parameters could be manufactured successfully with both of the APIs studied. Powder analysis indicated that the APIs display some fundamental differences in their physical properties, which was also reflected in powder mixture properties and, hence, eventually in processing. However, process parameters, especially mixer impeller speed, were not found to have any significant influence on end product quality. The study suggests that a CDC process can be a viable solution to resolve the challenges described. Moreover, manufacturing by using a universal platform formulation seems to be a feasible way for producing low-dose tablets.

Harnessing ordered mixing to enable direct-compression process for low-dose tablet manufacturing at production scale

2013 ◽  
Vol 239 ◽  
pp. 290-299 ◽  
Author(s):  
Chen Mao ◽  
Venkat R. Thalladi ◽  
Derrick K. Kim ◽  
Sarina H. Ma ◽  
David Edgren ◽  
...  
Keyword(s):  
Low Dose ◽  
Direct Compression ◽  
Compression Process ◽  
Production Scale ◽  
Tablet Manufacturing ◽  
Dose Tablet

Optimization of Microcrystalline Cellulose PH 101, Lactose, and Kollidon® K 30 To Obtain Co-Processed Excipient Through Spray Drying

2017 ◽  
Vol 7 (2) ◽  
Author(s):  
Kusuma P. ◽  
Syukri Y ◽  
Sholehuddin F. ◽  
Fazzri N. ◽  
Romdhonah . ◽  
...  
Keyword(s):  
Spray Drying ◽  
Microcrystalline Cellulose ◽  
Chemical Change ◽  
Direct Compression ◽  
Flow Properties ◽  
Scanning Calorimetry ◽  
Compression Process ◽  
Infrared Spectrophotometer ◽  
Physical Mixtures ◽  
Spray Dried

The most efficient tablet processing method is direct compression. For this method, the filler-binder can be made by coprocessing via spray drying method. The purpose of this study was to investigate the effect of spray dried co-processing on microcrystalline cellulose (MCC) PH 101, lactose and Kollidon® K 30 as well as to define the optimum proportions. Spray dried MCC PH 101, lactose, and Kollidon® K 30 were varied in 13 different mixture design proportions to obtain compact, free-flowing filler-binder co-processed excipients (CPE). Compactibility and flow properties became the key parameters to determine the optimum proportions of CPE that would be compared to their physical mixtures. The result showed that the optimum proportion of CPE had better compactibility and flow properties than the physical mixtures. The optimum CPE, consisting of only MCC PH 101 and Kollidon® K 30 without lactose, that were characterized using infrared spectrophotometer, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscope (SEM) indicated no chemical change therein. Therefore, this study showed that spray dried MCC PH 101, lactose and Kollidon® K 30 could be one of the filler-binder alternatives for direct compression process.

scholarly journals Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms

Processes ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 26
Author(s):  
Teodora Balaci ◽  
Bruno Velescu ◽  
Oana Karampelas ◽  
Adina Magdalena Musuc ◽  
George Mihai Nițulescu ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Molar Ratio ◽  
Mechanical Resistance ◽  
Direct Compression ◽  
Active Ingredients ◽  
Compression Process ◽  
Antioxidant Power

The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate.

scholarly journals FORMULATION OF RIZATRIPTAN BENZOATE SUBLINGUAL TABLETS PREPARED BY DIRECT COMPRESSION WITH DIFFERENT BIOADHESIVE POLYMER: IN VITRO AND EX VIVO EVALUATION

2017 ◽  
Vol 10 (16) ◽  
pp. 36
Author(s):  
Harmanpreet Singh ◽  
Pooja Jaiswal ◽  
Suksham Gupta ◽  
Simerjit Singh
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Systemic Circulation ◽  
Direct Compression ◽  
Compression Process ◽  
Rizatriptan Benzoate ◽  
Dissolution Tests ◽  
Ex Vivo Permeation ◽  
Bioadhesive Polymers

  Objective: The current investigation deals with formulation and evaluation of fast disintegrating sublingual tablets of rizatriptan benzoate (RTB) to produce its intended therapeutic effect for acute treatment of migraine. When the drug is given by sublingual route, it overcomes the first pass metabolism and quick entry of drug in systemic circulation is obtained. It would result in fast pharmacological response hence faster relief from migraine which is an important criterion in migraine therapy.Methods: In this study, RTB sublingual tablets were prepared using direct compression process using various bioadhesive polymers such as sodium carboxymethyl cellulose, hydroxyl propyl methyl cellulose-K4M, and chitosan at various concentration ranging 0.5-5% w/w along with sodium starch glycolate (SSG) or cross carmellose sodium (CCS) as super disintegrants at different concentration ranging 2-8% w/w.Results: The tablets disintegrated quickly and dissolution tests conclude that RTB was released from the formulation within the compendial limits. The formulations batches (A8 and B8) containing 2% w/w chitosan along with 2% w/w SSG or CCS which disintegrate rapidly and show high dissolution and ex vivo permeation were selected as optimized formulations.Conclusion: The results obtained from the study showed that the bioavailability problem of the drug has been solved as the drug is given by sublingual route and it directly enters into systemic circulation. Furthermore, the formulation overcomes the problems associated with migraine attack as fast disintegrating technology is used.

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. 

Low-dose capsule filling of inhalation products: Critical material attributes and process parameters

2014 ◽  
Vol 473 (1-2) ◽  
pp. 617-626 ◽  
Author(s):  
Eva Faulhammer ◽  
Marlies Fink ◽  
Marcos Llusa ◽  
Simon M. Lawrence ◽  
Stefano Biserni ◽  
...  
Keyword(s):  
Process Parameters ◽  
Low Dose ◽  
Critical Material ◽  
Critical Material Attributes

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.

Problems of Producing Thin-Walled and Elastic Elements by Selective Laser Sintering

2014 ◽  
Vol 223 ◽  
pp. 191-198 ◽  
Author(s):  
Tomasz Kozior
Keyword(s):  
Process Parameters ◽  
Significant Influence ◽  
Selective Laser Sintering ◽  
Additive Technology ◽  
Printing Process ◽  
Strength Tests ◽  
Thin Walled ◽  
Polyamide Powder ◽  
Printing Processes ◽  
Elastic Elements

The article describes the technology of making thin-walled components and elastic by additive technology SLS using a polyamide powder PA 2200. The characteristics of the selected elements and the results of their strength tests are presented. The research focuses on the anisotropy of the materials in the various models. Printing processes were investigated on surfaces perpendicular and parallel to the axis of the model. Based on measurements of deformation, coefficients of elasticity, and the influence of selected parameters of the printing process, the accuracy of tested elements were determined. Comparing results of the research indicated that there is a significant influence of direction and printing process parameters on elastic properties. Research can be helpful in the future in the design process of elastic and thin-walled components such as springs and bellows.

scholarly journals Assessment of fruit firmness of pepper using non-destructive physical measurements, in response to different growing and pruning technologies

2003 ◽  
Vol 9 (1) ◽  
Author(s):  
D. Tompos ◽  
S. Istella ◽  
T. Ignát
Keyword(s):  
Significant Influence ◽  
Quality Parameters ◽  
European Market ◽  
Fruit Firmness ◽  
Physical Measurements ◽  
Vegetable Products ◽  
Important Quality ◽  
Non Destructive ◽  
Pruning Methods

The European market demands vegetable products of the highest quality and this commercial quality must be maintained till the goods reach the customer. One of these important quality parameters is the fruit firmness of pepper. The experiments were aimed at to find out the influence of different growing methods (soil or rockwool-based) and pruning technologies (to 1, 2, 3 or 4 shoots) on the yield and fruit firmness of three pepper varieties (HO F1, Karpia Fl and Pritavit F1) which are common in Hungary. Fruit firmness was measured by the non-destructive impact method. On the basis of the results, in unheated forcing the pruning to 1, 2 or 3 shoots can be suggested for all three varieties, as well as the utilisation of rockwool in their growing. The non-destructive impact method has been found suitable for testing the fruit firmness of pepper varieties. In the experiments involving different growing mediums pepper stands were found to show significant differences, however the different pruning methods had no significant influence on fruit firmness.

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