Tabletting Articles

Dry Granulation and Compression of Spray-Dried Plant Extracts

The purpose of this research was to evaluate the influence of dry granulation parameters on granule and tablet properties of spray-dried extract (SDE) from Maytenus ilicifolia, which is widely used in Brazil in the treatment of gastric disorders. The compressional behavior of the SDE and granules of the SDE was characterized by Heckel plots. The tablet properties of powders, granules, and formulations containing a high extract dose were compared. The SDE was blended with 2% magnesium stearate and 1% colloidal silicon dioxide and compacted to produce granules after slugging or roll compaction. The influences of the granulation process and the roll compaction force on the technological properties of the granules were studied. The flowability and density of spray-dried particles were improved after granulation. Tablets produced by direct compression of granules showed lower crushing strength than the ones obtained from nongranulated material.

Journal: 
American Association of Pharmaceutical Scientists.

Effect of Polysulfonate Resins and Direct Compression Fillers on Multiple-Unit Sustained-Release Dex

The purpose of this work was to investigate the effect of different polysulfonate resins and direct compression fillers on physical properties of multiple-unit sustained-release dextromethorphan (DMP) tablets. DMP resinates were formed by a complexation of DMP and strong cation exchange resins, Dowex 50 W and Amberlite IRP69. The tablets consisted of the DMP resinates and direct compression fillers, such as microcrystalline cellulose (MCC), dicalcium phosphate dihydrate (DCP), and spray-dried rice starch (SDRS). Physical properties of tablets, such as hardness, disintegration time, and in vitro release, were investigated. A good performance of the tablets was obtained when MCC or SDRS was used. The use of rod-like and plate-like particles of Amberlite IRP69 caused a statistical decrease in tablet hardness, whereas good tablet hardness was obtained when spherical particle of Dowex 50 W was used.

Journal: 
American Association of Pharmaceutical Scientists.

Punch and Die Toolroom Logic

High quality tablet compression tooling is expensive, albeit consumable. With the potential for tooling damage during tablet production, transportation and storage, an acceptable method of cleaning, repairing, validating and storing tooling is required by anyone who manufactures tablets - and the regulatory inspection authorities.

For free full-text articles
Click Here

Journal: 
Pharmaceutical Technology Europe, Oct 1, 2002.

Comparative Evaluation of Tableting Compression Behaviors by Methods of Internal

This study evaluated tableting compression by using internal and external lubricant addition. The effect of lubricant addition o­n the enzymatic activity of trypsin, which was used as a model drug during the tableting compression process, was also investigated. The powder mixture (2% crystalline trypsin, 58% crystalline lactose, and 40% microcrystalline cellulose) was kneaded with 5% hydroxypropyl cellulose aqueous solution and then granulated using an extruding granulator equipped with a 0.5-mm mesh screen at 20 rpm. After drying, the sample granules were passed through a 10-mesh screen (1680 μm). A 200-mg sample was compressed by using 8-mm punches and dies at 49, 98, 196, or 388 MPa (Mega Pascal) at a speed of 25 mm/min. The external lubricant compression was performed using granules without lubricant in the punches and dies. The granules were already dry coated by the lubricant.

Journal: 
AAPS PharmSci. 2001; 3 (3): article 20.

Compression, Compaction, and Disintegration Properties of Low Crystallinity Cellulose

The tabletting characteristics of low crystallinity celluloses (LCPC)-LCPC-700, LCPC-2000, and LCPC-4000-prepared using agitation rates of 700, 2000, and 4000 rpm, respectively, during their regeneration from phosphoric acid, were evaluated and compared with those of Avicel PH-102 and Avicel PH-302. The mean deformation pressure values calculated from the linear region of the Athy-Heckel curves indicated LCPC-4000 to be the most ductile material. The area under the Athy-Heckel curve for LCPC-4000 was 330 MPa, whereas LCPC-700 and LCPC-2000 showed a corresponding value similar to that of Avicel PH-102 and Avicel PH-302 (192-232 MPa). The tensile strength of LCPC and Avicel compacts increased linearly with increasing applied pressures. A comparison of the area under the tensile strength-compression pressure curves indicated that LCPC-4000 formed the strongest tablets.

Journal: 
AAPS PharmSciTech. 2001; 2(2): article 7.

The Future of Compaction Pharmaceutical Tableting in the Twenty-First Century

Currently, high-production rates and continuous production processes favor existing tableting technologies. However, if tablet development becomes rate-limiting in the future, alternative technologies may prove attractive .


For full article
Click Here

Journal: 
Pharmaceutical Technology, Jun 1, 2004 .

Sticking and picking: Some causes and remedies

Sticking occurs when granules attach themselves to the faces of tablet press punches. Picking is a more specific term that describes product sticking o­nly within the letters, logos, or designs o­n the punch faces. This article explains the causes of sticking and picking and describes the steps you can take to resolve both problems.


For full-text article
Click Here


Journal: 
Tablets&Capsules, October 2003 .

The 3-D Model: Comparison of Parameters Obtained From and by Simulating Differen

The aim of this study is to apply 3-D modeling to data obtained from different tableting machines and for different compression wheels o­n a linear rotary tableting machine replicator. A new analysis technique to interpret these data by 3-D parameter plots is presented. Tablets were produced o­n an instrumented eccentric tableting machine and o­n a linear rotary tableting machine replicator. The materials used were dicalcium phosphate dihydrate (DCPD), spray-dried lactose, microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), and theophylline monohydrate. Tableting was performed to different maximum relative densities (ρ rel, max). Force, time, and displacement were recorded during compaction. The 3-D data plots were prepared using pressure, normalized time, and porosity according to Heckel. A twisted plane was fitted to these data according to the 3-D modeling technique. The resulting parameters were analyzed in a 3-D parameter plot.

Journal: 
AAPS PharmSciTech. 2003; 4(3): article 35.

The 3-D Model: Does Time Plasticity Represent the Influence of Tableting Speed?

The objective of this study is to test the hypothesis that time plasticity (parameter d from 3-D modeling) is influenced by tableting speed. Tablets were produced at different maximum relative densities (ρrel, max) o­n an instrumented eccentric tableting machine and o­n a linear rotary tableting machine replicator. Some 3-D data plots were prepared using pressure, normalized time, and porosity according to Heckel. After fitting of a twisted plane, the resulting parameters were analyzed in a 3-D parameter plot. The materials used were dicalcium phosphate dihydrate (DCPD), spray-dried lactose, microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), κ-carrageenan (CAR), and theophylline monohydrate (TheoM). The results show that tableting speed especially influences the parameter d (time plasticity) of the 3-D model for plastically and viscoelastically deforming materials such as MCC, HPMC, CAR, and TheoM.

Journal: 
AAPS PharmSciTech. 2003; 4(4): article 66.

Slow Conformational Dynamics in the Hamster Prion Protein

Prions cause neurodegenerative diseases, such as scrapie in sheep, bovine spongiformencephalopathy (BSE) in cattle, Creutzfeldt-Jakob disease (CJD), Gerstmann-Straussler-Scheinker syndrome (GSS), fatal familial insomnia (FFI), kuru, and a new variant of CJD in humans. These diseases are associated with conversion of the normal cellular form of the prion protein (PrPC) to a pathogenic scrapie form (PrPSc), which is apparently the infectious agent in transmitted forms of the disease. The sequences of PrPSc and the noninfectious precursor PrPC are identical. Although both isoforms are chemically identical, they possess very different physicochemical properties. PrPC is substantially helical, but PrPSc has ~40% -sheet.

For full article Click Here

Journal: 
Biochemistry, March 26, 2004.

Investigation of Various Factors Affecting Encapsulation on the In-Cap Automatic

The purpose of this study was to determine the factors that influence fill weight and weight variability of capsules produced o­n the In-Cap and to assess any differences in terms of capsule defects between gelatin and HPMC (Quali-V) shells. The In-Cap is an automatic tamping type capsule-filling machine and the low output of ~3000 capsules/hour makes it ideal for early formulation development and phase I/IIa clinical supplies manufacture. Four commonly used excipients (Avicel PH101, Avicel PH302, A-Tab, and Prosolv HD90) and a poorly flowing drug blend were encapsulated at various pin settings and powder bed heights. The average fill weight and coefficient of weight variation were determined. The percentage of defective capsules formed during encapsulation was calculated. Results of the study showed that pin setting was critical for controlling the fill weight and the weight variation.

Journal: 
American Association of Pharmaceutical Scientists.

An Overview of the Effect of Moisture on Compaction and Compression

The effects of moisture o­n the flow properties, tensile strength, Heckel plot (particle rearrangement, yield pressure), energies involved in compaction (gross, plastic, and elastic energies), and elastic recovery are reviewed. The identification and quantification of the numerous parameters that affect the compaction process are vital for product uniformity. For example, moisture adsorption plays an important role in physical and chemical stability, in the properties of solid dosage forms and excipients, and in polymers for sustained-release formulations. The vapor pressure of water in the atmosphere is quantified by the percent relative humidity (% RH). The moisture content at which a solid material produces a water vapor pressure equal to that of the surrounding environment is defined as the equilibrium moisture content (EMC). The solid’s resultant weight gain at a specified temperature and % RH is expressed as a percentage of its initial dry weight.

Journal: 
Pharmaceutical Technology, Jan 2, 2005 .

Effect of Particle Size of Hydroxypropylcellulose o­n Tablet Compressibility

Hydroxypropylcellulose (HPC) is a water-soluble cellulose ether, avaiolable in a range of molecular weights and particle sizes


For full article Click Here 





Journal: 
HERCULES, Pharmaceutical Technology Report.

New Technologies Optimize Biotech Process Efficiency

The pace of biotechnology advancement has never been more rapid, with the number of biotech research centers, academic programs, and proposed manufacturing sites at an all-time high. Though biotechnology products are targeting a steadily widening range of therapeutic applications, their manufacture also entails levels of complexity previously unseen in the pharmaceutical industry. As a result of this complexity, manufacturers have their eyes squarely focused on two critical considerations: time and cost. As a result, any technology that promises to reduce one or both of these factors, without compromising product quality, is sure to gain the industry’s attention.

View Full Article

Journal: 
Pharmaceutical Technology JUNE 2004.

Direct Compression: Microcrystalline Cellulose Grade 12 versus Classic Grade 102

Because direct compression is more economic and straightforward in terms of good manufacturing practice requirements than are wet granulation and dry compaction, the pharmaceutical industry is focusing increasingly on this process. Although coarse microcrystalline cellulose (MCC) grade 12 offers outstanding flow properties, the most commonly used grade for direct compression is the well-known fine grade 102. The reason for this preference is that many users expect segregation (and subsequent poor weight- and content-uniformity results) when combining fine active ingredients with coarse-grade excipients.

View Full Article

Journal: 
Pharmaceutical Technology MAY 2002.

Optimal Tablet Press Operation: Machine versus Granulation

A tablet press is one of the most complex machines used in the manufacturing environment. Clearly defining the basic principles in tablet press operation is essential to having a successful run. Learning key factors can help to avoid the many obstacles that can interrupt a successful run. Worldwide, more than 18 different companies make tablet presses. All tablet presses operate in the same basic way with only a few exceptions. This fact allowed the industry to define and create a standard for tablet press machines and tablet press tooling, which was published in the Tablet Specification Manual (TSM) by the American Pharmaceutical Association. The TSM can be acquired through any tooling or tablet press supplier. This article discusses how tblet press performance can be optimized by clearly distinguishing between granulation and machine issues; focusing on the importance of flow, compression, and ejection; and performing the necessary maintenance and quality control checks.

Journal: 
Pharmaceutical Technology JANUARY 2002.

A Systematic Evaluation of the Compression and Tablet Characteristics of Various Types of Lactose an

According to a 1993 survey by Shangraw and Demarest, direct compression is the preferred manufacturing process for pharmaceutical tablets (1). The major characteristics of a good, directly compressible filler are physical and chemical compatibility, compactibility, flowability, lubricity,and the ability to blend uniformly with the active pharmaceutical ingredients (APIs) and other excipients. The most commonly used fillers are lactose, microcrystalline cellulose (MCC), starch, and dibasic calcium phosphate (DCP). Various types of MCC, lactose, and DCP exist with distinct differences in their particle These differences affect the compression and tablet characteristics.

View Full Article

Journal: 
Pharmaceutical Technology JUNE 2001.

Effects of Natural and Pregelantinized Sorghum, Plantain, and Corn Starch Binders on the Compression

Starch is a multipurpose excipient in tablet formulations.
It can be used as a binder, disintegrant, and filler. Natural
starches also have been pregelatinized to increase
their cold-water swellability and increase their flowability
(1). Pregelatinization can be carried out by thermal methods
(2). Although some research has been carried out on the
compressional characteristics of natural starches (3,4), little or
no research appears to have been conducted on the effect of
pregelatinization on the compressional characteristics of starches
in relation to their usefulness in tablet formulations.
Sorghum and plantain starches obtained from Sorghum bicolor
L. (poaceae) and Musa paradisiaca L. (musaceae), respectively,
have been investigated as binders and disintegrants in
tablet formulations (5,6). However, it appears that no attempt
has been made to study the effects of these starches in either

Journal: 
Pharmaceutical Technology DRUG DELIVERY 2001.

Physical Properties and Compact Analysis of Commonly used Direct Compression Binders

This
study investigated the basic physico-chemical property and binding
functionality of commonly used commercial direct compression
binders/fillers. The compressibility of these materials was also
analyzed using compression parameters derived from the Heckel,
Kawakita, and Cooper-Eaton equations. Five classes of excipients were
evaluated, including microcrystalline cellulose (MCC), starch, lactose,
dicalcium phosphate (DCP), and sugar. In general, the starch category
exhibited the highest moisture content followed by MCC, DCP, lactose,
and finally sugar; DCP displayed the highest density, followed by
sugar, lactose, starch, and MCC; the material particle size is highly
processing dependent. The data also demonstrated that MCC had moderate
flowability, excellent compressibility, and extremely good compact
hardness; with some exceptions, starch, lactose, and sugar generally
exhibited moderate flowability, compressibility, and hardness; DCP had

Journal: 
AAPS PharmSciTech.2003; 4(4):article 62.

Compression, Compaction, and Disintegration Properties of Low Crystallinity Celluloses Produced

The tabletting characteristics of low crystallinity celluloses (LCPC)-LCPC-700, LCPC-2000, and LCPC-4000-prepared using agitation rates of 700, 2000, and 4000 rpm, respectively, during their regeneration from phosphoric acid, were evaluated and compared with those of Avicel PH-102 and Avicel PH-302. The mean deformation pressure values calculated from the linear region of the Athy-Heckel curves indicated LCPC-4000 to be the most ductile material. The area under the Athy-Heckel curve for LCPC-4000 was 330 MPa, whereas LCPC-700 and LCPC-2000 showed a corresponding value similar to that of Avicel PH-102 and Avicel PH-302 (192-232 MPa). The tensile strength of LCPC and Avicel compacts increased linearly with increasing applied pressures. A comparison of the area under the tensile strength-compression pressure curves indicated that LCPC-4000 formed the strongest tablets.

Journal: 
AAPS PharmSciTech. 2001; 2(2):article 7.

Evolutions in Direct Compression

very solid-dose formulation team starts out aiming for a direct-compression tablet. It’s the most straightforward, easiest to control, and least expensive manufacturing option. Direct compression, of course, uses two primary process steps, mixing and compression, to produce the finished tablet.Wet granulation adds five more operations: wet granulation, wet milling, drying, milling, and mixing again.

Each additional step requires equipment, operators, space, power, and expense…and every step lowers the yield and increases the risk of out-of-specification product. So the most attractive solution almost always is the familiar, undramatic standby, direct compression. “The basic tablet press has been fill, compress, and eject since about 1875,” says a veteran equipment marketer. “Ever since then, it’s been a matter of how do you control it better and now how do you clean it better.”

Journal: 
Pharmaceutical Technology, Apr 2, 2005.

Compression and Mechanical Properties of Tablet Formulations

Starch is one of the most widely used excipients in the manufacture of solid dosage forms. Researchers have tried to develop botanical starches for use as binders and disintegrants in tablet formulations (1–5). For example, sweet potato and cocoyam starches have shown potential as binding agents and/or disintegrants in tablet formulations (3, 6). The effects of these starches on compressional characteristics of the tablets and mechanical properties, however, have not been investigated. In this article, the effects of sweet potato and cocoyam starches on a paracetamol tablet formulation’s compressional characteristics and mechanical properties are compared with those of official cornstarch BP grade. The tablets’ compressional characteristics were studied using density measurements and the Heckel and Kawakita equations (7–9).

Journal: 
Pharmaceutical Technology, Apr 2, 2005

Evaluation of a New Coprocessed Compound Based on Lactose and Maize Starch for Tablet Formulation

The development of new direct compression excipients should include a comprehensive and rapid determination of deformation properties. The aim of this study was to characterize StarLac, a new coprocessed compound for direct compression based on lactose and maize starch. For this purpose, the effects of the base materials (maize starch and spray-dried lactose) were considered and the influence of the spray-drying process was investigated. This was performed by comparing the physical mixture of starch and spray-dried lactose at the same ratio as for StarLac. For analysis of the deformation behavior, the 3-D model and the Walker equation were applied; for verification, the Heckel equation and the pressure time function (a modified Weibull equation) were used.

Journal: 
AAPS PharmSci. 2004; 6 (2): article 16.