Magnesium Stearate Fatty Acid Composition, Lubrication Performance and Tablet Properties.

Magnesium stearate (MgSt) is a common tablet lubricant. As variations in MgSt properties are known to influence tablet attributes, the impact of MgSt fatty acid composition, particularly the significance of the stearate and palmitate contents, and its effects on tablet properties warrant further investigation. This study investigated the effect of MgSt with different stearate and palmitate contents but comparable physical properties (e.

Functionality of wet-granulated disintegrant in comparison to directly incorporated disintegrant in a poorly water-soluble tablet matrix.

Tablet disintegration is crucial for drug release and subsequent systemic absorption. Although factors affecting the disintegrant's functionality have been extensively studied, the impact of wet granulation on the performance of disintegrants in a poorly water-soluble matrix has received much less attention. In this study, the disintegrants, crospovidone (XPVP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), were wet-granulated with dibasic calcium phosphate dihydrate as the poorly water-soluble matrix and polyvinylpyrrolidone as the binder.

Influence of talc and hydrogenated castor oil on the dissolution behavior of metformin-loaded pellets with acrylic-based sustained release coating.

Multi-unit pellet system (MUPS) is of great interest as it is amenable to customization. MUPS comprises multi-particulates, usually as pellets or spheroids, which can be coated with diffusion barrier coatings. One commonly used diffusion barrier coating is the methacrylic acid copolymer, which can be used as a taste masking, enteric or sustained release polymer.

Surface Modification of lactose carrier particles using a fluid bed coater to improve fine particle fraction for dry powder inhalers.

Surface roughness of carrier particles can impact dry powder inhaler (DPI) performance. There are opposing views on the effect of roughness on DPI performance. Hence, a systematic approach is needed to modify carrier surfaces and evaluate the impact on drug delivery.

Alginate-based matrix tablets for drug delivery.

Introduction: As a nature-derived polymer with swelling and gelling properties, alginate has found wide biopharma-relevant applications. However, there is comparatively limited attention on alginate in tablet formulations. Therefore, this review aimed to provide an overview of the applications of alginate in solid dosage form formulations.

Relative Humidity Cycling: Implications on the Stability of Moisture-Sensitive Drugs in Solid Pharmaceutical Products.

The stability of a moisture-sensitive drug in tablet formulations depends particularly on the environment's relative humidity (RH) and the products' prior exposure to moisture. This study was designed to understand drug stability in relation to the moisture interaction of the excipients, moisture history of the tablets, and RH of the environment. The stability study was performed on tablets containing acetylsalicylic acid (ASA), formulated with common pharmaceutical excipients like native maize starch, microcrystalline cellulose (MCC), partially pregelatinized maize starch (PGS), dicalcium phosphate dihydrate (DCP), lactose, and mannitol.

Ensuring Product Stability - Choosing the Right Excipients.

The stability of pharmaceuticals is an important product quality attribute. Of the known factors affecting stability, moisture is often perceived as the most common cause of drug degradation by hydrolysis or other reactions facilitated by moisture as a medium. Excipients are a critical entity in formulations to enable drug delivery as well as efficient manufacture of pharmaceutical dosage forms.

Impact of Amylose-Amylopectin Ratio of Starches on the Mechanical Strength and Stability of Acetylsalicylic Acid Tablets.

The two main components of starch - amylose and amylopectin, are responsible for its interaction with moisture. This study investigated how moisture sorption properties of the starches with different amylose-amylopectin ratio impacted tablet properties including drug stability. The starch samples were equilibrated to 33, 53, and 75% relative humidity (RH) and then assessed for tabletability, compactibility, and yield pressure.

Investigation on the impact of different proportions of components in formulations on stability of a moisture sensitive drug.

Physicochemical and mechanical properties of tablets are largely dictated by formulation compositions. Different excipients possess different tableting and moisture sorption behaviors. Therefore, this study was designed to elucidate the relative influence of the proportion of components in formulations on tablet properties.

Insights into the Moisture Scavenging Properties of Different Types of Starch in Tablets Containing a Moisture-Sensitive Drug.

Starch is a commonly used excipient in the pharmaceutical industry. However, information on the effect of the moisture scavenging properties of starch to protect moisture-sensitive drugs is limited. The interaction between starch and moisture is of particular interest as moisture fugacity can impact drug stability.

Insights on the role of excipients and tablet matrix porosity on aspirin stability.

Excipient-moisture interaction can be a critical attribute in determination of product stability. This study aimed to investigate influence of integrating excipients having different moisture interaction into moisture sensitive drug formulations. Aspirin was formulated with maize starch (MS), microcrystalline cellulose (MCC) and calcium hydrogen phosphate dihydrate (DCP).

Impact of die wall material on the mechanical properties of paracetamol tablets.

Tablet quality can be affected by material, configuration and design of the tooling which comprise punches and dies. Much research attention had centred around punches, with very little reported on the dies. Dies with modified bore lining materials or inserts are available for special applications.

Investigation on the effect of roller compaction on paracetamol.

Roller compaction is a popular dry granulation method that has been associated with loss of tabletability. In this study, the effect of roller compaction on a model brittle elastic material, paracetamol, was examined. Roller compaction of paracetamol was carried out at three roll force to examine the effects of roll force on the tablet compaction properties.

Effects of Particle Surface Roughness on In-Die Flow and Tableting Behavior of Lactose.

Particle rearrangement takes place during the initial phase of tablet compaction. In this study, rough lactose particles were prepared by roller compaction, and their surface roughness modified by partial surface dissolution using a fluidized bed processor. Flow characteristics of the particles were determined using various flow methods, and their compaction characteristics studied using a compaction simulator with punches of different geometry and compaction pressure.

Influence of spray nozzle aperture during high shear wet granulation on granule properties and its compression attributes.

The distribution of granulating liquid is known to affect the high shear wet granulation process but the impact of the spray nozzle attributes is still unclear. While homogenous liquid distribution can be achieved by using a spray nozzle, the effect of different nozzle aperture sizes on granule properties is not well understood. In this study, nozzles of different aperture sizes were used to introduce the granulating liquid in high shear wet granulation using different process parameters.

Investigation on the impact of powder arching in small die filling.

The flow of particulate materials is critical during processes such as mixing, compression and packing. Non-cohesive arching, a feature characteristic of coarse and free-flowing particles, has been studied extensively for silos and hoppers. However, the arching of powders during die fill has received much less attention.

Comparative evaluation of powder flow parameters with reference to particle size and shape.

Powder flow is critical to the success of various pharmaceutical processes such as tableting and capsule filling. Despite a plethora of flow characterisation techniques and parameters available, powder flow still remains to be a not well understood subject. Inter-relationships between the various powder flow parameters in particular have not been well established.

Dissolution of fine particle fraction from truncated Anderson cascade impactor with an enhancer cell.

Dissolution testing for inhalers were previously conducted either on unfractionated drug-carrier powders or drug of specific aerodynamic particle size. In this study, the collection of the full fine particle fraction (FPF) was attempted on a single stage. Capsules containing 30 mg of 2% salbutamol sulfate (SS) was tested to have a FPF of 9 ± 1% using the full set of Andersen cascade impactor (ACI) and a modified Rotahaler® capable of achieving 4.

Equilibria, kinetics and mechanism for the degradation of the cytotoxic compound L-N-nitroarginine.

L-N-nitroarginine (LNNA), an analog of L-arginine, is a competitive inhibitor of nitric oxide synthase which causes the selective reduction of blood flow to tumor cells. Despite the potential of LNNA to function as an adjuvant in cancer therapies, its poor solubility and stability have hindered the development of an injectable formulation of LNNA that is suitable for human administration. This work, for the first time, details a systematic study on the determination of equilibrium K constants and the rate law of LNNA degradation.

Understanding die fill variation during mini-tablet production.

Reproducibility of die fill during tablet production is critical to ensure consistent tablet drug content and mechanical attributes. In the production of mini-tablets, tablets smaller than 6mm, achievement of uniform die fill is much more challenging. Powder flow is often associated with die fill accuracy but this relationship has not been well characterised especially for mini-tablets.

Tablet compression tooling - Impact of punch face edge modification.

The influence of punch face edge geometry modification on tablet compression and the properties of the resultant tablets produced on a rotary press were investigated. The results revealed that tablets produced from the punches with radius edge face geometry consistently displayed better physical quality; higher tensile strength and lower capping tendency. Modification of the angled edge of the bevel face to the curved edge of the radius face, enabled deeper punch penetration in the die cavity during the compression cycle, bringing about greater compact densification.

Powder Flow Testing: Judicious Choice of Test Methods.

Flow property of pharmaceutical powders can be assessed by various flow testers and test methods. In this study, eight commercially available lactose grades were sourced and tested for angles of repose, tapping studies, shear cell measurements, stirred powder rheometry, and avalanching powder measurements. The relationships between various flow parameters and particle size were analyzed.

Review of Disintegrants and the Disintegration Phenomena.

Disintegrant is one of the most important components in a typical tablet dosage form. It is responsible for ensuring the break-up of the tablet matrix upon ingestion. Disintegrants act by different mechanisms, and a number of factors may affect their performance.