Tablets & Capsules


Issue link:

Contents of this Issue


Page 52 of 67

Tablets & Capsules October 2019 43 s h o u ld b e f r e e -f l ow i n g, i n e r t, and compressible. Additionally, it should have a reproducible, nar- row particle size distribution, high dilution potential, and good com- pactability. Finally, it should also contribute to the tablet's microbi- ological, chemical, and mechanical stability. Currently marketed DC filler-binders provide most of these key attributes; however, depending on the nature and dose of the API, high dilution potential and good compactability remain challenging. T his ar ticle describes a st udy that used piroxicam to compare the compactability, disintegration, fri- ability, and dissolution profiles of three different DC filler-binders. The study also looked at whether for mulators could improve these prof iles by adding a d r y binder to a DC blend. Finally, the study tested the dry binders' capacity to improve a high-dose tablet formu- lation of natural calcium carbonate. Effect of dry binders in medium- dose DC formulations The study tested three DC fill- er-binders based on either micro- cr ystalline cellulose (MCC), lac- t o s e, o r d i c a l c i u m p h o s p h a t e under intellectual property protec- tion of excipient manufacturers, so they can be more expensive and harder to replace. Filler-binders have a consider- able impact on the tableting prop- er ties of low- and medium-dose tablet for mulations. Table 1 lists some examples of currently mar- keted DC filler-binders along with the composition, manufact ur ing method, and general properties of each. An optimal DC filler-binder ing in acceptance and use since the 1960s, when the first excipi- ents suitable for DC tableting were developed [2]. Figure 1 shows the manufacturing steps of the differ- ent tablet manufacturing processes and enu me r ate s the advant a ge s and disadvantages of DC tableting. T he advantages of DC tableting are well known [3]. Since it elim- inates several steps in the tablet manufacturing process, DC tablet- ing r ed uce s c apit al inve st ment, for mulation work, and manufac- t uring costs. Moreover, avoiding the granulation step may help to increase a drug product's stability and improve its dissolution profile. However, a DC process requires DC excipients, which may pres- e nt c e r t a in d is ad v a nt a g e s . F or instance, using DC excipients can increase the risk of segregation due to larger differences in particle size distribution between such excipi- ents and many active pharmaceu- tical ing redients (A PIs). In addi- tion, DC excipients are often less compactable than their non-DC versions, so tableting can be more challenging and the product's dilu- tion potential may be reduced [4]. Finally, DC excipients are usually Method Composition Ingredient type Material properties Spray drying Lactose monohydrate Spray-dried lactose Uniform size, spherical shape, good flow, low compactability, brittle deformation, reducing sugars Sieving (and/or milling) Dicalcium phosphate Dicalcium phosphate anhydrous Good flow, good compactability, non-hygroscopic, prone to capping, deformation by fragmentation, alkaline residues Co-drying Microcrystalline cellulose Colloidal silicon dioxide Silicified microcrystalline cellulose Good flow, good compactability, plastic deformation, incompatible with strong oxidizing agents Spray drying Lactose Microcrystalline cellulose Lactose monohydrate, and microcrystalline cellulose Superior flow and binding properties, plastic- brittle deformation, reducing sugars, incompatible with strong oxidizing agents Spray drying Lactose monohydrate Starch Lactose monohydrate and corn starch Good compactability, good flow, good disintegration, elastic-brittle deformation, reducing sugars, hygroscopic Table 1 Examples of DC filler-binders Since it eliminates several steps in the tablet manufacturing process, DC tableting reduces capital investment, formulation work, and manufacturing costs.

Articles in this issue

Archives of this issue

view archives of Tablets & Capsules - TC1019