I am trying to make a tablet formula for an active ingredient with a very light and airy structure, similar to fumed silicon dioxide. My constraints are that the tablet needs to be small with as high a percentage of active ingredient as possible.
I have tried several formulations using microcrystalline cellulose and dicalcium phosphate, but the issue is that the tablet comes out too soft. Using any reasonable amount of active ingredient (reasonable meaning greater than 20%) I can crack the tablet in half with my fingernail. The mixture is ultimately too light, and I physically can not put enough powder into the well of my tablet press in order to get a good, solid compression.
Is there any excipient I can add or any technique I can use that will create a good tablet in this instance?
First you should try dry granulation, than wet granulation as mentioned above. My personal tip is: 60:40 linear random copolymer of N-vinyl-2-pyrrolidone and vinyl acetate, eg. Plasdone S-630 (1 - 3 %) and ethanol (0,5 - 1,5 %) which is used immedialy before tabletting as spray - so you press wet mixture (in case using 3 % of Plasdone S-630, you have to use 1,5 % of ethanol). Then let me know, how it works.
why dont you try dry-granulation technique??
beside that you have to check the % of the binder being used
Use wet granulation process with starch+pvp-30+gelatin paste as a binder, will give you excellent hardness. try hard granulation.
You can use also DCP, Lactose which give you good hardness at low compression force.
you can also choose co processed excipients, a bit expensive.
The best solution is Top spray granulation process using Fluid Bed Processor. Disperse / dissolve the API in SLS-Water. The mixture is sprayed over / adhered to LUDIPRESS. The granulated mixture is suitably milled or sieved through #25 ASTM sieve and finally lubricate with 0.75% Mg Stearate and compress into tablets. LUDIPRESS is a multifunctional excipient of BASF where the compressibility, binding, disintegration and flow are optimal. The use of SLS-Water is to prevent the loss of API, ease of dispersibility / dissolution and complete tranfer from vessel to FBP bowl.
I developed a similar tablet formula with an API that had a lower bulk density/like aresoil and I had a similar issue, the final mixture was too light and not necessary I was obtaining good hardness besides the powder flowability was causing high mass variation during the compression process.
You need to verify your API characteristics and select the suitable manufacturing process according to its physicochemical and mechanical properties if your API has good plastic compaction dry granulation will be an option if you employ a high dilution excipient as MCC, SMCC or spray-dried lactose, also adding a little percentage of aerosil/syloid will improve your hardness because this will increase the points of the solid bridges during the dry granulation, another important point in dry granulation it's to select your dry binder, I highly recommend you to employ a polymer with small particle size and good plastic compaction properties as low viscosity HPM (Klucel), Copovidone (Kollidon VA64 Fine) or Avicel PH105.
On the other hand, not always dry granulation is the better option, especially if you are trying to obtaining good hardness and small tablets due to during the dry granulation your powder will decrease its limit or compaction whether for plastic or fragmentation behaviour. In my case I resolved the problem by wet granulation, you must select the correct wet binder to confer great plastic properties to your granules, try SMCC(prosolv 50) as a diluent for wet granulation due to it will conserve better compaction than just MCC after the wet granulation process. binders wet granulation: HPMC(Methocel E15 and E50), HPC, PVP, PEG. The use of a suitable binder will resolve your problem. You can also add spray-dried lactose or avicel 200 in the extragranular.
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