To improve disintegration for Microcrystalline cellulose (Grade preferably Avicel pH 101, bearing 50micron size) we can use Polyplasdone XL 10 (Crospovidone). Crospovidone is a synthetic water insoluble cross-linked homopolymer of N-vinyl-2-pyrrolidone. It is available in several grades differing mainly in the particle size, for example Polyplasdone® XL is a coarser grade while Polyplasdone® XL-10 and Polyplasdone® INF-10 are finer grades. It is commonly used as a disintegrant at a concentration ranging from 2–5% in solid dosage forms. Drug can be triturated with Polyplasdone XL 10 and physical interaction, if any must be evaluated using DSC or other suitable means. Polyplasdone XL 10 is better extrusion–spheronisation aid itself if used compared to Avicel® PH101 since it gave pellets with narrower particle size distribution, faster extrusion and spheronisation rates and a smoother surface. However, it can be tried along with MCC in trial proportions to get ambient results in case MCC is mandatorily required in the formulation. In case of BCS II drugs specifically, the requirements and targets are to be identified to define correct approach. For instance, is the drug required for sustained or immediate release profile etc. We can discuss this further if required. Please find an article for the statements I gave on http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2902318/.
I agree with you but why crospovidone can be used. Why not croscarmellose sodium. Secondly Microcrystalline cellulose is a known binding agent that make it satisfied for pellets in addition to the pellet disintegration is not required if pellets are used for sustained drug release. However, in cases of enteric coated pellets, the rapid disintegration of pellets is required to achieve a good therapeutic response. Also, the addition of hydrophilic polymers like PEG 400 or surfactants like polysorbate 80 can be advantageous. This is due to the channelling effect obtained with these polymers that cause high pore structure during wetting with water. If superdisintegrant like Crospovidone or croscarmellose sodium is added the swelling capability can be high.
If drug like BCS class II is tried in MCC pellets, the dissolution rate can be low. This may be due to the shrinkage of MCC pellets during drying process that leads to less porous structure. However, incorporation of PEG 400 as pore forming agent or surfactant in these MCC pellets can lead to higher dissolution rates that may be due to the porous structure caused by PEG 400. This with polysorbate 80 can act as dissolution enhancers in the dissolution medium leading to enhanced dissolution rate. You can find details in attached paper. I wait you for further discussion.
Article Novel disintegrating microcrystalline cellulose pellets with...
Dear Ramy!
Pl improve the clarity of the problem. Are these API loaded MCC pellets? Probably yes... Then what is the API BCS class, what is the therapeutic goal, what is the required drug release profile & so on?
Good luck!
-SSPoddar PhD.
Sodium starch glycolate with avicel pH 102 is the best combination to improve disintegration time of pellets.If you use providone as a binder for pelleting than it will be tough to disintegrate. HPMC 5 or 15 cps is the best binder in this case.
Hello all
I am trying to make gastroretentive pellets of the metronidazole. However I have problems in achieving a sustained release. The release I have been getting is immediate. I am making 200mg of metronidazole in a 500mg dosage form. I am using a kenwood mixer to granulate and extrusion spheronizer. Is there any excipients that you could suggest to retard the release. I have tried eudragit all the grades. I used hpmc but it tends to stick with the granulating fluid. Please could any one suggest excipients i may use
Hello all
I am also trying to make pellets of Famciclovir 250mg. Its an orodispersible formulation in which the pellets should dissolve in Stomach. The total weight of the tablet should not be more than 800mg. Can anyone suggest what are the extrusion aids and binder combinations for this product.
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