The influence of superdisintegrant choice on the rate of drug dissolution - Pharmaceutical Technology

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The influence of superdisintegrant choice on the rate of drug dissolution


Pharmaceutical Technology Europe
Volume 21, Issue 9

Even though the superdisintegrants gave similar disintegration results, the choice of superdisintegrant had a significant impact on drug dissolution.

As the discriminating media showed even greater differences in dissolution rate between the superdisintegrants studied, the discriminating media were highly effective at identifying differences between superdisintegrants selected.


The author says...
For the most poorly soluble drugs, crospovidone Type B was often the only superdisintegrant to yield a formulation achieving 80% drug release in the discriminating media. Overall, the results suggest that crospovidone Type B, which has a solvent-like chemistry and a high surface area resulting in high interfacial activity, is more effective at enhancing the dissolution rate of poorly soluble drugs.

Conclusion

At a time when formulators are faced with increasing numbers of poorly soluble drugs, it is very important to select superdisintegrants that maximize drug dissolution.

A comprehensive study conducted to evaluate the impact of crospovidone, croscarmellose sodium and sodium starch glycolate on the dissolution rates of poorly soluble drugs with varying aqueous solubility showed that crospovidone Type B provided the fastest rate of dissolution. The fact that tablet strength and disintegration times for the tablets containing each drug and all the superdisintegrants' studies were similar showed that tablet hardness and disintegration did not influence study results. Crospovidone Type B has unique chemistry, particle size and particle morphology that result in high interfacial activity, which significantly aid dissolution.

Jagdish Balasubramaniam is Manager, Pharmaceutical R&D, at International Specialty Products Pvt Ltd (India).

Tim Bee is Senior Director, Pharmaceuticals, at International Specialty Products (NJ, USA). Tel. +1 973 628 4148

References

1. J.R. Johnson et al., J. Pharm. Sci., 80(5), 469–471 (1991).

2. J.K. Pandit, M.K. Tripathi and R.J. Babu, Pharmazie, 52(7), 538–540 (1997).

3. A. Sakr, M. Bose and A. Menon, Pharm. Ind., 55(10), 953–957 (1993).

4. US Pharmacopeia, USP 31–NF 26 (2008).

5. S.A. Qureshi, Dissolution Technologies, 13(4), 18–23 (2006)


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