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Question

Posted on: January 18 2016

Problem with suppositories with lidocaine HCl and Triamcinolone acetonide

We try to make Trian after a stock break. After adding lidocaine HCl to the melted adeps solidus, the powder becomes viscous/sticky. The suppositories are not homogeneous and cannot be poured.

Answer

What contains triosuppositories:   The active substances are:   1 suppository contains: Triamcinolonacetonid 0.50 mg – Lidocaine Chlorhydrate 50 mg.

Other ingredients (excipients) are: Medium chain triglycerides – solid fat.  

for 20 suppositories this gives 10 mg triamcinolone acetonide or 100 mg trituration 1 in 10. Clearly insufficient to obtain a homogeneous distribution! We should be using lactose, about 750 mg per suppository being 15 g for 20 suppositories. Vann lidocaïneHCl you need 1g; Also insufficient to obtain a homogeneous distribution.  

Bring in a small smooth mortar 1 g lactose and rub it open to close the pores of the mortar. Add 100 mg Triam trituration and mix to homogenous and then add 1 g of lidocaïneHCl and mix to homogenous. Dilute this mixture with 14 g of lactose according to the rules of the art.   In Total We then have 16 g of mass multiplied by displacement factor   0.7 = 11.2 g powder. In   Assuming that the calibration value of your suppository form = 2 G, then you need 40 g-11.2 g = 28.8 suppository Mass. Melt that mass in a brewing pan at low temperature and slowly mix under stir the powder mass in the small mortar with the melted suppository mass. Transfer the contents of the mortar into the zetpilpan and, if necessary, heat slightly to the liquid. Pour under stir well the melted mass into the suppository form.    

The calculations were performed for 20 suppositories but it is consulted to count for 21 suppositories.  

Note: I see in the composition of triolic resource chain triglycerides or Miglyol mentioned. Apparently the company rubs the powders with Miglyol oil. I suspect that lidocaïneHCl may dissolve in this oil and therefore your problem does not occur?  

But the addition of oil will lead to a lowering of the STOL point and solving this problem is also not easy.