PubMed · 5244371
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F Gstirner, J Bolten. 1968. [On ointment bases from triglycerides].. https://doi.org/10.1002/ardp.19683010102
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We discuss here the effect of water-insoluble pharmaceutical aids on the nature of drug release from composite polymeric prodrugs synthesized by mechanochemical solid-state polymerization. Magnesium stearate (Mgst) and hydrogen castor oil (HCO) were used as water-insoluble pharmaceutical aids. Composite polymeric prodrugs were synthesized by the mechanochemical solid-state polymerization of a vinyl monomer of 5-fluorouracil (I) in the presence of Mgst or HCO. The molecular weight of the resulting polymeric prodrugs increased with increasing the content of Mgst or HCO. Prodrug hydrolysis was carried out in a heterogeneous system in phosphate buffer at pH 6.8 and 37 degrees C. The rate of drug release from the composite polymeric prodrug containing Mgst (Poly-Mgst) was faster than that from polymeric prodrug containing no pharmaceutical aids (Poly-Non), while hydrolysis of the composite polymeric prodrug containing HCO (Poly-HCO) was slower than Poly-Non. Scanning electron microscope (SEM) photos showed the surface of Poly-HCO was smoother than that of Poly-Non and Poly-Mgst. It was suggested that the slower drug release from Poly-HCO may be responsible for the smaller specific surface area than that of Poly-Non. It was also shown that the rate of drug release from the composite polymeric prodrugs decreases with increasing the content of Mgst or HCO. Hence, novel composite polymeric prodrugs with a variety of drug release rates can be prepared by mechanochemical solid-state polymerization in a totally dry process.
The present paper evaluated the tensile strength of tablets made from the dry binder Prosolv SMCC 90 and the influence of three concentrations of the lubricant magnesium stearate on the tensile strength of tablets manufactured from this material. The results were compared with the same evaluation in Avicel PH 102. The tested concentrations of the stearate were 0.4, 0.8 and 1.2%. The tablets were compressed by three press powers (3, 3.5, and 4 kN). On the basis of obtained results it can be stated that under the same press powers Prosolv SMCC 90 alone yields stronger compacts than Avicel PH 102. From the viewpoint of decreased strength of compacts by adding magnesium stearate, the dry binder Prosolv SMCC 90 is much less sensitive than Avicel PH 102. In Avicel PH 102 a marked decrease in tensile strength was recorded with an addition of 0.4%, which was not observed with Prosolv SMCC90. A more significant decrease in the strength of compacts was shown by the substance not until a stearate concentration of 0.8%. The highest employed stearate concentration of 1.2% decreases the tensile strength of tablets made from Prosolv SMCC 90 in the press powers of 3.5 and 4 kN two times less than the tensile strength of the compacts from Avicel PH 102.
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