Abstract
With the aim of developing a dosage form for the treatment of carcinoma colli, stick-like preparations containing bleomycin hydrochloride (BLM), carboquone (CQ), and 5-fluoro-uracil (5-FU) held in a mixture of hydroxypropyl cellulose (HPC) and Carbopol 934 (CP) were prepared and clinically tested in volunteers suffering from carcinoma colli after various in vitro tests. The results of preliminary tests of drug release using the agar gelbed method indicated that the addition of sodium lauryl sulfate enhanced the release of CQ, but the effect was not very great. Therefore, in order to enhance the release of CQ, the contents of HPC in the base and CQ were increased. The preparations of BLM and 5-FU of 2 mm diameter showed faster drug release than those of 4 mm diameter according to the Kerami filter method. In the preparations of 4 mm diameter, the release of CQ took place at almost the same rate as that of BLM, i. e., about 40% within 24 hr, due to the modification of the formula for the preparation of CQ. In the case of the preparation of 5-FU, the release was so rapid that about 100% of the drug was released within 24 hr. The present Kerami filter method seemed suitable and convenient for measuring the drug release from the present dosage forms. Clinical examination indicated the stick-like shape of the present dosage form to be favorable for the treatment of foci in the cervical canal. A high percentage of complete disappearance of the cancerous focus was obtained for patients of stage 0 in the cases of BLM and 5-FU, and a similar result was obtained for stage Ia in the case of CQ.
