Development of Non-Oral Type Sustained Release Formulation for Pain Control

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The purpose of this study was the development to formulate the sustained release analgesia to cancer pain management, which is suitable to condition and disease state of the patient. We produced self-setting hydroxyapatite-cement pharmaceutical formulation using hydroxyapatite noticed recently. Non-oral type sustained release formulation contained the pentazocine with the action of being excellent for cancer related pain, and we obtained following results.(1) In order to keep the elution of PTZ from the pharmaceutical formulation, we examined the compressive strength of the hydroxyapatite-cement pharmaceutical formulation and the elution of PTZ from hydroxyapatite cement. Under prescription of the hydroxyapatite cement as a seed crystal, the quantity of crystal hydroxyapatite was added 20-40 % to prepare the compressive strength of the PTZ-loaded hydroxyapatite-cement pharmaceutical formulation. Increasing the dosage of the hydroxyapatite as seed crystal, we found that the compressive … More strength of the PTZ-loaded pharmaceutical formulation decreased from 4.24 to 1.58 Mpa. Moreover, it was found that the dissolution rate of PTZ from this pharmaceutical formulation increased 299.71 to 197.47 ng/mL/hr by increasing the dosage of the hydroxyapatite as seed crystal. From these results, the dissolution rate of PTZ from the self-setting hydroxyapatite-cement pharmaceutical formulation could be controlled clearly.(2) We investigated the relationship between blood and brain concentration and the analgesic effect of PTZ after the subcutaneous implantation of the self-setting hydroxyapatite-cement pharmaceutical formulation to the rat. In the PTZ-loaded pharmaceutical formulation in this study, it was confirmed that the blood concentration continued by 96 hours, when PTZ of the same quantity was administered by the hydroxyapatite-cement pharmaceutical formulation and subcutaneous injection. MRT in the pharmacokinetic parameter of the PTZ-loaded pharmaceutical formulation, was 1.8-times of the subcutaneous injection of PTZ solution. We found out that the bran concentration of PTZ increased after the administration of the PTZ-loaded pharmaceutical formulation comparing the subcutaneous injection, It was clarified that the duration of analgesic effect of PTZ after the implantation of the PTZ-loaded pharmaceutical formulation was kept over 8-folds hours of the subcutaneous injection. Less