Benghuzzi H A, England B G, Bajpai P K
Department of Pathology, University of Michigan Medical School, Ann Arbor 48109.
Biomed Sci Instrum. 1991;27:197-203.
Several researchers have reported that there are drawbacks in using the current pharmacotherapeutic procedure for the treatment of endocrine insufficiency. Furthermore, such drugs have to be taken on a lifelong basis. Also, long term exposure to drugs seems to be necessary in the treatment of the most common endocrine disorders. Thus, the traditional routes of administration expose the body constantly to large fluctuating levels of drugs. This study presents a possible alternative route of administering the drugs for the treatment of the aforementioned cases. Ceramics, such as, tricalcium phosphate (TCP) have been used extensively in the dental and orthopedic fields. To date, the use of compressed TCP ceramic capsules as drug delivery systems has not been investigated. The objective of this study is to investigate the capability of calcined TCP amino acid-steroid matrix to deliver progesterone (P), in a sustained manner. Microcrystals of TCP were prepared by following standard laboratory procedures. Three different amino acids (cysteine, proline, and lysine) were incorporated (individually or in combination form) into the TCP matrix. Each matrix contained 100 mg of P and the homogeneous material was compressed at 5000 Kg compression load using a French Pressure Cell. The total amount of steroid released was monitored spectrophotometrically. The results of this study suggest that: (i) TCP- amino acid-steroid composites can be used to deliver steroids in a sustained manner. (ii) The amount of steroid released from the matrix system was found to be dependent upon the physiochemical characteristics of the amino acids.(ABSTRACT TRUNCATED AT 250 WORDS)
几位研究人员报告称,目前用于治疗内分泌功能不全的药物治疗方法存在缺陷。此外,此类药物必须终身服用。而且,在治疗最常见的内分泌疾病时,似乎有必要长期使用药物。因此,传统给药途径会使身体持续暴露于大幅波动的高药物水平中。本研究提出了一种针对上述病例给药的可能替代途径。陶瓷,如磷酸三钙(TCP),已在牙科和骨科领域广泛应用。迄今为止,尚未对压缩TCP陶瓷胶囊作为药物递送系统的用途进行研究。本研究的目的是研究煅烧TCP氨基酸 - 类固醇基质持续递送孕酮(P)的能力。按照标准实验室程序制备TCP微晶。将三种不同的氨基酸(半胱氨酸、脯氨酸和赖氨酸)单独或组合形式掺入TCP基质中。每个基质含有100毫克P,使用法国压力细胞在5000千克压缩负荷下将均匀材料压缩。通过分光光度法监测释放的类固醇总量。本研究结果表明:(i)TCP - 氨基酸 - 类固醇复合材料可用于持续递送类固醇。(ii)发现从基质系统释放的类固醇量取决于氨基酸的物理化学特性。(摘要截于250字)