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基于储存库的药物递送系统用于抑郁症的管理。

Depot based drug delivery system for the management of depression.

机构信息

VNS Institute of Pharmacy, Vidhya Vihar, Neelbud, Bhopal-463094(MP), India.

出版信息

Curr Drug Deliv. 2011 Sep;8(5):483-93. doi: 10.2174/156720111796642309.

Abstract

Depression is a common mental disorder discerns with depressed mood, loss of interest, the primary treatment methods are drug therapy, electroconvulsive therapy, psychotherapy, light therapy, vagus nerve stimulation, etc. A number of innovative delivery systems have been developed to address suboptimal therapy outcomes by enhancing drug delivery, assuring efficacy of treatment, reducing side effects, improving compliance and drug targeting specific locations resulting in a higher efficiency. Depot delivery offers the advantage of a very high loading, controlled release of drug for an extended period of time and reduces frequency of dosing. The increase in AUC and decrease in Cmax reflects that the depot formulations could reduce the toxic complications and limitations of conventional and oral therapies. Products at preclinical and clinical stages include formulations of naltrexone and buprenorphine for alcoholism/drug abuse, GLP-1 peptides for diabetes, r-hFSH for fertility, dopamine for nerve growth, dexamethasone for ocular treatment, melanotan for cancer prevention, plasmid DNA for cancer prevention, a variety of vaccines, octreotide generics, etc. Most depot formulations are comprised of biodegradable polymer-excipients that control the rate of drug release and resorbs during/after drug release. The major advantage of depot antipsychotics over oral medication was facilitation of compliance in medication taking. One class of biodegradable polymers that has gained wide acceptance and still attractive today is lactide/glycolide polymers. The greatest advantage of these degradable polymers is that they are broken down into biologically acceptable molecules that are metabolized and removed from the body via normal metabolic pathways. This versatile delivery system offers the advantage of a very high loading and controlled release of various drug for an extended period of time compared with plain delivery system. New formulations of depression can offer advantages over older formulations in terms of convenience, side effect profiles, efficacy, and/or a fast onset of action.

摘要

抑郁症是一种常见的精神障碍,其特征是情绪低落、兴趣丧失。主要治疗方法有药物治疗、电惊厥治疗、心理治疗、光疗、迷走神经刺激等。为了改善治疗效果,提高药物的靶向性,减少副作用,提高患者的顺应性,开发了许多创新的给药系统来改善治疗效果。

储库型给药系统的优势在于可以高载药量、延长药物释放时间、减少给药频率。AUC 的增加和 Cmax 的降低反映了储库制剂可以减少传统和口服治疗的毒性并发症和局限性。处于临床前和临床阶段的产品包括用于治疗酒精中毒/药物滥用的纳曲酮和丁丙诺啡、用于治疗糖尿病的 GLP-1 肽、用于生育的 r-hFSH、用于神经生长的多巴胺、用于眼部治疗的地塞米松、用于预防癌症的黑素原、用于预防癌症的质粒 DNA、各种疫苗、奥曲肽仿制药等。

大多数储库制剂由控制药物释放速度的可生物降解聚合物-赋形剂组成,并在药物释放期间/之后被吸收。与口服药物相比,储库型抗精神病药物的主要优势在于提高了患者服药的顺应性。

其中一种已被广泛接受且至今仍具吸引力的可生物降解聚合物是丙交酯/乙交酯聚合物。这些可降解聚合物的最大优势在于它们会被分解成生物可接受的分子,这些分子通过正常的代谢途径被代谢并从体内排出。与普通的给药系统相比,这种多功能的给药系统具有很高的载药量和控制药物释放的优点,可以延长药物的释放时间。

与旧的制剂相比,新的抑郁症制剂在便利性、副作用谱、疗效和/或快速起效方面可能具有优势。

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