Formulation/pharmaceutical excipients play a major role in formulating drug candidates,with the objectives of ease of administration,targeted delivery and complete availability.Many excipients used in pharmaceutical f...Formulation/pharmaceutical excipients play a major role in formulating drug candidates,with the objectives of ease of administration,targeted delivery and complete availability.Many excipients used in pharmaceutical formulations are orphanized in preclinical drug discovery.These orphan excipients could enhance formulatability of highly lipophilic compounds.Additionally,they are safe in preclinical species when used below the LD50 values.However,when the excipients are used in formulating compounds with diverse physico-chemical properties,they pose challenges by modulating study results through their bioanalytical matrix effects.Excipients invariably present in study samples and not in the calibration curve standards cause over-/under-estimation of exposures.Thus,the mechanism by which excipients cause matrix effects and strategies to nullify these effects needs to be revisited.Furthermore,formulation excipients cause drug interactions by moderating the pathways of drug metabolizing enzymes and drug transport proteins.Although it is not possible to get rid of excipient driven interactions,it is always advised to be aware of these interactions and apply the knowledge to draw meaningful conclusions from study results.In this review,we will comprehensively discuss a)orphan excipients that have wider applications in preclinical formulations,b)bioanalytical matrix effects and possible approaches to mitigating these effects,and c)excipient driven drug interactions and strategies to alleviate the impacts of drug interactions.展开更多
With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug del...With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug delivery systems, transdermal patch can maintain stable and effective plasma concentration and therapeutic effect in vivo for a long time after skin dressing delivery, which provides a safe and effective drug-delivery way for the therapy and prevention of some chronic diseases and partial analgesia in a simple and convenient way. Veterinary drug transdermal preparations have been developed both at home and abroad, and satisfactory results have been achieved in the experimental application. Based on the study of veterinary transdermal patches at home and abroad, this paper systematically describes the development and characteristics of transdermal patches, the factors affecting skin permeation and the evaluation this type of preparations in veterinary drugs.展开更多
文摘Formulation/pharmaceutical excipients play a major role in formulating drug candidates,with the objectives of ease of administration,targeted delivery and complete availability.Many excipients used in pharmaceutical formulations are orphanized in preclinical drug discovery.These orphan excipients could enhance formulatability of highly lipophilic compounds.Additionally,they are safe in preclinical species when used below the LD50 values.However,when the excipients are used in formulating compounds with diverse physico-chemical properties,they pose challenges by modulating study results through their bioanalytical matrix effects.Excipients invariably present in study samples and not in the calibration curve standards cause over-/under-estimation of exposures.Thus,the mechanism by which excipients cause matrix effects and strategies to nullify these effects needs to be revisited.Furthermore,formulation excipients cause drug interactions by moderating the pathways of drug metabolizing enzymes and drug transport proteins.Although it is not possible to get rid of excipient driven interactions,it is always advised to be aware of these interactions and apply the knowledge to draw meaningful conclusions from study results.In this review,we will comprehensively discuss a)orphan excipients that have wider applications in preclinical formulations,b)bioanalytical matrix effects and possible approaches to mitigating these effects,and c)excipient driven drug interactions and strategies to alleviate the impacts of drug interactions.
基金Supported by the Program for Technology Research and Development and Its Demonstration and Popularization of Beijing Vocational College of Agriculture(XY-YF-15-08)~~
文摘With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug delivery systems, transdermal patch can maintain stable and effective plasma concentration and therapeutic effect in vivo for a long time after skin dressing delivery, which provides a safe and effective drug-delivery way for the therapy and prevention of some chronic diseases and partial analgesia in a simple and convenient way. Veterinary drug transdermal preparations have been developed both at home and abroad, and satisfactory results have been achieved in the experimental application. Based on the study of veterinary transdermal patches at home and abroad, this paper systematically describes the development and characteristics of transdermal patches, the factors affecting skin permeation and the evaluation this type of preparations in veterinary drugs.
