The inherent hur dles posed by these drugs hamper their translatio n to actualmarket.Some of the problems associated include low aqueous solubility, poor permeability, erratic and poor absorption, inter and intra subject variability and significant positive food effect which leads to low and variable bioavailability.
Also, most of the class IV drugs are substrate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further potentiates the problem of poor therapeutic potential of these drugs. A decade back, extreme examples of class IV compounds were an exception rather than the rule, yet today many drug candidates under development pipeline fall into this category. Formulation and development of an efficacious delivery system for BCS class IV drugs is a herculean task for any formulator. The inherent hurdles posed by these drugs hamper their translation to actual market. The importance of the formulation composition and design to successful drug development is especially illustrated by the BCS class IV case. To be clinically effective these drugs require the development of a proper delivery system for both oral and per oral delivery. Ideal oral dosage forms should produce both a reasonably high bioavailability and low inter and intra subject variability in absorption. Also, ideal systems for BCS class IV should produce a therapeutic concentration of the drug at reasonable dose volumes for intravenous administration. ![]() Some of the techniques employed are lipid based delivery systems, polymer based nanocarriers, crystal engineering (nanocrystals and co-crystals), liquisolid technology, self-emulsifying solid dispersions and miscellaneous techniques addressing the P-gp efflux problem. The review also focuses on the roadblocks in the clinical development of the aforementioned strategies such as problems in scale up, manufacturing under cGMP guidelines, appropriate quality control tests, validation of various processes and variable therein etc. It also brings to forefront the current lack of regulatory guidelines which poses difficulties during preclinical and clinical testing for submission of NDA and subsequent marketing. Bcs Class 4 Drugs Series Of ReliableToday, the pharmaceutical industry has as its disposal a series of reliable and scalable formulation strategies for BCS Class IV drugs. However, due to lack of understanding of the basic physical chemistry behind these strategies formulation development is still driven by trial and error. BCS Class IV drugs-the inherent hurdles posed by them in their oral and per oral delivery along with the strategies to overcome them. Key advantages associated with lipid based drug delivery systems which improve oral and peroral delivery of BCS class IV drugs. Absorption mechanisms implemented by lipidic nanocarriers for improving the bioavailability of BCS class IV drugs. Figures - uploaded by Rohan Ghadi Author content All figure content in this area was uploaded by Rohan Ghadi Content may be subject to copyright. Bcs Class 4 Drugs Free Public FullBcs Class 4 Drugs For Free Public FullDiscover the worlds research 20 million members 135 million publications 700k research projects Join for free Public Full-text 1 Content uploaded by Rohan Ghadi Author content All content in this area was uploaded by Rohan Ghadi on Dec 18, 2017 Content may be subject to copyright. Some of the probl ems associat ed include low aqueous sol ubility, p oor permeabi lity, erra tic and poor ab sorption, in ter and int ra subject va riability an d signi - cant posit ive food effe ct which lead s to low and var iable bioava ilabilit y. Also, mos t of the class IV drugs are sub- strate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further p otentiates th e problem of poor the rapeutic pote ntial of these dr ugs. A decade back, ex treme ex- amples of class IV com pounds were an exce ption ratherthan the rule, yet today many drug can didates underde- velopmen t pipeline fa ll into thiscategory. Formulat ion and devel opment of anef cacious deliver y system for BCS class IV drugs ar e herculean tasks fo r any formulator.
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