#Bcs class 4 drugs list trial#
#Bcs class 4 drugs list series#

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 4 drugs list series#

Today, the pharmaceutical industry has as its disposal a series of reliable and scalable formulation strategies for BCS Class IV drugs.

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.

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. 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. This article highlights the various techniques and upcoming strategies which can be employed for the development of highly notorious BCS class IV drugs. Also, ideal systems for BCS class IV should produce a therapeutic concentration of the drug at reasonable dose volumes for intravenous administration. Ideal oral dosage forms should produce both a reasonably high bioavailability and low inter and intra subject variability in absorption. To be clinically effective these drugs require the development of a proper delivery system for both oral and per oral delivery. The importance of the formulation composition and design to successful drug development is especially illustrated by the BCS class IV case. The inherent hurdles posed by these drugs hamper their translation to actual market. Formulation and development of an efficacious delivery system for BCS class IV drugs are herculean tasks for any formulator. 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. 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. 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. Conclusion: From the present study, we can concluded that the optimized Apixaban solid dispersion may prove to be a suitable potential option for solubility enhancement, increased in-vitro drug release and effective delivery of BCS class II and IV drugs.BCS class IV drugs (e.g., amphotericin B, furosemide, acetazolamide, ritonavir, paclitaxel) exhibit many characteristics that are problematic for effective oral and per oral delivery. The Apixaban solid dispersion with polymer HPMC K15M resulted into highest increase in the solubility as compared to the other evaluated hydrophilic polymers. Results: The Solid dispersion of Apixaban showed improvement in the solubility in water by multiple folds when Apixaban used in combination with Hydrophilic polymers. To screen out the ratio of polymer and suitable polymer type for solid dispersion resulted into highest solubility as a response.

In this study, Apixaban was opted for formulating Solid dispersion with Hydrophilic polymers like HPMC E50 LV, HPMC E5, PEG 6000 and PVP K-30 by Spray drying method using a structured I optimal screening DOE. Methods: The solid dispersion is the technique for the formulation of water insoluble drugs to enhance their aqueous solubility, absorption as well as dissolution rate, which leading to enhancement of bioavailability of drugs as compared to conventional directly compressed tablets. Objectives: The present research work was aimed to enhance the solubility of Apixaban drug by using Solid Dispersion Technique. One of the major problems responsible for the low turnout in the development of new molecular entities as drug formulations is poor solubility and poor permeability of the lead compounds. Background: Solubility is an important physico-chemical factor affecting absorption of drug and its therapeutic effectiveness.