bcs class ii
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Author(s):  
RAHUL RADKE ◽  
NEETESH K. JAIN

Objective: The aim of this investigation was to enhance the solubility and bioavailability of the BCS class II poorly water-soluble drug ambrisentan by solid dispersion (SD) techniques using Gelucire 50/13 as a hydrophilic carrier. Methods: Solid dispersion of ambrisentan was prepared by kneading method using different dug: carrier ratios. Prepared SD was characterized for solubility, drug content, percentage yield, in vitro dissolution, ex vivo permeation and bioavailability. Solid-state characterization was performed by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Results: All the SDs formulations showed increase in drug solubility and dissolution when compared with its pure form. Aqueous solubility of the drug was found to be increased 8.23 fold in SD. DSC study showed that endothermic peak of the drug was disappeared in spectra of SD, confirming its amorphous conversion, XRD study revealed the reduction to almost absence of specific high-intensity peaks of drug which confirmed the reduction of crysatallinity of ambrisentan in SD. SEM of optimized SD formulation demonstrates the complete encapsulation and solubilization drug. In vitro dissolution study showed that optimized SD formulation (ASD4) gives the faster drug release of 101.5% in 60 min, as compare to its pure form and other SD formulations. Conclusion: Solid dispersion ASD4 prepared with 1:4 drug to carrier ratio showed the highest drug solubility and in vitro dissolution. The ex vivo and in vivo studies performed on optimized formulation ASD4 showed enhancement in drug permeability and bioavailability in Gelucire 50/13 based SD formulation.


2022 ◽  
Vol 12 (1) ◽  
pp. 63-69
Author(s):  
Salam Shanta Taher ◽  
Khalid Kadhem Al-Kinani ◽  
Zahraa Mohsen Hammoudi ◽  
Mowafaq mohammed Ghareeb

2021 ◽  
Vol 10 (6) ◽  
pp. 3806-3812
Author(s):  
Pritam Singh

BCS class II is well-known for the drugs, having poor aqueous solubility and high permeability. Simvastatin is also categorized as BCS class II, suffering from poor aqueous solubility, affecting its bioavailability. In an attempt to resolve this problem, solid dispersions of simvastatin were prepared by spray-drying method. Solid dispersions of simvastatin with PVP K25 and aerosol in ratio (1:1:1 to 1:5:1) and without aerosil 200 (1:1 to 1:5) were prepared by spray drying method. The dissolution test showed the enhancement of dissolution as compared to the pure drug and nearly equal to marketed formulation “SIMVOTIN 20mg” in both types of formulation, but formulations with aerosil 200 showed faster drug release as compared to the simple formulations without aerosil. The formulation containing the 1:3:1 (simvastatin: PVP K25: Aerosil 200) showed the faster drug release as compared to other formulation that do not contain the Aerosil 200. Other characterization studies were also performed such as FTIR, differential scanning colorimetry and powdered X-ray crystallographic studies. These studies showed the increased amorphous nature of the drug in the formulation, which explain the enhanced dissolution rate of the drug for these formulations.


2021 ◽  
Vol 14 (11) ◽  
pp. 1201
Author(s):  
Bharti Gupta ◽  
Varsha Mishra ◽  
Sankalp Gharat ◽  
Munira Momin ◽  
Abdelwahab Omri

One of the major impediments to drug development is low aqueous solubility and thus poor bioavailability, which leads to insufficient clinical utility. Around 70–80% of drugs in the discovery pipeline are suffering from poor aqueous solubility and poor bioavailability, which is a major challenge when one has to develop an ocular drug delivery system. The outer lipid layer, pre-corneal, dynamic, and static ocular barriers limit drug availability to the targeted ocular tissues. Biopharmaceutical Classification System (BCS) class II drugs with adequate permeability and limited or no aqueous solubility have been extensively studied for various polymer-based solubility enhancement approaches. The hydrophilic nature of cellulosic polymers and their tunable properties make them the polymers of choice in various solubility-enhancement techniques. This review focuses on various cellulose derivatives, specifically, their role, current status and novel modified cellulosic polymers for enhancing the bioavailability of BCS class II drugs in ocular drug delivery systems.


2021 ◽  
Author(s):  
Monica Pistone ◽  
Giuseppe Francesco Racaniello ◽  
Ilaria Arduino ◽  
Valentino Laquintana ◽  
Antonio Lopalco ◽  
...  

Abstract Niclosamide (NCS) is a drug that has been used as an anthelmintic and anti-parasitic active principle for about 40 years. Recently, some studies have highlighted its potential in treating various tumors, allowing a repositioning of this drug. Despite its potential, NCS is a Biopharmaceutical Classification System (BCS) Class II drug, and is consequently characterised by low aqueous solubility, poor dissolution rate and reduced bioavailability, which limits its applicability. In this work, we utilize a very novel technique, Direct Powder Extrusion (DPE) 3D printing, which overcomes the limitations of previously used techniques (Fused Deposition Modelling, FDM) to achieve direct extrusion of pharmaceutical grade powder mixtures consisting of NCS, hydroxypropyl methylcellulose (HPMC, Affinisol 15 LV), hydroxypropyl-b-cyclodextrin (HP-β-CD) and polyethylene glycol (PEG) 6000. For the first time, direct printing of powder blends containing HP-β-CD was explored. For all tablets, in vitro dissolution studies showed sustained drug release over 48 hours, but for tablets containing HP-β-CD, the release was faster. Solid-state characterisation studies showed that during extrusion, the drug lost its crystal structure and was evenly distributed within the polymer matrix. All printed tablets exhibited good mechanical and physical features and guarantee stability of the drug content for up to 3 months. This innovative printing technique has demonstrated the possibility to produce personalised pharmaceutical dosage forms starting directly from powders, avoiding the use of filament used by FDM.


Author(s):  
Thalita Martins da Silva ◽  
Thiago da Silva Honorio ◽  
Marcelo Henrique da Cunha Chaves ◽  
Marcelo Dutra Duque ◽  
Lucio Mendes Cabral ◽  
...  

Author(s):  
Madhavi Kasturi ◽  
Neelesh Malviya

Aims: The main objective of the current research work is to develop liquisolid compacts of BCS Class II drug ketoprofen with an intention to enhance the solubility of drug by applying liquisolid technique. Place and Duration of Study: Smriti College of Pharmaceutical Education between June 2018 June 2019. Methodology: Initially liquid medication was obtained by dissolving drug in suitable solvent. Saturation solubility studies were performed in various hydrophilic non-volatile solvents to select the solvent showing highest solubility for drug. This liquid medication was admixed with calculated amounts of carrier material (Avicel PH 102) and coating material (Cab-O-Sil) using Spireas mathematical model in order to obtain liquisolid formulations. Further, this powder mass of liquisolid system was compressed to form Ketoprofen liquisolid compact formulations ranging from TK1 to TK9. They were further subjected to post compression evaluation tests such as weight variation, hardness, friability, content uniformity, disintegration and in vitro dissolution studies. Results: Based on the solubility studies, PEG 400 was selected as solvent for ketoprofen drug. Rheological properties for the prepared liquisolid powder system were performed for all the formulations and they showed acceptable flow properties. The results obtained for the post compression evaluation tests of all the prepared liquisolid compacts were present within the acceptable limits. The disintegration time observed for all formulations were within 5 minutes. The results of in vitro release of all the liquisolid compacts showed enhanced release rates compared to that of directly compressed tablet. Lquisolid compact formulation TK7 showed maximum release of 97.62% of drug within 12 minutes in pH 7.4 phosphate buffer which was much higher when compared to that of directly compressed tablet. The SEM and PXRD studies for TK7 revealed conversion of crystalline to molecularly dispersed form of drug in the obtained liquisolid formulation. DSC and FTIR studies also revealed that there was no presence of any significant interaction between drug and excipients involved in the formulation. Conclusion: Finally, it could be concluded that Liquisolid technique was successful in enhancing the solubility and further dissolution profile of BCS Class II drug Ketoprofen.


2021 ◽  
Vol 1 (1) ◽  
pp. 100003
Author(s):  
Daniela A.S. Agostinho ◽  
Filipa Santos ◽  
José M.S.S. Esperança ◽  
Ana R.C. Duarte ◽  
Patrícia M. Reis

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