scholarly journals Approaches of increasing oral bioavailability of class ii active pharmaceutical ingredients in accordance with the biopharmaceutical classification system

2019 ◽  
Vol 0 (2(98)) ◽  
pp. 29-35
Author(s):  
V. V. Mohylyuk ◽  
L. L. Davtian ◽  
D. O. Novykov ◽  
M. G. Katynska ◽  
Yu. V. Shmyrova ◽  
...  
2020 ◽  
Vol 11 (2) ◽  
pp. 83-96
Author(s):  
Hetal P Thakkar ◽  
Deepika Vasava ◽  
Arpita A Patel ◽  
Rahul D Dhande

Aim: Formulate and evaluate liquisolid compacts of Itraconazole, a biopharmaceutical classification system class II drug, which has poor bioavailability. Materials & methods: PEG 600 was used as a nonvolatile solvent, Alfacel PH 200 as a carrier and Aerosil 200 as a coating material. The Itraconazole solution upon mixing with a carrier and coating material resulted in a dry powder, which was compressed into tablets. Results & conclusion: The optimized formulation exhibited a significantly higher drug dissolution (90.73% in 90 min) compared with conventional tablets and marketed capsules. The antifungal activity was retained in the formulation. Higher values of Cmax and AUC0-24 of the formulation compared with the plain drug indicated enhancement in oral bioavailability. The formulation was stable at room temperature as well as in accelerated conditions.


2020 ◽  
Vol 2 (2) ◽  
pp. 77
Author(s):  
Dwi Retno Sari ◽  
Yoga Windhu Wardhana ◽  
Taofik Rusdiana

Many techniques can be used to improve drug solubility, which is the development of the liquisolid technique. This technique has a mechanism for increasing the surface area of the drug as well as wetting from the addition of non-volatile solvents resulting in a lower surface tension and contact angle, so the solubility and drug release very increases. Liquisolid tablets show a lower contact angle compared to the conventional tablets. The liquisolid technique approach is also promising because the process is simple in making low production costs and allows the manufacturing industry, including non-volatile solvents, fillers, dryers, and disintegrants. Liquisolid characterized by specific instruments such as powder x-ray diffraction (PXRD), Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Several liquisolid techniques are described in this review. The liquisolid technique is proven and able to change the physicochemical properties of active pharmaceutical ingredients, especially the solubility, drug release, and stability of the formula so that this technique can be a solution for class II and IV BCS pharmaceutical active drug classes.Keywords: Active Pharmaceutical Ingredients, Contact Angle, Solubility, Drug Release, Stability, Liquisolid Technique


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 47-51
Author(s):  
G Sailesh ◽  
◽  
T. E. G. K. Murthy

Telmisartan is used in the treatment of hypertension. It exhibits poor water solubility. It belongs to class II of Biopharmaceutical Classification system (BCS). It needs enhancement in dissolution and hence bioavailability. The dissolution of drug was improved by coating the drug and carrier over sugar spheres.Size of sugar spheres and concentration of the carrier were two critical variables that were found to affect the dissolution of drug. A 22 factorial design was used to study the effect of concentration of carrier and size of the non-pareil seeds on dissolution. Dissolution of telmisartan was found to increase with increasing concentration of carrier and decreased with respect to size of non-pareil seeds.


CrystEngComm ◽  
2021 ◽  
Author(s):  
Indira S Divya ◽  
Amrutha Surendran ◽  
Sunil SeethaLekshmi ◽  
Sunil Varughese

The anti-malarial drug quinine (QUN) has poor aqueous solubility and belongs to Biopharmaceutical Classification System (BCS) Class-II. We report 12 novel molecular salts of QUN with α,ω-aliphatic dicarboxylic acids, and...


INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (4) ◽  
pp. 63-73
Author(s):  
Mahesh S. Soni ◽  
◽  
Atmaram P. Pawar ◽  
Chellampillai Bothiraja ◽  
Vinod L. Gaikwad ◽  
...  

The purpose of the present study is to highlight the discriminations if any, between the quality of low and high-cost medicines, which would help to select the right brand of medicine. In the present work, brands of medicines having high, medium, and low prices containing either of biopharmaceutical classification system class-II or class-IV drugs were comparatively evaluated for different pharmacopoeial standards as well as for biopharmaceutical classification system solubility and permeability. An ex vivo permeability test was carried out using a simple and non-invasive everted gut sac technique. Insignificant variation in pharmaceutical quality and permeability of the tested three types of brands was observed; however, the study could not consider the state of quality assurance facilities and parameters used while manufacturing these medicines. The study will help to make aware and assure medical and pharmacy practitioners and consumers for the selection of quality quality generic medicines.


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