PREPARATION AND CHARACTERIZATION LIQUISOLID COMPACTS OF BCS CLASS II DRUG FLURBIPROFEN

2021 ◽  
Vol 10 (10) ◽  
Keyword(s):  
Class Ii ◽  
Bcs Class Ii ◽  
Liquisolid Compacts

scholarly journals Formulation and development of some BCS Class II drugs

2019 ◽  
Vol 9 (2) ◽  
pp. 321-329
Author(s):  
SC Marapur ◽  
Rakesh Kumar Jat ◽  
J S Patil
Keyword(s):  
Drug Release ◽  
Propylene Glycol ◽  
Class Ii ◽  
In Vitro Drug Release ◽  
Bcs Class Ii ◽  
Carrier Materials ◽  
Volatile Liquid ◽  
Liquisolid Compacts ◽  
Drug Solution

The aim of this research was to develop and evaluate liquisolid compacts of Ezetimibe a bcs class II drug. The series of formulations containing Ezetimibe drug were formulated by using aerosil a colloidal silicone dioxide and avicel PH microcrystalline cellulose in different ratios by using suitable solvent. Solubility studies were performed in propylene glycol and polyethylene glycol (PEG-200, 400, 600) for the choice of the best non volatile liquid to dissolve Ezetimibe. On the basis of the solubility data PG was chosen as a good solvent for the Ezetimibe. Ezetimibe was dissolved in solvent PG for the preparation of solution of drug. The coating and carrier materials transferred to the drug solution and added 5% of disintegrating agent (Croscarmellose) was mixed completely and the blend is compressed into compacts. Formulated compacts were evaluated for all post compression parameters and the in-vitro drug release study was carried out. All the formulations have shown a very good drug release in  15 min except compressibility problems due to higher812 loading factor of liquid vehicle for the formulations. The selected formulation F11 containing 30% of drug solution has  shown good drug release of 100.01% in 15  min compared to dissolution of  pure drug and marketed tablet which shown 45.5%  and 81.6 % respectively.No interactions were found  between drug and polymers in FITR as well as DSC. XRD of selected formulation shows that drug present in the formulation is in amorphous form. Keywords: Ezetimibe HCl, Avicel PH, Aerosil 200, Propylene glycol, liquisolid compacts

scholarly journals Formulation and Evaluation of Liquisolid Compacts of BCS Class II Drug Ketoprofen

2021 ◽  
pp. 322-334
Author(s):  
Madhavi Kasturi ◽  
Neelesh Malviya
Keyword(s):  
Class Ii ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Bcs Class Ii ◽  
Liquid Medication ◽  
Compact Formulation ◽  
Solubility Studies ◽  
Liquisolid Compacts

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.

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

Improved Bioavailability of Oxcarbazepine, a BCS class II drug by Centrifugal Melt Spinning: In-vitro and in-vivo Implications

2021 ◽  
pp. 120775
Author(s):  
Sidra Nasir ◽  
Amjad Hussain ◽  
Nasir Abbas ◽  
Nadeem Irfan Bukhari ◽  
Fahad Hussain ◽  
...  
Keyword(s):  
Melt Spinning ◽  
Class Ii ◽  
Bcs Class Ii

Polymer strip films as a robust, surfactant-free platform for delivery of BCS Class II drug nanoparticles

2015 ◽  
Vol 489 (1-2) ◽  
pp. 45-57 ◽  
Author(s):  
Scott M. Krull ◽  
Ramana Susarla ◽  
Afolawemi Afolabi ◽  
Meng Li ◽  
Ye Ying ◽  
...  
Keyword(s):  
Class Ii ◽  
Bcs Class Ii ◽  
Drug Nanoparticles

Chapter 1 The Modern Pharmaceutical Development Challenge: BCS Class II and IV Drugs

2017 ◽  
pp. 1-18
Author(s):  
Gregory K.Webster ◽  
Robert G. Bell ◽  
J. Derek Jackson
Keyword(s):  
Class Ii ◽  
Pharmaceutical Development ◽  
Bcs Class Ii

scholarly journals Development of a BCS Class II Drug Microemulsion for Oral Delivery: Design, Optimization, and Evaluation

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Marwa Tlijani ◽  
Mohamed Ali Lassoued ◽  
Badr Bahloul ◽  
Souad Sfar
Keyword(s):  
Droplet Size ◽  
Oral Delivery ◽  
Classical Method ◽  
Ex Vivo ◽  
Physical Stability ◽  
Class Ii ◽  
Bcs Class Ii ◽  
Everted Gut Sac ◽  
Hydrophilic Lipophilic Balance ◽  
New Perspective

Our work is aimed at exploring the composition and the properties of microemulsion (ME), as a drug delivery system, to enhance the permeability across the gastrointestinal (GI) barrier of fenofibrate, a BCS class II drug. It is a prodrug that is converted rapidly after oral administration into a major active metabolite which is the fenofibric acid. It undergoes a nearly complete presystemic metabolism. Its main drawback is the low bioavailability of the metabolite. A quick selection of excipients was made based on the capacity of solubilization and the value of hydrophilic-lipophilic balance. The classical method of ME development was coupled with the factorial design in order to minimize the droplet size using a low concentration of surfactant. The optimized ME showed a droplet size of 48.5 nm and physical stability. The passive permeability evaluated using Sartorius was 1.6 times higher than that of the free drug. The ex vivo technique, performed using the everted gut sac model, showed a 2.5-fold higher permeability. This suggests that the carrier-mediated uptake/efflux may present the dominant transport mechanism of fenofibrate. The use of the excipients that inhibit GI P-glycoprotein may be a new perspective. Thus, this paper shows that the composition and the characteristics of ME may be explored to increase the permeability of fenofibrate across the GI membrane.

Sign in / Sign up

Export Citation Format

Share Document