scholarly journals Enhancement of dissolution rate of Clofibrate BCS Class –II drug by using liquisolid compact technology

2015 ◽  
Vol 6 (3) ◽  
pp. 288 ◽  
Author(s):  
Brahmaiah Bonthagarala ◽  
Pusuluri Dharani Lakshmi Sai ◽  
Venkata Sivaiah K. ◽  
Anil Kumar G. ◽  
B.Nageswara Rao ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Class Ii ◽  
Bcs Class Ii

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.

scholarly journals Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

2020 ◽  
Vol 13 (2) ◽  
pp. 80-93 ◽  
Author(s):  
Abikesh P.K. Mahapatra ◽  
Vinod Patil ◽  
Ravindra Patil
Keyword(s):  
Dissolution Rate ◽  
Class Ii ◽  
Systemic Circulation ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Solid Dosage ◽  
Bcs Class Ii ◽  
Pharmacological Response ◽  
Poorly Soluble ◽  
Low Solubility

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.

scholarly journals Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3469
Author(s):  
Chi Uyen Phan ◽  
Jie Shen ◽  
Kaxi Yu ◽  
Jianming Mao ◽  
Guping Tang
Keyword(s):  
Dissolution Rate ◽  
Photoelectron Spectroscopy ◽  
Class Ii ◽  
Crystal Habit ◽  
Factors Affecting ◽  
X Ray ◽  
Bcs Class Ii ◽  
Rate Limiting Step ◽  
In Vivo Pharmacokinetics

The dissolution rate is the rate-limiting step for Biopharmaceutics Classification System (BCS) class II drugs to enhance their in vivo pharmacokinetic behaviors. There are some factors affecting the dissolution rate, such as polymorphism, particle size, and crystal habit. In this study, to improve the dissolution rate and enhance the in vivo pharmacokinetics of sorafenib tosylate (Sor-Tos), a BCS class II drug, two crystal habits of Sor-Tos were prepared. A plate-shaped crystal habit (ST-A) and a needle-shaped crystal habit (ST-B) were harvested by recrystallization from acetone (ACN) and n-butanol (BuOH), respectively. The surface chemistry of the two crystal habits was determined by powder X-ray diffraction (PXRD) data, molecular modeling, and face indexation analysis, and confirmed by X-ray photoelectron spectroscopy (XPS) data. The results showed that ST-B had a larger hydrophilic surface than ST-A, and subsequently a higher dissolution rate and a substantial enhancement of the in vivo pharmacokinetic performance of ST-B.

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.

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