Design and optimization of clotrimazole–hydroxypropyl-β-cyclodextrin bioadhesive vaginal tablets using Anacardium occidentale gum by 32 factorial design

RSC Advances ◽  
2015 ◽  
Vol 5 (45) ◽  
pp. 35391-35404 ◽  
Author(s):  
Umme Hani ◽  
Gokul Krishna ◽  
H. G. Shivakumar

Clotrimazole (CTZ), a BCS class II drug, is widely employed in the treatment of vaginal candidiasis.

Author(s):  
Paras R. Vasanani ◽  
L. Patel ◽  
Chetan Detroja

Nanosuspensions are the dispersions of nanosized particles in a suitable vehicle prepared using surfactants or solubilizers to aid in nanosize distribution. Nanosuspension is best suited for dosage form development of poorly soluble drugs. According to the biopharmaceutical classification system, drugs with poor solubility fall either in BCS class II or BCS class IV. BCS class II drugs show poor solubility and good permeability; hence their bioavailability problems can be overcome by improving their solubility. Metaxalone is one such BCS class II drug from an oxazolidin-2-one class of centrally acting muscle relaxant drugs, indicated for relief of discomforts associated with acute, painful musculoskeletal conditions. Therefore, in present investigation, nanosuspension of Metaxalone has been formulated as an attempt to improve solubility and hence the overall bioavailability of Metaxalone. Media milling technique has been employed for nanosuspension preparation. Surfactant concentration (Poloxamer 407) and stirring time has been optimized using 32 factorial design to achieve desired particle size and saturation solubility responses as dependent variables. The particle size (PS) of 215.3 nm and maximum saturation solubility (SS) of 2805μg/ml was obtained as suggested solutions from factorial design which was further confirmed using check point analysis. Interaction of surfactant concentration and stirring time and their effect on particle size and saturation solubility was predicted using the contour plots and response surface plots. The optimized formulation showed around 99% metaxalone in vitro dissolution in comparison to around 46% dissolution from SKELAXIN® tablet at 30 minutes. These methodologies could therefore be employed successfully to improve solubility of any BCS class II drug and to predict effects and interactions of many experimental variables at the same time.


2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja

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.


Author(s):  
Sidra Nasir ◽  
Amjad Hussain ◽  
Nasir Abbas ◽  
Nadeem Irfan Bukhari ◽  
Fahad Hussain ◽  
...  
Keyword(s):  
Class Ii ◽  

Author(s):  
Mohamed Rahamathulla ◽  
Umme Hani ◽  
Ali Alqahtani ◽  
Gangadharappa. H.V ◽  
Yasmin Begum M ◽  
...  

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

2017 ◽  
pp. 1-18
Author(s):  
Gregory K.Webster ◽  
Robert G. Bell ◽  
J. Derek Jackson

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