Effect of Formulation Variables on Optimization of Gastroretentive In Situ Rafts of Bosentan Monohydrate HCl by 32 Factorial Design

2020 ◽  
pp. 47-63
Author(s):  
B. Sarada ◽  
G. Srividya ◽  
R. V. Suresh Kumar ◽  
M. Keerthana ◽  
M. Vidyavathi
Keyword(s):  
Factorial Design ◽  
32 Factorial Design ◽  
Formulation Variables

scholarly journals Application of DoE in polymers screening and optimization of in situ topical ϑilm-forming solution for spray formulation

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 2499-2515
Author(s):  
Nabil Abdullah ◽  
Amit B Patil
Keyword(s):  
Factorial Design ◽  
Drying Time ◽  
Flexible Film ◽  
Pharmaceutical Industries ◽  
Model Drug ◽  
32 Factorial Design ◽  
Spray Formulation ◽  
Experimental Values ◽  
The Relationship

DoE is a structured and organised method to determine the relationship between the effect of change in the concentration of the independent variables and its impact on the formulation, through establishing a mathematical model. Since the acceptance of the QbD approach by the regulatory authorities across the world, DoE has been widely implemented in the areas of screening and optimisation of the formulations by the pharmaceutical industries. The topical delivery of API still posses' limitations such as insufficient contact time, odd hours of application time, sticking to fabrics, formulation washing off, etc. To address these limitations, the researcher planned to develop an in situ polymeric sprays that will form a transparent and flexible film, & will not interfere with the applicant's routine. Polymers such as HPMC, Eudragit RS100, PVP K30, PVP K90, Carbopol, Propylene glycol, Soluplus, and pullulan whereas the plasticisers selected were sorbitol. Voriconazole, a second-generation triazole, was used as a model drug. The article is a technological demonstration, in which the screening of polymers as well as the optimised concentration of the polymeric will be selected through 32 factorial design. The aim of the present article is also to establish the relationship between the software response and experimental values. The experiments were designed using 32 factorial design which resulted in 9 trial runs. Each run was evaluated for drying time, viscosity, and stickiness. The resultant response surface Later the optimisation, to yield an optimised polymeric solution that can deliver a desired in situ films. Based on ANOVA comparison of variability due to treatment, the significance of the regression model was evaluated. Other procedures such as DSC, FRIR, Stickiness, pH, diffusion studies were also performed on the selected formulation.

scholarly journals Formulation and Development of Stable Metaxalone Nanosuspension Using 32 Factorial Design

2016 ◽  
Vol 8 (04) ◽  
Author(s):  
Paras R. Vasanani ◽  
L. Patel ◽  
Chetan Detroja
Keyword(s):  
Particle Size ◽  
Factorial Design ◽  
Surfactant Concentration ◽  
Class Ii ◽  
Poloxamer 407 ◽  
Saturation Solubility ◽  
Poor Solubility ◽  
Bcs Class Ii ◽  
Stirring Time ◽  
32 Factorial Design

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.

USE OF FACTORIAL DESIGN IN OPTIMIZATION OF MICROWAVE ASSISTED ORGANIC SYNTHESIS OF SOME AZOLES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (10) ◽  
pp. 24-33
Author(s):  
R. R Somani ◽  
◽  
G. J. Sanap ◽  
P. K Chaskar
Keyword(s):  
Factorial Design ◽  
Organic Synthesis ◽  
Maximum Yield ◽  
Minimum Time ◽  
Organic Reactions ◽  
Design Approach ◽  
Environment Friendly ◽  
Microwave Assisted ◽  
Synthetic Reactions ◽  
32 Factorial Design

In the era of environment friendly chemistry, Microwave Assisted Organic Synthesis (MAOS) has proved to be an effective tool to achieve maximum yield in minimum time without compromising on quality. The present work focuses on synthesis of some bioactive heterocyclic azoles using MAOS. However, the synthetic reactions are optimized using a known technique of factorial designing. Here, 32 factorial design approach is used to achieve the set targets of yields and purity. The outcome has been very promising and opens up new avenues for organic chemists who face challenges in optimizing organic reactions.

scholarly journals Optimization of ThermoreversibleIn SituNasal Gel of Timolol Maleate

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Swati Jagdale ◽  
Nirupama Shewale ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Ex Vivo ◽  
Nasal Delivery ◽  
Poloxamer 407 ◽  
Timolol Maleate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Pass Metabolism

Nasal route had shown better systemic bioavailability due to its large surface area, porous endothelial membrane, high total blood flow, and avoidance of first-pass metabolism. Timolol maleate is a beta blocker used primarily in the treatment of hypertension. Drug undergoes extensive hepatic first-pass metabolism (80%). The drug has half-life of 4 hrs. Oral bioavailability of timolol maleate is 61%. The aim of the present study was to optimize controlled releasein situnasal delivery for timolol maleate. HPMC and Poloxamer 407 were selected as polymer in formulation of thermoreversiblein situnasal gel. Optimization was carried out using 32factorial design. It was observed that formulations f1 and f4 revealed the highest % drug release, that is, 93.57% and 91.66%, respectively. Factorial design study indicated that the drug release and viscosity were most significant dependent factors.Ex vivodiffusion study through nasal mucosa indicated 67.26 ± 2.10% and 61.07 ± 2.49% drug release for f1 and f4 formulations. f1 was the optimized batch. This batch thus can act as a potential nasal delivery with enhanced bioavailability for the drug.

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