Expert design and desirability function approach for the development of diazepam thermally sensitive rectal gel

2020 ◽  
Vol 11 (1) ◽  
pp. 813-830 ◽  
Author(s):  
Seyed Hassan Montazam ◽  
Sara Salatin ◽  
Mitra Alami-Milani ◽  
Amir Naderi ◽  
Mitra Jelvehgari

Aim: The aim of the present work was to develop an in situ thermosensitive rectal gel for diazepam by using Expert-design for improving three factors and a three-level process was formed by using a cold method. Methods & materials: Response surface design was utilized to investigate the effect of independent variables like sodium chloride (NaCl, X1), poloxamer 407 (F-127, X2) and diazepam (X3), on different dependent variables such as gelation temperature, mucoadhesive strength, drug content, along with permeation and stability. Results: The obtained results revealed that the addition of diazepam enhanced the gelation temperature of hydrogel while it decreased the gel strength and mucoadhesive force. Conclusion: It is suggested that in situ hydrogels may be suitable candidates for rectal delivery.

Catalysts ◽  
2019 ◽  
Vol 9 (3) ◽  
pp. 249 ◽  
Author(s):  
Marek Inger ◽  
Agnieszka Dobrzyńska-Inger ◽  
Jakub Rajewski ◽  
Marcin Wilk

In this paper, the design of experiments and response surface methodology were proposed to study ammonia oxidation process. The following independent variables were selected: the reactor’s load, the temperature of reaction and the number of catalytic gauzes, whereas ammonia oxidation efficiency and N2O concentration in nitrous gases were assumed as dependent variables (response). Based on the achieved results, statistically significant mathematical models were developed which describe the effect of independent variables on the analysed responses. In case of ammonia oxidation efficiency, its achieved value depends on the reactor’s load and the number of catalytic gauzes, whereas the temperature in the studied range (870–910 °C) has no effect on this dependent variable. The concentration of nitrous oxide in nitrous gases depends on all three parameters. The developed models were used for the multi-criteria optimization with the application of desirability function. Sets of parameters were achieved for which optimization assumptions were met: maximization of ammonia oxidation efficiency and minimization of the N2O amount being formed in the reaction.


Author(s):  
Hussein K. Alkufi ◽  
Hanan J. Kassab

     Objective: The purpose of this study to develop and optimize nasal mucoadhesive in situ gel IG of sumatriptan ST (serotonin agonist) to enhance nasal residence time for migraine management.      Method: Cold method was used to prepare ST nasal in-situ gel, using thermosensitive polymers (poloxamer 407  and/or poloxamer 188) with a mucoadhesive polymer (hyaluronic acid HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, mucoadhesive force determination, viscosity,  in-vitro drug release, and the selected formula was subjected to ex-vivo permeation study and histological evaluation of the sheep mucosal tissue after application.     Results: The results showed that the formula IG7 prepared from poloxamer 407(19%), poloxamer188 (4%) and HA (0.5%)   had an optimum gelation temperature (32.66±1.52°C), gel  strength (43.66± 1.52 sec),  mucoadhesive force (8067.93± 746.45dyne\cm2), in-vitro drug release (95.98%) over 6hr, ex-vivo permeation study release (89.6%)  during the 6 h. study with no  histological or pathological change in the nasal sheep tissue.     Conclusion: The ease of administration via a nasal drop of ST coupled with less frequent administration and prolong drug release, will enhance patient compliance.


2019 ◽  
Vol 18 (2) ◽  
pp. 183-193 ◽  
Author(s):  
PK Lakshmi ◽  
K Harini

The present investigation was aimed to develop a thermo-reversible nasal in situ gel of atomoxetine hydrochloride (AH) with reduced nasal muco-ciliary clearance in order to improve residence time and targeting the brain through nasal mucosa for the treatment of attention-deficit hyperactivity disorder (ADHD). In situ gel formulations were prepared using different concentrations of the thermo-gelling poloxamer 407 and mucoadhesive polymers. Temperature-triggered ionic gelation is the mechanism involved. Taguchi L9 OA experimental design was employed for the optimization of the effect of independent variables (Poloxamer 407 and Carbopol 934P) on the response (gelation temperature). In situ gel formulation F4 having 20% poloxamer 407 and 0.3% carbopol 934P and formulation F6 having 20% poloxamer 407 and 0.2% HPMC K100 were optimized based on evaluation parameters. The gelation temperature of F4 and F6 was found to be 37°C ± 0.4 and 37°C ± 0.2, drug content 98.34 and 98.33% and drug release was 83.18, 82.4% in 4 hrs with a flux of 436.9 and 428.1 μg.cm2/hr, respectively. The release pattern of drug followed first-order kinetics with Higuchi release mechanism. The value of ‘n’ from Korsemeyer equation indicated the anomalous diffusional drug release. This study concluded that in situ gel enhanced the nasal residence time and thus may improve the bioavailability of the drug through nasal route by avoiding first pass metabolism Dhaka Univ. J. Pharm. Sci. 18(2): 183-193, 2019 (December)


Author(s):  
ANANTH PRABHU ◽  
MARINA KOLAND

Objective: The purpose of this study was to develop an in situ ocular gel of ofloxacin which aimed to prolong corneal residence time while controlling drug release. Method: In situ gelling solutions were prepared from Poloxamer 407, a temperature-sensitive gelling polymer and to which, mucoadhesive polymers such as hydroxypropyl methyl cellulose 15 cps and polyvinyl alcohol (PVA) were included to provide corneal adhesion. Drug incorporated gels were prepared and evaluated for their appearance, pH, gelation temperature, and in vitro drug release studies. Results: Incorporation of the drug into the formulation increased the gelation temperature while the addition of mucoadhesive polymers decreased the gelation temperature. Increasing the concentration of bio-adhesive polymers retarded the release of ofloxacin from the poloxamer solutions and drug release was sustained over a period of 9 h. PVA had no significant effect on the gelation temperature and could not sustain the drug release for a longer duration. The in vitro release profiles of the drug from all the formulations could be best expressed by Higuchi’s equation which indicated that gels followed matrix diffusion process and drug release from gel formulations followed first-order process. Conclusion: The results showed that the developed system would be promising in the treatment of ocular infections with the combined advantages of ease of administration, the accuracy of dosing, increased bioavailability, and prolonged retention time.


2018 ◽  
Vol 5 (1) ◽  
Author(s):  
Erik Wardhana, MM.

This study entitled "Analysis of Effect of Climate Organization and Competence Againt Employee PT. Hutama Karya ". The purpose of this study was to obtain information on the relationship between the free variable that organizational climate (X1) and competence (X2) with the dependent variable is employee performance (Y), either partially or simultaneously, This study used survey research methods with the correlational approach and predictive, which aims for the relationship and influence between independent and dependent variables. The sampling technique can be done randomly (simple random sampling) of 852 employees, which is considered to resprentatif is 89 people. And to solve problems, to analyze and examine the relationship and influence between the independent variables on the dependent variable used models kausalistik through regression analysis with SPSS 14.0


Author(s):  
Yesi Mutia Basri ◽  
Rosliana Rosliana

This research aim to examine the influence of personal background, political background, and council budget knowledge towards the role of DPRD on region financial control. This research is motivated by the fact that individual background will effect to individual behavior on political activity. Dependent variables in this research are personal background, political background, and council budges knowledge towards the role of DPRD on region financial control Independent variables are the role of DPRD on region financial control in planning, implementing, and responsibility steps. The data in this research consist of primary data that taken from questionnaires distributed directly to respondents. The collected are from 34 Respondents that members of DPRD at Pekanbaru. Hypothesis of this research are examine by using Multivariate Analysis of Variances (MANOVA). The result of this research HI personal background political background and budget knowledge have significant influence toward the role of DPRD on region financial control in planning steps.H2 personal background, politico I background and budget knowledge have no significant influence toward the role of DPRD on region financial control in Implementing steps. H3 personal background political background and budget knowledge have no significant influence toward the role of DPRD on region financial control in Controlling steps.


2020 ◽  
Vol 17 (6) ◽  
pp. 523-539
Author(s):  
Jalpa Patel ◽  
Dhaval Mori

Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.


2021 ◽  
Vol 11 (11) ◽  
pp. 5072
Author(s):  
Byung-Kook Koo ◽  
Ji-Won Baek ◽  
Kyung-Yong Chung

Traffic accidents are emerging as a serious social problem in modern society but if the severity of an accident is quickly grasped, countermeasures can be organized efficiently. To solve this problem, the method proposed in this paper derives the MDG (Mean Decrease Gini) coefficient between variables to assess the severity of traffic accidents. Single models are designed to use coefficient, independent variables to determine and predict accident severity. The generated single models are fused using a weighted-voting-based bagging method ensemble to consider various characteristics and avoid overfitting. The variables used for predicting accidents are classified as dependent or independent and the variables that affect the severity of traffic accidents are predicted using the characteristics of causal relationships. Independent variables are classified as categorical and numerical variables. For this reason, a problem arises when the variation among dependent variables is imbalanced. Therefore, a harmonic average is applied to the weights to maintain the variables’ balance and determine the average rate of change. Through this, it is possible to establish objective criteria for determining the severity of traffic accidents, thereby improving reliability.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 646
Author(s):  
Gábor Katona ◽  
Bence Sipos ◽  
Mária Budai-Szűcs ◽  
György Tibor Balogh ◽  
Szilvia Veszelka ◽  
...  

The aim of this study was to develop an intranasal in situ thermo-gelling meloxicam-human serum albumin (MEL-HSA) nanoparticulate formulation applying poloxamer 407 (P407), which can be administered in liquid state into the nostril, and to increase the resistance of the formulation against mucociliary clearance by sol-gel transition on the nasal mucosa, as well as to improve drug absorption. Nanoparticle characterization showed that formulations containing 12–15% w/w P407 met the requirements of intranasal administration. The Z-average (in the range of 180–304 nm), the narrow polydispersity index (PdI, from 0.193 to 0.328), the zeta potential (between −9.4 and −7.0 mV) and the hypotonic osmolality (200–278 mOsmol/L) of MEL-HSA nanoparticles predict enhanced drug absorption through the nasal mucosa. Based on the rheological, muco-adhesion, drug release and permeability studies, the 14% w/w P407 containing formulation (MEL-HSA-P14%) was considered as the optimized formulation, which allows enhanced permeability of MEL through blood–brain barrier-specific lipid fraction. Cell line studies showed no cell damage after 1-h treatment with MEL-HSA-P14% on RPMI 2650 human endothelial cells’ moreover, enhanced permeation (four-fold) of MEL from MEL-HSA-P14% was observed in comparison to pure MEL. Overall, MEL-HSA-P14% can be promising for overcoming the challenges of nasal drug delivery.


2021 ◽  
Vol 43 (2) ◽  
pp. 177-179 ◽  
Author(s):  
Chittaranjan Andrade

Students without prior research experience may not know how to conceptualize and design a study. This article explains how an understanding of the classification and operationalization of variables is the key to the process. Variables describe aspects of the sample that is under study; they are so called because they vary in value from subject to subject in the sample. Variables may be independent or dependent. Independent variables influence the value of other variables; dependent variables are influenced in value by other variables. A hypothesis states an expected relationship between variables. A significant relationship between an independent and dependent variable does not prove cause and effect; the relationship may partly or wholly be explained by one or more confounding variables. Variables need to be operationalized; that is, defined in a way that permits their accurate measurement. These and other concepts are explained with the help of clinically relevant examples.


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