scholarly journals FACTORIAL DESIGN USED IN OPTIMIZATION IMMEDIATE RELEASE SOLID DOSAGE RANITIDINE HYDROCHLORIC

2006 ◽  
Vol 28 (62) ◽  
Author(s):  
Antonio Zenon Antunes Teixeira ◽  
Garima Saini ◽  
Alexander Macgregor
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Immediate Release ◽  
Drug Dissolution ◽  
Drug Release Profile ◽  
Solid Dosage ◽  
Significant Difference ◽  
The Difference ◽  
32 Factorial Design ◽  
The Times

The aims of this study were to develop a predictive immediate release tablet formulation system for soluble drugs. Ranitidine hydrochloride, silicifiedmicrocrystallinecellulose (SMCC), polyplasdone XL and hydroxyprophylmethylcellulose (HPMC) E6 were evaluated for powder properties. The effects of binder (HPMC E6) and disintegrant (Polyplasdone XL) were investigated. A 32 factorial design was applied to optimize the drug release profile. The amount of binder and disintegrant were selected as independent variables. The times required for 50% (t50) and 80% (t80) drug dissolution and similarity factor (f2) were chosen as dependent variables. The results of factorial design indicated that a high amount of binder and low amount of disintegrate favored the preparation of drug release. The difference (f1) and similarity (f2) factors were used to measure the relative error and the closeness (similarity) between the factorial design batches and brand name drugs. No significant difference was observed between the brand drug and ranitidine batches F1, F2, F5, F6 and F9. Ranitidine batch F2 yielded the highest value of f2(71%)and the lowest of f1(10%). This research indicates that the proper amount of binder and disintegrant can produce drug dissolution profiles comparable to their brands.

Formulation Development of Aceclofenac Loaded Nanosupension by Three Square (32) Factorial Design

2012 ◽  
Vol 4 (4) ◽  
pp. 1575-1583
Author(s):  
Atul A Patak ◽  
Jorwekar, P ◽  
P D Chaudhari
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
In Vivo Studies ◽  
Differential Scanning Calorimetric ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Calorimetric Analysis ◽  
32 Factorial Design

In the present study, aceclofenac loaded polymeric nanosuspension were formulated and evaluated.  Aceclofenac is a potent analgesic under BCS Class II. Due to the need for its frequent dosing, aceclofenac is an ideal candidate for sustained or controlled drug delivery. For optimization of prepared formulation, the three square (32) factorial design was used.  Tween 80 (X1) and combination of Eudragit RL 100 and RS 100 (X2) were used as independent variables and particle size (Y1), entrapment efficiency (Y2), and Percent drug release (Y3) were taken as dependent variables. The formulations were evaluated for particle size, zeta potential and drug entrapment. The in vitro drug release profile supports nanosuspension form to be used as a sustained release vehicle for aceclofenac. The formulation was characterized by differential scanning calorimetric analysis, in vivo studies and stability testing.

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Water Solubility ◽  
Tween 80 ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Bacterial Conjunctivitis ◽  
Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

In-Vitro Functionality of Clozapine Biphasic Release Minitablet Using Advanced Statistical Tools

2021 ◽  
Vol 11 ◽  
Author(s):  
Hardik Rana ◽  
Rushikesh Chaudhari ◽  
Vaishali Thakkar ◽  
Tejal Gandhi
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Ethyl Cellulose ◽  
Dosage Form ◽  
Immediate Release ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Precipitation Inhibitor

Background: The better control of the drug release with immediate effect is the major concern to achieve better therapeutic action and patient compliance. The failure of the solid dispersion complex during storage as well as in-vivo is another concern for the oral solid dosage form. Objective: The prime objective of the present study was to optimize the biphasic minitablet incorporating quality by design approach using the combination of waxy erodible and water-impermeable excipients. Exploration of Soluplus as a precipitation inhibitor and Dexolve as a solubility enhancer in oral solid dosage form was the secondary objective. Methods: The drug-Excipient compatibility study was assessed by FTIR. Clozapine was chosen as a model drug that has poor aqueous solubility. The complex was formulated using B-cyclodextrin or HP B-CD or Dexolve by kneading method. The screening of solubility enhancers and their amount were performed based on phase solubility study. The precipitation inhibitor was screened as per the parachute effect study. Immediate release minitablets were formulated using a direct compression method using different disintegrating agents. The IR minitablets were evaluated for different evaluation parameters. The sustained release minitablets was formulated by hot-melt granulation technique incorporating the Precirol ATO 5 as a waxy excipient and ethyl cellulose as water impermeable excipient. The SR minitablet was optimized using a central composite design. The amount of Precirol ATO 5 and ethyl cellulose were chosen as independent variables and % drug release at 1, 6, and 10 h was selected as responses. The designed batches were evaluated for different pre and post compressional parameters. The IR and SR minitablets were filled in a capsule as per dose requirement and evaluated for in-vitro drug release. The in-vivo plasma concentration was predicted using the Back calculation of the Wagner – Nelson approach. Results: Drug – Excipient study revealed that no significant interaction was observed. Dexolve was screened as a solubility enhancer for the improvement of the solubility of clozapine. The Soluplus was chosen as a precipitation inhibitor from the parachute effect study. The immediate-release tablet was formulated using Prosolv EASYtab SP yield less disintegration time with better flowability. The sustained release mini-tablet was formulated using Precirol ATO 5 and ethyl cellulose. Two-dimensional and three-dimensional plots were revealed the significant effect of the amount of Precirol ATO 5 and ethyl cellulose. The overlay plot locates the optimized region. The in-vitro drug release study revealed the desired drug release of the final combined formulation. The in-vivo plasma concentration-time confirms the drug release up to 12h. Conclusion: The biphasic mini-tablets were formulated successfully for better control of drug release leads to high patient compliance. The use of soluplus as a precipitation inhibitor is explored in the oral solid dosage form for a poorly aqueous drug. Prosolv EASYtab SP was incorporated in the formulation as super disintegrant. The amount of Precirol ATO 5 and ethyl cellulose had a significant effect on drug release in sustained-release minitablet. The approach can be useful in the industry.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE PATCHES OF NICERGOLINE FOR BUCCAL DRUG DELIVERY BY USING FACTORIAL DESIGN OF EXPERIMENT (DOE)

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (07) ◽  
pp. 52-57
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Design Of Experiment ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Drug Content ◽  
Release Study

The aim of this research was to develop mucoadhesive buccal patches of nicergoline by using Factorial Design of Experiment, in order to provide a sustained release of drug into the systemic circulation. A 33 factorial experimental design was employed for optimization and to study the effect of formulation variables on responses R1 (% swelling index), R2 (% drug content), R3 (mucoadhesion time) and R4 (mucoadhesion strength). In vitro drug release study was performed on the optimized formulations. All the prepared formulations had good mechanical strength, mucoadhesion strength, neutral surface pH and drug content up to 98.17%. In vitro drug release study revealed that F-5 formulation showed promising sustained drug release profile (98.21%) for over 8 h and could be a potential substitute for marketed conventional formulations. The developed formulation (F5) was found to be optimized with considerably good stability and extended drug release profile.

scholarly journals Randomized clinical study comparing active heating methods for prevention of intraoperative hypothermia in gastroenterology

2019 ◽  
Vol 27 ◽  
Author(s):  
Regina Maria da Silva Feu Santos ◽  
Ilka de Fatima Santana Ferreira Boin ◽  
Cristina Aparecida Arivabene Caruy ◽  
Eliane de Araújo Cintra ◽  
Nathalia Agostini Torres ◽  
...  
Keyword(s):  
Categorical Variables ◽  
Chi Square ◽  
Randomized Clinical Study ◽  
Intraoperative Hypothermia ◽  
Forced Air Warming ◽  
Significant Difference ◽  
Chi Square Test ◽  
Intraoperative Period ◽  
The Difference ◽  
The Times

ABSTRACT Objective: to compare the efficacy of three active heating methods in the prevention of intraoperative hypothermia in open gastroenterological surgeries. Method: randomized clinical trial with a sample of 75 patients, whose initial body temperature measured by a tympanic thermometer. Esophageal temperature <36ºC was considered hypothermic. Patients were divided into three groups using: thermal mattress, underbody forced-air warming blanket and heated infusion system. The tympanic and esophageal temperatures were measured at different times of the intraoperative period, but the temperature considered gold standard was the esophageal. To evaluate the homogeneity of the groups, we used chi-square test (categorical variables). In the comparison of temperature measurements over time, the analysis of variance (ANOVA) and the contrast profile test were used for the difference in temperature between the times. The non-parametric Kruskal-Wallis test was used to compare the three groups. The level of significance was 5%. Results: regarding the studied variables, the groups were not homogeneous as to the categorical variable sex. All patients presented hypothermia during the intraoperative period (p> 0.05). Conclusion: there was no significant difference between the heating methods in the prevention of intraoperative hypothermia. REBEC - Brazilian Registry of Clinical Trials (RBR- no. 52shjp).

scholarly journals Crushed Tablets: Does the Administration of Food Vehicles and Thickened Fluids to Aid Medication Swallowing Alter Drug Release?

2014 ◽  
Vol 17 (2) ◽  
pp. 207 ◽  
Author(s):  
Yady Juliana Manrique-Torres ◽  
Danielle J Lee ◽  
Faiza Islam ◽  
Lisa M Nissen ◽  
Julie A.Y. Cichero ◽  
...  
Keyword(s):  
Drug Release ◽  
Orange Juice ◽  
Immediate Release ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Thickening Agents

Purpose. To evaluate the influence of co-administered vehicles on in vitro dissolution in simulated gastric fluid of crushed immediate release tablets as an indicator for potential drug bioavailability compromise. Methods. Release and dissolution of crushed amlodipine, atenolol, carbamazepine and warfarin tablets were tested with six foods and drinks that are frequently used in the clinical setting as mixers for crushed medications (water, orange juice, honey, yoghurt, strawberry jam and water thickened with Easythick powder) in comparison to whole tablets. Five commercial thickening agents (Easythick Advanced, Janbak F, Karicare, Nutilis, Viscaid) at three thickness levels were tested for their effect on the dissolution of crushed atenolol tablets. Results. Atenolol dissolution was unaffected by mixing crushed tablets with thin fluids or food mixers in comparison to whole tablets or crushed tablets in water, but amlodipine was delayed by mixing with jam. Mixing crushed warfarin and carbamazepine tablets with honey, jam or yoghurt caused them to resemble the slow dissolution of whole tablets rather than the faster dissolution of crushed tablets in water or orange juice. Crushing and mixing any of the four medications with thickened water caused a significant delay in dissolution. When tested with atenolol, all types of thickening agents at the greatest thickness significantly restricted dissolution, and products that are primarily based on xanthan gum also delayed dissolution at the intermediate thickness level. Conclusions. Dissolution testing, while simplistic, is a widely used and accepted method for comparing drug release from different formulations as an indicator for in vivo bioavailability. Thickened fluids have the potential to retard drug dissolution when used at the thickest levels. These findings highlight potential clinical implications of the addition of these agents to medications for the purpose of dose delivery and indicate that further investigation of thickened fluids and their potential to influence therapeutic outcomes is warranted. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals FORMULATION AND EVALUATION OF LIDOCAINE HYDROCHLORIDE CHEWABLE TABLET

2018 ◽  
Vol 11 (11) ◽  
pp. 190
Author(s):  
Harshada Anil Kasar ◽  
Asish Dev ◽  
Subhakanta Dhal
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Release Rate ◽  
Statistical Models ◽  
Drug Dissolution ◽  
Lidocaine Hydrochloride ◽  
Dissolution Profile ◽  
Stability Studies ◽  
Drug Release Rate ◽  
Chewable Tablets

Objective: The objective of this study was to formulate and optimize a chewable formulation of lidocaine hydrochloride using a 32 factorial design for optimized the superdisintegrant concentration.Methods: Various concentrations of sodium starch glycolate (SSG) (13.33 mg, 26.66 mg, and 40 mg) of superdisintegrant and starch (50 mg, 83 mg, and 116.66 mg) were added in the formulation; nine formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. The models were tested for significance. Procedure to manufacture chewable tablets by direct compression was established.Results: The results show that the presence of a superdisintegrant is desirable for chewable formulation. The best-optimized batch F7 found the batch having starch of amount 116.66 mg and SSG 13.33 mg. All the prepared batches of tablets were within the range. Optimized batch F7 showed drug content 102.46±0.0543, wetting time 18±1.7320, friability 0.65±0.0216, and drug release rate 99.97±0.0124% at the end of 30 min.Conclusion: It can be concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 is the optimized formulation which compiles official specifications of chewable tablets. The optimized batch was evaluated for thickness, weight variation, hardness, friability, drug dissolution, and stability study for 3 months. The similarity factor was calculated for comparison of dissolution profile before and after stability studies. After 30 min the drug release rate for batch F7 was 98.97% (Table 6). Hence, the results of stability studies reveal that the developed formulation has good stability.

scholarly journals Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DDP-4 Inhibitor

2021 ◽  
Vol 24 (2) ◽  
pp. 168-179
Author(s):  
Tanoy Saha ◽  
Md Mahbubul Alam ◽  
Dilshad Noor Lira ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
Dosage Forms ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Dosage ◽  
Release Tablet

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

Formulation and In vitro Evaluation of Gastroretentive Floating Bioadhesive Tablets of Nizatidine using Factorial Design

2019 ◽  
Vol 9 (3) ◽  
pp. 234-239
Author(s):  
Vidya Sabale ◽  
Hardikkumar Chaudhari ◽  
Prafulla Sabale
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Methyl Cellulose ◽  
Lag Time ◽  
Content Uniformity ◽  
H2 Receptor Antagonist ◽  
Drug Release Profile ◽  
Drug Content ◽  
Weight Variation ◽  
Carbopol 934P

Background: The aim of the present study was to formulate and evaluate floating bioadhesive tablets of Nizatidine which is a competitive, reversible H2-receptor antagonist. Floatingbioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong gastric residence time was prepared. Methods: Polymers used were Hydroxy Propyl Methyl Cellulose (HPMC) K15M as matrix forming water swellable release retarding polymer and carbopol 934P as bioadhesive polymer. The gas generating agents used were sodium bicarbonate and citric acid. The prepared floating bioadhesive tablets of Nizatidine were optimized by 32 factorial design to study independent variable X1 (concentration of CP 934P) and X2 (concentration of HPMC K15M) and dependent variables as floating lag time, cumulative percentage drug release at 12h and swelling index. Tablets were evaluated for various parameters such as hardness, friability, drug content, swelling behavior, floating lag time, bioadhesive strength, drug release profile and stability. Results: All the formulations passed the test for weight variation, hardness, content uniformity and showed acceptable results with respect to drug content (97.93 ± 0.57) and % friability. The tablet containing 25% HPMC K15M and 13.75 % Carbopol 934P was selected as optimized formulation which showed the floating lag time of 74.34±2.08 seconds, drug release of 97.03±0.55% at 12 h (R12h,%), S.I as 79.24±0.87 at 9 h and bioadhesive strength as 10.0023±21.47 g. Stability of the formulation was proved using stability study. Conclusion: The formulated tablets have a potential for controlled release of the drug through floatation and bioadhesion.

scholarly journals Formulation, Characterisation and Evaluation of the Ethosuximide Oral Immediate Release Tablets

2020 ◽  
Vol 11 (2) ◽  
pp. 1807-1813
Author(s):  
Naga Sujan M ◽  
Kunal K Mehta ◽  
Amit B Patil ◽  
Anusha Vajhala
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Immediate Release ◽  
Rice Starch ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Release Studies

The present study is aimed to formulate, characterization, and evaluate oral immediate-release tablets of Ethosuximide. It is employed as an anti-epileptic agent used in the treatment of epilepsy, in all the age groups who were≥ 1 year. The dosage form is formulated by directly compressing the blend and granulating the powder blend by wet granulation methods. The optimized formulation is achieved by the trial and error method by changing the concentration of lactose monohydrate and di-basic calcium phosphate dehydrate as diluents, sodium starch glycolate as Super-dis-integrant, rice Starch as an intra-granular binder, hydroxypropyl cellulose as binder talc as a lubricant. Evaluation parameters such as micrometric properties, disintegration time along with in-vitro drug release studies were performed for characterizing the dosage form. In-vitro drug release studies were carried out using 0.1 N HCl as dissolution media with 75 rpm and temperature of 370C ± 50C by employing USP apparatus II (Paddle type). Estimation of the % drug release of the tablet was carried out using the UV method. The prepared formulation and the marketed formulation were tested for the in-vitro drug release profile and the prepared formulation was compared with the marketed formulation. All the evaluated result was found to be within the specifications. Therefore, from the obtained evaluation results F6 trail was selected as the best formulation.

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