scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF ELEMENTARY OSMOTIC TABLET OF LISINOPRIL DIHYDRATE

2017 ◽  
pp. 20-27
Author(s):  
BHUSHAN A. BHAIRAV ◽  
PRADNYA M. KHANDAGALE ◽  
R. B. SAUDAGAR
Keyword(s):  
Sodium Chloride ◽  
Drug Release ◽  
Release Rate ◽  
Flow Property ◽  
Stability Study ◽  
Formulation Development ◽  
Drug Release Rate ◽  
Accelerated Stability ◽  
Response Percentage

Objective: Lisinopril Dihydrate is one of the antihypertensive drug used to control the high blood pressure. Osmotically Controlled release tablet of Lisinopril Dihydrate was performed for reducing dosing frequency and patient compliance.Methods: Elementary osmotic tablets of Lisinopril Dihydrate were developed using Sodium chloride as a key ingredient which gives osmogent property which provides driving force inside the core tablet and which leads to release of the drug. Microcrystalline cellulose used as a release retardant material in the present work. Different formulations were prepared by varying the concentrations using 32 factorial designs. It was applied to see the effect of variables Sodium chloride (X1) and MCC (X2) on the response percentage drug release as a dependent variable. These formulations were evaluated for, Hardness, Flow property, Thickness, Friability, Drug content and In vitro drug release. Tablets were coated with a semipermeable membrane using 5% w/v cellulose acetate(CA) in acetone and PEG 400(1%) used as Plasticizer. Coated Elementary osmotic tablets were drilled for delivery orifice using a standard micro drill of diameter size 0.8 mm.Results: Drug release rate was increased as the increase in the concentration of sodium chloride and release rate decreased on increasing the concentration of MCC. Drug release rate was directly proportional to delivery orifice size. SEM Study carried out for detection of diameter size of the delivery orifice. The FTIR studies demonstrate that there was no interaction between polymer and drug.Conclusion: The optimized formulation was stable for 3 mo of accelerated stability study

Effects of Four Mesostructures on their Drug Release Properties

2013 ◽  
Vol 645 ◽  
pp. 125-128
Author(s):  
Wei Zeng
Keyword(s):  
Drug Release ◽  
Mesoporous Materials ◽  
Release Rate ◽  
Drug Efficacy ◽  
Drug Release Rate ◽  
Ordered Mesoporous Materials ◽  
Ordered Mesoporous ◽  
Fast Release ◽  
Mcm 41

Five ordered mesoporous materials, SBA-1, MCM-48, SBA-7, MCM-41 and SBA-15, were prepared and tested as mesophase drug delivery systems with an anti-inflammatory drug, ibuprofen. The results of these mesostructures on in vitro ibuprofen delivery indicated that the mesoporous materials with cage-like structure, SBA-1 and SBA-7, had unfavorable load and release properties. MCM-48 also showed fast release rate due to its opening channel. However, the hexagonal mesostructure in MCM-41 and SAB-15 was advantageous for extending drug release rate although a little difference existed between them. Compared with commercial ibuprofen capsule, the release system based on MCM-41 materials displayed the drug efficacy in a longer time.

Development of Acrylic Matrix Type Ketoprofen Patch

2012 ◽  
Vol 506 ◽  
pp. 533-536
Author(s):  
Nanthida Wonglertnirant ◽  
S. Tipwichai ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Pressure Sensitive Adhesive ◽  
Drug Release Rate ◽  
Matrix Type ◽  
Adhesive Matrix ◽  
Pressure Sensitive ◽  
Transdermal Patches ◽  
Significant Difference

Ketoprofen transdermal patches (KTPs) were fabricated using an acrylic pressure sensitive adhesive (PSA) polymer. The influence of different factors (amount of PSA, drug content, and pressure applying on the backing membrane during preparation) on the characteristics of ketoprofen patch (thickness, W/A ratio, and adhesiveness of matrix film) and in vitro drug release behavior were investigated. The results revealed the successful fabrication and a good physical appearance of KTPs using acrylic PSA. Microscopic observations, FTIR spectra, and DSC thermograms were permitted to demonstrate that the drug was dispersed molecularly in the polymer. As the amount of PSA in the adhesive matrix was increased, the release rate of ketoprofen was decreased. Contrarily, the drug release rate was increased corresponding to the increase of ketoprofen content in the adhesive matrix. There was no significant difference in the release rate when the pressure applying on the backing membrane was varied. The kinetic of ketoprofen release from acrylic matrix type transdermal patches followed the Higuchis diffusion model.

scholarly journals DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

Design, Development and Optimization of Pulsatile Core in Cup Tablets of Naproxen

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
Rutu H. Patel ◽  
ImadHadi Hameed ◽  
Kunal N. Patel ◽  
Madhabhai M. Patel
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Major Effect ◽  
Stability Study ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
Accelerated Stability ◽  
Excipient Compatibility

The aim of the present study to prepare Pulsatile release tablet of naproxen for the treatment of rheumatoid arthritis. The drug delivery system was designed to deliver the drug at a time when it could be most needful for the patient. Drug excipient compatibility studies were carried out using DSC and found to be compatible with each other. Pulsatile tablet was prepared by direct compression method using different type and amount of superdisintegrants and coating polymers and evaluated for pre and post compression parameters. Box Behnken design was applied to optimize responses. Concentrations of Sodium starch glycolate (SSG) (X1), Ethyl cellulose (EC) (X2), and HPMC K100M (X3) were selected as independent variables while Lag time (Y1) and % drug release at 8 hrs (Y2) were selected as dependent variables. The prepared tablets were evaluated for post compression parameters and results indicated that concentration of SSG has major effect on in vitro drug release while concentration of EC and HPMC K100M has major effect on Lag time. Batch BE13 prepared with SSG 35mg, EC 175mg, and HPMC K100M 75 mg was found to be best batch as it achieves predetermined lag time of 5 hr 02 min and 99.32% of drug release. There was no significant variation in formulation at the end of six month accelerated stability study.

scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals Drug release rate in vitro and bioavailability of new controlled release suspension of spherical matrix of ibuprofen.

1989 ◽  
Vol 4 (2) ◽  
pp. 100-104
Author(s):  
Yoshiaki Kawashima ◽  
Taro Iwamoto ◽  
Toshiyuki Niwa ◽  
Hirofumi Takeuchi ◽  
Tomoaki Hino ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate

scholarly journals Liqui-Tablet: the Innovative Oral Dosage Form Using the Newly Developed Liqui-Mass Technology

2021 ◽  
Vol 22 (3) ◽  
Author(s):  
Matthew Lam ◽  
Kofi Asare-Addo ◽  
Ali Nokhodchi
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Dosage Form ◽  
Oral Dosage ◽  
Dissolution Profile ◽  
Drug Release Rate ◽  
Accelerated Stability ◽  
Micro Tomography ◽  
Distribution Of Components ◽  
Tablet Dosage

AbstractIn this study, an attempt was made to produce Liqui-Tablets for the first time. This was carried out through the compaction of naproxen Liqui-Pellets. The incentive to convert the novel Liqui-Pellet into Liqui-Tablet was due to the array of inherent advantages of the popular and preferred tablet dosage form. The study showed that naproxen Liqui-Tablet could be successfully produced and the rapid drug release rate (100% drug release ~ 20 min) could be achieved under pH 1.2, where naproxen is insoluble. It was observed that the different pH of the dissolution medium affected the trend of drug release from formulations with varying amounts of liquid vehicle. The order of the fastest drug-releasing formulations was different depending on the pH used. The presence of Neusilin US2 showed considerable enhancement in the drug release rate as well as improving Liqui-Tablet robustness and hardness. Furthermore, images from X-ray micro-tomography displayed a uniform distribution of components in the Liqui-Tablet. The accelerated stability studies showed acceptable stability in terms of dissolution profile.

scholarly journals Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Himanshu Bhatt ◽  
Bhargavi Naik ◽  
Abhay Dharamsi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Statistical Design ◽  
Aqueous Solubility ◽  
Stability Study ◽  
Design Variables ◽  
Accelerated Stability ◽  
Eudragit S100 ◽  
Enteric Polymers

The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in Cmax⁡ and Tmax⁡ found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release.

scholarly journals Factors affecting performance and manufacturability of naproxen Liqui-Pellet

2020 ◽  
Vol 28 (2) ◽  
pp. 567-579
Author(s):  
Matthew Lam ◽  
Ali Nokhodchi
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Flow Property ◽  
Major Effect ◽  
Coating Material ◽  
Drug Release Profile ◽  
Pellet Size ◽  
Drug Release Rate ◽  
R Value ◽  
Pellet Formulation

Abstract Aim Liqui-Pellet is potentially an emerging next-generation oral pill, which has shown promising results with unique advantages as well as displaying potential for commercial feasibility. Since Liqui-Pellet technology is still in its infancy, it is important to explore the parameters that can affect its performance, particularly the drug release rate. Therefore, the aim of this study is to investigate thoroughly the effect of Avicel PH101 (carrier) and Aerosil 300 (coating material) ratio (R-value) in Liqui-Pellet. Methods Key parameter for Liqui-Pellet formulation in this study was the ratio of carrier and coating material. Tests were carried out to assess the physicochemical properties of different formulations. This involved looking into particle size, robustness, flowability, solid-state and drug release profile. The morphology of Liqui-Pellet was investigated by SEM. Results It is found that R-value does not have a major effect on the success of Liqui-Pellet production. However, R-value does seem to have an effect on Liqui-Pellet size at a certain water content level and a slight effect on the drug release rate. A decrease in Avicel PH101 concentration and an increase in Aerosil 300 concentration in Liqui-Pellet formulations can reduce Liqui-Pellet size and slightly increase drug release rate by 9% after 2 h. The data shows Liqui-Pellet is resistant to friability, able to achieve exceptional flow property and have smooth surfaces, which is critical for applying coatings technology. Such properties are ideal in terms of commercial manufacturing. The XRPD and DSC both show the reduction in formulation crystallinity, which is expected in Liqui-Pellet formulation as a result of solubility of the drug in the co-solvent used in the preparation of Liqui-Pellets. Conclusion Overall it seems that R-value can affect Liqui-Pellet drug release rate and size but not on the production success rate. Graphical abstract

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