scholarly journals Formulation development and in vitro evaluation of bilayer tablets Nicardipine

2021 ◽  
pp. 40-49
Author(s):  
P.Vamsikrishna ◽  
T.Malyadri ◽  
Ch.Saibabu
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Dosage Form ◽  
Extended Release ◽  
Diffusion Mechanism ◽  
Immediate Release ◽  
Zero Order ◽  
Fickian Diffusion ◽  
Formulation Development ◽  
Pvp K30

The present work aims to develop a stable and optimized bilayer dosage form containing immediate release &extended release drug Nicardapine as an extended-release dosage form. A potent calcium channel blocker with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardio depressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. It has a plasma half-life of about (8.6h) and bioavailability is 15-45% orally. For the formulation of Bilayered tablets polymers such as Ethylcellulose, Sodium CMC, CCS, SSG, Magnesium stearate, Talc, PVP-K30, and MCC. Fourier transform Infrared spectroscopy confirmed the absence of any drug/ polymers/ excipients interactions. Preformulation studies were carried out to optimize the ratios required for various Ethylcellulose, Sodium CMC, CCS, SSG, MCC, and PVP-K30. Based on various evaluation parameters formulation M6 (IR) & M6F3 (SR) were selected as optimized formulation. It was observed that Formulations M6 (IR) & M6F3 (SR) gave maximum drug release within time. All formulations were subjected for drug release kinetics studies viz. Zero-order, First order, Higuchi matrix, Peppasmodel equations, and the formulations of floating sustained-release formulations followed the zero-order release with non-fickian diffusion mechanism. Thus conclusion can be made that a stable dosage form can be developed for  Nicardapine as immediate release & sustained release by Bilayered tablets.

scholarly journals Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Log P ◽  
Physical Parameters ◽  
Direct Compression ◽  
Formulation Development ◽  
Compression Technique

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

SUSTAINED RELEASE MATRIX TABLETS OF DICLOFENAC SODIUM EMPLOYING KOLLIDON SR, PEG 6000, LACTOSE MONO HYDRATE AND EUDRAGIT S100 IN COLON TARGET

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (10) ◽  
pp. 38-43
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
B. Srinivasa Rao ◽  
J. Vijayaratana
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Diclofenac Sodium ◽  
Zero Order ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Colon Targeting ◽  
Zero Order Kinetics ◽  
Eudragit S100 ◽  
Lag Period

Matrix Tablets, each containing 50 mg of diclofenac sodium, are prepared employing Kollidon SR by direct compression method. All the tablets were found to be non-disintegrating in acidic (pH1.2) and alkaline (pH 7.4) fluids. As such, the prepared tablets were of good quality with respect to drug content, hardness and friability. As the tablets formulated were non- disintegrating in acidic fluids, they are considered suitable for colon targeting. From the drug release study, it may be concluded that the (DK2) E2 formula of diclofenac sodium matrix tablets gives the desired release profile by showing a minimal release during the lag period of 5 h and complete release at the end of 12 h. The tablets having the optimised formula (DK2)E2, having 25% Kollidon SR with 5% of channelling agent (Eudragit S100 to that of Kollidon SR) showed minimal release of 27. 4% in the lag period of 5 hours and 99.3 % of the drug was released y the end of 12 h. The diclofenac sodium matrix tablets formulated by employing Kollidon SR and various channelling agents showed non-Fickian diffusion mechanism and followed zero order kinetics. The optimized formula (DK2) E2 follows Supercase II transport as mechanism for drug release and it follows zero order kinetics. Matrix tablets (DK2) E2 formulated employing 25% Kollidon SR and 5% Eudragit S100 are best suited to be used for colon targeting of diclofenac sodium.

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.

scholarly journals Use of Response Surface Methodology in the Formulation and Optimization of Bisoprolol Fumarate Matrix Tablets for Sustained Drug Release

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Jadupati Malakar ◽  
Amit Kumar Nayak ◽  
Soumita Goswami
Keyword(s):  
Response Surface Methodology ◽  
Drug Release ◽  
Sustained Release ◽  
Response Surface ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Order Model ◽  
Sustained Drug Release ◽  
Predicted Values

The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 23 factorial design. The effects of the amounts of calcium alginate, HPMC K4M, and Carbopol 943 in bisoprolol fumarate matrix tablets on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness were analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized bisoprolol fumarate matrix tablets showed prolonged sustained release of bisoprolol fumarate over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.

Development and Evaluation of Gastrobioadhesive Glimepiride Sustained Release Matrix Tablet Using Aegle Marmelos Polysaccharide

2020 ◽  
Vol 14 (1) ◽  
pp. 5297-5306
Author(s):  
M. A. Shende ◽  
Yogesh P Khedkar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Residence Time ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Matrix Tablet ◽  
Aegle Marmelos ◽  
Gastric Residence Time ◽  
Weight Variation

The purpose of present study was to formulate and evaluate glimepiride gastrobioadhesive drug delivery using Aegle Marmelos polysaccharide and synthetic polymer for prolongation of gastric residence time and reduce the dosing frequency. Glimepiride matrices were prepared by direct compression method and evaluated with an aim of presenting glimepiride as sustained release for improving the patient’s compliance. A central composite design (CCD) was employed as Aegle Marmelos polysaccharide (X1) and HPMC K4M (X2) independent variables to optimize the glimepiride in terms of sustained release and gastrobioadhesive. The response (Y1) as bioadhesive strength, (Y2) percentage drug releases at 8 h and (Y3) time (t50) required to 50% drug release were measured for each trial and statistical equations with significant interaction terms were derived to predict relation. The physical properties of all formulations hardness, friability, drug content and weight variation were found within limits indicating that the prepared matrix tablets met the USP specifications. Among all the formulations, F1 formulation found to be optimized based on the criteria of attaining the maximum value of drug released Q8 of 98.58±1.12%, 18.43 g bioadhesive strength and time to 50% drug release (t50) of 6 h. An in-vitro drug release studies reveals that as concentrations of polymers increases the drug release decreases, producing sustained release of glimepiride. The release co-efficient values ‘n’ (˂0.3645) indicated that the drug release (F1) followed fickian diffusion mechanism kinetics. A glimepiride gastroadhesive matrix was developed to enhance its bioavailability by prolonging the gastric residence time with desirable release modulation for a once daily administration.

scholarly journals FORMULATION DEVELOPMENT AND IN VITRO EVALUATION OF ALENDRONATE BUCCAL TABLETS

2019 ◽  
Vol 9 (4-s) ◽  
pp. 363-369
Author(s):  
SANJAY KUMAR GUPTA ◽  
Sradhanjali Patra ◽  
Syed Adnan Akber
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Ethyl Cellulose ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Extensive Literature ◽  
Formulation Development ◽  
Alendronate Sodium ◽  
Buccal Tablets

The aim of this work was to develop a mucoadhesive buccal tablet for the buccal delivery of the alendronate via buccal mucosa. Buccal tablets of alendronate are designed to release drug at mucosal site for extended period of time without wash out of drug by saliva. Alendronate sodium is a bisphosphonates which has antiresorptive effect which is implicated in the prophylaxis and treatment of osteoporosis. Sodium alginate, ethyl cellulose and carbopol were selected as mucoadhesive polymers on the basis of their matrix forming properties. The objective of the study is to improve the bioavailability of alendronate buccal tablets. Extensive literature survey was done for the collection of theoretical and technical data. The methodology part includes the explanation of implemented methods in the present study. In present study, an attempt was made to design mucoadhesive buccal tablets containing alendronate, sodium alginate, ethyl cellulose and carbopol using as polymers. The tablets were prepared by direct compression method. The formulations were evaluated for hardness, thickness, friability, weight variation, drug content estimation, surface pH determination, swelling index, in vitro drug release. In vitro bioadhesive strength & in vitro release studies showed that formulation F11 showed optimum bioadhesive & exhibited optimum drug release 97.6% in 7hr. Kinetics results reveals that the F11 formulation follows zero order kinetics as correlation coefficient (r2) values are higher than that of first- order release kinetics.Optimized formula F11 show drug is released by non-Fickian diffusion mechanism. The stability studies of formulation F11 prepared mucoadhesive buccal tablets of alendronate were stable. Overall evaluations of the mucoadhesive of tablets show good mucoadhesive properties.

scholarly journals Formulation Development and Evaluation of Doxofylline Sustained-Release Tablets by Using Chitosan and Guar Gum

2021 ◽  
pp. 552-567
Author(s):  
Pawan Avhad ◽  
Revathi Gupta
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Dosage Form ◽  
Guar Gum ◽  
The Body ◽  
Natural Polymer ◽  
Natural Polymers ◽  
Formulation Development ◽  
Sustained Release Tablets

The sustained-release dosage form is a well-characterized and reproducible dosage form that is designed to control drug release profile at a certain rate to reach desired drug concentration in blood plasma or at the target site. There is immense demand in the market for new sustained-release formulations used for new drug molecules which release the drug at a sustained rate. Doxofylline is one of the widely useful drugs in the market and needs to be given in a single dose for a long duration of time. For the same, we have prepared a sustained released Doxofylline tablet. Aim: This research was done to design, formulate and evaluate Doxofylline sustained-release tablets by using different concentrations of Chitosan and Guar Gum.  Methods: The factorial design was used to prepare Doxofylline sustained-release tablet. Doxofylline sustained-release tablets were prepared to employ different concentrations of Chitosan, Guar Gum, Lactose, and Magnesium Stearate in different combinations by wet granulation technique. Total 9 formulations were designed, formulated, and evaluated for the hardness, thickness, friability, % drug content, and in-vitro drug release. Results: A study of the release of drug by in-vitro found that F8 is to be the best efficient formulation which consists of both Chitosan and Guar Gum helped in delayed the release of drug up to 24 hours and performs excellent release of drug in starting hours of drug release in the body. The drug released from the F8 formulation indicates the kinetic model of First Order, by anomalous diffusion. The formulation F8 shows optimum thickness, hardness and at 40ºC±2 99.35% drug release after 24 hours shows optimum formulation.  Conclusion: This study concludes that better drug release was observed by using natural polymers.  Doxofylline with natural polymer shows good release and better dissolution rate as compared with a single synthetic polymer. Synthetic drug with natural polymer shows more future scope and this work will help the researcher in the future.

scholarly journals Novel insight into Potential Leishmanicidal Activities of Transdermal Patches of Nigella Sativa: Formulation Development, Physical Characterizations and In vitro In vivo Assays

2021 ◽  
Author(s):  
Barkat Ali Khan ◽  
Yasmin Asmat ◽  
Tariq Hayat Khan ◽  
Mughal Qayum ◽  
Sultan Muhammad Alshahrani ◽  
...  
Keyword(s):  
Drug Release ◽  
Nigella Sativa ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Formulation Development ◽  
Standard Drug ◽  
Drug Permeation ◽  
Transdermal Patches

Abstract Cutaneous Leishmaniasis (CL) is the most common type of Leishmaniasis which annually affects 1.5 million people worldwide. About 90% of cases are reported from countries such as Iran, Afghanistan, Pakistan, Iraq, and Saudi Arabia. The purpose of the present study was to fabricate transdermal patches of Nigella sativa (NS), characterize and to check its in vitro in vivo anti-Lieshmanial activity. Hydroalcohlic extract was analyzed for preliminary phytochemicals. Five formulations of transdermal patches (NS1, NS2, NS3, NS4 and NS5) were prepared by solvent evaporation method. The optimized formulation NS5 was characterized for FTIR, smoothness, brittleness, clarity, thickness, folding endurance, uniformity of weight, percent moisture content, in-vitro drug release, release kinetics, ex vivo drug permeation and in-vitro anti-Lieshmanial activity. In vivo anti-Lieshmanial activity was assessed in 30 patients (n = 30) suffering from CL. The FTIR studies showed no incompatibility among the active extract and polymers. In vitro anti-Lieshmanial assay was 194.6 ± 1.88 % as compared to standard drug (p > 0.05) and in vivo anti-Lieshmanial activity was 75 %. The drug release after 24 hours was 87.0 ± 0.94% in NS5 which showed non-Fickian diffusion mechanism while drug permeation across rabbit skin after 24 hours was up to 80.0 ± 0.91%. The results concluded that problems related to the medications parenterally used for Lieshmanial treatment can be managed by applying extract of Nigella sativa seeds in the form of transdermal patch.

scholarly journals Development and Characterization of Atorvastatin Calcium Sustained Release Tablet Using Carbomer-974 and Hypromellose-15000 cps

2017 ◽  
Vol 9 (2) ◽  
pp. 247-254 ◽  
Author(s):  
S. Akbar ◽  
R. Bhatta ◽  
M. A. Rahman ◽  
M. S. Hossain ◽  
M. S. Bhuiyan ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Diffusion Mechanism ◽  
Zero Order ◽  
Release Profile ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Sustained Release Formulation ◽  
Atorvastatin Calcium

A new sustained release formulation of Atorvastatin Calcium tablet, exhibiting improved swelling property and compatibility to prolong the drug release was prepared. Sustained release tablets were formulated using varying concentration of Carbomer-974 and Hypromellose-15000 cps, by direct compression method. Physical characteristics, compactibility, swelling index and drug content uniformity of the prepared formulations were determined. The drug release studies was carried out in USP dissolution test apparatus II (paddle) using phosphate buffer of pH 6.8 as dissolution medium for 8 hours and documented the effects of polymers on the drug release profile. The release mechanism was explored and explained with Zero order & Higuchi kinetic models. Formulation F1 and F5 were best fitted in the Higuchi model, representing diffusion mechanism of drug release, while Formulations F2, F3 and F4 showed Zero order model of drug release profile. The drug release pattern, compactibility and swelling index property of the formulated preparations were concentration dependent of the polymers used. Further study is necessary to evaluate the in vitro-in vivo relationship, but this study will be helpful for future to exploit the potential of this drug delivery system for the benefit of the mankind.

scholarly journals Formulation Development and Evaluation of Rosuvastatin Sustained Release Tablets

2019 ◽  
pp. 238-247
Author(s):  
Raghavendra Kumar Gunda ◽  
Prasada Rao Manchineni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Dissolution ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Polynomial Equations ◽  
Formulation Development ◽  
Sustained Release Formulation ◽  
Significant Difference

Purpose: The main objective of present research investigation is to formulate the sustained release formulation of Rosuvastatin. Rosuvastatin, an antihyperlipidemic agent, belongs BCS class-II agent.Methods: The SR tablets of Rosuvastatin were prepared employing different concentrations of HPMCK4M and SCMC in different combinations by Direct Compression using 32 factorial design. The concentration of Polymers , HPMCK4M and SCMC required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and  90% (t90%)  were selected as dependent variables.Results and Discussion: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and  the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept, slope & regression coefficient  were calculated. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F4) containing 30 mg of HPMCK4M and 40 mg of SCMC, is the most similar formulation (similarity factor f2= 89.561, dissimilarity factor f1= 1.543 & No significant difference, t= 0.0056) to marketed product (CRESTOR).Conclusion: The selected formulation (F4) follows Zero order, Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.963).

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