scholarly journals FORMULATION AND EVALUATION OF COMPRESSION COATING FLOATING TABLETS OF CARVEDILOL PHOSPHATE ONCE DAILY DOSE

2018 ◽  
Vol 10 (6) ◽  
pp. 82
Author(s):  
Subhranshu Panda ◽  
C. H. Surya Kumari ◽  
G. Puniya
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Dosage Form ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Immediate Release ◽  
Once Daily ◽  
Daily Dose ◽  
Compression Coating ◽  
Gastro Retentive

Objective: The rationale for the study was to develop a once-daily dose of immediate as well as a gastro-retentive form of carvedilol phosphate by compression coating floating technique.Methods: In the presented study the core tablet was containing half the quantity of the drug formulated as floating drug delivery using different controlled release polymers blend in various proportions like ethyl cellulose, carbopol, hydroxypropyl methylcellulose (HPMC) K4, K15, and K100 by direct compression method. Outer coat layer was formulated with rest of the drug with the blend of different super disintegrants in various proportions like crospovidone, croscarmellose sodium (CCS), sodium starch glycolate (SSG) for the immediate release of the drug. Both the immediate and controlled formulation was separately formulated from sf1 to sf9 and f1 to f9 respectively. Based on the evaluation parameters finally, formulation F1 to F9 were formulated by applying compression coating floating method. These formulations were characterized for their tablet density, disintegration time, floating lag time, in vitro drug release, drug-excipients interaction and accelerated stability studies etc.Results: The result revealed formulation sf9 containing SSG of 15% was able to 97.2% of drug release within 15 min towards the achievement of immediate release. Similarly, the formulation f9 containing 0.5:0.5:4.5 ratios of ethyl cellulose, carbopol and HPMC K15 was able to 95.3% of drug release within 16h. From compressed coat tablets batches of F1 to F9, based on the dissolution data F9 was considered as an optimized formulation which was able to release 48.6% of drug release within 15 min and cumulatively controlled the release up to 96.4% for 16 h, followed zero-order kinetics and Higuchi pattern.Conclusion: The results obtained in this research work clearly indicated that the compression coating floating tablet of carvedilol phosphate was the best dosage form for the treatment of hypertension. Results of the evaluation of prepared batches indicate that the batch F9 is a promising formulation for both a quick onset of action as well as gastro-retentive dosage form to maintain the constant drug action which would improve the maximum therapeutic efficacy and patient compliance.

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 FORMULATION OPTIMIZATION OF PROMETHAZINE THEOCLATE IMMEDIATE RELEASE PELLETS BY USING EXTRUSION-SPHERONIZATION TECHNIQUE

2018 ◽  
Vol 10 (1) ◽  
pp. 30
Author(s):  
Shelar Vishwas S. ◽  
Shirolkar Satish V. ◽  
Kale Rupali N.
Keyword(s):  
Drug Release ◽  
Motion Sickness ◽  
Dosage Form ◽  
Corn Starch ◽  
Research Work ◽  
Immediate Release ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Extrusion Spheronization ◽  
Pellet Formulation

Objective: Promethazine theoclate is a BCS Class II drug having anti-histaminic property and mainly used for the treatment of motion sickness and postoperative emesis. The main objective of the research work was to formulate and optimize immediate release pellets of promethazine theoclate by using the extrusion-spheronization technique to offer immediate release dosage form suitable for treatment of nausea and vomiting associated with motion sickness and post-operative conditions.Methods: Immediate release pellets of promethazine theoclate were prepared by using microcrystalline cellulose (MCC) and corn starch as filler and disintegrant respectively along with other excipients. Pellet formulation was further optimized for bulk density, disintegration time and percent drug release after 10 min. using 32 factorial design. Formulations were also characterized for drug-polymer interactions using Differential Scanning Calorimetry (DSC), surface morphology by Scanning Electron Microscopy (SEM) and other physicochemical properties.Results: Optimised pellet formulation contains 2.5:4.5:1 ratio of MCC: Corn Starch: Drug and spheronization time of 60 seconds showing highest percent yield of 78% and immediate drug release of 100.52±0.65% after 10 min.Conclusion: Promethazine theoclate pellets formulated in this study can serve as an alternative to tablet dosage form which can give immediate drug release for treatment of motion sickness and postoperative emesis.

scholarly journals EFFECT OF POLYMERS ON THE PHYSICOCHEMICAL AND DRUG RELEASE PROPERTIES OF TRANSDERMAL PATCHES OF ATENOLOL

2018 ◽  
Vol 10 (4) ◽  
pp. 68
Author(s):  
Manish Kumar ◽  
Vishal Trivedi ◽  
Ajay Kumar Shukla ◽  
Suresh Kumar Dev
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
High Moisture ◽  
Transdermal Drug Delivery System ◽  
Permeable Membrane ◽  
Transdermal Patches ◽  
Egg Membrane ◽  
Hydrophilicity And Hydrophobicity

Objective: The objective of this research work was to develop a transdermal drug delivery system containing atenolol with different ratios of hydrophilic and hydrophobic polymeric combinations, using solvent evaporation technique and to examine the effect of hydrophilicity and hydrophobicity of polymers on the physicochemical and drug release properties of transdermal patches.Methods: Solvent casting method has been used to formulate transdermal patches. Hydroxypropyl methylcellulose (HPMC), Polyvinylpyrrolidone (PVP), Ethylcellulose (EC) in different combination ratios were used as the polymer. Propylene glycol was used as a plasticizer. Permeation enhancers such as span 80 were used to enhance permeation through the skin. In vitro diffusion study was carried out by franz diffusion cell using egg membrane as a semi-permeable membrane for diffusion.Results: Result showed that the thickness of the all batch of patches varied from 0.32 to 0.39 mm with uniformity of thickness in each formulation. Formulations F1 to F3 had high moisture content varied from 2.07±0.09 to 2.56±0.15 and high moisture uptake value varied from 3.21±0.35 to 4.09±0.38, due to a higher concentration of hydrophilic polymers. Drug content of all batches was ranged between 85.92±1.32 to 95.71±1.42. Folding endurance values off all batches were more than 75. Formulation batches F1 to F3 showed higher cumulative drug release varied from 61.34% to 68.11% as compared to formulation batches F4 to F6.Conclusion: Higher proportion of hydrophilic polymer in the formulation of transdermal patches, gives higher percentage drug release from prepared patches. The finding of the study indicates that hydrophilicity and hydrophobicity of polymer effects the physicochemical and drug release properties of transdermal patches and an optimum proportion of hydrophilic and hydrophobic polymer is required for the preparation of effective transdermal patches. 

scholarly journals Formulation and investigation of crushed puffed rice-chitosan-HPMC based polymeric blends as carrier for sustained stomach specific drug delivery of piroxicam using 3(2) Taguchi mathematical design studies

2018 ◽  
Vol 6 (11) ◽  
pp. 61-80 ◽  
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Pharmaceutical Journal ◽  
Weight Variation ◽  
Zero Order Release ◽  
Puffed Rice

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf

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.

scholarly journals Felodipine β-cyclodextrin complex as an active core for time delayed chronotherapeutic treatment of hypertension

2012 ◽  
Vol 62 (3) ◽  
pp. 395-410 ◽  
Author(s):  
Kunal P. Pagar ◽  
Pradeep R. Vavia
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Coating Layer ◽  
Research Work ◽  
Fold Increase ◽  
Lag Time ◽  
Dissolution Enhancement ◽  
Cyclodextrin Complex ◽  
Nmr Studies ◽  
Active Core

The present research work deals with the development of a time delayed chronotherapeutic formulation of felodipine (FD) aimed at rapid drug release after a desired lag time in the management of hypertension. The developed system comprises a drug core embedded within a swellable layer and coated with an insoluble, water permeable polymeric system. FD cyclodextrin complex was used as an active core while ethyl cellulose was used as an effective coating layer. Dissolution studies of the complex revealed that there was a 3-fold increase in dissolution of the complex compared to plain FD. This dissolution enhancement and rapid drug release resulted from FD amorphisation, as confirmed by XRD, DSC and SEM studies. FTIR and 1H NMR studies confirmed the complex formation between FD and cyclodextrin based on the observed hydrogen bond interactions. FD release was adequately adjusted by using a pH independent polymer, i.e., ethyl cellulose, along with dibutyl phthalate as plasticizer. Influence of formulation variables like polymer viscosity, plasticizer concentration, super disintegrant concentration in the swellable layer and percent coating weight gain was investigated to characterize the lag time. Upon permeation of water, the core tablet swelled, resulting in the rupture of the coating layer, followed by rapid drug release. The developed formulation of FD showed a lag time of 5-7 h, which is desirable for chronotherapeutic application.

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablet of Itopride

2021 ◽  
Vol 11 (5) ◽  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Ethyl Cellulose ◽  
Chemical Interaction ◽  
Research Work ◽  
Matrix Tablets ◽  
Crystalline Cellulose ◽  
Matrix Tablet ◽  
Natural Polymers ◽  
Drug Release Profile

The objective of this research work was to carry out design and evaluation of sustained release matrix tablets of Itopride by use of natural and synthetic polymers. Matrix tablets were prepared by wet granulation technique by using natural polymers like Carbopol 934, Tamarind poly saccharide, Locust bean gum, Ethyl cellulose, HPMC K 100 as matrix forming agent and excipients such as Lactose, Starch 1500, Magnesium stearate, MCC and talc were used. The dissolution medium consisted of 900 ml of 0.1 N HCl for first 2 hours and then 7.4 phosphate buffer for remaining 10 hours. The release of Itopride from matrix containing lactose, micro crystalline cellulose and starch 1500 as diluents. The drug release rate was found in order of lactose> micro crystalline cellulose>starch 1500. The formulation was optimized on the basis of acceptable tablet properties and in-vitro drug release. The release data were fit into different kinetic models (zero-order, first- order, Higuchi’s equation and Korsmeyer-Peppas equation). Optimized formulation was tested for their compatibility with Itopride by FT-IR studies, which revealed that there is no chemical interaction occurred with polymer and other excipients. The drug release profile of the best formulation was well controlled and uniform throughout the dissolution studies. Keywords: Matrix tablets, Itopride, Carbopol 934, HPMC K 100, Ethyl cellulose.

scholarly journals Gastro-retentive floating beads of curcumin β-cyclodextrin complex to treat stomach tumors

2011 ◽  
Vol 1 (1) ◽  
pp. 12 ◽  
Author(s):  
Shishu Goindi ◽  
Kamalpreet Mann ◽  
Nidhi Aggarwal
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Solubility ◽  
Pharmacokinetic Studies ◽  
Cyclodextrin Complex ◽  
Enhanced Solubility ◽  
Tumor Studies ◽  
Gastro Retentive

The aim of present study was to develop a multi-unit gastro-retentive floating dosage form of curcumin with targeted and sustained release characteristics. Although, protective effect of curcumin against inflammation and cancer is well documented, the clinical potential is underutilized owing to the physicochemical properties of the molecule which lead to poor oral bioavailability. Aqueous solubility of curcumin was enhanced by complex formation with β-cyclodextrin (β-CD). This complex with enhanced solubility profile was further used to prepare multiple unit floating beads. Floating beads of curcumin β-cyclodextrin complex (FBCC) were prepared by dripping a mixture of sodium alginate and hydroxypropyl methylcellulose solution into calcium chloride solution acidified with acetic acid. FBCC were evaluated for percent drug entrapment, diameter, surface topography, buoyancy,<em> in vitro</em> release and pharmacodynamic activity against Benzo(a) pyrene [B(a)P] induced forestomach papillomas in albino female mice (Balb/C strain). The investigation revealed that floating beads possessed optimum formulation characteristics. The drug release from FBCC was fickian and sufficiently sustained for 12 h. Results of antitumor studies against B(a)P induced neoplasia of forestomach suggests that the tumor incidence significantly reduced (50%) using FBCC where as pure curcumin resulted in only 25% reduction. A multi-unit floating dosage form of curcumin β-CD complex possessing sustained release characteristics was developed for targeting gastric tumors. Results of i<em>n vitro</em> studies and anti-tumor studies in animals suggest that FBCC can be safely and effectively used to treat neoplasia of stomach. However, these preliminary investigations warrant further pharmacokinetic studies and clinical evaluation in humans

scholarly journals Once daily baclofen sustained release or gastro-retentive system are acceptable alternatives to thrice daily baclofen immediate release at same daily dosage in patients

2009 ◽  
Vol 57 (3) ◽  
pp. 295 ◽  
Author(s):  
ShravantiS Bhowmik ◽  
NitinG Sampat ◽  
RahulV Kulkarni ◽  
Nathaniel Sase ◽  
NishithH Joshi ◽  
...  
Keyword(s):  
Sustained Release ◽  
Immediate Release ◽  
Once Daily ◽  
Gastro Retentive

scholarly journals Cardiometabolic and psychological effects of dual-release hydrocortisone: a cross-over study

2021 ◽  
Vol 184 (2) ◽  
pp. 253-265
Author(s):  
Rosemary Dineen ◽  
Julie Martin-Grace ◽  
Khalid Mohamed Saeed Ahmed ◽  
Isolda Frizelle ◽  
Anjuli Gunness ◽  
...  
Keyword(s):  
Cardiometabolic Risk ◽  
Unmet Needs ◽  
Immediate Release ◽  
Dose Equivalent ◽  
Once Daily ◽  
Cardiovascular Morbidity And Mortality ◽  
Daily Dose ◽  
The Mean ◽  
Dual Release

Background Adrenal insufficiency (AI) is associated with increased cardiovascular morbidity and mortality and reduced quality of life (QoL). Optimum glucocorticoid (GC) dosing and timing are crucial in the treatment of AI, yet the natural circadian secretion of cortisol is difficult to mimic. The once-daily dual-release hydrocortisone (DR-HC) preparation (Plenadren®), offers a more physiological cortisol profile and may address unmet needs. Methods An investigator-initiated, prospective, cross-over study in patients with AI. Following baseline assessment of cardiometabolic risk factors and QoL, patients switched from their usual hydrocortisone regimen to a once-daily dose equivalent of DR-HC and were reassessed after 12 weeks of treatment. Results Fifty-one patients (21 PAI/30 SAI) completed the study. Mean age was 41.6 years (s.d. 13), and 58% (n = 30) were male. The median daily HC dose before study entry was 20 mg (IQR 15–20 mg). After 3 months on DR-HC, the mean SBP decreased by 5.7 mmHg, P = 0.0019 and DBP decreased by 4.5 mmHg, P = 0.0011. There was also a significant reduction in mean body weight (−1.23 kg, P = 0.006) and BMI (−0.3 kg/m2, P = 0.003). In a sub-analysis, there was a greater reduction in SBP observed in patients with SAI when compared to PAI post-DR-HC. Patients reported significant improvements in QoL using three validated QoL questionnaires, with a greater improvement in PAI. Conclusion Dual-release hydrocortisone decreases BP, weight and BMI compared with conventional HC treatment, even at physiological GC replacement doses. Additionally, DR-HC confers significant improvements in QoL compared to immediate-release HC, particularly in patients with PAI, which is also reflected in the patient preference for DR-HC.

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