Studying Drug Release through Polymeric Controlled Release Formulations in United States Pharmacopoeia 2 Apparatus Using Multiphysics Simulation and Experiments

Aim: Dosing frequency is a major hurdle in geriatrics with frequent drug administration. In such cases, oral controlled release floating formulations are helpful which causes reduction in dosing frequency and fluctuation of drug levels in plasma. The main aim of the current research was to prepare Captopril floating controlled release formulations in order to achieve extended gastric retention in the upper GIT. Methodology: Captopril tablets were prepared using different concentrations of poly ethylene oxide water soluble resin (PEO WSR) 303 (5% to 30%) by direct compression technique. Captopril formulations CSP1 and CSP6 were formulated using PEO WSR 303. Pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using 0.1N hydrochloric acid as dissolution medium. Results: The dissolution studies showed controlled drug release up to 12h. The formulation CSP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 97.97% at 12h. Almost similar drug release profile was also observed for CSP6 which was prepared using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug in Gastro intestinal tract (GIT). Formulation CSP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation CSP15 showed very less buoyancy lag time of 5sec. Characterization studies like Fourier Transform Infra Red spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) were also carried out. Conclusion: The prepared Captopril floating tablets could be an alternative formulation for prolonged drug release.

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Formulation and Evaluation of Metoprolol Controlled Release Formulations

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i55b33855 ◽

2021 ◽

pp. 122-132

Author(s):

Ramakrishna Vydana ◽

Chandra Sekhar Kothapalli Bonnoth

Keyword(s):

Controlled Release ◽

Drug Release ◽

Sodium Bicarbonate ◽

Research Work ◽

Lag Time ◽

Drug Formulation ◽

Dissolution Studies ◽

Controlled Release Formulations ◽

Characterization Studies ◽

Prolonged Drug Release

Aim: The main perspective of the present research work was to prepare Metoprolol floating controlled release formulations. Methodology: After performing the characterization studies, Metoprolol tablets were prepared using various concentrations of poly ethylene oxide (PEO) WSR 303 (5% to 30%) by direct compression method. Formulations MP1 and MP6 were formulated using PEO WSR 303. Various pre and post compression parameters were evaluated. Dissolution studies were performed for the prepared tablets using dissolution medium of 0.1N hydrochloric acid. Results: Characterization studies like Fourier Transform Infra Red (FTIR) and Scanning Electron Microscopy (SEM) for Metoprolol, Polyethylene oxide WSR 303 and their combination were carried out, which revealed that there is no interaction between drug and polymer. The dissolution studies showed the controlled release pattern of Metoprolol up to 24h. The formulation MP5 prepared using 25% w/w of PEO WSR 303 showed maximum drug release of 98.22% at 24h. Similar drug release profile was observed for MP6 which was formulated using 30%w/w PEO WSR 303. These two formulations were further added with various concentrations of sodium bicarbonate (5% to 15%) and citric acid (2.5% to 10%) which enhanced floating of drug. Formulation MP8 containing 10% of sodium bicarbonate with 25% PEO WSR 303 showed less buoyancy lag time and prolonged drug release. Formulation MP15 showed very less buoyancy lag time of 4sec. Conclusion: Thus the prepared Metoprolol floating tablets showed prolonged drug release which could be a promising formulation for anti-hypertensive patients.

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Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.3.8 ◽

1970 ◽

Vol 9 (3) ◽

pp. 3318-3329

Author(s):

Kranthi Kumar Kotta ◽

L. Srinivas

Keyword(s):

Controlled Release ◽

Drug Release ◽

Xanthan Gum ◽

Diffusion Mechanism ◽

Matrix Tablets ◽

Fickian Diffusion ◽

Content Uniformity ◽

In Vitro Drug Release ◽

Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

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Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.5.6 ◽

2018 ◽

Vol 11 (5) ◽

pp. 4259-4268

Author(s):

Nirmala Rangu ◽

Gande Suresh

Keyword(s):

Controlled Release ◽

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Magnesium Stearate ◽

Zero Order ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Dissolution Profile ◽

Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

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Optimization Study to Develop Once-a-day Controlled Release Formulation of Metoclopramide with Predictable Design Space

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/10.37285/ijpsn.2008.1.1.6 ◽

1970 ◽

Vol 1 (1) ◽

pp. 71-76

Author(s):

Rajesh Dubey ◽

Udaya K. Chowdary ◽

Venkateswarlu V.

Keyword(s):

Controlled Release ◽

Drug Release ◽

Design Space ◽

Release Kinetics ◽

Release Profile ◽

Release Formulation ◽

Linear Effect ◽

Controlled Release Formulation ◽

The Difference ◽

Face Centered

A controlled release formulation of metoclopramide was developed using a combination of hypromellose (HPMC) and hydrogenated castor oil (HCO). Developed formulations released the drug over 20 hr with release kinetics following Higuchi model. Compared to HCO, HPMC showed significantly higher influence in controlling the drug release at initial as well as later phase. The difference in the influence can be explained by the different swelling and erosion behaviour of the polymers. Effect of the polymers on release was optimized using a face-centered central composite design to generate a predictable design space. Statistical analysis of the drug release at various levels indicated a linear effect of the polymers’ levels on the drug release. The release profile of formulations containing the polymer levels at extremes of their ranges in design space was found to be similar to the predicted release profile

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Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

Current Drug Therapy ◽

10.2174/1574885515666200331104440 ◽

2020 ◽

Vol 15 ◽

Author(s):

Balaji Maddiboyina ◽

Vikas Jhawat ◽

Gandhi Sivaraman ◽

Om Prakash Sunnapu ◽

Ramya Krishna Nakkala ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Rate ◽

Zero Order ◽

Water Soluble ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

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