scholarly journals APPLICATION OF NOVEL NATURAL POLYMER FOR CONTROLLING THE RELEASE OF FENOVERINE FROM CONTROLLED RELEASE MATRIX TABLETS

2017 ◽  
Vol 9 (2) ◽  
pp. 1 ◽  
Author(s):  
Ajit Kulkarni ◽  
Trushali Mandhare ◽  
Nagesh Aloorkar
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Natural Polymer ◽  
In Vitro Drug Release ◽  
Dissolution Studies ◽  
Drug Content

Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices.Methods: In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study.Conclusion: Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.Keywords: Pullulan, Fenoverine, Hydroxypropyl methyl cellulose, Controlled release, In vitro

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

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.

FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 27-35
Author(s):  
A. A Bakliwal ◽  
◽  
D. S. Jat ◽  
S. G. Talele ◽  
A. G. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Synthesis Method ◽  
Ultra Sound ◽  
Size Analysis ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals SOLUBILITY ENHANCEMENT OF CELECOXIB BY SOLID DISPERSION TECHNIQUE AND INCORPORATION INTO TOPICAL GEL

2019 ◽  
pp. 294-300
Author(s):  
AMRIN SHAIKH ◽  
PRASHANT BHIDE ◽  
REESHWA NACHINOLKAR
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
In Vitro Drug Release ◽  
Peg 6000 ◽  
Topical Gel ◽  
Drug Content ◽  
Vitro Release

Objective: The aim of the present investigation was to design gels for the topical delivery of celecoxib and evaluate with an aim to increase its penetration through the skin and thereby its flux. Method: The solubility of celecoxib is shown to be increased by preparing solid dispersions (SDs) using carriers such as mannitol, polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG) 6000 and urea by solvent evaporation, fusion, and coevaporation methods. In vitro release profile of all SD was comparatively evaluated and studied against the pure drug. The prepared SD was subjected for percent practical yield, drug content, infrared spectroscopy, differential scanning calorimetry analysis, X-ray diffraction studies, and scanning electron microscopy (SEM) imaging. The celecoxib gel was prepared using hydroxypropyl methyl cellulose (HPMC) and Carbopol containing a permeation enhancer dimethyl sulfoxide (DMSO) at different proportions and evaluated for drug content, pH, viscosity, spreadability, extrudability, stability, and in vitro drug release. Results: Faster dissolution rate was exhibited by SD containing 1:5 ratio of celecoxib: PVP K-30 prepared by coevaporation method. In vitro drug release of celecoxib, gels revealed that formulation with HPMC has higher drug release as compared to Carbopol. Conclusion: The increase in dissolution rate for SD is observed in the following order of PVP K-30>urea>mannitol>PEG 6000. The CPD5 gel containing a SD CP5 and 20% DMSO showed the best in vitro release 74.13% at the end of 6 h.

scholarly journals Development and Characterization of Ofloxacin & Prednisolone Loaded Nanostructured Lipid Carriers (Nlc) for Topical Route

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Morphological Characteristics ◽  
Nanostructured Lipid Carriers ◽  
Diffusion Method ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Aim: The present study was designed to develop and characterize nanostructured lipid carriers (NLC) of Ofloxacin and Prednisolone for topical use in case of infections associated with inflammation. Materials and Methods: Ofloxacin was obtained as gift sample from Mankind Pharma Ltd, VillKyarta, P.O. Misserwal, Poonta Sahib, Sir Mour. H.P. Whereas Prednisolone was purchased from Yarrow chem., Mumbai. It was evaluated for its pre-formulation studies (organoleptic properties, melting point, solubility, compatibility, max. wavelength of absorption). NLCs were prepared through melt-emulsification followed by ultra-sonication technique. Further optimized batch of NLCs was incorporated into Gel. Formulated NLCs were evaluated in terms of morphological characteristics, particle size (Polydispersity Index), drug content, In-vitro drug release (using egg membrane), drug release kinetics (Ritger-Peppas diffusion method). Finally, gel containing NLCs was studied by physical characteristics, pH, viscosity, spreadability, drug content, In-vitro drug release and its kinetics. Results and Discussion: In pre-formulation study, drugs were found having the similar properties as described in Indian Pharmacopoeia (IP) and United States Pharmacopoeia (USP). SEM photomicrograph revealed that NLCs were spherical with more or less smooth surface; particle size 512.3-1703 nm and PDI- 0.399-0.742 (ofloxacin) and particle size 539.3-1736.7 nm and PDI- 0.335 - 0.711 (prednisolone);drug content was found in range of 56.7 - 75.6% for ofloxacin and 65.9 – 81.8% for prednisolone. NLC1 demonstrated maximum release rate with 83.37±1.70% and NLC8 73.96±0.53%.NLC6 was best fitted in Korsmeyer - peppas model as the regression coefficients were 0.960, 0.964, 0.977, 0.950, 0.980 & 0.987 respectively and prednisolone NLC 9 (0.953) and they were close to 1. Conclusion: In conclusion, the prepared NLCs had prolonged release effects with good potential for topical delivery of NLC based gel formulation of ofloxacin& prednisolone.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION

2018 ◽  
Vol 11 (6) ◽  
pp. 148
Author(s):  
Srinivasa Rao Baratam ◽  
Vijayaratna J
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Linear Regression Method ◽  
In Vitro Drug Release ◽  
Sustained Drug Delivery

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

2021 ◽  
pp. 4429-4434
Author(s):  
C.C. Patil ◽  
J. Vekatesh ◽  
S. R Karajgi ◽  
Vijapure Vitthal ◽  
Ashwini G. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Fourier Transforms ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

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