Implementation of time release technology in formulation development and evaluation of sustained release tablet of Lornoxicam

In present study, the attempts have been made to formulate sustained release tablets of lornoxicam by direct compression method. Based on viscosity grades different proportions of hydrophilic polymers (HPMC K4M, HPMC K15M, HPMC K100M) are used for preparation of lornoxicam sustained release matrix tablet. The drug excipient mixtures were subjected to preformulation studies comprising of micromeritic properties. The tablets were subjected to various studies like as physicochemical studies, in vitro drug release, kinetic studies, etc. FTIR studies shown there was no interaction between drug and polymers. The physicochemical properties of tablets were found within the limits. Lornoxicam is a first generation analgesic, inflammatory and antipyretic agent used in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. From developed formulations batch F1 have shown zero order drug release behavior and prolong drug release over a period of 12 h which was deemed as suitable and optimum formulation for sustained drug delivery. Results of the present study indicated the suitability of the low viscous polymer in the proportion of (drug:polymer) 1:1 in the preparation of sustained release formulation of lornoxicam.

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Preparation, Characterization and In Vitro Evaluation of IVM Loaded Poly(lactic-Co-Glycolic Acid) (PLGA) Microspheres

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.311-313.1751 ◽

2011 ◽

Vol 311-313 ◽

pp. 1751-1754

Author(s):

Gui Yu Li ◽

Xi Hong Lu ◽

Xue Hu Li ◽

Lei Tao ◽

Jian Ping Liang

Keyword(s):

Drug Release ◽

Sustained Release ◽

High Performance ◽

Glycolic Acid ◽

Drug Release Profile ◽

Release Formulation ◽

Sustained Release Formulation ◽

Drug Delivery Carrier ◽

Drug Sustained Release

Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.

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Development and Characterization of Glipizide Loaded Sustained Release Nanoparticles

Current Nanomedicine ◽

10.2174/2468187309666190620145438 ◽

2019 ◽

Vol 9 (3) ◽

pp. 232-242 ◽

Cited By ~ 1

Author(s):

Rutuja Deshmukh ◽

Mrunal Waghulde ◽

Satyendra Mishra ◽

Jitendra Naik

Keyword(s):

Drug Release ◽

Sustained Release ◽

Drug Uptake ◽

Sustained Drug Release ◽

Release Formulation ◽

Sustained Release Formulation ◽

Fourier Transformed Infrared Spectroscopy ◽

Wide Range ◽

Repeated Dosing

Background: Treating the disease like diabetes is essential due to its wide range of spreading and heredity issues. Glipizide is the commonly used drug for the treatment of diabetes. Glipizide loaded sustained release nanoparticles have been developed to avoid repeated dosing. Objective: The study aimed to develop glipizide-loaded sustained release nanoparticles and characterize them for different studies. Methods: The aim of the present study was to develop glipizide-loaded sustained release nanoparticles using different polymers by the solvent evaporation method. The polymers; Eudragit (RS 100) in combination with Polycaprolactone (PCL) were used to encapsulate glipizide. Optimization of all parameters was performed as per Design Expert software by utilizing a 32 full factorial design. The developed nanoparticles were characterized using Fourier transformed infrared spectroscopy, X-ray diffraction, scanning electron microscopy and in-vitro drug release study. Results: FE-SEM showed that the surface morphology of nanoparticles was smooth and spherical as well as in an oval shape. FTIR shows there is no interaction between polymers and drug. XRD results showed that the crystallinity of pure glipizide reduced from 89.5 to 56.7% when converted into sustained release nanoparticles formulation. Sustained drug release over the period of 12 h was observed due to well encapsulation of glipizide by the polymers. Conclusion: Glipizide loaded nanoparticles were developed with good encapsulation efficiency using a combination of two different biocompatible polymers. The drug release behavior showed that they can be used to develop the sustained release formulation to reduce the side effect caused by over drug uptake as compared to the conventional formulation.

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Formulation Development and Evaluation of Sustained Release Matrix Tablets of Guaiphenesin

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.3.7 ◽

2016 ◽

Vol 9 (3) ◽

pp. 3312-3316

Author(s):

Ganesh D. Basarkar ◽

Ketan H. Shah ◽

Madhuri B. Sonawane

Keyword(s):

Drug Release ◽

Sustained Release ◽

Rice Bran ◽

Half Life ◽

Water Soluble ◽

Matrix Tablet ◽

Formulation Development ◽

Sustained Release Formulation ◽

Rice Bran Wax ◽

Melt Granulation

In this study we sought to formulate and evaluate sustained release matrix tablet of guaiphenesin by melt granulation technology. The sustained release tablets were prepared by melt granulation technique using rice bran wax as a drug retardant and dibasic calcium phosphate (DCP) as a channelling agent. Guaiphenesin is an expectorant and has a short plasma half-life of one hour. Because of high frequency of administration and short biological half-life, guaiphenesin was considered as model drug. Sustained release formulation that would maintain plasma levels for 12 hours is sufficient for twice daily dosing of guaiphenesin. The compatibility of drug and wax was examined by differential scanning calorimetry (DSC). The effect of waxes at different (drug: wax) concentrations on the release profile of drug from matrix formulation were studied. Drug release was studied at pH 1.2 for 2 hour and pH 6.8 for 10 hours. A significant retardation in the drug release was observed by increasing the wax concentration. The drug release study revealed that wax concentration of 30% to be optimum. Dissolution study showed 99% drug release within 12 hrs. Kinetic modelling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. These results suggest that the rice bran wax has good release retardant property for highly water-soluble drug such as guaiphenesin.

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FORMULATION DEVELOPMENT AND EVALUATION OF MATRIX TABLET TRAZODONE HYDROCHLORIDE USING NATURAL POLYMER

International Research Journal of Pharmacy ◽

10.7897/2230-8407.1208156 ◽

2021 ◽

Vol 12 (8) ◽

pp. 46-51

Author(s):

Jeetendra Kushwaha ◽

Dev Sharan Chaturvedi ◽

Manisha Verma ◽

Kuldeep Kumar Tiwari ◽

Neelesh Anuragi

Keyword(s):

Drug Release ◽

Sustained Release ◽

Research Work ◽

In Vitro Release ◽

Matrix Tablets ◽

Average Weight ◽

Release Kinetic ◽

Matrix Tablet ◽

Formulation Development ◽

Trazodone Hydrochloride

Increased complications and costs of marketing of innovative drugs focused greater attention to the development of sustained release (SR) or controlled release (CR) drug delivery systems. Trazodone Hydrochloride (TRZ) is a well-known chemical compound that is used as an antidepressant that belongs to a selective serotonin reuptake inhibitor (SARI). The objective of present work was to develop and evaluated oral sustained release matrix tablet of TRZ. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. No interactions were observed between TRZ and excipients from the Fourier transform infrared spectroscopy. The present research work was successful in improving the efficacy TRZ oral therapy as the drug release was extended for 12 hours thus reducing dosing frequency thereby improving patient compliance. The study also revealed the applicability of HPMC K-15, Gaur gum and PVP K30 as rate-controlling polymers in matrix tablets. The hydrophilic matrix of HPMC alone cannot control the release TRZ effective for 12 h while when combined with guar gum, may slow down the release of the drug and therefore, can be successfully employed for the formulation of matrix tablets SR. It may be concluded from the study that; the optimized formulation F-8 was shown maximum drug release 99.12 % in 12 h of dissolution. The release kinetic data of formulation F-8 shown first order release kinetics (R2 = 0.980).

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FORMULATION DEVELOPMENT OF MATRIX TABLET OF STAVUDINE BY USING CARBOXY METHYL TAMARIND KERNEL POWDER AS A NOVEL DRUG RELEASE RETARDING AGENT

INDIAN DRUGS ◽

10.53879/id.52.04.10235 ◽

2015 ◽

Vol 52 (04) ◽

pp. 28-36

Author(s):

R. R Karmarkar ◽

◽

M. P Wagh ◽

S.R Baviskar ◽

S.H Patil ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Matrix Tablet ◽

Formulation Development ◽

Compression Technique ◽

Novel Drug ◽

Carboxy Methyl

The aim of the present study was to evaluate carboxy methyl tamarind kernal powder as a novel drug release retarding agent. To evaluate the same, sustained release matrix tablets of stavudine were prepared by using HPMC K4M and carboxy methyl tamarind kernal powder, by using a direct compression technique. The formulations were prepared by using different drug: polymer ratios into formulations such as F1 to F9. The compressed tablets were evaluated for thickness, hardness, friability, drug content and in vitro dissolution rates. Formulation F6, having a hardness of 5.46 ± 0.25, showed the desired release profile for a period of 24 h in simulated intestinal fluids (pH 7.4). Kinetic data treatment indicated that the release of stavudine from the matrix tablet follows coupling of diffusion and erosion mechanisms. The study proves that the optimized sustained release tablet is capable of releasing the drug in a sustained manner for 24 h.

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FORMULATION, EVALUATION AND OPTIMIZATION OF SUSTAINED-RELEASE DRUG DELIVERY SYSTEM OF CISAPRIDE TABLET

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2021v13i9.41799 ◽

2021 ◽

pp. 56-62

Author(s):

DARSHIT RAM ◽

HIMANSHU PANKHANIYA

Keyword(s):

Drug Release ◽

Flow Property ◽

Matrix Tablets ◽

Release Kinetic ◽

Matrix Tablet ◽

Compression Technique ◽

Release Formulation ◽

Preformulation Studies ◽

Full Factorial

Objective: Cisapride is a novel prokinetic agent is best candidate for GERD. Cisapride 20 mg can be given thrice in a day given along with Proton pump inhibitor. By developing the sustain release formulation of Cisapride, the frequency of both drug can be reduce to once only to obtain good therapeutic response. Methods: Cisapride SR Tablets were prepared by direct compression technique with HPMC K4M and HPMC K100M polymers. Followed by various evaluation tests including in vitro disintegration and dissolution, the formulation was optimized by 32 full factorial designs with drug release kinetic analysis, compatibility studies (FTIR) and stability studies. Results: Results of Preformulation studies of the Cisapride indicate that it has poor flow property and compressibility property. To improve the flow and compressibility property, it was beneficial to use the directly compressible grade components in the formulation of tablet. Results of DSC study shown that there is no change in drug’s melting peak after the preparation of tablet. Hydrophilic matrix of HPMC K4M and HPMC K100M in combination sustained the Cisapride release effectively for more than 12h. The result indicates that the combination of HPMCK4M and HPMCK100M can be successfully, On the basis of the preliminary trials in the present study a32 full factorial design was employed to study the effect of independent variables, i.e. concentration of HPMCK4M(X1) and concentration of HPMCK100M(X2)on dependent variables like% drug release Q2, Q6 and Q10. Drug release is also dependent on the size of matrix tablets so, size and surface area was kept constant. Factorial batches F018, F019, F020, and F021 give the f2 value 75-100. Factorial batch F019 gives the highest f2 value 86.04 and also all the hour’s drug release was within the specified limits. Conclusion: The prepared formulation of Cisapride sustains release matrix tablet was stable and effective in treatment.

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Formulation Development and Evaluation of Rosuvastatin Sustained Release Tablets

Journal of Pharmaceutics and Therapeutics ◽

10.18314/jpt.v5i1.1459 ◽

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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FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

Journal of Pharmaceutical and Scientific Innovation ◽

10.7897/2277-4572.105218 ◽

2021 ◽

Vol 10 (5) ◽

pp. 131-136

Author(s):

Asim pasha ◽

C N Somashekhar

Keyword(s):

Drug Release ◽

Sustained Release ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Prolonged Release ◽

Matrix Tablet ◽

Direct Compression ◽

Dissolution Profile ◽

Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

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FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i5.17475 ◽

2017 ◽

Vol 10 (5) ◽

pp. 285

Author(s):

S Shanmugam

Keyword(s):

Drug Release ◽

Sustained Release ◽

Xanthan Gum ◽

Diffusion Mechanism ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Release Kinetic ◽

Natural Polymers ◽

In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism. Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies

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Response Surface Optimization of Sustained Release Metformin-Hydrochloride Matrix Tablets: Influence of Some Hydrophillic Polymers on the Release

ISRN Pharmaceutics ◽

10.5402/2012/364261 ◽

2012 ◽

Vol 2012 ◽

pp. 1-10 ◽

Cited By ~ 1

Author(s):

Amitava Roy ◽

Kalpana Roy ◽

Sarbani Roy ◽

Jyotirmoy Deb ◽

Amitava Ghosh ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Hydroxypropyl Methylcellulose ◽

Dissolution Kinetics ◽

Matrix Tablets ◽

Metformin Hydrochloride ◽

Wet Granulation ◽

Matrix Tablet ◽

Response Surface Optimization

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X60, X120, T50, T90, n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable.

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