Development and Evaluation of Hydrodynamically Balanced System of Tramadol Hydrochloride by Using Chitosan and Locust Bean Gum

2020 ◽  
Author(s):  
Surabhi Ghildiyal
Keyword(s):  
Molecular Weight ◽  
Drug Release ◽  
Zero Order ◽  
Locust Bean Gum ◽  
Tramadol Hydrochloride ◽  
Gastric Residence Time ◽  
Release Pattern ◽  
Release Studies ◽  
Locust Bean

The main purpose of the study was the development and evaluation of a hydrodynamically balanced capsule of Tramadol HCl by using chitosan and locust bean gum as a natural polymer that prolongs the gastric residence time. Chitosan with different grades (low molecular weight, medium and high molecular weight) and locust bean gum were used as drug release retarding agents. The hydrodynamically balanced capsule of tramadol HCl was prepared by ordered mixing technique. The concentration of both the polymers was optimized to achieve the sustained release of the drug (TH) for 10 hours. Then the prepared capsules were evaluated for buoyancy test and in vitro drug release was performed and another characterization analysis was also considered like FTIR study, DSC/DTG/TGA study and interaction study were also performed based on characterization analysis. From these studies, it was confirmed that there is no interaction observed between drug and excipient. The drug release studies show that the retarding drug release pattern is dependent on the concentration and molecular weight of the polymer as the concentration /molecular weight increases the retarding drug release pattern was also improved. And the synergistic action of retarding drug release was observed by the addition of another polymer i.e locust bean gum. Release pattern was fitted with the different kinetic models like Zero order, First order, Higuchi model and KorsmeyerPeppas and it was concluded from the models that the drug release pattern obeys zero-order model which signifies high therapeutic efficacy and minimum side effects.

Formulation Study and Evaluation of Matrix and Three-Layer Matrix Tablets Oral Controlled Drug Delivery System Based on Xanthan Gum and Locust Bean Gum

2010 ◽  
Vol 3 (2) ◽  
pp. 1006-1014
Author(s):  
Y. Madhusudan Rao ◽  
S L Ahmed ◽  
M L Narsu ◽  
S J Mohan
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Crystalline Cellulose ◽  
Locust Bean Gum ◽  
The Matrix ◽  
Locust Bean ◽  
Diltiazem Hcl

The present study was carried out to develop oral controlled release matrix tablets and three layer matrix tablets of highly water soluble diltiazem HCl using natural polymers Xanthan gum (XG), locust bean gum (LBG) and a mixture XG: LBG in 1:1 ratio as matrix forming agent, and anionic Sodium Carboxyl Methyl Cellulose as release retardant layer on the matrix core, Di calcium Phosphate (DCP) and Micro crystalline Cellulose (MCC) as fillers. Matrix core tablets were prepared with by granulation technique.The characterization of physical mixture of drug and excipeints was performed by infra red spectroscopy. The finding of the study indicated that the matrix tablets prolonged the release, but predominantly in a first order fashion, layering with SCMC granules on the matrix core, provided linear drug release with zero order kinetics. The influence of layers on matrix core and release rate was described by the peppas equation, model independent approach, Mean dissolution time (MDT) and dissolution efficiency (D.E 8%). The addition of SCMC layers on the matrix core could notably influence the dissolution behavior and mechanism of drug release. Increasing the quantity of layers caused decreased values of k and increased n value, in a linear relationship. MDT for matrix tablet (S6)  and three layer matrix tablets (S6L3) was found to be 5.16h and 11.97h, D.E 8% was 76.23% and 66.21% respectively.  These indicated that the release of drug is slower from the three layer matrix tablets. Type of fillers has a limited effect on the drug release mechanism from matrix tablets. Stability studies revealed that the formulation was stable at 45°±2°C and 75±5%RH. Hence natural polymer as matrix core and anionic polymer SCMC as retardant layer in the form of three layer matrix tablets provided the zero order release of highly water soluble Diltiazem HCl. 

scholarly journals Formulation and in vitro Evaluation of Piroxicam Emulgel

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Y Bindu Vani ◽  
C. Surya Prakash Reddy
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Evaluation Studies ◽  
Tween 80 ◽  
Zero Order ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Release Studies ◽  
Span 80

The present work is concerned with the formulation and evaluation of Piroxicam emulgel employing carbopol 934 and xanthan gum as polymers. The emulgel is prepared by combining the gel and emulsion. The gel in formulations were prepared by dispersing Carbopol 934 and xanthan gum separately in purified water with constant stirring at a moderate speed and then the pH was adjusted to 4 to 5.4 using Tri-ethanol amine (TEA). The oil phase in the emulsion consists of oleic acid and span-80. The aqueous phase in the emulsion was prepared using Tween-80, propylene glycol and distilled water. The prepared emulgel formulations were subjected to evaluation studies like Physical appearance, rheological studies, estimation of drug content and in-vitro drug release. The appearance of prepared emulgel was white. The pH of the emulgel was found to be 5.4. The in vitro drug release studies revealed that formulation F1 showed 85.20% and formulation F2 showed 79.23% of drug release at the end of 8 hrs. The drug release of F1 formulation follows zero order kinetics.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF CHRONOMODULATED DRUG DELIVERY SYSTEM BY ZAFIRLUKAST

2021 ◽  
pp. 211-220
Author(s):  
N. SHIVA KRISHNA ◽  
B. JAYANTHI ◽  
A. MADHUKAR
Keyword(s):  
Drug Release ◽  
Lag Time ◽  
Early Morning ◽  
Release Profile ◽  
Locust Bean Gum ◽  
In Vitro Drug Release ◽  
The Core ◽  
Locust Bean ◽  
Core Tablet

Objective: The main objective of the present study was to formulate and evaluate a time-controlled single-unit oral pulsatile drug delivery system containing Zafirlukast for the prevention of nocturnal asthma attacks. To provide time-scheduled drug release for Asthma disease. It is used for preventing asthmatic attacks at early morning. Pulsatile release dosage form is increasing patient compliance by reducing the dosing frequency, especially in the early morning. Methods: Core tablets were prepared by incorporating different concentrations of natural and synthetic super disintegrants. Drug-containing core tablets (ZC1-ZC15) with different compositions of natural super disintegrants (Plantago ovata seed powder, Locust bean gum) synthetic super disintegrants (Sodium starch glycolate (SSG), Cross carmellose sodium (CCS), Crospovidone (CP)) were prepared by direct compression technique. The core tablets were subjected to pre-formulation, physicochemical and In vitro drug release studies. The fast disintegrating core tablet formulation was selected and press-coated tablets (P1-P11) were prepared with different compositions of hydrophobic polymers Eudragit RS100, Eudragit RL 100, Ethylcellulose and hydrophilic polymers Hydroxypropyl methylcellulose K4M, K100M. The optimized formulation was selected and quantified based on in vitro drug release profile in simulated gastric and intestinal fluids. Results: The pre and post-compression parameters of tablets were also found to be within limits. Formulation ZC5 with 16 mg of Locust bean gum showed the least disintegrating time, i.e., 22.13 sec, and was selected as the best immediate release core tablet. The press-coated tablet formulation P8 having 62.5 mg Eudragit RS100 and 62.5 mg of HPMC K4M in ratio 1:1 over the core tablet ZC5 showed rapid and drug release nearly after 4 h lag time and 98.86 % up to 12 h. Accelerated stability studies of the optimized formulation P8 indicated no significant difference in release profile after 3 mo. Conclusion: The in vitro dissolution study showed that lag time before drug release was highly affected by the coating amount level and nature of coating polymer used. Time-controlled pulsatile release tablets can be prepared using press-coating techniques.

scholarly journals FORMULATION DEVELOPMENT, CHARACTERIZATION AND IN- VITRO EVALUATION OF FLOATING MATRIX DOSAGE FORM OF TRAMADOL HYDROCHLORIDE USING VARIOUS POLYMERS

2017 ◽  
Vol 10 (2) ◽  
pp. 281
Author(s):  
Sarada Anepu ◽  
Lohithasu Duppala ◽  
Soma Sundari M
Keyword(s):  
Methyl Cellulose ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Tramadol Hydrochloride ◽  
Floating Tablets ◽  
Gastric Residence Time ◽  
Weight Variation ◽  
Floating Drug Delivery ◽  
Release Studies

Objective: The purpose of present study was to formulate the gastro retentive floating tablets of tramadol hydrochloride for enhancement of the gastric residence time.Methods: The floating tablets were prepared by direct compression method and evaluated for hardness, thickness, and friability of the tablets. The in vitro drug release studies were performed for different formulations and to optimize the best formulae based on the dissolution profiles.Results: Fourier transform infrared spectroscopy and differential scanning calorimetry studies revealed that there was no interaction between tramodol hydrocholride and excipients. The formulated tablets were evaluated for properties like weight variation, hardness, thickness, friability, drug content, density and floating properties, matrix integrity and complied with USP requirements. The tablets of optimized formula had floating lag time of 120, 72 and 96 seconds and the tablets remained in the floating condition for more than 12 h. The results of drug excipients compatibility studies suggest that there was no significant change in the physical appearance of these blends, when stored at 40 °C/75% RH for a period of 4 weeks.  Among various trial formulations developed with different concentration of polymer F3 (HPMC K4 M with 120mg of polymer), F5 (HPMC K15 M with 100 mg polymer), F11 (PEO WSR 303 with 100mg polymer), were chosen as the optimized formulations based on the release profile.Conclusion: Tramodol HCl floating tablets were successfully made using various polymers for the enhancement of the gastric residence time. From the present study it was concluded that hydroxy propyl methyl cellulose K 4 M can be used as effective polymer for the formulation of floating effervescent tablets of highly soluble drug indicating successful development of sustained release floating drug delivery system.Key words: Tramodol HCl, floating tablets, PEO 303 WSR, PEO N60, HPMC K 4 M, HPMC K15 M and HPMC K 100 M. 

scholarly journals A NOVEL APPROACH OF LOCUST BEAN GUM MICROSPHERES FOR COLONIC DELIVERY OF MESALAMINE

2018 ◽  
Vol 10 (1) ◽  
pp. 86 ◽  
Author(s):  
V. N.l. Sirisha ◽  
M. Chinna Eswariah ◽  
A. Sambasiva Rao
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Locust Bean Gum ◽  
Ionic Gelation ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
S 100 ◽  
Locust Bean ◽  
Eudragit S 100

Objective: The objective of the present study was to formulate site-specific drug delivery of mesalamine using Locust bean gum.Methods: The core microspheres were prepared by ionic gelation method using CaCl2 solution and cross-linked with glutaraldehyde and were further coated with pH-sensitive polymer eudragit S-100(1.5-4.5 ml) to retard the drug release in the upper gastrointestinal environment (Stomach and small intestine). Microspheres were characterized by ftir spectroscopy, differential scanning calorimetry and evaluated by scanning electron microscopy (SEM), particle size analysis, entrapment efficiency and in vitro drug release studies in different simulated gastric fluids. Stability studies were carried out for one month at 40±2 °C/75±5% RH.Results: The SEM images revealed the surface morphology was rough and smooth for core and coated microspheres, respectively. The optimized batch (ILBG6) of core microspheres(for 7hr), coated microspheres and coated microspheres in presence of rat caecal contents (8%w/v) for 24hr exhibited 98.44±2.48, 73.58±3.49 % and 98.28±4.42 drug release, respectively. The drug release from all locust bean gum microsphere formulations followed higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the korsmeyer-peppas equation with an fickian kinetics mechanism. Finally, stability studies suggested the change in entrapment efficiency and in vitro drug release of microspheres was minimal, indicating good stability of the formulation.Conclusion: The microspheres formed using natural polysaccharide locust beangum by ionic gelation method are capable of colon targeting the anti-inflammatory drug, mesalamine for the treatment of ulcerative colitis.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET USING LOCUST BEAN GUM AS A NATURAL SUPERDISINTEGRANT AND COMPARISON WITH THE MARKETED PREPARATION

2021 ◽  
Vol 15 (5) ◽  
pp. 13-20
Author(s):  
Namrata S Mane ◽  
Namrata A Muddalwar ◽  
Priya V Nikam ◽  
Narendra R Dighade
Keyword(s):  
Dosage Form ◽  
Diclofenac Sodium ◽  
Locust Bean Gum ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Locust Bean ◽  
Ir Study

The aim was to formulate and evaluate fast dissolving tablets of diclofenac sodium to improve the bioavailability of the drug and patient compliance. Fast dissolving tablets of diclofenac sodium were prepared by direct compression method by using superdisintegrants (locust bean gum) in 2%, 3%, 4% 5% & 6% concentration respectively. Tablets were formulated by using natural superdisintegrants locust bean gum (LBG). This formulated mixture i.e., drug and LBG was mixed with other excipients and the tablets were compressed by direct compression. Formulated tablets were characterized by FTIR, pre-compression and post-compression parameters. The In vitro drug release studies were performed in pH 6.8 phosphate buffer. Formulated tablets were characterized by FTIR, the results of IR study showed that there was no interaction between superdisintegrant and pure drug, the results of FTIR study showed that drug was stable in the final formulated tablet. The drug content was evaluated with the help of assay. Five (F1-F5) formulations were evaluated for pre-compression and post-compression parameters and all the results were in the standard limits. Formulated dosage form may be an effective alternative to conventional dosage form which can be effectively used in the treatment of inflammation specially in cases of acute pain.

scholarly journals SODIUM ALGINATE–LOCUST BEAN GUM IPN HYDROGEL BEADS FOR THE CONTROLLED DELIVERY OF NIMESULIDE-ANTI-INFLAMMATORY DRUG

2017 ◽  
Vol 9 (10) ◽  
pp. 245 ◽  
Author(s):  
C. Madhavi ◽  
P. Kumara Babu ◽  
Y. Maruthi ◽  
A. Parandhama ◽  
O. Sreekanth Reddy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Locust Bean Gum ◽  
Inflammatory Drug ◽  
Hydrogel Beads ◽  
Release Studies ◽  
Locust Bean ◽  
Anti Inflammatory

Objective: The objective of this study was to formulate and evaluate the drug release studies using locust bean gum (LBG) and sodium alginate (NaAlg) and cross-linked with glutaraldehyde for the controlled release (CR) of nimesulide, an anti-inflammatory drug.Methods: Locust bean gum (LBG) and sodium alginate (NaAlg) blend hydrogel beads were prepared by an extrusion method using glutaraldehyde as a crosslinker. Nimesulide an anti-inflammatory drug was encapsulation within LBG/NaAlg blend hydrogel beads. Morphology, size, encapsulation efficiency and drug release from these hydrogel beads were evaluated by different characterization techniques such as fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), x-ray diffraction (X-RD) studies.Results: Drug-loaded hydrogel beads were analyzed by FTIR, which indicates the interaction between drug and polymers. DSC thermograms on drug-loaded microbeads confirmed the polymorphism of nimesulide and indicated a molecular level dispersion of the drug in the hydrogel beads. SEM confirmed the spherical nature and rough surface of the hydrogel beads produced. X-RD study was performed to understand the crystalline nature of drug after encapsulated into the hydrogel beads and confirmed the complete dispersion of the drug in the polymer matrix. In vitro release studies conducted in pH-7.4 which indicated a dependence of release rate on the amount of drug loading and the amount of LBG/NaAlg, but slow release rates were extended up to 48 h. The cumulative release data were fitted to an empirical equation to compute diffusion exponent (n) which indicated the non-fickian trend for drug release.Conclusion: These results clearly demonstrated that the ability of these newly developed hydrogel beads containing nimesulide for its sustained release could possibly be advantageous to patient compliance with reduced dosing interval.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Gastroretentive Floating Capsules of Risedronate Sodium: Development, Optimization, in vitro and in vivo Evaluation in Healthy Human Volunteers

2015 ◽  
Vol 8 (2) ◽  
pp. 2835-2842
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Arun Kumar Jarathi ◽  
Suresh Gande ◽  
Viswaja Medipally ◽  
Ramesh Bomma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Zero Order ◽  
Wet Granulation ◽  
Capsule Formulation ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
X Ray ◽  
Human Volunteers

Background and the purpose of the study: Risedronate sodium inhibits osteoclast bone resorption and modulates bone metabolism. Risedronate has a high affinity for hydroxyapatite crystals in bone and is a potent antiresorptive agent. In the present investigation efforts were made to improve the bioavailability of risedronate sodium by increasing the residence time of the drug through sustained-release matrix capsule formulation via gastroretentive mechanism. Capsules were prepared by wet granulation technique. The influence of gel forming agents, amount of risedronate and total weight of capsules on physical properties, in vitro buoyancy, drug release, FTIR, DSC, X-ray studies were investigated. The release mechanisms were explored and explained by applying zero order, first order, Higuchi and Korsmeyer equations. The selected formulations were subjected to stability study at 40 °C/75% RH, 25 °C/60% RH for the period of three months. For all formulations, kinetics of drug release from capsules followed Higuchi’s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release. Formulation containing 25 mg HPMC K4M and 75 mg HPMC K100 LV (F-8) showed zero order release profile. There was no significant change in the selected formulation, when subjected to accelerated stability conditions over a period of three months. X-ray imaging in six healthy human volunteers revealed a mean gastric retention period of 5.60 ± 0.77 hrs for the selected formulation. Stable, sustained release effervescent floating capsules of risedronate sodium could be prepared by wet granulation technique.  

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

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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