scholarly journals FORMULATION AND EVALUATION OF MELOXICAM MICROSPHERES FOR COLON TARGETED DRUG DELIVERY

2021 ◽  
pp. 45-51
Author(s):  
SHRADHA KISHOR DHAS ◽  
GANESH DESHMUKH
Keyword(s):  
Sodium Alginate ◽  
Targeted Drug Delivery ◽  
Targeted Delivery ◽  
Discharge Rate ◽  
Dissolution Medium ◽  
In Vitro Drug Release ◽  
The Core ◽  
Release Studies ◽  
Incorporation Efficiency

Objectives: The objective of this research was to organize and evaluate colon specific microspheres of the meloxicam for the treatment of colorectal cancer. Methods: Sodium alginate microspheres were prepared by ionotropic gelation method using different ratios of meloxicam and sodium alginate (1:1, 1:2, and 1:3). Eudragit-coating of meloxicam, sodium alginate microspheres was performed by coacervation phase separation technique. Results: The microspheres were characterized by shape, particle size, size distribution, incorporation efficiency, in vitro drug release studies and stability studies. The outer surfaces of the core and coated microspheres, which were spherical in shape, were rough and smooth, respectively. The size of the core microspheres ranged from 20 to 52 μm, and therefore the size of the coated microspheres ranged from 107 to 178 μm. The core microspheres sustained the discharge for 10 h during a pH progression medium mimicking the condition of gastrointestinal tract. The release studies of coated microspheres were performed during a similar dissolution medium as mentioned above. In acidic medium the discharge rate was much slower, however the drug was released quickly at pH 7.4 and their release was sustained up to 24 h. Conclusions: It’s concluded from this investigation that Eudragit-coated sodium alginate microspheres are promising controlled release carriers for colon-targeted delivery of meloxicam.

scholarly journals Formulation and Evaluation of Pseudoephedrine Hydrochloride Loaded Alginate Microbeads

2020 ◽  
Vol 10 (3) ◽  
pp. 137-141
Author(s):  
Rashmi Dahima
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Cost Effective ◽  
Alginate Beads ◽  
Controlled Delivery ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Multiple Unit ◽  
Effective Carrier

Multiple unit dosage forms such as microbeads have increased acceptance because of added even spreading of the drug in the gastrointestinal tract, unvarying drug absorption, abridged local irritation and removal of undesirable intestinal retaining of polymeric material, when compared to non-disintegrating single unit dosage form. The purpose of the presented research is to develop microbeads of pseudoephedrine hydrochloride utilizing sodium alginate as the hydrophilic carrier in combination with HPMC as drug release modifier to lessen the dosing frequency and thereby advance the patient compliance. The microbeads were formulated by varying concentrations of HPMC and calcium chloride. The optimum formulation was chosen based upon in vitro drug release studies and further evaluated. The compatibility of drug-polymer was studied using FTIR analysis. The prepared formulation underwent evaluation for various parameters like drug entrapment, microbeads size, swelling index, mucoadhesive property and stability. No significant drug-polymer interactions were observed in compatibility studies and the formulation was found to be stable on 45 days storage. The formulations exhibited an extended drug release pattern which was the ultimate aim of the study. The microbeads represented good yield, high drug entrapment, low microbeads size and appropriate swelling property. The in vitro wash-off test indicated that the sodium alginate microbeads represent decent mucoadhesive properties. Henceforth, the formulated HPMC coated sodium alginate beads can be utilized as a substitute and cost-effective carrier for the oral controlled delivery of pseudoephedrine hydrochloride. Keywords: microbeads, pseudoephedrine hydrochloride, sodium alginate, drug release

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.

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

scholarly journals FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

2021 ◽  
pp. 144-151
Author(s):  
KUMAR BABU PASUPULETI ◽  
VENKATACHALAM A. ◽  
BHASKAR REDDY KESAVAN
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
The Core ◽  
Coated Tablet ◽  
Tablet Formulations ◽  
Core Tablet

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

scholarly journals DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Tablet Properties ◽  
Vitro Release

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Design and evaluation of Pulsatile drug delivery of Losartan Potassium

2014 ◽  
Vol 12 (2) ◽  
pp. 119-123
Author(s):  
MS Ashwini ◽  
Mohammed Gulzar Ahmed
Keyword(s):  
In Vitro Release ◽  
Losartan Potassium ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Weight Variation ◽  
Release Studies ◽  
The Stability ◽  
Vitro Release

The study was designed for the investigation of pulsatile device to achieve time or site specific release of Losartan potassium based on chronopharmaceutical considerations. The basic design involves the preparation of cross linked hard gelatin capsules by using formaldehyde, then the drug diluent mixture were prepared and loaded in, which was separated by using hydrogel plugs of different polymers of different viscosities. Prepared formulations were subjected to evaluation of various parameters like weight variation, percentage drug content, in vitro drug release and stability studies. Weight variation and percentage drug content results showed that they were within the limits of official standards. The in-vitro release studies revealed that the capsules plugged with polymer HPMC showed better pulsatile or sustained release property as compared to the other formulations. The stability studies were carried out for all the formulations and formulations F1 & F2 were found to be stable. Dhaka Univ. J. Pharm. Sci. 12(2): 119-123, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17610

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