Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

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.

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DESIGN AND DEVELOPMENT OF TOPICAL HYDROGEL FORMULATION OF IRBISARTAN

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2019v11i4.34924 ◽

2019 ◽

pp. 79-83

Author(s):

ZEESHAN SHAIKH

Keyword(s):

Angiotensin Ii ◽

Drug Release ◽

Matrix Tablets ◽

Wet Granulation ◽

Burst Release ◽

Angiotensin Ii Receptor ◽

In Vitro Drug Release ◽

Dsc Studies ◽

Ft Ir

Objective: Irbesartan is an antihypertensive with limited bioavailability. The objective of the study was to develop controlled release matrix tablets of irbisartan drug. Methods: Tablets were prepared by wet granulation process. Result: In vitro drug release study revealed that HPMC causes initial burst release of drug hence combining HPMC sustained the action for 8 h (95.92±0.57% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism for drug release. Compared to conventional tablets, the release of model drug from these HPMC matrix tablets was prolonged, leading to achieve an effective therapy with a low dosage of the drug, to reduce the frequency of medication. The pharmacological and clinical properties of irbesartan, a noncompetitive angiotensin II receptor type 1 antagonist, successfully used for more than a decade in the treatment of essential hypertension. Results: Compatibility Studies In order to investigate the possible interactions between irbesartan and distinct polymers and/or diluents, FT-IR and DSC studies were carried out. FT-IR results proved that the drug was found to be compatible with excipients as wave numbers are almost similar for pure drug and also drug excipients mixture. In picture 1 and 2. DSC studies indicate that chosen excipients for the formulation were found to be compatible with the active ingredient as the melting endothermic peaks are in the range of 250-320 °C which is same as the melting point of irbisartan. Conclusion: Irbesartan exerts its antihypertensive effect through an inhibitory effect on the pressure response to angiotensin II. Irbesartan 150–300 mg once daily confers a lasting effect over 24 h, and its antihypertensive efficacy is further enhanced by the coadministration of hydrochlorothiazide.

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Formulation and Evaluation of Pseudoephedrine Hydrochloride Loaded Alginate Microbeads

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i3.4094 ◽

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

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Formulation, Development and Evaluation of Chewable Bi-layered Tablets for Treating Gastro Esophageal Reflux Disease

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i4-s.4224 ◽

2020 ◽

Vol 10 (4-s) ◽

pp. 92-99

Author(s):

Ankur Vasoya ◽

Sunil Kumar Shah ◽

C K Tyagi ◽

Prabhakar Budholiya ◽

Harish Pandey

Keyword(s):

Calcium Carbonate ◽

Drug Release ◽

Sodium Bicarbonate ◽

Sodium Alginate ◽

Acid Neutralization ◽

In Vitro Drug Release ◽

Neutralization Capacity ◽

Acid Neutralization Capacity ◽

Bilayer Tablets

The purpose of this research work was to formulate raft-forming chewable bilayer tablets of sodium alginate using a raft-forming agent along with gas-generating agents. Tablets were prepared by wet granulation and evaluated for raft strength, acid neutralization capacity, weight variation, % drug content, thickness, hardness, friability and in vitro drug release. Various raft-forming agents were used in preliminary screening. The amount of sodium alginate, amount of calcium carbonate and amount sodium bicarbonate were selected as variables. Raft strength, acid neutralization capacity and drug release at 30 min were selected as responses.Tablets containing sodium alginate were having maximum raft strength as compared with other raft-forming agents. Acid neutralization capacity and in vitro drug release of all factorial batches were found to be satisfactory. Prepared tablets were found to be pharmaceutically equivalent to the marketed product. It was concluded that raft-forming chewable bilayer tablets prepared using an optimum amount of sodium alginate, calcium carbonate and sodium bicarbonate could be an efficient dosage form in the treatment of gastro oesophageal reflux diseases. Keywords: Chewable bilayer tablet, Sodium alginate, Raft forming agent, Acid Neutralizing capacity

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Formulation and Evaluation of Gastroretentive Nanoparticles of Repaglinide

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.1.8 ◽

2014 ◽

Vol 7 (1) ◽

pp. 2363-2370

Author(s):

P M Jamkar ◽

K N Gujar ◽

S B Nemmaniwar ◽

N B Kulkarni

Keyword(s):

Particle Size ◽

Drug Release ◽

Sodium Alginate ◽

Encapsulation Efficiency ◽

Research Work ◽

Crosslinking Agent ◽

Controlled Drug Release ◽

Dsc Studies ◽

Ft Ir ◽

Novel Drug

Controlled drug release system is one of the most favourable technique of novel drug delivery system owing to its reproducibility and ease of formulation. Nanotechnology is very useful for controlling the drug release and thus improving the pharmacokinetic and pharmacodynamic properties of the drug. The technique improves patient compliance by reducing both dose and the frequency of administration and thus minimizing the local as well as systemic toxic effects. The aim of the present research work was to formulate and evaluate gastroretentive nanoparticles of Repaglinide, an anti-diabetic drug by using the ionotropic gelation method. Repaglinide has a very short half-life of 1 hour with bioavailability 56%. Sustained release mucoadhesive nanoparticles of Repaglinide were prepared to increase the drug residence time in gastrointestinal tract and thus improving the bioavailability of drug. The mucoadhesive nanoparticles were prepared by using chitosan and sodium alginate as polymers; calcium chloride as the crosslinking agent. Different formulations were prepared with varying concentrations of chitosan and sodium alginate in order to achieve the optimum particle size and maximum encapsulation efficiency. The particle size of nanoparticles was found to be in the range of 300 nm to 756 nm. Drug encapsulation efficiency ranged between 56% to 80% with controlled drug release upto 88% in phosphate buffer pH 7.4 and 75% drug release in 0.1N HCl in 12 hrs. FT-IR and DSC studies showed that the drug and polymers were compatible. The results of swelling study and bioadhesive strength indicated that optimized formulation exhibited excellent mucoadhesive properties

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DESIGN AND IN VITRO EVALUATION OF MUCOADHESIVE BUCCAL FILMS OF LERCANIDIPINE HCL

INDIAN DRUGS ◽

10.53879/id.50.07.p0031 ◽

2013 ◽

Vol 50 (07) ◽

pp. 31-40

Author(s):

H. Doddayya ◽

◽

S.S Patil ◽

M Suman ◽

P Kumar ◽

...

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Release Mechanism ◽

In Vitro Drug Release ◽

Dsc Studies ◽

Zero Order Kinetics ◽

Accelerated Stability ◽

Buccal Films ◽

Lercanidipine Hydrochloride

Lercanidipine hydrochloride, an anti hypertension drug, undergoes extensive first pass metabolism to inactive metabolites leading to very poor oral bioavailability. To overcome this problem, buccal films of Lercanidipine hydrochloride were prepared by solvent casting method, employing HPMC, HPC (alone and in combination with PVP) and PVP K30. The film thickness, weight, folding endurance, mucoadhesive strength and time were dependent on the nature and concentration of polymers used. The optimized film (F12, HPMC 3% and PVP 1.5%) showed: Swelling index (51.26 ± 1.90 %), ex vivo mucoadhesive strength (12.64 ± 0.83 grams) and time (3.6 ± 0.5hrs). In vitro drug release was inversely proportional to the polymeric concentration. Ex- vivo drug release studies carried out using goat buccal membrane was slower (42.90%, 6 hrs) compared to in vitro drug release (74.2%, 8hrs) for the same formulation (F12). The drug release mechanism for the optimized formulation followed zero order kinetics. FT-IR and DSC studies revealed the absence of any interaction between the formulation ingredients. The films remained stable during the accelerated stability conditions.

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In vitro drug release profiles of pH-sensitive hydroxyethylacryl chitosan/sodium alginate hydrogels using paracetamol as a soluble model drug

International Journal of Biological Macromolecules ◽

10.1016/j.ijbiomac.2017.02.061 ◽

2017 ◽

Vol 99 ◽

pp. 71-78 ◽

Cited By ~ 54

Author(s):

Pitchaya Treenate ◽

Pathavuth Monvisade

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Ph Sensitive ◽

In Vitro Drug Release ◽

Soluble Model ◽

Alginate Hydrogels ◽

Model Drug ◽

Release Profiles

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Effect of Various Electrolytes on Theophylline Loaded Sodium Alginate Beads Prepared by Ionic Cross Linking Technique

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v11i2.14578 ◽

2013 ◽

Vol 11 (2) ◽

pp. 181-189

Author(s):

Sheikh Tasnim Jahan ◽

Sams Mohammad Anowar Sadat ◽

Muhammad Rashedul Islam ◽

ATM Zafrul Azam ◽

Jakir Ahmed Chowdhury

Keyword(s):

Drug Release ◽

Sodium Alginate ◽

Electrolyte Concentration ◽

Research Work ◽

Three Dimensional ◽

Alginate Beads ◽

Water Soluble ◽

Cross Linking ◽

Bonding Structure

The purpose of t h e present research work was to prepare alginate beads containing water soluble drug theophylline using ionic cross linking technique, with electrolyte type and concentration as variables. In this study, the beads were characterized and evaluated in respect of their surface morphology, swelling index and in vitro kinetics. The comparative study among the three polyvalent cationic cross linking agents CaCl2 , BaCl2 and Al2 (SO4)3 were investigated based on their cationic charges. Divalent cation, Ca2+ and Ba2+ containing beads showed simultaneous decrease in drug release with increasing electrolyte amount. In case of Al3+ -alginate beads, the delay in release was due to the ability of Al3+ to form three dimensional bonding structure with the sodium alginate inside the beads. As a result, swelling of beads is delayed leading to slow disintegration. Scanning electron microscope (SEM) photomicrographs revealed that with the increase in the electrolyte concentration the density of the cross link is also increased. When the electrolyte concentration is 5 % then the beads surface is rough and rod shape drug is visible. But when the electrolyte concentration is increased from 10 % to 15 % the surface is comparatively smoother and both the swelling property and in vitro drug release are decreased. Most of the formulations followed Higuchi drug release model. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14578 Dhaka Univ. J. Pharm. Sci. 11(2): 181-189, 2012 (December)

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EUDRAGIT COATED ALGINATE BEADS BEARING OXALIPLATIN LOADED LIPOSOMES: FORMULATION, OPTIMIZATION AND IN VITRO CHARACTERIZATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i6.43199 ◽

2021 ◽

pp. 170-177

Author(s):

ANKITA TIWARI ◽

SANJAY K. JAIN

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Entrapment Efficiency ◽

Alginate Beads ◽

Molar Ratio ◽

Specific Drug ◽

Sustained Drug Release ◽

In Vitro Drug Release ◽

Vesicle Size

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.

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FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF CIPROFLOXACIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i1.28603 ◽

2019 ◽

Vol 11 (1) ◽

pp. 198

Author(s):

Shailaja Pashikanti ◽

Jyothsna B.

Keyword(s):

Calcium Carbonate ◽

Drug Release ◽

Sodium Alginate ◽

Gelling Agent ◽

In Vitro Drug Release ◽

In Situ Gel ◽

Degradable Polymer ◽

Gel Formulations

Objective: The objective of the study was to develop floating in situ gel formulations of Ciprofloxacin that has a narrow absorption window and mainly absorbed in the proximal areas of GIT. These formulations increases the targeted action on bacteria for a longer time that can be used in the treatment of Helicobacter pylori (H. pylori) infections and urinary tract infections.Methods: In situ gel formulations were prepared by varying concentrations of sodium alginate as in situ gel forming bio-degradable polymer and calcium carbonate as a cross-linking agent. The formulations were evaluated for Physical appearance, pH, in vitro drug release, viscosity, in vitro floating behaviour, in vitro gelling capacity and drug content. FTIR was conducted for Ciprofloxacin, excipients used and optimized formulation.Results: All the formulations showed an optimum viscosity that will allow ease of administration and swallowing. Floating lag time of all formulations was between 32-70 seconds and floated for>12 h. The in vitro gelling capacity increased with increasing the polymer and gelling agent concentrations. Increase in polymer concentration decreased the rate and extent of the drug release. Among all the formulations, F4 containing 4% w/v of sodium alginate and 4% w/v of calcium carbonate showed sustained in vitro drug release (95.6%) over an extended period of 12 h. FTIR studies revealed no interaction between drug and excipients used. Drug release from the formulations followed First order kinetics with Fickian diffusion.Conclusion: Ciprofloxacin was successfully formulated as a pH-triggered floating in situ gelling system using sodium alginate.

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