Sustained-release dosage form of nitrofurantoin. Part 1. Preparation of microcapsules and in vitro release kinetics

Ertan, Gökhan; Sarigüllü, I.; Karasulu, H. Yeşim; Güneri, Tamer

doi:10.3109/02652049409040443

Cited by 8 publications

(4 citation statements)

References 8 publications

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“…Microcapsules of ketoconazole were prepared by means of a phase separation technique, which is a simple coacervation method (Ertan et al 1994). Sodium carboxymethylcellulose is added into boiling water and mixed thoroughly until it cools.…”

Section: Preparation Of Microcapsulesmentioning

confidence: 99%

Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery

Karasulu

Taneri

Sanal

et al. 2002

Journal of Microencapsulation

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Microcapsules of ketoconazole with 1:1 and 1:2 core-wall ratios were prepared by means of the phase separation technique using sodium carboxymethylcellulose as a coating material. The microcapsules were mixed with effervescent granules and were tabletted. Dissolution studies of microcapsules, tabletted microcapsules and commercial ovules were carried out with a new basket method (horizontal rotating basket). A good sustained action was obtained with tablets. Micromeritic investigations were carried out on microcapsules in order to standardize the microcapsule product and to optimize the pilot production of the dosage forms prepared with these microcapsules. Bulk volume and weight, tapping volume and weight, fluidity, angle of repose, weight deviation, relative deviation, particle size distribution, density and porosity values of the microcapsules were determined. In addition, to evaluate whether some kind of glidant will be needed during tabletting of microcapsules, the Hausner ratio o and consolidaton index were also calculated and it may be concluded that microcapsules do not need any glidant.

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Section: Preparation Of Microcapsulesmentioning

confidence: 99%

Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery

Karasulu

Taneri

Sanal

et al. 2002

Journal of Microencapsulation

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“…Microparticles prepared with the combination of NTF}CAP}CAB in the ratio of 1.0: 0.4 :1.6 showed the greatest delay in drug release in SGM. Earlier work by Ertan et al (1994) showed that a sustained-release dosage form of NTF as microcapsules could be prepared by a carboxymethylcel-lulose± aluminium sulfate coacervation technique. With their polymer mixture, approximately 60 % of the drug was released in SGM in 5 h compared with the 20 % released by our formulation of NTF}CAP}CAB (1.0 : 0.4 : 1.6).…”

Section: In-vitro Dissolution Studiesmentioning

confidence: 99%

“…However, the gastric side-eOE ects could not be completely overcome by using macrocrystals in the formulation. Therefore, many attempts have been made to reduce the gastric side-eOE ects by controlling the drug release in the stomach, for example by using sustained release tablets, hard gelatin capsules and microcapsules (Baichwal & Shetty 1982 ;Eldem & Capan 1983 ;Ertan et al 1994). However, when these dosage forms are used to treat childhood urinary tract infections, which occur in 2 % of boys and 8 % of girls by 10 years of age (Roy 1999), the di culty of swallowing tablets or capsules could result in non-compliance.…”

Section: Introductionmentioning

confidence: 99%

Polymer-coated microparticles for the sustained release of nitrofurantoin

Liu

Chan

2002

Journal of Pharmacy and Pharmacology

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Suspensions of nitrofurantoin (NTF) microparticles for controlled release were investigated in this study. The microparticles were enteric coated with various combinations of the two polymers, cellulose acetate phthalate/cellulose acetate butyrate (CAP/CAB) by a modified solvent evaporation method. Ratios of NTF to the two polymers (NTF/CAP/CAB) ranged from 1.0:1.6:0.4,1.0:1.0:1.0,1.0: 0.4:1.6 to 1.0:0.0:2.0. The encapsulation efficiency, percentage yield, determined by comparing the final mass of the microparticles with the initial mass of the ingredients used, distribution of particle size and the in-vitro dissolution profiles of the microparticles were determined. Based on light photographs for the evaluation of the microparticle morphology, the drug crystals appeared to be encapsulated sufficiently by the enteric polymers. In our study, the microparticles enteric coated with CAP/CAB in the ratio of 0.4:1.6 displayed the most satisfactory in-vitro release profile (reduced release in the simulated gastric fluid and sustained release in the simulated intestinal fluid). Thus, microparticles with NTF/CAP/CAB in the ratio of 1.0:0.4:1.6 were formulated into a suspension for further bioavailability and ulcerogenicity studies in Sprague-Dawley rats, with the suspension of NTF crystals as a control. The bioavailability study was carried out in eight rats fed with either the free NTF or the corresponding microparticles in a cross-over design. The ulcerogenicity study was carried out in three groups of six rats each: one group received no drug treatment; the control group was treated with free NTF; and the third group was treated with enteric-coated NTF microparticles. The bioavailability of NTF from the microparticles was comparable with the control. More importantly, there was notably less ulceration of the gastric mucosa observed after dosing with the microparticle suspension compared with that after the administration of the control suspension.

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“…Several research studies have investigated the reduction of these side effects of NF using macrocrystalline [12] and the sustained release of oral dosage forms e.g. tablets [13], capsules, microcapsules [14] and microparticles [15].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Chitosan-Gelatin Films with Na<sub>2</sub>SO<sub>4</sub> Cross-Linked for Controlled-Release of Nitrofurantoin

Somphon

Samnaree

2017

KEM

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This work prepared and characterized of chitosan (Cs)-gelatin (Gel) films for the controlled release of the nitrofurantoin (NF) antibacterial drug. The side effects of NF are nausea and emesis due to its high absorption rate immediately after oral administration. The use of Cs-Gel films enables economic production of the drug carrier system. Cs-Gel films were prepared by mixing Cs with Gel at different ratios and were cross-linked with Na2SO4 with different concentrations. NF was loaded into the films by soaking of drug solution. Films were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and evaluated for thickness, water absorption capacity, swelling behaviour and invitro NF drug release in phosphate buffer solution pH 5.8 and pH 7.4. The results indicated that additional amount of gelatin and sulfate ion cross-linked to the films increased the swelling, water absorption ability and also improved NF release.

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Sustained-release dosage form of nitrofurantoin. Part 1. Preparation of microcapsules and in vitro release kinetics

Cited by 8 publications

References 8 publications

Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery

Sustained release bioadhesive effervescent ketoconazole microcapsules tabletted for vaginal delivery

Polymer-coated microparticles for the sustained release of nitrofurantoin

Preparation and Characterization of Chitosan-Gelatin Films with Na<sub>2</sub>SO<sub>4</sub> Cross-Linked for Controlled-Release of Nitrofurantoin

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