• Archives of Pharmacal Research
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• v.14 no.4
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• pp.298-304
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• 1991

Isoprinosine, an antiviral agent with a bitter taste, has been clinically used up to a maximum of 4 g daily in 4-8 doses. In this investigation, isoprinosine was microencapsulated with ethylcellulose 22 cps, 50 cps and 100 cps by means of polymer deposition from cyclohexane through temperature change. Complete removal of cyclohexane from the microcapsules was necessary, since ethylcellulose-coated microcapsules obtained from cyclohexane medium were heavily solvated with cyclohexane and formed lumps even after drying. The displacement of cyclohexane by n-hexane during isolation of microcapsules (Method III) or the freezing of the anal-washed microcapsules before drying (Mothod II) provided the dried products which were more discrete microcapsules than those which were simply dried in the air overnight (Method I). Method III was especially the most effective procedure in preparing finer and more discrete microcapsules. The drug-release from microcapsules was influenced by the ratio of core to wall, the viscosity grade of ethylcellulose and the overall microcapsule size. The release rate was adequately fitted to both the first-order and the diffusion-controlled processes. It is therefore possible to design the release-controlled microcapsules with ethylcellulose of different viscosity along with various core to wall ratio.

• Journal of Pharmaceutical Investigation
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• v.17 no.2
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• pp.67-73
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• 1987

Propranolol hydrochloride was microencapsulated with ethylcellulose by means of phase separation from cyclohexane. The surface of the microcapsules examined using scanning electron microscope was porous. The dissolution rate of drug from microcapsules decreased as the weight ratio of propranolol hydrochloride to ethylcellulose decreased and as the size of microcapsules increased. The dissolution rate of drug from microcapsules decreased as the viscosity of ethylcellulose and pH of dissolution medium decreased.

• Journal of Pharmaceutical Investigation
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• v.16 no.1
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• pp.12-17
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• 1986

Etilefrine hydrochloride was microencapsulated with ethylcellulose by phase separation method to develop a sustained release dosage form. The results of dissolution test carried out with various microcapsules showed that the drug release was decreased with increasing the particle size of microcapsules at a constant core to wall ratio, and with decreasing the core to wall ratio. Also ethylcellulose 50 cps and fast stirring rate (900 rpm) was better in decreasing the drug release than ethylcellulose 22 cps and slow stirring rate (300 rpm), respectively.

• Archives of Pharmacal Research
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• v.7 no.1
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• pp.33-40
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• 1984

In domethacin was microencapsulated with ethylcellulose using a modified spherical agglomeration process, aiming at a sustained release proparation without side effects on the stomach. The surface morphology of the microcapsules was examined using scanning electron microscopy. The microcapsules were porous and spherical, and their porosity increased with increasing the viscosity of ethylcellulose. In vitro dissolution process followed Higuchi's diffusion model for first 3 hr. Release rate of the drug from microcapsules decreased as the viscosity of ethylcellulose was decreased. The release rate also decreased with increasing the microcapsule size. The microcapsules induced less gastric ulcer in rats than raw drug.

• YAKHAK HOEJI
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• v.28 no.3
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• pp.169-177
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• 1984

Release characteristics of salicylic acid from ethylcellulose(EC) films containing varying ratio of dieththylphthalate (DEP) were studied. Mathematical analysis of the release data showed that the release behavior actually conforms with the Higuchi's diffusion-controlled model. The release rate constants(k) were independent from the film thickness and the pH of release medium, but were proportional to the concentration of salicylic acid itself. The logarithm of the release rate constant (log k) increased as the concentration of DEP was increased. In conclusion, hydrophobic plastisizer DEP seemed to be very useful in controlling release rate constant of slightly soluble drugs as like salicylic acid without changing it's release characteristics.

• Journal of Pharmaceutical Investigation
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• v.15 no.2
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• pp.53-62
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• 1985

Pivampicillin hydrochloride is a kind of broad spectrum antibiotics with bactericidal action, and is used in many countries, although it has bitter taste, unpleasant odour and side effects of irritating gastric mucosa, nausea, penicillin allergy, etc. For the improvement of such side effects of pivampicillin hydrochloride, microcapsules, with wall of ethylcellulose, have been prepared by coacervation method. The shape was observed through the scanning electron microscope, the release of the drug into an aqueous medium was studied and the effects of core: ethylcellulose ratio were interpreted as well as making sensory evaluation of taste and odour. There was decreasing trend in dissolution rate of the drug with the increase of core: ethylcellulose ratios, and the smaller microcapsules released their contents more rapidly. A linear relationship was established between the amount of ethylcellulose and the time for 60% release of the drug, and the release pattern was found to have similar characteristics to the release of the drug from an insoluble porous matrix. The release of the drug in the artificial intestinal fluids (pH 6.8) was found to be similar to that in water, while the release in the artificial gastric juice (pH 1.2) was slightly slower. Bioavailability of microcapsule was compared with that of pivampicillin hydrochloride in rabbits using serum concentration and urinary excretion measurements. Microcapsule gave showed slightly higher serum level than pivampicillin hydrochloride from 2 hours after administration, while no significant difference was observed in the accumulated urinary excretion rate between pivampicillin hydrochloride and microcapsule. The ulcer index of pivampicillin hydrochloride administered group was 2.6, and microcapsule administered group was 1.5, while control group was 0.8. Therefore it may be concluded that microencapsulation of pivampicillin hydrochloride is a useful pharmaceutical approach to protect the gastrointestinal tract from being injured by direct contact of pivampicillin hydrochloride without any significant difference of bioavailability.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.127-136
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• 1999

In order to eliminate demerits of conventional dosage forms, dipotassium glycyrrhizate was formulated as a slim mucoadhesive film type dosage form. The mucoadhesive drug layer gel containing dipotassium glycyrrhizate was prepared using $Noveon^{\circledR}$ AA-1, hydroxypropylcellulose-M, ethylcellulose N 100 and citric acid, and the protective layer gel by using ethylcellulose N 100, $Eudragit^{\circledR}$ RS and castor oil. The viscosity of drug layer gel of mucoadhesive film was enhanced as the increased amount of $Noveon^{\circledR}$ AA-1 or hydroxypropyl cellulose-M. The drug content was unifonnly $1160{\pm}14.6\;{\mu}g$, and was varied within 3.5%. The optimum film dosage form showed a good fluidity and malleability of drug layer, with 179 g of thickness, pH 5.7, 411 min of in vitro adhesion time and 172 g in gravity adhesive strength. The release time of drug from the mucoadhesive film was significantly shorter but was delayed when polymers such as ethylcellulose was added. From these results, the new mucoadhesive film may be effective for the treatment of aphthous stomatitis.

• Journal of Pharmaceutical Investigation
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• v.5 no.1
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• pp.41-48
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• 1975

Extrusion-Spheronization Processing (ESP) was applied to preparate sustained release spherical particles as a form of matrix spherical particle (MSP). dl-methylephedrine HCI (ME) was the drug chosen and several dissolution retardants and binders were selected to estimate a relatively good formulation on this purpose. The effect of physicochemical nature, concentration, and solvents of these dissolution retardants and binders on regularity in shape of MSP and in vitro release rate was investigated. The effect of Particle size of matrix particles was also evaluated. It is, therefore, concluded that this ESP would be a relatively good preparation method of sustained release MSP of ME which has the sustained action of about 5 and 8 hours by formulating of ethylcellulose and ethylcellulose-paraffin as a dissolution retardant, respectively, and then ethylcellulose solution of 80% EtOH is recommended as a binder.

• Journal of Pharmaceutical Investigation
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• v.38 no.6
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• pp.381-385
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• 2008

Isosorbide dinitrate is an oral assiatant therapy agent of angina pectoris, myocardial infarction and congestive heart failure. The objective of this study was to formulate sustained release containing isosorbide dinitrate and assess their formulation variables. Pellets were prepared by fluid bed process and consist of drug layer and membrane layer. The pellets were coated with ethylcellulose along with $5{\sim}15%$ of plasticizer such as triacetin and diethyl butylrate. In vitro evaluation study was performed by comparative dissolution test between test and reference isosorbide dinitrate preparation. We could prepare sustained pellets of isosorbide dinitrate by fluid bed process which were reduced process time and had high content. The pellet coated with 1% ethylcellulose and triacetin(l5%) had a similar dissolution behavior compare to reference isosorbide dinitrate preparation controlling initial dissolution and those of dissolution at 30 min were 17.25 and 17.09%, respectively. Difference factor and similarity factor were $0{\sim}15$ and $50{\sim}100$ and there was no significant difference in bioequivalence between formulations. It might be concluded that our sustained release pellet of isosorbide dinitrate could be an alternatively delivery system to reference drug preparation.

• Journal of Pharmaceutical Investigation
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• v.19 no.1
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• pp.29-37
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• 1989

For the prevention of the aggregation during microencapsulation, the effects and role of polyisobutylene(PIB), as a protective colloid, were studied. The effects of sealant treatment on the microencapsulation were studied. Methyldopa was microencapsulated with ethylcellulose (EC) by polymer deposition from cyclohexane by temperature change using PIB. The EC-microencapsulated methyldopa was sealed with spermaceti. The dissolution of methyldopa was influenced by the drug to wall ratio. When PIB was used, low aggregation of microcapsules occurred and the surface was smooth with a few pores. Treatment of microcapsules with spermaceti retarded the release of methyldopa, the release being affected by the percentage of sealant used and the particle size of the product.