A New Method for Preparation of Enteric-Coated Microcapsules from Aqueous Medium(Pharmaceutical)

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A new and simple method for preparation of enteric-coated microcapsules (MC) from an aqueous medium was developed. The principle is based on the neutralization reaction between the enteric polymer dissolved in a weakly alkaline solution and the acidic drug used as a core material. Aspirin and carboxymethyl ethyl cellulose (CMEC) were used as model core and wall-forming materials, respectively. CMEC was dissolved in water by addition of sodium hydroxide, and aspirin crystals were poured into the solution. The aqueous phase near the crystal surface changed from alkaline to acidic, and the dissolved CMEC became insoluble locally, so that it adhered to the drug surface and formed a seamless film enveloping the crystal uniformly. The influence of the preparation conditions on such properties of the MC as release behavior in the 1st or the 2nd fluid of JPX, wall thickness, yield of single capsules and so on was investigated. As a result, some of MC were found to show a half-release time (t_<50>) of about 300min in the 1st fluid, but they dissolved rapidly in the 2nd fluid and showed an enteric-coated nature. The use of the minimum amount of sodium hydroxide required to dissolved CMEC was desirable to obtain MC of good enteric quality. As the amount of aspirin was increased, t_<50> in the 1st fluid decreased. The properties of MC were significantly influenced by the microencapsulation temperature, and t_<50> took the largest value at about 40℃.
公益社団法人日本薬学会の論文
1986-12-25

A New Method for Preparation of Enteric-Coated Microcapsules from Aqueous Medium(Pharmaceutical)

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