Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1993-07-16
1995-04-04
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
42840224, 514777, 514937, 514951, 514975, 264 41, A61K 916, A61K 950, A61K 3170
Patent
active
054035945
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new method for preparing microencapsulated spiramycin granules as well as to the formulations obtained from these granules.
Spiramycin, as well as its salts and its esters, is an antibiotic with a broad activity spectrum whose use by the oral route especially in children is limited because of problems of taste. Indeed, spiramycin, its salts or its esters, has physical or chemical properties which cause, at the level of the taste buds, a bitterness which results in a problem of ingestion which may lead to the rejection of the medicinal product by vomiting phenomena.
In adults, it has been possible to circumvent these disadvantages by administering spiramycin in the form of a tablet coated with a polymer or a glaze which avoids all contact between the active ingredient and the taste buds. In young children, this solution cannot be envisaged. The pharmaceutical industry has long been searching for a liquid form which can be administered to children or to adults, which permits a correct masking of the bitterness of the active ingredient even in solution.
The preparation of microcapsules of spiramycin coated with a protein, the latter being preferably albumin, is known via the Spanish Certificate of Importation No. 550171/7. It is specified in this text that the microcapsules can be used for the preparation of liquid suspensions. The method for preparing the said microcapsules is not easy to implement, it consists in preparing a mixture of spiramycin and albumin, in coagulating the albumin with heat, then in washing the solid obtained several times, in centrifuging it and then in drying it. It is specified in the text that the microcapsules have an irregular shape.
The present invention has made it possible to prepare ready-for-use granules composed of spiramycin encapsulated in albumin and diluted with a mixture of sugars and aromatic substances. The mode of preparation is greatly facilitated compared with the method described in the Spanish certificate mentioned above. Indeed, it no longer requires intermediate stages for washing the microcapsules in order to remove the solvent and makes it possible, in addition, to carry out all the stages in the same apparatus until the final formulation is obtained.
This method for preparing ready-for-use spiramycin formulations consists: at pH 7.5 to 8.5 in the presence of an antifoaming agent; the presence of an antifoaming agent; granulating it and drying it by stirring under vacuum; of stages 1 and 2 based on an albumin over spiramycin weight ratio of between 0.3 and 0.5, in heating the mixture to a temperature of between 35.degree. and 40.degree. C. in order to emulsify it, and then in heating it to a higher temperature in order to coagulate the albumin; preceding mixture at a temperature of less than 65.degree. C., under a pressure of less than 100 torrs; the fifth stage, based on a weight ratio of between five to one and fifty to one, optionally adding aromatic substances, sweeteners and/or colourings.
According to one embodiment of the invention, during the first stage, an aqueous solution, buffered to pH 7.5-8.5 by mixing disodium and monopotassium phosphate, is prepared in particular. The antifoaming agent which is added to this solution may be of chemical or physical origin. The physical agent may be a vacuum, the chemical agent may be chosen from anionic, cationic or nonionic surface-active agents (fatty acid esters and/or ethers). The use of sorbitan oleate is preferred. According to a preferred embodiment of the invention, about 0.3% by weight of sorbitan trioleate is added as antifoaming agent to the buffered aqueous solution and finally albumin is added based on a weight ratio relative to the buffered aqueous solution of about 20%. The stirring is maintained for a few hours until the albumin dissolves completely.
According to an improved embodiment of the invention, the pH is preferably adjusted to between 7.9 and 8.1 and the temperature is maintained between 25.degree. and 35.degree. C.
According to one embodiment of the
REFERENCES:
Derwent Publications Ltd., Abstract, Accession No. 87-066792, Jan. 1987.
Calvo Ana
Del Rio Luis A.
Esteban Manuel
Rona Robert
Oehler Ross J.
Page Thurman K.
Parker III Raymond S.
Rhone-Poulenc Rorer S.A.
Savitzky Martin F.
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