前苏联专利SU1748630A3 Compound for incapsulation of biologically active substance

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专利摘要:
Composition pour l'enrobage d'une substance biologiquement active qui est stable dans un milieu dont le pH est supérieur ou égal à 5 et qui permet la libération de la substance active dont le pH est inférieur ou égal à 3,5 constituée d'un copolymère aminé basique (copolymère vinylpyridine-styrène) et d'une substance hydrophobe dont le point de fusion est supérieur à 60°C (acide stéarique), la teneur en substance hydrophobe étant comprise entre 50 et 90% de la masse totale de l'enrobage, ainsi que les granulés constitués d'un noyau contenant la substance biologiquement active enrobé par cette composition.
公开号:SU1748630A3
申请号:SU4203248
申请日:1987-09-03
公开日:1992-07-15
发明作者:Ардейон Пьер；Отан Пьер；Буррен Поль；Картиллье Андре
申请人:Рон-Пуленк Санте (Фирма)；
IPC主号:

专利说明:

"
Yo
. FIELD: feed production.
The purpose of the invention is to increase the stability of the composition at a pH equal to or higher than 5 and release of the biologically active substance at a pH of less than 3.5 while reducing the toxicity of the composition. Example 1. A fluidized bed method in a tank equipped with a WURSTER system is coated with 350 g methionine, pre-granulated in the form of spherical particles, with a content of 98%, the average diameter of which is 0.5-0.63 mm, with a solution having the following composition:
Stearic acid
(11.1gp. 68 - 69 ° С,
acid number 19 198) 88 g
Copolymer of 2-vinylpyridine a-styrene (70 - 80) 22 g Copolymer of 2-1,2-dichloroethane 500 cm3 Ethanol500 cm3
Antistatic (Labrazol, registered trademark GAHHEFO SSE) 3 cm3
The viscosity of the 2-vinylpyridine-styrene copolymer (70-80) is 0.5 W (measured at a concentration of 5 g / L in dimethylformamide at 20 ° C).
The solution maintained at 27 ° C is sprayed for 3 hours AO minutes. 392 g of coated granules with 73% methionine are obtained.
Salting out methionine is determined by dispersing 8 g of the resulting Pu2
00
about
00
about

with
3
the granules in 1 liter of the buffer solution maintained at 40 ° C and stirred with a magnetic stirrer.
Salted amount of methionine is monitored at sampling, the experiments are carried out at pH 6 and 2.
The results are summarized in table 1. „
Example 2 p. 2. Work as in Example 1, but spraying the composition of 1 h 30 min. Get 450 granules with a methionine content of 71.6%
The results of the salting out experiments are shown in Table 1,
EXAMPLE 3 Example 1 is employed, but a coating composition containing 48.8 g of stearic acid and 12.2 g of 2-vinylpyridine-styrene copolymer (70-30) is used, and spraying occurs. for 1 h at 47 ° C Get 400 g of granules with a methionine content of 82% „
The results of the salting out experiments
given in table1,
Example 4: Work as in Example 1, but using a coating composition containing 40 g of stearic acid and 10 g of 2-vinylpyridine-styrene copolymer (70-30), and spraying for 45 minutes at 45 ° s Obtain 381 g of granules with a methionine content of 86% 0
The results of experiments on salting out are given in table 1.
Example 5: Work as in Example 1, but replacing 1,2-dichloroethane.
methylene chloride.
The solution maintained at 30 ° C is sprayed for 44 minutes. Obtain 448 g of granules with a methionine content of 76.8%,
The results of the experiments on salting out are given in table 1,
Example 6: Dissolve 88 g of stearic acid (m.p. 66.9 ° C, acid number 199) and 22 g of 2-vinylpyridine-styrene copolymer (70 - 30) in 80 g of methyl isobutyl ketone.
This solution is heated to 85 ° C and added in 8 minutes to a solution mixed with a Polytron-type turbine 990 cm3 of water and 4.2 cm3 of 10% sodium (by volume). An emulsion is obtained, liquid and homogeneous at a temperature higher than or equal to 54 ° C.
According to the method of a fluidized bed in a tank equipped with a WURSTER system, cover 350 g of methionine preliminarily granulated in the form of spherical particles, with a content of 98%, the average diameter of which is -:
748630
g,
I
u S „
ten
IS
20
25
thirty
35
,,
40
e) 45
%- 50
| A, (55 -:
It is 0.5-0.63 mm, the emulsion obtained above.
The emulsion maintained at 64 ° C is sprayed for 69 minutes. Get 434 g of the coated granules with a methionine content of 78%.
The results of experiments on salting out are given in table 1.
Example 7: Work as in Example 6, but using an emulsion obtained by dispersion at 8 ° C, thief pactw 88 g of stearic acid and 22 g of 2-vinylpyridine-styrene copolymer (70-30) in 80 g of methyl isobutyl ketone in 495 cm3 of water and 4.2 cm3 of 10% (by volume) sodium.
The emulsion, maintained at 66 ° C, is sprayed for 33 minutes. 440 g of coated granules with a methionine content of 77.8% are obtained.
The results of experiments on salting out are given in table 1.
Example Work according to Example 6, replacing 80 g of methyl isobutyl ketone with 80 g of butyl acetate.
The emulsion, maintained at 63 ° C, is sprayed for 65 minutes. 436 g of coated granules with a methionine content of 79% are obtained.
The results of experiments on salting out are given in table 1.
Example 9: Work as in Example 1, but replacing 350 g of methionine with lysine hydrochloride, previously granulated in the form of spherical particles, the average diameter of which is 0.63 - 0.80 mm and a titer of 82%. - Spray time 3 h 30 min at 27 - 30 ° C. Obtain 450 g of granules containing 60.0% lysine hydrochloride.
The results of experiments on salting out are given in table 2.
Example 10: Work as in Example 9, but using a coating composition containing 93.5 g of stearic acid and 16.5 g of 2-vinylpyridine-styrene copolymer (70-30), and spraying for 3 hours. 16 min at 28 - 30 ° C. Obtain 380 g of granules containing lysine hydrochloride.
The results of experiments on salting out are given in table 2.
Example 11: Work as in Example 9, but using a coating composition containing 99 g of stearic acid and 11 g of 2-vinyl copolymer
pyridine styrene (70 - 30), and sprayed for 3 hours and 15 minutes at 29 - 35 ° C. Get g granules with a content of 60.2% lysine hydrochloride „
The results of the salting out experiments are given in Table 2
Example 12: Work as in Example 9, but using a coating composition containing 77 g of stearic acid and 33 g of 2-vinylpyridine-styrene copolymer (70-30), and spraying for 1 h 50 min at 32 -. Get A60 g of granules with lysine hydrochloride content of 58, H%.
The results of the salting out experiments are given in .2.
Example 13: Work as in Example 9, but using a coating composition containing 60.5 g of stearic acid and A3.5 g of 2-vinylpyridine-styrene copolymer (70-30), and spraying for 2 hours. 10 min at 39 - 1 ° С. Get 60 g of granules with a content of lysine hydrochloride of 59.8%.
The results of the salting out experiments are given in Table 2.
PRI me R I. Work as in Example 9, but spraying is carried out for 1 h 30 min at 37 - 39 ° C. Part 55 g of granules with a lysine chlorohydrate content of 61% is obtained.
The results of experiments on salting out are given in table 2.
Example 15: Work as in Example 9, but using a solution of the composition for coating in pure tetrahydrofuran and spraying for 2 hours at 20 ° C.
57 g of granules with a lysine hydrochloride content of 60.7% are obtained.
The results of experiments on salting out are given in table 3.
Example 16: Work as in Example 9, but using a solution of the composition for coating in a mixture of ethanol - tetrahydrofuran 1-1 (by volume) and spraying for 1 hour kQ min at 20 ° C. 57 g of granules with a lysine hlrhydrate content are obtained. 62%.
The results of experiments on salting out are listed in Table 2.
Example 17: Work at stage 9, but using a solution of the composition for coating in a mixture of ethanol 8630
acetone 1-1 (by volume) and sprayed for 3 hours and 30 minutes at r40 ° C. 455 g of granules are obtained with a lysine hydrochloride content of 59.2%.
The results of experiments on salting out are given in table 2.
Example 18. Work as in example 9, but using a composition for JQ coating, not containing antistatic
The solution maintained at 35 ° C is sprayed for 1 hour and 0 minutes. 56 g of coated granules with co. holding lysine hydrochloride 60%. jj - the results of experiments on salting out are given in table 2.
Example 19: Work as in Example 9, but using a coating solution in which 1,2-dichloroethane 20 is replaced with the same amount of chloro-. that methylene.
The solution maintained at 35 ° C is sprayed for 2 minutes. 55 g of coated granules with a content of 25 to 59% lysine hydrochloride are obtained.
The results of experiments on salting out are given in table 2.
EXAMPLE 20 This emulsion prepared according to Example 6 is used to coat 350 g of lysine hydrochloride, previously granulated in the form of spherical particles, the average diameter of which is 0.6335 0.80 mm with a titer of 82%.
The emulsion maintained at 65 ° C is sprayed for 6 hours. 51 g of coated granules are obtained with a lysine chlorohydrate content of 57%.
40 The results of the salting out experiments are given in table 2,
The efficacy in vivo of the proposed formulations for coating 45 can be shown as follows.
test, v
Samples of coated granules (approximately 0.5 g) are introduced into 6 packets of
0 nylon, having a mesh of 300 300 microns. The bags are placed on h8 h in the hem of the fatigue sheep. The bags are then removed and washed. One product is used for 3 or k sheep. The amount of active substance contained in the packets is determined by an appropriate method.
The results are shown in Table 3.
32.2 M), 9 9.2
6.6 11.1
having
114.8 g
28.7 g 650 cm3 650 cm3
71
EXAMPLE 23: By the Spray coating method, 350 g of granules containing vitamin A acetate, the diameter of which is 0.5-0.8 mm, are coated and have the following composition, in wt.%:
Vitamin A Acetate
Gelatin
Laktza
Glycemy
Stabilizers solution, for coating, the following composition:
Stearic acid
Copolymer of 2-vinylpyridine-styrene (70 - 30)
Ethanol
1,2-dichloroethane
The solution maintained at 3 ° C is sprayed at the rate of 10 cm3 / min. Covered granules are obtained, in which the grown titer of vitamin A is 618,000 uJ / r, the starting granules have a titer uJ / r.
Salting out in a test tube is determined at 37 ° C in artificial gastric medium at pH 1.2 in the presence of pepsin (by USE XX).
After 2 hours, the percentage of salted active substance is 93% for coated granules and 86% for the original granules.
eight
After 8 hours, the rumen resistance is 96.0 and 3.2% for the coated
granules and granules.
3.0 i 2.2% - for initial
five
6
S
The table shows the number of components in the composition, corresponding to the examples.

权利要求:
Claims (1)
[1]
Invention Formula
A composition for encapsulating a biologically active substance, including an amine-containing polymer and a hydrophobic substance, characterized in that, in order to increase the stability of the composition at pH 5 and release the biologically active substance, pH Ј 3.5 while reducing the toxicity of the composition, The polymer containing the composition contains a copolymer of styrene with 2-vinylpyridine, and as a hydrophobic substance, stearic acid with a melting point of 66.9 - 69 ° C and an acid number of 19 - T99 in the following ratio of components,%: copolymer with Tyrol with 2-vinylpyridine 10.0-5.0; stearic acid with a melting point of 66.9 - 69 ° C and an acid number of 191 - 199 55.0 - 90.0
Table3
eleven
Table
12

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HUT45402A|1988-07-28|

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AU613873B2|1991-08-15|

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优先权:

申请号 | 申请日 | 专利标题

FR8612412A|FR2603458B1|1986-09-04|1986-09-04|NOVEL COMPOSITIONS FOR COATING FOOD ADDITIVES FOR RUMINANTS AND FOOD ADDITIVES THUS COATED|

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