RU96102011A - XINAFOAT SALMETEROL WITH ADJUSTABLE PARTICLE SIZE - Google Patents

XINAFOAT SALMETEROL WITH ADJUSTABLE PARTICLE SIZE

Info

Publication number
RU96102011A
RU96102011A RU96102011/04A RU96102011A RU96102011A RU 96102011 A RU96102011 A RU 96102011A RU 96102011/04 A RU96102011/04 A RU 96102011/04A RU 96102011 A RU96102011 A RU 96102011A RU 96102011 A RU96102011 A RU 96102011A
Authority
RU
Russia
Prior art keywords
salmeterol xinafoate
salmeterol
particle size
carrier
xinafoate
Prior art date
Application number
RU96102011/04A
Other languages
Russian (ru)
Other versions
RU2136655C1 (en
Inventor
Питер Йорк
Мэйзен Ханн
Original Assignee
Глаксо Груп Лимитед
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB939313650A external-priority patent/GB9313650D0/en
Application filed by Глаксо Груп Лимитед filed Critical Глаксо Груп Лимитед
Publication of RU96102011A publication Critical patent/RU96102011A/en
Application granted granted Critical
Publication of RU2136655C1 publication Critical patent/RU2136655C1/en

Links

Claims (16)

1. 4-Гидрокси- α- [[[6-(4-фенилбутокси) гексил] амино] метил]-1,3- бензолдиметанол (сальметерол), 1-гидрокси-2-нафталинкарбоксилат (ксинафоат) в удобной в обращении и легко ожижаемой кристаллической форме с регулируемыми размером и формой частиц.1. 4-Hydroxy-α- [[[6- (4-phenylbutoxy) hexyl] amino] methyl] -1,3-benzenedimethanol (salmeterol), 1-hydroxy-2-naphthalene carboxylate (xinafoate), easy to handle and easy to handle fluidizable crystalline form with adjustable particle size and shape. 2. Сальметерол ксинафоат по п.1, отличающийся тем, что он находится в форме, имеющей динамическую объемную плотность менее 0,1 г • см- 3.2. Salmeterol xinafoate according to claim 1, characterized in that it is in a form having a dynamic bulk density of less than 0.1 g • cm - 3 . 3. Сальметерол ксинафолат по п.1 или 2, отличающийся тем, что его динамическая объемная плотность составляет от 0,01 до 0,075 г • см- 3.3. Salmeterol xinafolate according to claim 1 or 2, characterized in that its dynamic bulk density is from 0.01 to 0.075 g • cm - 3 . 4. Сальметерол ксинафоат по пп.1 - 3, отличающийся тем, что он имеет размер частиц 1 - 10 мкм. 4. Salmeterol xinafoate according to claims 1 to 3, characterized in that it has a particle size of 1 to 10 microns. 5. Сальметерол ксинафоат по пп.1 - 4, отличающийся тем, что он имеет коэффициент однородности 1 - 20. 5. Salmeterol xinafoate according to claims 1 to 4, characterized in that it has a uniformity coefficient of 1 to 20. 6. Сальметерол ксинафоат по пп.1 - 5, отличающийся тем, что он имеет респирабельную фракцию 14% и более по массе. 6. Salmeterol xinafoate according to claims 1 to 5, characterized in that it has a respirable fraction of 14% or more by weight. 7. Сальметерол ксинафоат по пп.1 - 6, отличающийся тем, что он имеет респирабельную фракцию 15 - 30% по массе. 7. Salmeterol xinafoate according to claims 1 to 6, characterized in that it has a respirable fraction of 15-30% by weight. 8. Сальметерол ксинафоат по пп.1 - 7, отличающийся тем, что он имеет когезионную способность 0 - 20%. 8. Salmeterol xinafoate according to claims 1 to 7, characterized in that it has a cohesive capacity of 0 - 20%. 9. Сальметерол ксинафоат по пп.1 - 8, отличающийся тем, что он имеет когезионную способность 0 - 5%. 9. Salmeterol xinafoate according to claims 1 to 8, characterized in that it has a cohesive capacity of 0-5%. 10. Сальметерол ксинафоат по пп.1 - 9, отличающийся тем, что он находится в форме чистого полиморфа I и имеет единственную эндотерму около 123,5oС определяемую дифференциальной сканирующей калориметрией.10. Salmeterol xinafoate according to claims 1 to 9, characterized in that it is in the form of pure polymorph I and has a single endotherm of about 123.5 o C determined by differential scanning calorimetry. 11. Сальметерол ксинафоат по пп.1 - 10, отличающийся тем, что он находится в форме чистого полиморфа II и имеет единственную эндотерму около 135,8oС, определяемую дифференциальной сканирующей калориметрией.11. Salmeterol xinafoate according to claims 1 to 10, characterized in that it is in the form of pure polymorph II and has a single endotherm of about 135.8 ° C, determined by differential scanning calorimetry. 12. Фармацевтический состав, содержащий сальметерол ксинафоат по пп.1 - 11 вместе с фармацевтически приемлемым носителем. 12. A pharmaceutical composition comprising salmeterol xinafoate according to claims 1 to 11 together with a pharmaceutically acceptable carrier. 13. Состав по п.12, отличающийся тем, что носитель представляет собой диоксид кремния или гидроксипропилцеллюлозу. 13. The composition according to p. 12, characterized in that the carrier is a silicon dioxide or hydroxypropyl cellulose. 14. Состав по п.12, отличающийся тем, что носитель представляет собой лактозу. 14. The composition according to p. 12, characterized in that the carrier is lactose. 15. Состав по п.14, отличающийся тем, что он имеет форму сухого порошка, пригодного для ингаляции. 15. The composition according to p. 14, characterized in that it has the form of a dry powder suitable for inhalation. 16. Состав по пп.12 - 15, отличающийся тем, что он имеет форму многокомпонентных частиц, содержащих сальметерол ксинафоат и носитель. 16. The composition according to PP.12 to 15, characterized in that it has the form of multicomponent particles containing salmeterol xinafoate and a carrier.
RU96102011A 1993-07-01 1994-06-30 Salmeterol xinafoate exhibiting controlled particle size and pharmaceutical composition RU2136655C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB939313650A GB9313650D0 (en) 1993-07-01 1993-07-01 Method and apparatus for the formation of particles
GB9313650.5 1993-07-01
PCT/GB1994/001425 WO1995001324A1 (en) 1993-07-01 1994-06-30 Salmeterol xinafoate with controlled particle size

Publications (2)

Publication Number Publication Date
RU96102011A true RU96102011A (en) 1998-05-20
RU2136655C1 RU2136655C1 (en) 1999-09-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
RU96102011A RU2136655C1 (en) 1993-07-01 1994-06-30 Salmeterol xinafoate exhibiting controlled particle size and pharmaceutical composition

Country Status (20)

Country Link
US (1) US5795594A (en)
EP (1) EP0706507B1 (en)
JP (1) JP3839042B2 (en)
CN (1) CN1062854C (en)
AT (1) ATE184870T1 (en)
AU (1) AU684795B2 (en)
BR (1) BR9406995A (en)
CA (1) CA2165830C (en)
DE (1) DE69420844T2 (en)
DK (1) DK0706507T3 (en)
ES (1) ES2138085T3 (en)
FI (1) FI956343A (en)
GB (1) GB9313650D0 (en)
GR (1) GR3032065T3 (en)
HK (1) HK1004216A1 (en)
HU (1) HUT73733A (en)
NO (1) NO304940B1 (en)
NZ (1) NZ267696A (en)
RU (1) RU2136655C1 (en)
WO (1) WO1995001324A1 (en)

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