US4127622A
Expired / Lapsed
US
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Process for the preparation of hollow particulates
Assignee: Eisai Co Ltd
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Filing: 1975-09-19
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Granted: 1978-11-28
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Expires: 1995-09-19
Abstract
Abstract A hollow particulate for gastric medicines and other durable medicines suspendable in the gastric juice and remainable in the stomach for a long period of time is provided which has been prepared by dissolving ethylcellulose in a lower chlorinated hydrocarbon, or a mixed solution of the lower chlorinated hydrocarbon and a lower chlorofluorinated hydrocarbon and/or water, so that the concentration of ethylcellulose is 0.5 - 4% by weight on the basis of the total weight of the resulting solution, and then spray-drying the solution at an inlet temperature of higher than 50° C.
Inventors
- 👤 Sumio Watanabe
- 👤 Yasuhiko Mizuno
- 👤 Masanori Kayano
- 👤 Yoshio Ishino
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 05:56
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0053; A61K9/0065; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047; A61K9/5089
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
136 words
A process for preparing spherical, hollow particulates, which comprises dissolving ethylcellulose in a solvent selected from the group consisting of a lower chlorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon and a lower chlorofluorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon, a lower chlorofluorinated hydrocarbon and water, and a mixture of a lower chlorinated hydrocarbon and water, to form a solution having a concentration of ethylcellulose of 0.5-4% by weight based on the total weight of the solution, and spray-drying the solution by introducing said solution into a spray dryer at an inlet temperature for the spray dryer of higher than 50° C., to obtain spherical, hollow particulates having a diameter of about 10-200 μ, an internal space volume ratio of greater than about 50%, and an apparent density of less than about 0.7.
Claim 2
Dependent Claim
136 words
A process for preparing spherical, hollow particulates, which comprises dissolving ethylcellulose in a solvent selected from the group consisting of a lower chlorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon and a lower chlorofluorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon, a lower chlorofluorinated hydrocarbon and water, and a mixture of a lower chlorinated hydrocarbon and water, to form a solution having a concentration of ethylcellulose of 0.5-4% by weight based on the total weight of the solution, and spray-drying the solution by introducing said solution into a spray dryer at an inlet temperature for the spray dryer of higher than 50° C., to obtain spherical, hollow particulates having a diameter of about 10-200 μ, an internal space volume ratio of greater than about 50%, and an apparent density of less than about 0.7.
Claim 3
Dependent Claim
163 words
A process for preparing a shperical particulate material composed of a shell of ethylcellulose completely surrounding a pharmacologically active ingredient, which comprises dissolving ethylcellulose in a solvent selected from the group consisting of a lower chlorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon and a lower chlorofluorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon, a lower chlorofluorinated hydrocarbon and water, and a mixture of a lower chlorinated hydrocarbon and water, to form a solution having a concentration of ethylcellulose of 0.5-4% by weight based on the total weight of the solution, mixing a pharmacologically active ingredient, and optionally a pharmaceutical excipient, with said solution, and spray-drying the resultant mixture by introducing said mixture into a spray dryer at an inlet temperature for the spray dryer of higher than 50° C., to obtain spherical, hollow particulates having a diameter of about 10-200 μ, an internal space volume ratio of greater than about 50%, and an apparent density of less than about 0.7.
Claim 4
Dependent Claim
163 words
A process for preparing a shperical particulate material composed of a shell of ethylcellulose completely surrounding a pharmacologically active ingredient, which comprises dissolving ethylcellulose in a solvent selected from the group consisting of a lower chlorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon and a lower chlorofluorinated hydrocarbon, a mixture of a lower chlorinated hydrocarbon, a lower chlorofluorinated hydrocarbon and water, and a mixture of a lower chlorinated hydrocarbon and water, to form a solution having a concentration of ethylcellulose of 0.5-4% by weight based on the total weight of the solution, mixing a pharmacologically active ingredient, and optionally a pharmaceutical excipient, with said solution, and spray-drying the resultant mixture by introducing said mixture into a spray dryer at an inlet temperature for the spray dryer of higher than 50° C., to obtain spherical, hollow particulates having a diameter of about 10-200 μ, an internal space volume ratio of greater than about 50%, and an apparent density of less than about 0.7.
Claim 5
Dependent Claim
15 words
A process as claimed in claim 2, wherein the solvent is a lower chlorinated hydrocarbon.
Claim 6
Dependent Claim
23 words
A process as claimed in claim 2, wherein the solvent is a mixture of a lower chlorinated hydrocarbon and a lower chlorofuorinated hydrocarbon.
Claim 7
Dependent Claim
24 words
A process as claimed in claim 2, wherein the solvent is a mixture of a lower chlorinated hydrocarbon, a lower chlorofluorinated hydrocarbon and water.
Claim 8
Dependent Claim
20 words
A process as claimed in claim 2, wherein the solvent is a mixture of a lower chlorinated hydrocarbon and water.
Claim 9
Dependent Claim
21 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is a medicine which effects the gastric mucous membrane.
Claim 10
Dependent Claim
28 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is a medicine which is absorbed by the gastric mucous membrane to exhibit its medicinal effects.
Claim 11
Dependent Claim
20 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is a medicine which effects the gastric juice.
Claim 12
Dependent Claim
15 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is an antacid.
Claim 13
Dependent Claim
16 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is an anti-pepsin agent.
Claim 14
Dependent Claim
19 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is local anesthetic accelerator of gastric motion.
Claim 15
Dependent Claim
15 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is benactyzine hydrochloride.
Claim 16
Dependent Claim
14 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is oxethazaine.
Claim 17
Dependent Claim
15 words
A process as claimed in claim 2, wherein the excipient is a precipitated calcium carbonate.
Claim 18
Dependent Claim
18 words
A process as claimed in claim 2, wherein the pharmacologically active ingredient is S-PI of the formula ##STR1##
Claim 19
Dependent Claim
33 words
A process as claimed in claim 2, wherein the total weight amount of the pharmacologically active ingredient and, if present, the pharmaceutical excipient, is less than 8 times the weight of the ethylcellulose.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-11-27 | 1982-05-29 | 1982-11-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-11-27 | 1986-05-29 | 1986-11-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-11-27 | 1990-05-29 | 1990-11-28 | $7700.00 | Window Closed / Lapsed |