US4145410A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Method of preparing a controlled-release pharmaceutical preparation, and resulting composition
Assignee: LIPID SPECIALTIES Inc A CORP OF
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Filing: 1977-06-17
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Granted: 1979-03-20
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Expires: 1997-06-17
Abstract
Abstract A method of preparing a controlled-release pharmaceutical compound for oral administration, which pharmaceutical compound is subject to enzymatic hydrolysis on oral administration, which method comprises encapsulating the pharmaceutical compound with a synthetic phosphatidyl compound having a modified polarhead moiety which increases the resistance of the phosphatidyl compound to phospholipase C hydrolysis.
Inventors
- 👤 Barry D. Sears
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:27
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/66; A61K31/683; A61K31/685; A61K47/00; A61K47/06; A61K47/24; B; B82; B82Y; B82Y5/00; C; C07; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/08; C07F9/09; C07F9/10; C07F9/28; C07F9/54; C07F9/5407; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
118 words
In a method for preparing a controlled-release pharmaceutical composition for oral administration, the method which comprises: forming an aqueous emulsion of phospholipid encapsulating agent with the pharmaceutical compound whose release is to be controlled; coagulating the emulsion to entrap the pharmaceutical compound within the phospholipid agent; and recovering the pharmaceutical composition as prepared, the improvement which comprises: employing as the phospholipid encapsulating agent a synthetic fatty-acid phosphatidyl C 1 -C 10 alkyl-N-C 1 -C 4 trialkyl quaternary-ammonium hydroxide compound, with the proviso that the alkyl of the alkyl-N group is not an ethyl group when the alkyl groups of the N-trialkyl radicals are methyl groups, and which phosphatidyl quaternary-ammonium compound is resistant to enzymatic hydrolysis of phospholipase C.
Claim 2
Dependent Claim
118 words
In a method for preparing a controlled-release pharmaceutical composition for oral administration, the method which comprises: forming an aqueous emulsion of phospholipid encapsulating agent with the pharmaceutical compound whose release is to be controlled; coagulating the emulsion to entrap the pharmaceutical compound within the phospholipid agent; and recovering the pharmaceutical composition as prepared, the improvement which comprises: employing as the phospholipid encapsulating agent a synthetic fatty-acid phosphatidyl C 1 -C 10 alkyl-N-C 1 -C 4 trialkyl quaternary-ammonium hydroxide compound, with the proviso that the alkyl of the alkyl-N group is not an ethyl group when the alkyl groups of the N-trialkyl radicals are methyl groups, and which phosphatidyl quaternary-ammonium compound is resistant to enzymatic hydrolysis of phospholipase C.
Claim 3
Dependent Claim
18 words
The method of claim 1 wherein the fatty acid is a C 14 to C 20 fatty-acid radical.
Claim 4
Dependent Claim
26 words
The method of claim 1 wherein the alkyl-N of the quaternary-ammonium compound is butyl-N or propyl-N, and the trialkyl groups are all the same alkyl group.
Claim 5
Dependent Claim
14 words
The method of claim 3 wherein the trialkyl groups are methyl or ethyl groups.
Claim 6
Dependent Claim
44 words
The method of claim 1 wherein the quaternary-ammonium compound is selected from the group consisting of: dimyristoyl phosphatidyl ethyl-N-dimethyl, propyl ammonium hydroxide; dimyristoyl phosphatidyl ethyl-N-dimethyl, ethyl ammonium hydroxide; dimyristoyl phosphatidyl propyl-N-trimethyl ammonium hydroxide; dimyristoyl phosphatidyl butyl-N-trimethyl ammonium hydroxide; and dimyristoyl phosphatidyl propyl-N-triethyl ammonium hydroxide.
Claim 7
Dependent Claim
11 words
The method of claim 1 wherein the pharmaceutical compound is insulin.
Claim 8
Dependent Claim
10 words
The controlled-release composition prepared by the method of claim 6.
Claim 9
Dependent Claim
19 words
The method of claim 1 wherein the encapsulated pharmaceutical compound is enzymatically hydrolyzed by phospholipase C in the stomach.
Claim 10
Dependent Claim
11 words
The controlled-release pharmaceutical composition prepared by the method of claim 1.
Claim 11
Dependent Claim
23 words
The method of claim 1 which comprises: sonification of the pharmaceutical compound and the synthetic phospholipid compound together to encapsulate the pharmaceutical compound.
References Cited (Backward Citations)
US4016100A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-19 | 1982-09-18 | 1983-03-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-19 | 1986-09-18 | 1987-03-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-19 | 1990-09-18 | 1991-03-20 | $7700.00 | Window Closed / Lapsed |