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US4053580A Expired / Lapsed US ⏱️ 0.0 years remaining

Microsealed pharmaceutical delivery device

Assignee: GD Searle LLC
•
Filing: 1976-09-20
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Granted: 1977-10-11
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Expires: 1996-09-20
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Abstract

Abstract The present invention is concerned with a pharmaceutical delivery device comprising a biologically acceptable silicone polymer matrix having microsealed compartments of 10-200 microns throughout, wherein the microsealed compartments contain a pharmaceutical in a hydrophilic solvent system. The biologically acceptable silicone polymer matrix is formed by in situ cross linking of a liquid, biologically acceptable silicone polymer in an emulsion of pharmaceutical in the hydrophilic solvent system and liquid biologically acceptable silicone polymer. The biologically acceptable silicone polymer matrix is placed in a sealed or unsealed biologically acceptable polymer container. The rate of release of pharmaceutical is controlled by altering the solubility characteristics of the hydrophilic solvent system and/or the biologically acceptable polymer matrix, the rate of release being independent of the time when the ratio of the partition coefficient of the pharmaceutical between the hydrophilic solvent system and biologically acceptable silicone polymer matrix to the solubility of the pharmaceutical in the hydrophilic solvent system is between 1 and 10 -4 ml/mcg.

Inventors

  • 👤 Yie W. Chien
  • 👤 Howard J. Lambert

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 20:46
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0087; A61K9/0092; A61K9/0012; A61K9/0019; A61K9/0024; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2031; A61K9/2036

Claims Analysis

Total Claims: 27
Claim 1
Independent Claim 124 words
A microsealed pharmaceutical delivery device comprising a sectioned length of flexible medical grade silicone polymer hollow tubing as a biologically acceptable polymer container with as many perforations in the wall of the tubing when unsealed at each end as to expose up to 40% of an inner biologically acceptable silicone polymer matrix contained with the biologically acceptable polymer container, said biologically acceptable silicone polymer matrix having the formula ##STR9## wherein R is alkoxy having 1-7 carbon atoms, alkyl having 1-10 carbon atoms, phenyl, vinyl, or allyl, wherein n is about 100-5000 and having 10-200 micron microsealed compartments throughout, said microsealed compartments containing pharmaceutical saturated 20-70 w/v% polyethylene glycol molecular weight 450-6000, 20-70 v/v% propylene glycol, or 20-70% 1-3-butanediol in water as hydrophilic solvent system.
Claim 2
Dependent Claim 124 words
A microsealed pharmaceutical delivery device comprising a sectioned length of flexible medical grade silicone polymer hollow tubing as a biologically acceptable polymer container with as many perforations in the wall of the tubing when unsealed at each end as to expose up to 40% of an inner biologically acceptable silicone polymer matrix contained with the biologically acceptable polymer container, said biologically acceptable silicone polymer matrix having the formula ##STR9## wherein R is alkoxy having 1-7 carbon atoms, alkyl having 1-10 carbon atoms, phenyl, vinyl, or allyl, wherein n is about 100-5000 and having 10-200 micron microsealed compartments throughout, said microsealed compartments containing pharmaceutical saturated 20-70 w/v% polyethylene glycol molecular weight 450-6000, 20-70 v/v% propylene glycol, or 20-70% 1-3-butanediol in water as hydrophilic solvent system.
Claim 3
Dependent Claim 219 words
As in claim 1, a microsealed pharmaceutical delivery device comprising a section length of flexible medical grade silicone polymer hollow tubing as a biologically acceptable polymer container with as many perforations in the wall of the tubing when unsealed at each end as to expose up to 40% of an inner biologically acceptable silicone polymer matrix contained and allowed to set within the biologically acceptable polymer container by placing therein a well stirred emulsion of pharmaceutical saturated 20-70 2/v% polyethylene glycol molecular weight 450-6000, 20-70 v/v% propylene glycol, or 20-70% 1-3-butanediol in water as hydrophilic solvent system, medical grade room temperature vulcanizing silicone polymer elastomer and stannous octanoate cross-linking agent; said inner biologically acceptable silicone polymer matrix having 10-200 micron microsealed compartments throughout, said microsealed compartments containing a pharmaceutical saturated in said hydrophilic solvent system wherein the ratio of the partition coefficient of the pharmaceutical between the hydrophilic solvent system and inner biologically acceptable silicone polymer matrix to the solutility of the pharmaceutical in the hydrophilic solvent system is between 1 and 10 -4 (ml/mcg), said pharmaceutical being diffusible through the inner biologically acceptable polymer container at a constant rate when the microsealed pharmaceutical delivery deivce is in an aqueous environment, said hydrophilic solvent being non-diffusible through the inner biologically acceptable silicone polymer matrix and biologically acceptable polymer container.
Claim 4
Dependent Claim 89 words
As in claim 1 a microsealed pharmaceutical delivery device comprising a biologically acceptable polymer container constructed of flexible medical grade silicone polymer hollow tubing having the formula ##STR10## wherein n is about 5000 and R is phenyl, loweralkyl, vinyl, or allyl and an inner biologically acceptable silicone polymer matrix contained within the biologically acceptable polymer container, said inner biologically acceptable polymer matrix having the formula ##STR11## wherein R is alkoxy having 1-7 carbon atoms, alkyl having 1-10 carbon atoms, phenyl, vinyl, or allyl and wherein n is about 100-5000.
Claim 5
Dependent Claim 15 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is a progestin.
Claim 6
Dependent Claim 14 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is progesterone.
Claim 7
Dependent Claim 15 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is 17α-ethynyl-4-estrene-3β,17β-diol diacetate.
Claim 8
Dependent Claim 15 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is 17α-ethynl-11β-methylestr-4-ene-3β,17β-diol 3,17-diacetate.
Claim 9
Dependent Claim 14 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is 17α-acetoxy-11β-methyl-19-norpregn-4-en-3,20-dione.
Claim 10
Dependent Claim 15 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is an estrogen.
Claim 11
Dependent Claim 14 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is mestranol.
Claim 12
Dependent Claim 15 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is ethynyl estradiol.
Claim 13
Dependent Claim 14 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is estradiol-3-methylether.
Claim 14
Dependent Claim 14 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is estradiol.
Claim 15
Dependent Claim 16 words
As in claim 1, a microsealed pharmaceutical delivery device wherein the pharmaceutical is an adrenocortical steroid.
Claim 16
Dependent Claim 14 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is desoxycorticosterone acetate.
Claim 17
Dependent Claim 13 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is prednisolone.
Claim 18
Dependent Claim 14 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is a diuretic.
Claim 19
Dependent Claim 15 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is 7α-ethoxycarbonyl-17-hydroxy-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone.
Claim 20
Dependent Claim 15 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is 17-hydroxy-7α-methoxycarbonyl-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone.
Claim 21
Dependent Claim 13 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is diisopropylamino-2-phenyl-2-(pyridyl)butyramide.
Claim 22
Dependent Claim 14 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is testosterone propionate.
Claim 23
Dependent Claim 13 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is metronidazole.
Claim 24
Dependent Claim 14 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is 7α-acetylthio-17α-(2-carboxyethyl)-17α-hydroxyandrost-4-ene-3-one lactone.
Claim 25
Dependent Claim 21 words
As in claim 1, a pharmaceutical delivery device wherein the pharmaceutical is a combination of ethynodiol diacetate and mestranol or ethynylestradiol.
Claim 26
Dependent Claim 47 words
As in claim 1, a microsealed pharmaceutical delivery device comprising an unsealed sectioned length of said flexible medical grade silicone polymer tubing as a biologically acceptable polymer container with said inner biologically acceptable silicone polymer matrix contained and set in situ within the biologically acceptable polymer container.
Claim 27
Dependent Claim 21 words
As in claim 1, a pharmaceutical delivery device wherein the solvent is 20-60 w/v polyethyleneglycol of molecular weight of about 4000-6000.

References Cited (Backward Citations)

US3279996A Cited
US3545439A Cited
US3518340A Cited
US3845761A Cited
US3710795A Cited
US3797485A Cited
US3832458A Cited
US3946106A Cited
US3992518A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-10-10 1981-04-11 1981-10-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-10-10 1985-04-11 1985-10-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-10-10 1989-04-11 1989-10-11 $7700.00 Window Closed / Lapsed

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