# US 10,500,163 B2 · Radiation sterilization of hypercompressed polymer dosage forms

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- Number: US 10,500,163 B2
- Document ID: US10500163B2
- Status: Granted
- Kind: B2
- Application number: 16/031,665
- Filed: 2018-07-10
- Published: 2019-01-17
- Granted: 2019-12-10
- Earliest claimed: 2017-07-11
- Assignees: Sustained Nano Systems LLC
- Applicants: Sustained Nano Systems LLC
- Inventors: Barry M. Libin; Jeffrey M. Liebmann; Weiliam Chen
- Web page: https://patentgrep.com/patent/US10500163B2

## CPC

- A61K 9/0051: {Ocular inserts or implants}
- A61K 9/5089: {Processes}
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 9/204: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61L 2/087: Particle radiation, e.g. electron-beam, alpha or beta radiation
- A61P 27/02: Ophthalmic agents
- A61L 2103/05: Living organisms or biological materials
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A sterile pharmaceutical dosage form which comprises an ester capped lactide polymer, glycolide polymer or a lactide-glycolide copolymer hypercompressed with an active pharmaceutical ingredient wherein said sterile pharmaceutical dosage form has been sterilized with an electron beam and a method of preparing said sterile pharmaceutical dosage form.

## Claims

### Claim 1

A sterile pharmaceutical dosage form which comprises an ester capped lactide polymer, ester capped glycolide polymer or an ester capped lactide-glycolide copolymer that is hypercompressed with an active pharmaceutical ingredient wherein said sterile pharmaceutical dosage form has been sterilized with an electron beam.

### Claim 2 (depends on 1)

A sterile pharmaceutical dosage form as defined in claim 1 where the active pharmaceutical ingredient is selected from the group consisting of steroids, non-steroidal anti-inflammatory drugs, antihistamines, antibiotics, mydriatics, beta-adrenergic antagonists anesthetics,alpha-2-beta adrenergic agonists, mast cell stabilizers, prostaglandin analogues, sympathomimetics, parasympathomimetics, antiproliferative agents, agents to reduce ocular angiogenesis and neovascularization, vasoconstrictors, anti-neoplastic agents, a polynucleotide, or a recombinant protein analog an angiogenic inhibitors and combinations thereof.

### Claim 3 (depends on 2)

A sterile pharmaceutical dosage form as defined in claim 2 where the therapeutic agent is a steroid.

### Claim 4 (depends on 1)

A sterile pharmaceutical dosage form as defined in claim 1 where the polymer is selected from the group consisting of ester capped poly(dl-lactide), ester capped polyglycolide,ester capped poly(glycolide-co-lactide), and ester capped poly(glycolide-co-dl-lactide), or a mixture of any of the foregoing.

### Claim 5 (depends on 4)

A sterile pharmaceutical dosage form as defined in claim 4 where the dosage form has been compressed by the application of 50K psi to 350K psi.

### Claim 6 (depends on 5)

A sterile pharmaceutical dosage form as defined in claim 5 where the dosage form has been compressed by the application of 100 Kpsi to 300 Kpsi.

### Claim 7 (depends on 5)

A sterile pharmaceutical dosage form as defined in claim 5 where the dosage form has been compressed by the application of 200 Kpsi to 300 Kpsi.

### Claim 8 (depends on 1)

A method of preparing a sterile hypercompressed pharmaceutical dosage form according to claim 1 where the active pharmaceutical ingredient is selected from the group consisting of peptides and proteins.

### Claim 9

A method of preparing a sterile hypercompressed pharmaceutical dosage form of an ester capped lactide polymer, ester capped glycolide polymer or an ester capped lactide-glycolide copolymer which comprises:
(a) combining an active pharmaceutical ingredient with an ester capped lactide polymer, an ester capped glycolide polymer or an ester capped lactide-glycolide copolymer to form a powdered product;
(b) hypercompressing the powdered product of step (a) to form a hypercompresed dosage form; and
(c) exposing the hypercompressed dosage form of step (b) to a sterilizing amount of an E-beam radiation source to form a sterilized product.

### Claim 10 (depends on 9)

A method of preparing a sterile hypercompressed pharmaceutical dosage form according to claim 9 where the active pharmaceutical ingredient is selected from the group consisting of steroids, non-steroidal anti-inflammatory drugs, antihistamines, antibiotics, mydriatics, beta-adrenergic antagonists anesthetics, alpha-2-beta adrenergic agonists, mast cell stabilizers, prostaglandin analogues, sympathomimetics, parasympathomimetics, antiproliferative agents, agents to reduce ocular angiogenesis and neovascularization, vasoconstrictors, anti-neoplastic agents, a polynucleotide, or a recombinant protein analog an angiogenic inhibitors and combinations thereof.

### Claim 11 (depends on 9)

A method of preparing a sterile hypercompressed pharmaceutical dosage form according to claim 9 where the dosage form has been compressed by the application of 50K psi to 350K psi.

### Claim 12 (depends on 9)

A method of preparing a sterile hypercompressed pharmaceutical dosage form according to claim 9 where the dosage form has been compressed by the application of 100 Kpsi to 300 Kpsi.

### Claim 13 (depends on 9)

A method of preparing a sterile hypercompressed pharmaceutical dosage form according to claim 9 where the dosage form has been compressed by the application of 200 Kpsi to 300 Kpsi.