Solid pharmaceutical dosage formulations and processes

Patent metadata

Field	Value
Publication number	US-11464745-B2
Application number	US-201716463728-A
Country	US
Kind code	B2
Filing date	Nov 27, 2017
Priority date	Nov 28, 2016
Publication date	Oct 11, 2022
Grant date	Oct 11, 2022

Abstract

A process for producing a solid pharmaceutical dosage formulation, said process comprising powder bed fusion selective laser 3-dimensional printing of a mixture comprising: (a)a drug; and (b)an excipient; whereinat least one of said drug and said excipient absorbs electromagnetic radiation at a wavelength emitted by the laser; or (a)a drug; (b)an excipient; and (c)an absorbent material which absorbs electromagnetic radiation at a wavelength emitted by the laser.

First claim

The invention claimed is:

1. A process comprising: powder bed fusion selective laser 3-diminsional printing of a powder mixture comprising: (a) a drug; and (b) an excipient; wherein at least one of said drug and said excipient absorbs electromagnetic radiation at a wavelength emitted by the laser; or (a) a drug; (ab) an excipient; and (c) an absorbent material with absorbs electromagnetic radiation at a wavelength emitted by the laser, the absorbent material selected from the group consisting of iron oxide, titanium oxide, silicates, carmine, candurin, phtalacyanine, diazos, or mixtures thereof; and producing an oral formulation to the exclusion of a surgically inserted implant.

2. The process as claimed in claim 1 , wherein said powder bed fusion selective laser 3-dimensional printing comprises selective laser sintering 3-dimensional printing or selective laser melting 3-dimensional printing, or a mixture thereof.

3. The process as claimed in claim 1 wherein said excipient absorbs electromagnetic radiation at a wavelength emitted by the laser.

4. The process as claimed in claim 1 wherein said electromagnetic radiation is electromagnetic radiation within the infrared, visible or ultraviolet regions of the electromagnetic spectrum.

5. The process as claimed in claim 1 wherein the laser power is at least 1.5 W.

6. The process as claimed in claim 1 wherein said mixture is a heterogeneous mixture.

7. The process as claimed in claim 1 wherein the laser emits electromagnetic radiation having a wavelength in the range of from 200 nm to 11 μm without degradation of the drug.

8. The process as claimed in claim 1 wherein said printing is performed using a scan speed in the range of from 20 mm/s to 300 mm/s;
and/or
wherein said printing is performed using a surface temperature in the range of 40-180° C.

9. The process as claimed in claim 1 wherein said mixture comprises from 0.01 wt. % to 85 wt. % of the said drug by total weight of the mixture.

10. The process as claimed in claim 1 wherein said mixture comprises two or more excipients;
and/or
wherein said mixture comprises from 15 wt. % to 99.5 wt. % of the said excipients by total weight of the mixture.

11. The process as claimed in claim 1 wherein the said excipient comprises or consists of a polymer;
optionally wherein said polymer comprises at least one enteric polymer; or wherein said polymer comprises at least one pH-independently soluble polymer;
and/or
wherein said polymer has a glass transition temperature in the range of from −100° C. to 250° C.

12. The process as claimed in claim 11 wherein said polymer is selected from the group consisting of methyl acrylate-methacrylic acid copolymers, ethyl acrylate-methacrylic acid copolymers, cellulose acetate succinate, hydroxy propyl methyl cellulose phthalate, hydroxypropylmethyl cellulose acetate succinate, polyvinyl acetate phthalate, methyl methacrylate-methacrylic acid copolymers, shellac, cellulose acetate trimellitate, sodium alginate, zein, polyethylene oxide, ethylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, vinylpyrrolidone-vinyl acetate copolymers, gelatin, polysaccharides and mixtures thereof.

13. The process as claimed in claim 1 wherein said mixture comprises from 0.1 wt. % to 50 wt. % of the said absorbent material by total weight of the mixtures.

14. The process as claimed in claim 1 wherein said mixture comprises: (a) 1-50 wt. % of a drug selected from anti-inflammatory, steroid or antieoplastic drugs by total weight of the mixture, (b) 20-80 wt. % of an enteric polymer selected from methyl acrylate-methacrylic acid copolymers, ethyl acrylate-methacrylic acid copolymers, cellulose acetate succinate, hydroxy propyl methyl cellulose phthalate, hydroxypropylmethyl cellulose acetate succinate, polyvinyl acetate phthalate, methyl methacrylate-methacrylic acid copolymers, shellac, cellulose acetate trimellitate, sodium alginate, zein, polyethylene oxide, ethylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, vinylpyrrolidone-vinyl acetate copolymers, gelatin, polysaccharides and mixtures thereof, by total weight of the mixture; and (c) 0.1-30 wt. % of at last one absorbent material selected from the group consisting of iron oxide, titanium oxide, silicates, carmine, candurin, phthalocyanine, diazos or mixtures thereof, by total weight of the mixture.

15. A solid pharmaceutical dosage formulation produced by the process of claim 1 ; said solid pharmaceutical dosage formulation optionally having a laminated core comprising multiple layers, each layer comprising: (a) a drug, (b) an excipient, and (c) optionally an absorbent material selected from the group consisting of iron oxide, titianium oxide, silicates, carmine, candurin, phtalacyanine, diazos, or mixture thereof.

16. The solid pharmaceutical dosage formulation of claim 15 wherein said solid dosage formulation is bioadhesive and/or mucoadhesive.

17. A solid pharmaceutical dosage formulation, the surface of which comprises a drug and a sintered polymer and/or sintered absorbent material.

18. The solid pharmaceutical dosage formulation of claim 17 wherein said drug is suspended in a matrix comprising: (a) An excipient which absorbs electromagnetic radiation at a wavelength of 380 nm to 800 nm; or (b) an excipient; and (c) an absorbent material selected from the group consisting of iron oxide, titanium oxide, silicates, carmine, candurin, phtalocyanine, diazos, or mixtures thereof, which absorbs electromagnetic radiation at a wavelength of 380 nm to 800 nm.

19. The solid pharmaceutical dosage formulation claim 15 having a laminated core comprising multiple layers, each layer comprising: (a) a drug, (b) an excipient, and (c) optionally an absorbent material selected from the group consisting of iron oxide, titanium oxide, silicates, carmine, candurin, phtalocyanine, diazos, or mixtures thereof.

20. A process comprising: powder bed fusion selective laser 3-diminensional printing of a powder mixture comprising (a) a drug; and (b) an excipient; wherein at least one of said drug and said excipient absorbs electromagnetic radiation at a wavelength emitted by the laser; or (a) a drug; (ab) an excipient; and (c) an absorbent material which absorbs electromagnetic radiation at a wavelength emitted by the laser, the absorbent material selected from the group consisting of iron oxide, titanium oxide, silicates, carmine, candurin, phtalocyanine, diazos, or mixtures thereof; and producing an oral formulation having a controlled release of the drug.

Assignees

• Ucl Business Plc

Inventors

• Basit Abdul
• Goyanes Alvaro
• Gaisford Simon
• Fina Fabrizio

Classifications

• A61K31/606

  having amino groups · CPC title

• B33Y70/10

  Composites of different types of material, e.g. mixtures of ceramics and polymers or mixtures of metals and biomaterials · CPC title

• A61K9/1635

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/2095 Primary

  Tabletting processes · CPC title

• A61K9/0056

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title