# US 8,771,740 B2 · Process for producing nanoparticles by spray drying

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- Number: US 8,771,740 B2
- Document ID: US8771740B2
- Status: Granted
- Kind: B2
- Application number: 11/438,240
- Filed: 2006-05-21
- Published: 2006-09-21
- Granted: 2014-07-08
- Earliest claimed: 1999-12-20
- Applicants: Nicholas J. Kerkhof
- Inventors: Nicholas J. Kerkhof
- Web page: https://patentgrep.com/patent/US8771740B2

## CPC

- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 31/175: having the group [IMAGE cpc-sch-A61K-0950.gif] , >N—C(O)—N=N— or[IMAGE cpc-sch-A61K-0951.gif] , e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazones; Thioanalogues thereof
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047)
- A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)}
- 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)

## Abstract

Nanoparticles of a compound are produced by spraying a solution of the compound into a heated chamber. The resulting product comprises a free flowing mixture of nanoparticles of the compound.

## Claims

### Claim 1

A process for producing particles wherein the particles are produced by:
preparing a solution of a pharmaceutical compound in a liquid medium in which the compound is dissolved; and
spraying the solution of the dissolved compound into an empty heated chamber at a rate of 25 to 50 ml/min, wherein the spraying step produces particles of the compound having a mean diameter of 50 nm to 3000 nm in the heated chamber.

### Claim 2 (depends on 1)

The process of claim 1, wherein said particles of said compound have a mean diameter from about 1000 nm to about 2000 nm.

### Claim 3 (depends on 1)

The process of claim 1, wherein said particles of said compound have a mean diameter of less than 1000 nm.

### Claim 4 (depends on 1)

The process of claim 1, wherein the resulting particles of said compound have a mean diameter of about 50 nm to about 1000 nm.

### Claim 5 (depends on 1)

The process of claim 1, wherein the resulting particles of said compound have a mean diameter of about 300 to about 800 nm.

### Claim 6 (depends on 1)

The process of claim 1, wherein the compound is substantially water insoluble.

### Claim 7 (depends on 6)

The process of claim 6, wherein the liquid medium comprises at least one non-aqueous solvent.

### Claim 8 (depends on 1)

The process of claim 1, wherein the liquid medium comprises at least one aqueous solvent.

### Claim 9 (depends on 1)

The process of claim 1, wherein the chamber comprises a heated, fluidized bed of carrier particles.

### Claim 10 (depends on 1)

The process of claim 1, wherein the compound solution comprises a carrier molecule.

### Claim 11 (depends on 1)

The process of claim 1, wherein said compound is selected from proteins, peptides, active agents, analgesics, anti-inflammatory agents, anthelmintics, anti-arrhythmic agents, antibiotics, anticoagulants, antidepressants, antidiabetic agents, antiepileptics, antihistamines, antihypertensive agents, antimuscarinic agents, antimycobacterial agents, antineoplastic agents, immunosuppressants, antithyroid agents, antiviral agents, anxiolytic sedatives, astringents, beta-adrenoceptor blocking agents, contrast media, corticosteroids, cough suppressants, diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics, haemostatics, immunological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin, prostaglandins, radio-pharmaceuticals, sex hormones, anti-allergic agents, stimulants, sympathomimetics, thyroid agents, vasodilators and xanthines.

### Claim 12 (depends on 10)

The process of claim 10, wherein said carrier molecule is selected from the group consisting of xylitol, mannitol, sorbitol, arabinose, ribose, xylose, glucose, mannose, galactose, sucrose, lactose, sodium lauryl sulfate, docusate sodium and hydroxy propyl methyl cellulose.

### Claim 13 (depends on 1)

The process of claim 1, wherein said spraying step occurs from one or more spraying nozzles in an apparatus equipped with an insert for (a) top spray using a Wurster-type column, (b) bottom spray using a Wurster-type column, or (c) tangential spray using a rotor disk.

### Claim 14 (depends on 1)

The process of claim 1, wherein said dissolved compound solution further comprises one or more other substances that alter the release profile of the compound from the resulting particles.

### Claim 15 (depends on 14)

The process of claim 14, wherein said one or more other substances are surface modifiers or surfactants.

### Claim 16 (depends on 14)

The process of claim 14, wherein said one or more other substances are selected from the group consisting of gelatin, casein, lecithin, gum acacia, cholesterol, tragacanth, stearic acid, benzalkonium chloride, calcium stearate, glyceryl monostearate, cetostearyl alcohol, cetomacrogol emulsifying wax, sorbitan esters, polyoxyethylene alkyl ethers, polyoxyethylene caster oil derivatives, polyoxyethylene sorbitan fatty acid esters, polyethylene glycols, polyoxyethylene stearates, colloidol silicon dioxide, phosphates, sodium dodecylsulfate, carboxymethylcellulose calcium, carboxymethylcellulose sodium, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethycellulose phthalate, noncrystalline cellulose, magnesium aluminum silicate, triethanolamine, polyvinyl alcohol, and polyvinylpyrrolidone.

### Claim 17 (depends on 1)

The process of claim 1, wherein said particles are combined with a pharmaceutically acceptable carrier or diluent to form a pharmaceutical composition.

### Claim 18 (depends on 17)

The process of claim 17, wherein said composition is administered to a user.

### Claim 19 (depends on 18)

The process of claim 18, wherein said administration occurs via oral gastrointestinal delivery, buccal delivery, sublingual delivery, pulmonary delivery, nasal delivery, vaginal delivery, rectal delivery, ocular delivery, otic delivery, epidermal delivery, dermal delivery or parenteral delivery.