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PROCESS FOR PREPARING MELT GRANULATED PHARMACEUTICAL FORMULATION

IP.com Disclosure Number: IPCOM000244857D
Publication Date: 2016-Jan-22
Document File: 6 page(s) / 55K

Publishing Venue

The IP.com Prior Art Database

Abstract

The present disclosure provides a process for preparing a pharmaceutical formulation comprising: (i) loading a drug into a granulator; (ii) heating the granulator to partially melt the drug; (iii) granulating the remaining drug with the partially melted drug of step (ii); and (iv) processing the granules of step (iii) with one or more pharmaceutically acceptable excipients into a pharmaceutical formulation. Alternatively, the drug can be completely melted and processed into a pharmaceutical formulation.

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PROCESS FOR PREPARING MELT GRANULATED PHARMACEUTICAL FORMULATION

Abstract

The present disclosure provides a process for preparing a pharmaceutical formulation comprising: (i) loading a drug into a granulator; (ii) heating the granulator to partially melt the drug; (iii) granulating the remaining drug with the partially melted drug of step (ii); and (iv) processing the granules of step (iii) with one or more pharmaceutically acceptable excipients into a pharmaceutical formulation.  Alternatively, the drug can be completely melted and processed into a pharmaceutical formulation.

The present disclosure provides processes for preparing melt granulated pharmaceutical formulations, wherein the processes do not require use of any thermoplastic binder.  Instead, a partially melted drug is used a granulating agent.  The present disclosure is suitable for thermodynamically stable drugs.

Reported herein is a process for preparing a pharmaceutical formulation comprising:

(i)   loading a drug into a granulator;

(ii)  heating the granulator to partially melt the drug;

(iii) granulating the remaining drug with the partially melted drug of step (ii); and

(iv) processing the granules of step (iii) with one or more pharmaceutically acceptable excipients into a pharmaceutical formulation. 

Alternatively, the drug can be completely melted and processed into a pharmaceutical formulation.

Also reported herein is a process for preparing a pharmaceutical formulation comprising:

(i)   loading a drug into a granulator;

(ii)  heating the granulator to completely melt the drug;

(iii) cooling the melted drug of step (ii) to form solidified drug particles;

(iv) milling the solidified drug particles of step (iii); and

(v)  processing the milled particles of step (iv) with one or more pharmaceutically acceptable excipients into a pharmaceutical formulation.

The drug is selected from the group comprising metaxalone, efavirenz, atazanavir, acetaminophen, nelfinavir, praziquantel, sulfadiazine, sulphamethoxazole, sultamicillin, acetyl salicylic acid, L-carbocysteine, theophylline, amoxicillin, carbamazepine, levodopa, ibuprofen, acyclovir, celecoxib, albendazole, cefuroxime axetil, diloxamide, valproic acid, indinavir, linezolid, mebendazole, nalidixic acid, niclosamide, oxacarbazepine, and pharmaceutically acceptable salts, esters, or solvates thereof.  Preferably the drug is metaxalone.

The granulator is a rapid mixer granulator, a twin screw granulator, a tumbling granulator, or a fluidized bed granulator.  Preferably, the granulator is a rapid mixer granulator.

In the present disclosure, the drug is loaded into the granulator.  The granulator is heated so that a portion of the drug which is in contact with the hot side walls of the granulator gets melted.  This melted drug then acts as a granulating agent to granulate the remaining portion of the drug present in the granulator.  The granulator may be heated after loading the drug or alternatively it may be...