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Pharmaceutical formulations comprising (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid

IP.com Disclosure Number: IPCOM000223373D
Publication Date: 2012-Nov-20
Document File: 5 page(s) / 38K

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The IP.com Prior Art Database

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Pharmaceutical formulations comprising (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid

The present disclosure relates to pharmaceutical formulations comprising (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid (Compound 1). Compound 1 acts as a voltage-dependent calcium channel α2-δ subunit ligand and possesses analgesic, anticonvulsant and anxiolytic properties.

Generally, the pharmaceutical blend, typically in bulk form, is used to form a pharmaceutical capsule for oral dosing of Compound 1. The capsule, particularly a gelatine capsule, of a proper size, may comprise from 10 to 500 mg of Compound 1 within the pharmaceutical blend, particularly 25, 50, 75, 100, 150, 200, 225 or 300 mg of Compound 1 per capsule.

The solid blend can be made by normal pharmaceutical means for blending an active ingredient with an excipient. Typically the blending is achieved by mixing in a suitable mixer and, optionally, milling and sieving the mixture to obtain a relative homogenous and intimate blend. The mixing can be done in one or more steps and can include additional excipients added in various orders.

Alternatively, the mixture of Compound 1 and pregelatinized starch and/or maize starch components may be granulated, with or without additional excipients, by means of wet or dry granulation, by processes known in the art, to form the blend in a form of a granulate. The granulate may be screened and/or milled to obtain a blend with suitable technological properties/sizes.

The pharmaceutical blend is useful in forming pharmaceutical dosage forms such as capsules and tablets.

The excipients used in the formulations are selected from lactose monohydrate (Foremost Fastflow 316, Lactochem Fine 200#, Lactochem Crystals 100#, Tablettose 80, Flowlac 100 or Pharmatose DCL 11), maize starch (National 781551 or Unipure FL), pregelatinized starch (Starch 1500 or Superstarch 200), erythritol (Erylite Erythritol fine, Zerose Erythritol), talc. Other excipients of similar quality can be used.

1. Formulation strategy with lactose monohydrate

The pharmaceutical composition A comprising Compound 1(25, 50, 75, 100, 150, 200, 225 or 300 mg per capsule), further contains lactose monohydrate, maize starch and a lubricant such as talc. The composition A is shown in Table 1.

The pharmaceutical composition B comprising Compound 1 (25, 50, 75, 100, 150, 200, 225 or 300 mg per capsule), further contains lactose monohydrate, pregelatinised starch and a lubricant such as talc. The composition B is shown in Table 2.

2. Formulation strategy without lactose monohydrate

The pharmaceutical compositions C, D and E comprising Compound 1 (25, 50, 75, 100, 150, 200, 225 or 300 mg per capsule) are free of lactose, and further contain pregelatinized starch and a lubricant such as talc. The compositions C, D and E are shown in Tables 3, 4 and 5.

The pharmaceutical compositions F, G, H comprising Compound 1 (25, 50, 75, 100, 150, 200, 225 or 300 mg per capsule) are free of lactose, and further cont...