Methods and compositions for soft anticholinergic esters
AssigneeBodor Laboratories, Inc.
InventorNicholas S. Bodor
Life of this patent
Estimating the term…
Abstract
Intra-oral formulations comprising soft anticholinergic alkyl esters are useful for treating excessive drooling conditions in subjects, such as humans, suffering from sialorrhea. Preferably, at least one soft anticholinergic ester is provided in an effective amount or concentration in an anhydrous intra-oral formulation that can inhibit excessive drooling resulting from a condition known as sialorrhea.
Claims58
An intra-oral composition, said composition comprising:
- (a) at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2 position and the R, S or RS stereoisomeric configuration at the 1′ and 3′ positions, or being a mixture thereof;
- and
- (b) at least one anhydrous, non-toxic pharmaceutically acceptable carrier or excipient, wherein the carrier or excipient is suitable for intra-oral administration;
- provided that said intra-oral composition is anhydrous;
- and that said intra-oral composition comprises an anti-excessive-salivation effective amount of from about 1 mg to about 10 mg per adult dose of the compound of formula (2), or from about 0.02 mg/kg to about 1.0 mg/kg per pediatric dose of the compound of formula (2).
An intra-oral composition, said composition comprising:
- (a) at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2 position and the R, S or RS stereoisomeric configuration at the 1′ and 3′ positions, or being a mixture thereof;
- and
- (b) the dried residue of an about 15% to about 50% solution or suspension of the compound of formula (2) in an anhydrous ethanol, wherein the dried residue is suitable for intra-oral administration;
- provided that said intra-oral composition or at least the portion(s) thereof which is/are in contact with said compound, is/are anhydrous and that said composition comprises from about 0.02 mg/kg to about 1.0 mg/kg per pediatric dose of the compound of formula (2), said composition being in the form of a solid or film.
A composition inhibiting acetylcholine from binding to salivary muscarinic cholinergic receptors, the composition comprising at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2-position and the R, S or RS stereoisomeric configuration at the 1′ and 3′-positions, or being a mixture thereof, and a pharmaceutically acceptable non-toxic carrier or excipient therefor, wherein the carrier or excipient is suitable for delivery of the composition to the salivary glands.
A composition for inducing dry mouth, the composition comprising an effective amount of at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2-position and the R, S or RS stereoisomeric configuration at the 1′ and 3′-positions, or being a mixture thereof, and a pharmaceutically acceptable non-toxic carrier or excipient therefor, wherein the composition is formulated for topical administration, and wherein the induced dry mouth is sufficient to minimize or substantially reduce salivation, and wherein the carrier or excipient is suitable for delivery of the composition to the salivary glands.
A patch for treating sialorrhea, the patch comprising at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2-position and the R, S or RS stereoisomeric configuration at the 1′ and 3′-positions, or being a mixture thereof, and a pharmaceutically acceptable non-toxic carrier or excipient therefor, in an amount of compound of formula (2) of from about 1 mg to about 10 mg per adult dose, or from about 0.02 mg/kg to about 1.0 mg/kg per pediatric dose, wherein the carrier or excipient is suitable for delivery of the composition to the salivary glands.
An intra-oral composition, said composition comprising:
- (a) at least one compound having the formula:
- wherein R is methyl or ethyl, said compound having the R stereoisomeric configuration at the 2 position and the R, S or RS stereoisomeric configuration at the 1′ and 3′ positions, or being a mixture thereof;
- and
- (b) a taste masking agent;
- and
- that said intra-oral composition comprises an anti-excessive-salivation effective amount of from about 1 mg to about 10 mg per adult dose of the compound of formula (2), or from about 0.02 mg/kg to about 1.0 mg/kg per pediatric dose of the compound of formula (2);
- and that said intra-oral composition which is capable of dissolving in the mouth.
Dependencies are inferred from the claim text.