Abstract: The invention relates to coating of suppositories containing free unsaturated fatty acid, fatty acid ethyl ester and fatty acid monoglyceride that are susceptible to oxidative degradation. The coating retards oxidative degradation of unsaturated fatty acids and gives the suppository a non-oily and smooth surface. The coating will enhance the shelf-life of the suppository and allow their storage at room temperature for extended time period. The coating may or may not contain medicament such as local anesthetic or steroid. According to this invention chemically unstable fatty acids in coated suppositories can be used to stimulate the process of defecation or to treat disorders such as hemorrhoids, bacterial infections, viral infections and inflammations, as well as against fissura ani and pruritus ani. Furthermore, coating suppositories, that contain high concentrations of free fatty acids, can reduce acid induced rectal irritation.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention relates to fatty acid stimulation of rectal mucosa initiating the process of defecation, acting as a laxative. Furthermore, the invention relates to the usage of free fatty acids, fatty acid mixtures and fatty acid extracts from marine lipids in pharmaceutical formulations such as suppositories, ointments, tablets and gelatin capsules for treatment and prevention of multiple disorders like constipation, hemorrhoids, bacterial infections (e.g. helicobacter pylori), viral infections (e.g. herpes simplex virus infections) and inflammations, as well as against fissura ani and pruritus ani.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention relates to fatty acid stimulation of rectal mucosa initiating the process of defecation, acting as a laxative. Furthermore, the invention relates to the usage of free fatty acids, fatty acid mixtures and fatty acid extracts from marine lipids in pharmaceutical formulations such as suppositories, ointments, tablets and gelatin capsules for treatment and prevention of multiple disorders like constipation, hemorrhoids, bacterial infections (e.g. helicobacter pylori), viral infections (e.g. herpes simplex virus infections) and inflammations, as well as against fissura ani and pruritus ani.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with ?-cyclodextrin in an aqueous complexation medium comprising ?-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with ?-cyclodextrin and its inclusion complexes.

Abstract: This invention relates to a new method to improve the complexation efficacy of a basic active substance and a cyclodextrin using an acidic volatile substance. The invention further relates to a method to prepare high-energy complexes of a basic active substance and a cyclodextrin that form super-saturated solutions when dissolved. Also, the present invention relates to a pharmaceutical formulation comprising said complex and the use of such a formulation in therapy.

Abstract: Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.

Abstract: Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.

Abstract: The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with &bgr;-cyclodextrin in an aqueous complexation medium comprising &bgr;-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with &bgr;-cyclodextrin and its inclusion complexes.

Abstract: The invention provides a method for enhancing the complexation of a cyclodextrin with a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agrochemical, comprising combining from about 0.1 to about 70% (weight/volume) of a cyclodextrin, from about 0.001 to about 5% (weight/volume) of a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, and said lipophilic and/or water-labile active ingredient in an aqueous medium, the polymer and cyclodextrin being dissolved in the aqueous medium before the active ingredient is added, the aqueous medium which comprises the polymer and cyclodextrin being maintained at from about 30.degree. to 150.degree. C. for a period of from about 0.1 to about 100 hours before, during and/or after the active ingredient is added, optionally followed by removal of water.

Abstract: The invention provides a method for enhancing the complexation of a cyclodextrin with a lipophilic and/or water-libile drug, comprising combining from about 0.1 to about 70% (weight/volume) of a cyclodextrin and from about 0.01 to about 5% (weight/volume) of a pharmaceutically acceptable, pharmacologically inactive, water-soluble polymer in an aqueous medium with a lipophilic and/or water-labile drug to form a drug complex, optionally followed by removal of water. Related methods, co-complexes of drug/cyclodextrin/polymer, pharmaceutical compositions and cyclodextrin/polymer complexing agents are also provided.

Abstract: Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

Abstract: A composition and method for enhancing permeability of topical drugs wherein the agent which enhances the permeability of the drug is selected from the group consisting of (1) a choline ester having the formula:[CH.sub.3 (CH.sub.2).sub.n --COOCH.sub.2 CH.sub.2 N.sup.+ (CH.sub.3).sub.3 ]X.sup.- or[CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH(CH.sub.2).sub.n --COOCH.sub.2 CH.sub.2 N.sup.+ (CH.sub.3).sub.3 ]X.sup.-wherein m and n are integers in the range of from 0 to 30 and X.sup.- is a pharmaceutically acceptable anion and (2) a mixture of the choline ester and an acid having the formula:CH.sub.3 (CH.sub.2).sub.n --COOH orCH.sub.3 (CH.sub.2).sub.m CH.dbd.CH(CH.sub.2).sub.n --COOHor a pharmaceutically acceptable salt thereof.

Abstract: Pharmaceutical preparations comprised of a pharmaceutically active ingredient and a carrier which comprises a percutaneous penetration enhancer comprised of 2-ethyl-1, 3-hexanediol alone or in combination with oleic acid is disclosed. The 2-ethyl-1, 3-hexanediol may be present in an amount in the range of about 50% to 100% based on the weight of the carrier. The oleic acid may be used in combination with 2-ethyl-1, 3-hexanediol in an amount of about 1 to 40% based on the weight of the carrier to provide a synergistic effect with respect to percutaneous penetration enhancement. The compound 2-ethyl-1, 3-hexanediol as used alone and/or in combination with the oleic acid has been found to significantly enhance the delivery of a drug, to a patient, from a transdermal delivery system.

Abstract: This invention relates to sulfur-substituted phenylacetamides of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are H or CH.sub.3 ; R.sub.4 is SR.sub.5, ##STR2## R.sub.5 and R.sub.6 may be the same or different and are lower alkyl containing 1-4 carbon atoms and R.sub.5 and R.sub.6 may be taken together with S to form a 5-7 member ring; and X.sup.- is a pharmaceutically acceptable anion, which exhibit arrhythmia activity.