KR950703333A - Pharmaceutical Compositions Containing Nonionic Surfactants - Google Patents

Abstract

The weak compositions of the present invention comprise an enzymatically unstable pharmaceutical active that can penetrate the barrier or a barrier permeation enhancer for penetrating the barrier and one or more nonionics that can prevent the active agent from being inactivated by the enzyme. Requires a surfactant. Methods of inhibiting the degradation of the enzymatically unstable pharmaceutical actives by the gastrointestinal enzymes include mixing the actives with nonionic surfactants.

Description

Pharmaceutical Compositions Containing Nonionic Surfactants

Since this is an open matter, no full text was included.

Claims (19)

A weak composition for oral administration comprising an enzymatically unstable pharmaceutical active that can penetrate the barrier and one or more nonionic surfactants that can prevent the active agent from being inactivated by the enzyme. The composition of claim 1, wherein the active agent is a peptide having a molecular weight of less than about 3,000. The composition according to claim 1 or 2, wherein the nonionic surfactant is ethoxylated alcohol, ethoxylated fatty acid, sorbitan derivative, ethoxylated alkyl phenol, or monoglyceride. 4. The nonionic surfactant according to claim 3, wherein the nonionic surfactant is ethoxylated lauric acid, polyoxyethylene (40) stearate, polyoxyethylene (20) sorbitan monooleate, polyoxyethylene (23) lauryl ether, Nonyl phenoxypoly (ethyleneoxy) ethanol-30, nonylphenoxypoly (ethyleneoxy) ethanol-50, or a mixture of polyethylene glycol-1500 esters of glyceryl and palm seed oil, mono-octanoin, monodecanoin, or mono A composition characterized by being olein. The composition of claim 1, wherein the oil is included. 6. The composition of claim 5 wherein said oil monoglycerides, diglycerides, or triglycerides. The triglyceride of claim 6, wherein the triglyceride is a vegetable oil or capric acid / capric triglyceride, the mono glyceride is monooctanoin or monodecanoine and the diglyceride is glycelyl-1,2-dioctanoate A composition characterized by being (1) an enzymatically unstable pharmaceutical active that can penetrate the barrier only in the presence of a barrier permeation enhancer, (2) one or more nonionic systems that can prevent the active agent from being inactivated by the enzyme and are not barrier permeability enhancers Pharmaceutical composition for oral administration containing surfactant and (3) barrier permeability promoter other than the said nonionic surfactant. The composition of claim 8, wherein the nonionic surfactant has an HBL value of about 14 to VII 20. The composition of claim 9, wherein the nonionic surfactant is an ethoxylated alcohol, an ethoxylated fatty acid, a sorbitan derivative, an ethoxylated alkyl phenol, or a monodlylide. The nonionic surfactant according to claim 10, wherein the nonionic surfactant is selected from ethoxylated lauric acid, polyoxyethylene (40) stearate, polyoxyethylene (20) sorbitan monooleate, polyoxyethylene (23) lauryl ether, Or nonylphenoxypoly (ethyleneoxy) ethanol-30, nonylphenoxypoly (ethyleneoxy) ethanol-50, a mixture of polyethyleneglycol-1500 esters of glyceryl and palm oil, monooctanoin, monodecanoin, or mono A composition characterized by being olein. The composition of claim 8, wherein the active agent is a polypeptide having a molecular weight of about 150 to 150,000. A method of inhibiting degradation of an active agent, characterized by mixing an enzymatically unstable pharmaceutical active that can penetrate the barrier by an enzyme with a nonionic surfactant that can prevent the active agent from being inactivated by the enzyme. The method of claim 13, wherein the active agent is a peptide having a molecular weight of less than about 3000. The composition of claim 13, wherein the nonionic surfactant is ethoxylated alcohol, ethoxylated fatty acid, sorbitan derivative, ethoxylated alkyl phenol, or monoglyceride. The nonionic surfactant according to claim 13, wherein the nonionic surfactant is selected from ethoxylated lauric acid, polyoxyethylene (40) stearate, polyoxyethylene (20) sorbitan monooleate, polyoxyethylene (23) lauryl ether, Or nonylphenoxypoly (ethyleneoxy) ethanol-30, nonylphenoxypoly (ethyleneoxy) ethanol-50, or a mixture of glyceryl and polyethylene glycol-1500 esters of palm seed oil, monooctanoin, monodecanoin, or mono A composition characterized by being olein. A method of orally administering an active agent to a patient, wherein the enzymatically unstable pharmaceutical active that can penetrate the barrier is co-administered with one or more nonionic surfactants that can prevent the active agent from being inactivated by the enzyme. . Enzymatically unstable pharmaceutical actives that can penetrate the barrier only in the presence of barrier permeability enhancers, one or more nonionic surfactants that can prevent the active agent from being inactivated by enzymes and are not barrier permeability enhancers and the nonions A method for orally administering an active agent to a patient, characterized by simultaneous administration of a barrier permeation enhancer other than the systemic surfactant to the patient. A pharmaceutical composition for oral administration comprising an enzymatically unstable pharmaceutical active that exhibits its therapeutic activity in the stomach or intestine and at least one nonionic surfactant that can prevent the active agent from being inactivated by the enzyme. ※ Note: The disclosure is based on the initial application.