Oral insulin therapy
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Accused Products
Abstract
Pharmaceutical dosage forms for oral administration to a patient for the treatment of diabetes, comprising insulin and a delivery agent that facilitates insulin transport in a therapeutically effective amount to the bloodstream and that result in a lower incidence of vascular diseases associated with the repeated administration of insulin are disclosed. Also disclosed is a method of attenuating the undesirable incidence of diseases associated with chronic dosing of insulin is provided whereby the oral administration to a patient of insulin along with a suitable delivery agent that facilitates the absorption of insulin from the gastrointestinal tract of the patient in a therapeutically effective amount, for treatment of diabetes.
53 Citations
131 Claims
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1-58. -58. (canceled)
- 59. An oral dosage form comprising a dose of unmodified insulin that achieves a therapeutically effective reduction in blood glucose after oral administration to a human diabetic patient as compared to an untreated diabetic patient.
- 92. A method of treating impaired glucose tolerance, achieving glucose homeostasis, treating early-stage diabetes, or treating late-stage diabetes, comprising administering to a human patient an oral dosage form of unmodified insulin that achieves a therapeutically effective reduction in blood glucose after oral administration to a human diabetic patient.
- 106. A method of providing a therapeutically effective orally administrable unit dose of unmodified insulin, comprising combining from about 2 to about 23 mg of unmodified insulin with from about 1 to about 800 mg of a pharmaceutically acceptable delivery agent that facilitates absorption of said insulin from the gastrointestinal tract of human diabetic patients, and orally administering said unit dose to a human diabetic patient to provide a therapeutic effect.
- 108. A method of treating a human diabetic patient, comprising orally administering an oral dosage form comprising an effective dose of insulin pre-prandially to a human diabetic patient, such that an insulin tmax at a time point from about 0.25 to about 1.5 hours after oral administration is attained and blood glucose concentration of the patient is effectively controlled in response to the meal as manifested by providing a blood glucose concentration which does not vary by more than about 40% for the first hour after oral administration from the baseline (fasted) blood glucose concentration in the patient, and which provides a return to baseline plasma insulin levels in the patient no later than 4 hours after oral administration.
- 110. A method of treating diabetics, comprising orally administering to diabetic patients on a chronic basis an oral insulin treatment comprising a dose of unmodified insulin together with a delivery agent that facilitates the absorption of the insulin from the gastrointestinal tract to provide a therapeutically effective reduction in blood glucose and a peak blood plasma insulin concentration that is reduced relative to the peak blood plasma insulin concentration of an equivalent therapeutically effective reduction in blood glucose concentration achieved by subcutaneous injection of insulin.
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120. A method of treating diabetes and reducing the incidence and or severity of hyperinsulinemia associated with chronic dosing of insulin, comprising orally administering on a chronic basis to a diabetic patient a dose of insulin and a delivery agent that facilitates the absorption of the dose of insulin from the gastrointestinal tract to provide therapeutically effective control and/or reduction in blood glucose concentrations, and a mean systemic plasma insulin concentration of the diabetic patient that is reduced relative to the mean systemic plasma insulin concentration provided by subcutaneous injection of insulin in an amount effective to achieve equivalent control and/or reduction in blood glucose concentration in a population of human diabetic patients.
- 121. A method of reducing the incidence and/or severity of one or more disease states associated with chronic administration of insulin, comprising treating diabetic patients via oral administration on a chronic basis with a therapeutically effective dose of a pharmaceutical composition which comprises insulin and a delivery agent that facilitates the absorption of insulin from the gastrointestinal tract, such that the pharmaceutical composition provides a therapeutically effective reduction in blood glucose and a peak serum insulin concentration of the diabetic patient that is reduced relative to the peak serum insulin concentration of an equivalent therapeutically effective reduction in blood glucose concentration achieved by subcutaneous injection of insulin.
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128. A method of treating diabetes and reducing the incidence and or severity of hyperinsulinemia associated with chronic dosing of insulin, comprising orally administering on a chronic basis to a diabetic patient a dose of insulin and a delivery agent that facilitates the absorption of the dose of insulin from the gastrointestinal tract to provide a therapeutically effective reduction in blood glucose and a peak serum insulin concentration of the diabetic patient that is reduced relative to the peak serum insulin concentration of an equivalent therapeutically effective reduction in blood glucose concentration achieved by subcutaneous injection of insulin.
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129. A method of reducing the exposure of the vasculature of diabetic patients to hyperinsulinemic conditions, comprising orally administering an oral insulin treatment comprising a dose of insulin together with a delivery agent which facilitates the absorption of said insulin from the gastrointestinal tract on a chronic basis to diabetic patients to reduce blood glucose levels in said diabetic patients by a desired amount, such that the concentration of insulin circulating in the blood of said diabetic patients as a result of insulin treatment is reduced relative to the peak serum insulin concentration of an equivalent therapeutically effective reduction in blood glucose concentration achieved by subcutaneous injection of insulin.
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130. A method of attenuating processes resulting from the reaction to a mild injurious stimulus in multiple areas of the response to increases in mRNA during insulin treatment, comprising orally administering an oral insulin treatment comprising a dose of insulin together with a delivery agent which facilitates the absorption of said insulin from the gastrointestinal tract on a chronic basis to diabetic patients to reduce blood glucose levels in said diabetic patients by a desired amount, such that the concentration of insulin circulating in the blood of said diabetic patients as a result of insulin treatment is reduced relative to the peak serum insulin concentration of an equivalent therapeutically effective reduction in blood glucose concentration achieved by subcutaneous injection of insulin.
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131. A method of treating diabetic patients, comprising orally administering an oral insulin treatment comprising a dose of insulin together with a delivery agent which facilitates the absorption of said insulin from the gastrointestinal tract on a chronic basis to diabetic patients to reduce blood glucose levels in said diabetic patients by a desired amount, such that the concentration of insulin circulating in the blood of said diabetic patients as a result of said oral insulin treatment is not substantially greater than normal physiological levels.
Specification