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Particles for inhalation having rapid release properties

A particle and rapid technology, applied in the direction of organic active ingredients, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as patient pain, reduce dosing frequency, improve coordination and comfort degree, the effect of high initial release

Inactive Publication Date: 2004-08-04
ADVANCED INHALATION RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diabetics often require daily insulin injections, often multiple, which can be painful for the patient

Method used

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  • Particles for inhalation having rapid release properties
  • Particles for inhalation having rapid release properties
  • Particles for inhalation having rapid release properties

Examples

Experimental program
Comparison scheme
Effect test

example

[0157] Material

[0158] In vivo studies in rats, most of the insulin used for spray drying was obtained from BioBras (Belo Horizonte, Brazil) or Sigma (Saint Loius, MO). In in vitro studies as well as in vivo studies in humans, Humulin®, Lente® (Humulin® L human insulin zinc suspension), Humulin® R (regular soluble insulin (IR)), Humulin® Ultralente® (Humulin® U) and Humalog® 100 (insulin lispro (IL)), was obtained from Eli Lilly Company (Indianapolis, IN; 100 U / ml). These solutions were stored at 2-8°C.

[0159] Mass Median Aerodynamic Diameter - MMAD (μm)

[0160]The mass median aerodynamic diameter was determined using an Aerosizer / Aerodisperser (Amherst Process Instrument, Amherst, MA). About 2 mg of the powder formulation was added to an air disperser and the aerodynamic diameter was determined by time of flight measurement.

[0161] fine fraction

[0162] The fines fraction can be used as a way to characterize the aerosol behavior of a dispersed powder. The fine p...

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PUM

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Abstract

The invention generally relates to formulations having particles comprising phospholipids, bioactive agent and excipients and the pulmonary delivery thereof. Dry powder inhaled insulin formulations are disclosed. Formulations comprising DPPC, insulin and sodium citrate which are useful in the treatment of diabetes are disclosed. Also, the invention relates to a method of for the pulmonary delivery of a bioactive agent comprising administering to the respiratory tract of a patient in need of treatment, or diagnosis an effective amount of particles comprising a bioactive agent or any combination thereof in association, wherein release of the agent from the administered particles occurs in a rapid fashion.

Description

technical field [0001] The present invention relates to inhalable microparticles with rapid release properties. Background technique [0002] Pulmonary administration of biologically active agents such as therapeutic, diagnostic and prophylactic agents offers an attractive alternative to oral, transdermal and parenteral administration. That is, pulmonary administration can often be accomplished without medical intervention (self-administration), avoiding the pain often associated with injectable therapy, and, moreover, enzymatic degradation of bioactive agents and pH-mediated The amount of degradation (often encountered in oral therapy) can be significantly reduced. In addition, the lungs provide a large mucosal surface for drug absorption, and the absorbed drug does not have the first-pass effect of the liver. Furthermore, there has been evidence that higher bioavailability of various molecules (eg, macromolecules) can be obtained by pulmonary administration or inhalation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/12A61K9/127A61K9/16A61K9/72A61K9/14A61K31/137A61K31/195A61K38/28A61K38/30A61K47/02A61K47/12A61K47/16A61K47/18A61K47/24A61K47/48A61L9/04A61P3/10A61P43/00
CPCA61K47/48053A61K38/28A61K9/1617A61K9/0075A61K47/544A61P43/00A61P3/10
Inventor 詹妮弗·L·施米特克陈东浩理查德·P·巴泰基戴维·A·爱德华兹杰弗里·S·赫凯奇
Owner ADVANCED INHALATION RES
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