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Protein and peptide medicine carrier and its preparation method and application

A technology of protein peptides and drugs, applied in drug combinations, pharmaceutical formulas, peptide/protein components, etc., can solve rare problems, achieve the effect of reducing damage, reducing surface tension, and simple and feasible process

Inactive Publication Date: 2007-10-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There are few reports on the study of exogenous PS as a carrier for pulmonary drug delivery. At present, there are no reports at home and abroad that exogenous PS as a drug carrier exerts systemic effects after pulmonary drug delivery.

Method used

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  • Protein and peptide medicine carrier and its preparation method and application
  • Protein and peptide medicine carrier and its preparation method and application
  • Protein and peptide medicine carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0027] Take dipalmitoylphosphatidylcholine 13.5mg, phospholipid 6.8mg, palmitic acid 2.7mg, dissolve with chloroform and ethanol (1:1, V / V), remove the organic solvent by rotary evaporation, vacuum dry, add normal saline, 40- After hydration at 60°C for 2 hours, the artificial lung surfactant DLP was obtained by ultrasound. Insulin solution was added to the prepared DLP, and the ice bath was pulsed with ultrasound to obtain the INS-APS system-IDLP. Determination of the minimum surface tension of DLP and IDLP, see Table 1. 6 normal Wistar rats were fasted for 14 hours before the administration, without water. 4 IU / kg IDLP was given by tracheal infusion, blood was collected from the tail vein at 0, 15, 30, 60, 90, 120, 180, 240, 300, and 360 min, and centrifuged at 3000 rpm for 10 min. Glucose oxidase method was used to measure blood glucose level, and radioimmunoassay was used to measure serum insulin level, as shown in Figure 1. The relative pharmacological bioavailability ...

Embodiment example 2

[0029] Take 13.5 mg of dipalmitoylphosphatidylcholine and 1.5 mg of cetyl alcohol, dissolve them in ethanol, remove the organic solvent by rotary evaporation, dry in vacuo, add tyloxapol normal saline solution, hydrate at 40-60°C for 2 hours, and obtain the product by ultrasonication Artificial lung surfactant DHT. Insulin solution was added to the prepared DHT, and the ice bath was pulsed with ultrasound to obtain the INS-APS system-IDHT. Determination of the minimum surface tension of DHT and IDHT, see Table 1. 6 normal Wistar rats were fasted for 14 hours before the administration, without water. 4IU / kgIDHT was given by tracheal infusion, blood was collected from the tail vein at 0, 15, 30, 60, 90, 120, 180, 240, 300, and 360 min, and centrifuged at 3000 rpm for 10 min. Glucose oxidase method was used to measure blood glucose level, and radioimmunoassay was used to measure serum insulin level, see Figure 2. The pharmacological relative bioavailability of IDHT reaches 38%...

Embodiment example 3

[0031]Take 13.5 mg of dipalmitoylphosphatidylcholine and 4.5 mg of phosphatidylglycerol, dissolve them in chloroform, remove the organic solvent by rotary evaporation, dry in vacuum, add normal saline, hydrate at 40-60°C for 2 hours, and obtain artificial lung surfactant by ultrasound DPG. Insulin solution was added to the prepared DPG, and the ice bath was pulsed with ultrasound to obtain the INS-APS system-IDPG. Determination of the minimum surface tension of DPG and IDPG, see Table 1. 6 normal Wistar rats were fasted for 14 hours before the administration, without water. 4 IU / kg IDPG was given by tracheal infusion, blood was collected from the tail vein at 0, 15, 30, 60, 90, 120, 180, 240, 300, and 360 min, and centrifuged at 3000 rpm for 10 min. Glucose oxidase method was used to measure blood glucose level, and radioimmunoassay was used to measure serum insulin level, see Figure 3. The pharmacological relative bioavailability of IDPG reaches 36%, which is 1.3 times tha...

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Abstract

The invention pertains to the pharmaceutical preparation field, in particular it relates to the application of peptide and protein drug carrier and its preparation method as the drug carrier in the lung administration, according to the invention, the artificial pulmonary surfactant (APS) having drug absorption-promoting and pulmonary protective functions as a lung administered drug carrier, in particular as the carrier of protein and peptide drug to further provides a drug-APS system. The experiment proves that it can reduce alveolus surface tension, increase the lung compliance, stabilize the intra-alveolar pressure, promote the drug absorption administered from the lungs, and decreases the damage to lungs as the carrier of peptide and protein drug.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations. The invention relates to a protein polypeptide drug carrier, in particular to an artificial pulmonary surfactant (APS) protein polypeptide drug carrier capable of promoting drug absorption and protecting lung function, its preparation method and its application as a drug carrier in pulmonary administration. Background technique [0002] Due to its large absorption area, rich blood volume, tight and thin alveolar-capillary junctions, and low biological enzyme activity, pulmonary drug delivery has become a research hotspot for protein and polypeptide drug delivery routes. Since the lung is also an important place for gas exchange in the circulatory system, dust particles in the air, various pathogens and various chemical substances can cause toxic reactions if their toxicity exceeds the immune defense capacity of the lung itself. Clinical studies suggest that slight effects on respirator...

Claims

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Application Information

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IPC IPC(8): A61K47/24A61K47/12A61K47/10A61K38/28A61P11/00
Inventor 裴元英季颖
Owner FUDAN UNIV
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