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Drug-loaded polyelectrolyte capsules in response to phosphatase concentration and preparation method thereof

A polyelectrolyte and phosphatase technology, applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Inactive Publication Date: 2009-04-01
RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the stability of the internal environment in the body, the electrolyte concentration, body temperature and blood pH cannot be changed arbitrarily, so the controlled release of drugs through changes in physical parameters has certain limitations.

Method used

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  • Drug-loaded polyelectrolyte capsules in response to phosphatase concentration and preparation method thereof
  • Drug-loaded polyelectrolyte capsules in response to phosphatase concentration and preparation method thereof
  • Drug-loaded polyelectrolyte capsules in response to phosphatase concentration and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Preparation of Polyelectrolyte (PAH / PSS-β-Glycerophosphate) Empty Shell Capsules

[0021] (1), preparation of gelatin microspheres

[0022] Dissolve 0.5g of gelatin in 10ml of water, swell for 10 minutes, heat and dissolve in a water bath at 55°C, prepare a 5% solution, quickly pour it into 8-9ml of acetone, let it stand for layers, and remove the upper white turbidity solution, the remaining part was redissolved in a water bath, and the pH value was adjusted between 3.2-3.8 with acetic acid, and the acetone solution was added dropwise until the liquid was milky white, with one or two drops in excess, quickly transferred to a round bottom flask, and placed in an ice bath After stirring with a magnetic stirrer for 10 minutes, 200 μl of 8% glutaraldehyde was added to cure for 30 minutes. Stop stirring, remove gelatin, and place in a small beaker.

[0023] (2), preparation of PSS-β-glycerophosphate complex

[0024] Prepare 1000 mL of anionic polyelectrolyte...

Embodiment 2

[0033] Example 2 Preparation of Doxorubicin Polyelectrolyte (PAH / PSS-β-Glycerophosphate) Capsules

[0034] Get the doxorubicin solution 10mL of 100ug / mL and add in the cavity capsule that 20mg makes among the embodiment 1, after adding 0.7mol / L NaCl to adjust the salt concentration, place in the shaker 20 ℃ of constant temperature oscillations 24h, high-speed centrifugation (5000r / min×5min) the above solution, discard the supernatant, and the precipitate is a polyelectrolyte capsule carrying doxorubicin.

Embodiment 3

[0035] Example 3 Physicochemical Properties of Polyelectrolyte (PAH / PSS-β-Glycerophosphate) Empty Shell Capsules

[0036] TEM pictures of the capsules are shown in figure 1 shown. It can be seen from the figure that the prepared capsules have better sphericity and better dispersibility in the solution, and the particle size measured under electron microscope is mostly 200-300nm.

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Abstract

The invention relates to an intelligent drug controlled release system which is formed by adding organic phosphate component into polyelectrolyte capsule wall. The intelligent drug controlled release system has the advantages that the component of the polyelectrolyte capsule can respond to the concentration of acid phosphatase in the blood serum of a patient with tumour and influence the permeability of the capsule wall to achieve the effect of releasing drugs intelligently; and as a tumour marker, the acid phosphatase is used for observing the development and treatment effect of the tumour in the clinical work. The vitality increase of removed blood serum of the patient with prostate cancer can be dozens of times normal value, and the acid phosphatase in the blood serum of the patients with stomach cancer, colon cancer, breast cancer, hypothyroid cancer, kidney cancer, ovary cancer, malignant lymphogranulomatosis and multiple myeloma can also have moderate increase, therefore, a drug loaded polyelectrolyte capsule intelligent drug controlled release system with the acid phosphatase as the response can process drug controlled release treatment on various tumors. The intelligent drug controlled release system uses the tumour marker phosphatase as the drug controlled release condition, so the intelligent drug controlled release system has better practical application meaning.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a drug-loaded polyelectrolyte capsule capable of responding to the concentration of phosphatase and a preparation method thereof. Background technique [0002] As we all know, tumor has become a major malignant disease that endangers human beings all over the world. Chemotherapy is one of the methods to treat tumors. Many clinical chemotherapeutic drugs, such as doxorubicin, have a broad anticancer spectrum and significant clinical efficacy, and can treat a variety of tumors. However, due to their severe cardiotoxicity, bone marrow suppression and other side effects, their clinical application is limited. application. [0003] In the past, drug release systems were mostly designed as ring-opening systems. Drugs can only be released in a predetermined program and are usually not affected by changes in the external environment. In recent years, we have begun to study the use of a closed-...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/704A61K47/24A61K47/32A61K47/42A61J3/00A61P35/00
Inventor 李培勇姜磊杨晓玲
Owner RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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