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Controllable release system of glucocorticoid and its preparation and use

A glucocorticoid and system technology, applied in the field of medicine, can solve the problems of affecting the quality of life of patients, serious side effects, inconvenience of patients' life, etc., to reduce the frequency and side effects of drugs, control the release stability, and achieve effective and convenient clinical use. Effect

Inactive Publication Date: 2004-01-28
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Intravenous corticosteroids and oral corticosteroid pills have many pitfalls
First, serious side effects
Second, it is inconvenient to use, requiring frequent injections or oral medications, which brings great inconvenience to the patient's life and affects the patient's quality of life, especially for long-term medication.
Third, it is difficult to achieve local drug administration, causing other non-infected parts to suffer side effects from the drug at the same time
Therefore, even if doctors carefully consider and use drugs carefully when administering drugs to patients, it is difficult to accurately control the dosage, which increases the risk of using hormone therapy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0024] (1) Weigh 150 mg hydrocortisone powder, stir and mix with 5 ml of 1% collagen solution for 3 minutes, then add 5 ml of 1% chitosan solution, and continue stirring and mixing. In addition, 0.64 g of monoglyceride and 0.36 g of sorbitan monolaurate (SPAN20) were weighed and dissolved in 40 ml of paraffin oil by heating. Subsequently, under high-speed stirring at 5000rpm, ultrasonic waves of 150W power were applied to assist emulsification, and at the same time, a mixture of hydrocortisone, collagen and chitosan was slowly added for emulsification for 30 minutes to obtain emulsion A.

[0025] (2) Weigh 12g of gelatin, dissolve it in 120ml of distilled water by heating, and add 3g of Tuwen 80 at the same time, fully dissolve. Under high-speed stirring at 5000rpm, apply 150W ultrasonic power to assist emulsification, and at the same time slowly add emulsion A in (1) and emulsify for 30 minutes to form a new emulsification system B.

[0026] (3) Measure 400ml of paraffin oil...

Embodiment 2

[0029] A little of the dried drug microcapsules in Example 1 were dispersed in distilled water, and the particle morphology was detected under a microscope, which was close to spherical. Particle size analyzer analysis shows that the particle diameter is in the range of 5-50 μm, mainly 10-20 μm. Scanning electron microscope analysis showed that the surface of the microcapsule particles was relatively smooth, but there were many wrinkles.

[0030] Weigh three portions of 0.5g of drug microcapsules, add 50ml of pre-prepared PBS buffer solutions with three different pH values ​​(6.0, 7.2, 8.0), and shake in a constant temperature water bath at 37°C. Samples were taken at 7h, 12h, 24h, 48h, 72h, 120h, and 168h, and the drug release was analyzed by liquid chromatography.

[0031] The results showed that the prepared glucocorticoid microcapsules had a maximum drug load of 25 mg / g, and the drug release amount was about 70% in 168 hours (ie 7 days), and there was no "burst release" p...

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Abstract

The invention discloses a controllable release system of glucocorticoid, the preparing method and the application. The controllable release sytem is the glucocorticoid microcapsule, uses natural biodegradable high-molecular material as the base material of glucocorticoid drug, and adopts ultrasonic micro-capsulizating technique of combination of emulsification and mechanical mixing to wrap the drug in the microsphere composed of the base material to make microcapsule; further prepare the drug's powder, capsule, plaster, tablet and injection or pill, able to effectively control the release rate and stability of the drug, maintain the needed blood concentration, and on the premise of assuring the cure effect, largely reduce the frequency of dosing or injecting and the side effect of the drug.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a controllable release system of glucocorticoids and its preparation and application. Background technique [0002] Glucocorticoids are a class of steroid hormones secreted by the adrenal cortex, which have strong pharmacological effects such as anti-inflammatory, anti-allergic, immunosuppressive and anti-toxic. Clinically, it is widely used in the treatment of arthritis, ophthalmic inflammation, anti-rejection after keratoplasty, rheumatoid arthritis, systemic lupus erythematosus, vasculitis and other autoimmune diseases. [0003] Traditional drug preparations use general drug carriers. At the initial stage after taking the drug or injection, the blood drug concentration will gradually increase according to the body's absorption of the drug, and the highest concentration may exceed the poisoning limit concentration; then with the release of the drug in the drug , the am...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/52A61K31/573A61P19/02A61P27/02A61P29/00A61P37/06A61P37/08A61P39/02
Inventor 谢德明
Owner JINAN UNIVERSITY
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