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Long-acting injection preparation of sterides 5 alpha-reductase inhibitor and preparation method thereof

A technology for reductase inhibitors and long-acting injection preparations, which is applied in the field of long-acting injection preparations and its preparation, and can solve the problems of patents, literature reports, and inconvenience of long-acting injections of steroidal 5α-reductase inhibitors.

Active Publication Date: 2011-07-27
黄芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a course of treatment for Apretide lasts for 4 months, and at least 3 courses of treatment are taken, which is very inconvenient for elderly patients with limited mobility, many daily medications, forgetful patients, patients with dysphagia or bedridden patients.
[0005] However, the existing research and patents on Aprelate are tablets, dripping pills, microspheres or controlled-release pellets, and there are no patents and literature reports on long-acting injections of steroidal 5α-reductase inhibitors.

Method used

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  • Long-acting injection preparation of sterides 5 alpha-reductase inhibitor and preparation method thereof
  • Long-acting injection preparation of sterides 5 alpha-reductase inhibitor and preparation method thereof
  • Long-acting injection preparation of sterides 5 alpha-reductase inhibitor and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Will 4g RG 503 was dissolved in 9 g of dimethyl sulfoxide (DMSO), resulting in a viscous polymer solution. Add 1.2g of Apretide, mix evenly, sterilize with cobalt radiation, and aseptically dispense, each syringe is pre-filled with 1.4g of finished product.

[0053] In vitro drug release checks:

[0054] Take 8 finished products, inject the same amount of the finished product in each syringe into the bottom of two 1L reagent bottles respectively, record the injection volume, slowly add 900 mL of 0.001 mol preheated at 37 °C along the wall of the reagent bottle / L sodium hydroxide solution, put it in a constant temperature shaking box at 37°C and shake at a speed of 100rpm, and take two bottles of samples at 0.5 hours, 2 hours, 24 hours, 2 days, 4 days, 6 days, 10 days, and 14 days for testing . Absorbance was measured at 267 nm by UV spectrophotometry. Calculate the release amount by external standard method, and draw the release curve as figure 1 shown, from fig...

Embodiment 2

[0058] 3.5g RG 752H was dissolved in 5.2 g of ethyl acetate to give a viscous polymer solution. After adding 0.45g of dutasteride and 10mg of zinc carbonate and suspending evenly, each syringe was prefilled with 0.9mL of the suspension and freeze-dried. Resuspend with sterile N-methylpyrrolidone before injection.

[0059] In vitro drug release checks:

[0060] Take 5 tubes of the finished product, resuspend them with sterile N-methylpyrrolidone, inject the finished product in the syringe into the bottom of 4 reagent bottles with a volume of 1L in 4 times, record the injection volume, and slowly add it along the wall of the reagent bottle 900mL of phosphate buffer solution with pH 7.0 preheated at 37°C containing 2% SDS, shaken at a speed of 100rpm in a 37°C constant temperature shaking box, and shaken at 0.5 hour, 1 day, 2 days, 4 days, 7 days, respectively Two bottles of samples were taken at 14 days, 21 days, 28 days, 35 days and 42 days for testing. Absorbance was meas...

Embodiment 3

[0064] Pick R503H and After R203H was mixed in a weight ratio of 8:2, 4 g of the mixture was dissolved in 9 g of ethanol, and 1.2 g of micronized aprelate (75 μm<D90<100 μm), 25 mg of magnesium hydroxide, 0.50 g sucrose acetate isobutyrate (SAIB). A physiological saline solution containing 2.0% medium chain triglycerides was prepared. Take 10 g of the above-mentioned physiological saline solution and add it into the suspension, high-speed emulsification, freeze-drying, and granulation. Make the particle diameter less than 100μm. Divide according to dosage requirements. Suspend with 2.5% sterile phospholipid solution before injection.

[0065] In vitro drug release checks:

[0066] Into 16 bottles of 900mL 0.001mol / L sodium hydroxide solution preheated at 37°C, weigh 750mg of the above-mentioned granules respectively, and shake at a speed of 100rpm in a constant temperature shaking box at 37°C. Two bottles of samples were taken each day, 4 days, 6 days, 10 days, and 14...

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Abstract

The invention relates to a long-acting injection preparation of sterides 5 alpha-reductase inhibitor and a preparation method thereof. The long-acting injection preparation of sterides 5 alpha-reductase inhibitor contains the sterides 5 alpha-reductase inhibitor as a medicinal active component, a pharmaceutically acceptable and biodegradable controlled release auxiliary material and a solvent. The long-acting injection provided by the invention can dispense with the inconvenience of oral dosing for a long time or mistakes in medication, medicines used to be taken twice per day or once per day are taken once per several weeks or once per several months, and also the blood concentration in a human body is kept in an effective concentration range for several weeks or for several months without frequent medication, thus meeting the medication requirements of oblivious aged patients who are inconvenient to move and take many medicines per day, patients with dysphagia or bedridden patients.

Description

technical field [0001] The invention relates to a long-acting injection preparation and a preparation method thereof, in particular to a steroid 5α-reductase inhibitor long-acting injection preparation and a preparation method thereof. Background technique [0002] The 5α-reductase in the human body has two isoenzymes, type I and type II. The type I enzyme is mainly distributed in the hair follicles of the scalp, and the type II enzyme is mainly found in the prostate. 5α-reductase can increase the content of dihydrotestosterone (DHT) in prostate tissue, causing benign prostatic hyperplasia, prostate cancer, male baldness and other diseases. Men generally begin to have pathological changes of hyperplasia after the age of 40. According to relevant domestic statistics, the incidence of benign prostatic hyperplasia in men at the age of 50 exceeds 50%, and it can reach 90% at the age of 80. The main symptoms of benign prostatic hyperplasia are dysuria, frequent urination, slow s...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/10A61K45/00A61K47/14A61K47/22A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P9/00A61P13/08A61P17/00A61P35/00
Inventor 黄芳
Owner 黄芳
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