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Sirolimus gel preparation

A technology of sirolimus gel and gel preparation, applied in the field of pharmaceutical preparations, can solve the problems of affecting the absorption rate, instability, poor acid-base tolerance of sirolimus and the like

Active Publication Date: 2021-09-03
HANGZHOU ZHONGMEI HUADONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the water insolubility of sirolimus, which affects its absorption rate in the gastrointestinal tract, the bioavailability of oral preparations is very low (only 14% to 17%), so it is necessary to explore new dosage forms of sirolimus
[0004] Studies have found that sirolimus has poor acid-base tolerance and is easy to degrade under high temperature conditions, that is, sirolimus has the disadvantage of instability, so the storage conditions of sirolimus-related products are relatively harsh, such as sirolimus raw materials The storage condition of the drug is -20°C. Sirolimus tablets need to be stored under 25°C in a light-shielded airtight environment. Sirolimus oral solution needs to be kept in the dark and stored in an amber dispenser at 2-8°C, such as at room temperature. Storage (up to 25°C), up to 30 days

Method used

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  • Sirolimus gel preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 The stability of sirolimus solution with different ethanol proportions

[0026] Weigh 0.2g of sirolimus and add 10g of ethanol to dissolve, add an appropriate amount of purified water to 100g to obtain a sirolimus solution with 10% ethanol, and prepare 30%, 50%, 70%, and 100% ethanol in the same way. The sirolimus solution with different proportions of ethanol was carried out for stability setting out, and the sirolimus solution was kept away from light, and the content of sirolimus in the solution was determined according to high performance liquid chromatography (Chinese Pharmacopoeia 2020 edition general rule 0512).

[0027] Chromatographic conditions and system adaptability test: Octylsilane bonded silica gel was used as filler, methanol-water-acetonitrile (30:30:40) was used as mobile phase, detection wavelength was 277nm, column temperature was 40°C, theoretical plate The number is not less than 1500 according to the main peak of sirolimus.

[0028] ...

Embodiment 2

[0033] Example 2 Sirolimus Gel Stability of Different Ethanol Proportions

[0034] To prepare sirolimus gels in 10% ethanol:

[0035] Step a. Weigh 0.2g sirolimus and add to 10g ethanol for dissolving;

[0036] Step b. Weigh 1g of carbomer, add appropriate amount of purified water, fully swell overnight, and add triethanolamine to adjust the pH to 5.06;

[0037] Step c. Slowly add the sirolimus solution into the carbomer matrix, add an appropriate amount of purified water to 100 g as needed, stir until it is in a gel state, and obtain a sirolimus gel with 10% ethanol concentration, and measure the pH of the gel Value is 5.55

[0038] The sirolimus gel with 50% ethanol concentration was prepared in the same step, and the pH value of the final gel was determined to be 5.60

[0039] The sirolimus gels with different ethanol proportions were stably sampled and operated in the dark, and the content of sirolimus in the gels was determined according to high performance liquid chro...

Embodiment 3

[0052] Sirolimus gel stability under different pH value conditions of embodiment 3

[0053] Preparation of sirolimus gels at different pH:

[0054] Step a. Weigh 0.2g sirolimus and add to 50g ethanol for dissolving;

[0055]Step b. Weigh 1g of carbomer, add appropriate amount of purified water, fully swell overnight, add different amounts of triethanolamine dropwise to adjust pH, and obtain gel matrix with different pH;

[0056] Step c. Slowly add the sirolimus solution obtained in step a to the gel matrix obtained in step b, add an appropriate amount of purified water to 100 g as needed, measure the pH, add triethanolamine as needed to adjust the pH again, and finally stir until In the gel state, sirolimus gels with different pHs in the table below were obtained.

[0057] The sirolimus gels with different pH were carried out in a stable setting, operated in the dark, and the content of sirolimus in the gel was determined by high performance liquid chromatography. The result...

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Abstract

The invention provides a sirolimus gel preparation. The preparation does not use a conventional stabilizer, and the sirolimus gel preparation with better stability is obtained by optimizing components of the gel preparation and controlling the dosage of ethanol and the pH value of a prescription. The conventional lofting data of the preparation shows that the content change of the active substance sirolimus is small, and the accumulative release amount can reach 99.40% at most after 3-hour in-vitro release.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sirolimus gel preparation. Background technique [0002] Sirolimus (Sirolimus, also known as rapamycin Rapamycin, abbreviated as RPM) is a macrolide antibiotic produced by Streptomyces hygroscopicus isolated from Canadian soil samples. It has strong antifungal activity and also has Antitumor activity. In 1977, Martel RR reported that RPM had a strong inhibitory effect on the immune response of rats. Since then, researchers from various countries have carried out extensive research on the immunosuppressive activity, pharmacokinetics, toxicology, mechanism of action and clinical application of RPM, proving that RPM is a new generation of immunosuppressant with a unique mechanism of action. In September 1999, Wyeth Pharmaceuticals of the United States successfully developed sirolimus oral solution, which was approved by the FDA as an immunosuppressant for t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/436A61K47/10A61P31/10A61P35/00A61P37/06A61P37/02
CPCA61K9/06A61K31/436A61K47/10A61P31/10A61P35/00A61P37/06A61P37/02
Inventor 戚卫蕊喻进雷伯开吴笑笑袁哲哲
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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