Water-soluble progesterone injection composition and preparation method of same

A technology of injection and progesterone, which is applied in drug combinations, diseases, blood diseases, etc., can solve the problems of large pain response, large irritation, complicated process, etc., and achieve the effect of small pain response, stable properties and simple process

Inactive Publication Date: 2017-05-31
南京斯泰尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the common progesterone injections on the market are oil-soluble injections. This type of injections has a greater pain response when injected, is highly irritating, and is prone to allergies, and it is easy to cause drug deposition in local muscle tissue, causing lumps and pain, etc., especially for long-term use. It is very inconvenient and brings inconvenience to clinical use
In order to solve this problem, Chinese patent CN101152186A adopts progesterone medicine to prepare submicron emulsion and then prepares progesterone injection. This method improves the pain and allergy of traditional oil solution progesterone injection to a certain extent, and also It has less irritation and long-term use tolerance, but the preparation process also adds water phase, oil phase preparation, heating homogenization, cooling dilution and other processes, and the process is more complicated
There are also literatures that use hydroxypropyl-β-cyclodextrin as a solubilizer. When the amount reaches a certain ratio, the solubility of progesterone in water can be increased, and then an aqueous solution of progesterone injection can be prepared. However, hydroxypropyl-β-cyclodextrin Although it has a good solubilization effect, in order to achieve its solubilization effect on progesterone, the maximum content of hydroxypropyl-β-cyclodextrin in the prescription is 40%, and there will be certain risks in the safety of injections

Method used

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  • Water-soluble progesterone injection composition and preparation method of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Progesterone Injection (Specification: 5mg: 1ml)

[0033] prescription:

[0034] Progesterone 5g

[0035] Hydroxypropyl-β-cyclodextrin 25g

[0036] Tromethamine 2g

[0037] Sodium chloride 0.2 g

[0038] Add water for injection to 1L

[0039] Weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, tromethamine, and sodium chloride into the water, stir to dissolve, add the prescribed amount of progesterone and sodium chloride, stir and dissolve at 60°C, and adjust the pH to about 7.5 . The prepared medicinal solution is prefiltered with a 0.45 μm microporous membrane, and the filtrate is finely filtered with a 0.22 μm microporous membrane. The finely filtered medicinal solution is filled in ampoules and melted. The progesterone injection was obtained by autoclaving (121° C., 15 min).

Embodiment 2

[0040] Example 2 Progesterone Injection (Specification: 10mg: 1ml)

[0041] Progesterone 10g

[0042] Hydroxypropyl-β-cyclodextrin 120g

[0043] Tromethamine 5g

[0044] Sodium chloride 0.1g

[0045] Water for injection 1L

[0046] Weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, tromethamine, and sodium chloride and add them to water, stir to dissolve, add the prescribed amount of progesterone drug and sodium chloride, stir to dissolve at 50°C, and adjust the pH to about 7.0. Use a 0.45 μm microporous membrane for primary filtration of the prepared medicinal solution, and fine filter the filtrate with a 0.22 μm microporous membrane. The finely filtered medicinal solution is filled in ampoules and melted. The progesterone injection was obtained by autoclaving (121°C, 15min).

[0047] Table 2 Results of accelerated test of progesterone injection (Example 2, 40±2°C, 75%±5%RH).

[0048] Appearance traits pH Content (mg / ml) relative substance(%)...

Embodiment 3

[0050] Example 3 Progesterone Injection (Specification: 20mg: 1ml)

[0051] Progesterone 20 g

[0052] Hydroxypropyl-β-cyclodextrin 200 g

[0053] Tromethamine 4 g

[0054] Sodium hydrogen phosphate 0.2 g

[0055] Water for injection 1L

[0056] Weigh the prescribed amount of hydroxypropyl-β-cyclodextrin, tromethamine, and sodium chloride into water, stir to dissolve, add the prescribed amount of progesterone and sodium hydrogen phosphate, stir to dissolve at 50°C, and adjust the pH to about 6.0 . The prepared medicinal solution is pre-filtered with a 0.45 μm microporous membrane, and the filtrate is finely filtered with a 0.22 μm microporous membrane. The finely filtered medicinal solution is filled in ampoules and melted. The progesterone injection was obtained by autoclaving (121° C., 15 min) for sterilization.

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Abstract

The invention relates to a water-soluble progesterone injection and a preparation method of same. The progesterone injection includes progesterone, hydroxypropyl-beta-cyclodextrin, tromethamine, and water for injection. Through the synergistic solubilization effect of the hydroxypropyl-beta-cyclodextrin and tromethamine, usage amount of the hydroxypropyl-beta-cyclodextrin is greatly reduced and use safety of the injection is improved. The invention also provides the preparation method of the water-soluble progesterone injection.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a progesterone injection composition using water as a solvent and a preparation method thereof. Background technique [0002] Progesterone is a sex hormone drug often used clinically, it has the function of regulating hormone balance, progesterone has the general effect of progesterone, and is widely used in clinical practice, mainly used for menstrual disorders, such as amenorrhea, functional uterine bleeding, corpus luteum insufficiency , Threatened miscarriage and recurrent miscarriage, treatment of premenstrual tension syndrome, and estrogen cycles against the effect of pure estrogen on the endometrium. [0003] Progesterone is a fat-soluble substance and is insoluble in water. In addition to oral administration, there are mainly two routes of administration, vaginal administration and injection, on the market. More than 90% of progesterone in plasma is combined with...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/57A61K47/69A61K47/18A61P15/00A61P7/04A61P15/06
CPCA61K9/0019A61K9/08A61K31/57A61K47/18
Inventor 姚静谢晓燕张自强
Owner 南京斯泰尔医药科技有限公司
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