Progesterone suspending injection and preparation method thereof

A suspension injection and progesterone technology, which is applied in blood diseases, pharmaceutical formulations, liquid delivery, etc., can solve the problems of strong pain response, insoluble progesterone, and large pain response, so as to increase dispersion and suspension capacity, Good thermal stability and good safety effect

Inactive Publication Date: 2017-12-08
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 solution injections. This type of injections has a greater pain response, greater irritation, and is prone to allergies when injected, and it is easy to cause drug deposition in local muscle tissue, causing lumps and pain. It is very inconvenient and brings inconvenience to clinical use
In Chinese patent CN101152186A, progesterone drugs are used to prepare submicron emulsions, and then prepared into progesterone suspension injections. This method improves the pain and allergies of traditional oil-soluble progesterone injections to a certain extent, and also has less irritation and long-term use tolerance, but the pain of oil solution injection is still stronger than that of aqueous solution injection, and there are more types of excipients used in the preparation process, and the preparation of water phase and oil phase is also added in the preparation process. , cooling, dilution and other processes, the process is complicated
[0005] In summary, the main problems to be solved by the present invention are: solving the technical difficulty of progesterone being insoluble in water, oil solution progesterone injection injection with strong pain response, conventional solubilization means not suitable for preparing progesterone into solution injection , to develop progesterone into a suspension injection with stable properties and less pain response during injection

Method used

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  • Progesterone suspending injection and preparation method thereof
  • Progesterone suspending injection and preparation method thereof
  • Progesterone suspending injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Progesterone Suspension Injection (Specification: 5mg: 1ml)

[0036] Prescription: Dosage (g)

[0037] Progesterone 5

[0038] SBA-15 10

[0039] Povidone K15 1

[0040] Add water for injection to 1L

[0041] The progesterone raw material is micronized by jet milling until the particle size D90 is 8.56 μm. Weigh the prescribed amount of micronized progesterone raw material and mix with SBA-15 for 20 minutes. Dissolve povidone K15 with an appropriate amount of water for injection, then add the co-ground powder of progesterone and SBA-15 into the aqueous solution of povidone K15, add water for injection and stir to disperse evenly, form a stable suspension, and constant volume. Fill the medicinal solution into ampoules and seal them. The progesterone suspension injection was obtained by autoclaving (115° C., 30 min).

Embodiment 2

[0042] Example 2 Progesterone Suspension Injection (Specification: 10mg: 1ml)

[0043] Prescription: Dosage (g)

[0044] Progesterone 10

[0045] SBA-15 20

[0046] Povidone K15 2

[0047] Add water for injection to 1L

[0048] The progesterone raw material is micronized by jet milling until the particle size D90 is 4.60 μm. Weigh the prescribed amount of micronized progesterone raw material and mix with SBA-15 for 20 minutes. Dissolve povidone K15 with an appropriate amount of water for injection, then add the co-ground powder of progesterone and SBA-15 into the aqueous solution of povidone K15, add water for injection and stir to disperse evenly, form a stable suspension, and constant volume. Fill the medicinal solution into ampoules and seal them. The progesterone suspension injection was obtained by autoclaving (121° C., 15 min).

[0049] attached image 3 The data show that: the aqueous progesterone suspension injection was set at an accelerated temperature of 40±...

Embodiment 3

[0052] Example 3 Progesterone Suspension Injection (Specification: 20mg: 1ml)

[0053] Prescription: Dosage (g)

[0054] Progesterone 20

[0055] SBA-15 40

[0056] Povidone K15 2

[0057] Add water for injection to 1L

[0058] The progesterone raw material was micronized by jet milling until the particle size D90 was 3.19 μm. Weigh the prescribed amount of micronized progesterone raw material and mix with SBA-15 and grind for 25 minutes. Dissolve povidone K15 with an appropriate amount of water for injection, then add the co-ground powder of progesterone and SBA-15 into the aqueous solution of povidone K15, add water for injection and stir to disperse evenly, form a stable suspension, and constant volume. Fill the medicinal solution into ampoules and seal them. The progesterone suspension injection was obtained by autoclaving (121° C., 15 min).

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Abstract

The invention relates to progesterone suspending injection and a preparation method thereof. The progesterone suspending injection comprises progesterone, SBA-15, povidone K15 and injection water. According to the invention, under the effect of physical mechanical force, the well-organized crystal structure of the progesterone is damaged but is not suffered from chemical degradation and SBA-15 and progesterone molecule are interacted through hydrogen bond, so that the amorphous progesterone molecule is loaded onto a nanometer structure duct, can be attached to the SBA-15 loading a large quantity of drug molecules and can be maintained under amorphous state; the amorphous progesterone molecule reacts with the povidone K15 through the hydrogen bond, so that the amorphous state is more stable and a certain suspending assisting function is achieved; the technical problems that the progesterone is difficult to dissolve in water, the oil-soluble progesterone injection brings a strong injection pain response and a conventional solubilizing method is not suitable for preparing the progesterone into the injection can be solved; and the progesterone is developed into the injection with stable nature and without pain response in the injection process.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a progesterone suspension injection and a preparation method thereof. Background technique [0002] Progesterone is a natural progestin, insoluble in water, soluble in organic solvents such as ethanol. Progesterone is a commonly used sex hormone drug, which can regulate hormone balance and is widely used in clinical practice. Treatment of catatonia, with estrogen cycles to counteract the effects of estrogen alone on the intima. [0003] Oral progesterone is rapidly destroyed in the gastrointestinal tract and liver. Currently, in addition to oral administration, there are mainly two routes of administration, vaginal administration and injection. More than 90% of progesterone in plasma is combined with protein, and only 3% is free. Its metabolites are mainly combined with glucuronic acid and excreted in urine. At present, the common progesterone injections on the market ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/32A61K31/57A61K47/52A61P15/00A61P7/04A61P15/06A61P5/34
CPCA61K9/0019A61K9/10A61K31/57A61K47/32
Inventor 姚静刘宇婧王雪敏
Owner 南京斯泰尔医药科技有限公司
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