Prednisolon-base injection solution

FIELD: medicine, pharmacy.

SUBSTANCE: treatment involves using the injection solution based on water-soluble prednisolon formulation containing sodium salt and accessory additive. Prednisolon sodium phosphate is used as prednisolon water-soluble formulation, and anhydrous sodium hydrogen phosphate and sodium dihydrogen phosphate dihydrate taken in the ratio = (1.375-1.5):1, respectively, are used as sodium salt, and propylene glycol is used as an additional additive in the following ratio of components, wt.-%: prednisolon sodium phosphate (as measured for prednisolon), 2.5-3.5; anhydrous sodium hydrogen phosphate, 0.045-0.055; sodium dihydrogen phosphate dihydrate, 0.03-0.04; propylene glycol, 12-17, and injection water, the balance, up to 100%. Invention can be used in producing hormonal preparation prednisolon in injection formulation for treatment of rheumatism, infectious nonspecific polyarthritis, bronchial asthma, leukemia and other diseases. Invention provides enhancing stability of prednisolon-containing solution and prolonged storage time.

EFFECT: improved and valuable properties of solution.

3 tbl, 2 ex

 

The invention relates to the field of medicine and is suitable for the production of the hormonal drug prednisolone in injectable form for the treatment of rheumatism, infectious nonspecific polyarthritis, asthma, leukemia and other

Prednisone is a white crystalline powder, practically insoluble in water.

The prior art various forms of prednisone, for example in the form of tablets (U.S. Pat. USA 4708867, the United Kingdom patent No. 862376, Pat. RF 2153340, Pat. PF No. 2187307), ointments (U.S. Pat. Of the Russian Federation No. 2093185, Pat. U.S. No. 3711602), microcapsules (U.S. Pat. Of the Russian Federation No. 2139046), eye and ear drops.

It is noted that many therapeutically useful steroids have low solubility in conventional pharmaceutical carriers or solvents, so attempt to increase their solubility for introduction into the body, for example the introduction in their molecules modifying the solubility or groups to improve the properties of the media and the selection of solvents.

Known emulsion of the type oil-in-water containing prednisolone, oil containing castor oil, emulsifier in the form of phospholipids of egg yolk, water for injection, an agent for regulating isotonicity glycerin, hydrate of sodium oxide to regulate pH (U.S. Pat. Of the Russian Federation No. 2141313). The emulsion is used for injecting into the patient. The emulsion is about the fully good chemical and physical stability with minimal oxidation.

Functional and structural analogue of prednisolone is hydrocortisone, he is also an intermediate for receiving prednisolone.

Known liposomal composition for intra-articular injection for relief of aseptic inflammation, containing dipalmitoylphosphatidylcholine, cholesterol, hydrocortisone acetate and saline. Intra-articular injections can reduce the number of hidrocortisona 5 times in comparison with microcrystalline form. The use of hydrocortisone acetate is allowed to obtain a homogeneous emulsion by increasing the solubility of hydrocortisone in the water, but much more complicated process (U.S. Pat. Of the Russian Federation No. 2078564).

In an emergency requiring immediate increase of corticosteroids in the blood (acute adrenal insufficiency, shock, asthma attacks), using soluble drug prednisolone injection - prednisolone hemisuccinate. Powder prednisolone hemisuccinate dissolved in sterile water for injection, add isotonic solution of sodium chloride and glucose solution or poliglyukina (Medmaravis, Drugs, 2001, vol. 2, p.29-30). This composition is selected as a prototype. The disadvantage is the low stability of the drug and small storage period.

The purpose of this izaberete the Oia - the stability of the solution containing prednisolone during long term storage.

The objective is achieved by the fact that the use of solution for injection on the basis of water-soluble forms of prednisolone containing a salt of sodium and auxiliary additive. When this water-soluble form of prednisolone is prednisolone sodium phosphate, and as the sodium salt using sodium phosphate disubstituted anhydrous and one-deputizing 2-water, taken in the ratio (1,375 to 1.5):1, respectively, as an auxiliary additive use propylene glycol in the following ratio of ingredients, wt.%:

prednisolone sodium phosphate (in terms of prednisolone) of 2.5-3.5

sodium phosphate disubstituted anhydrous 0,045-0,055

sodium phosphate one-deputizing 2 - water 0,03-0,04

propylene glycol 12-17

water for injections the rest up to 100%

The invention is illustrated by the following examples.

Example 1. In water for injection is dissolved calculated quantity of sodium disubstituted phosphate anhydrous, sodium phosphate one-deputizing 2-water, propylene glycol and mix, then add the calculated amount of prednisolone sodium phosphate is stirred until complete dissolution 10 minutes, bring up to the required volume with water for inacti (pH of 7.5). The process is conducted at ControlTemplate. The solution is sterile filtered through a membrane filter with a size of 0.22 μm and fill vials with a volume of at least 1.0 ml Ampoules sealed and subjected to sterilization.

Example 2. The product is prepared analogously to example 1. The difference is in the amount of the ingredients (see table 1).

The resulting solution is a clear liquid that contains no mechanical or other impurities, stable. May be stored for a long time. When the chemical and bacteriological pollution control is not revealed. Meets the requirements of GFK. The stability of the solution is tested in the conditions of sterilization (steam sterilizer temperature 100°C sterilization time 30 min). If the solution does not change in the sterilization conditions, there shall be a further test of his method of accelerated aging at 40-70°C. Before and after sterilization and during accelerated aging is controlled color solution, spectrophotometric determination of prednisolone and the pH value of the solution. The results of the experiment are presented in table 2 and 3.

Studies pharmacologically activity solution prednisolone showed that the excipients do not affect the pharmacological activity of the drug, which remains constant after sterilization and after 1 and 3 years of storage.

Table 1

The composition of the solution
IngredientsExample 1, wt.%Example 2, wt.%
Prednisolone sodium phosphate (in terms of prednisolone)2,53,5
sodium phosphate disubstituted anhydrous0,0450,055
sodium phosphate one-deputizing 2-water0,030,04
propylene glycol1712
Water for injection80,42584,405
Quality indicators:  
PH7,57,51
colorcolorless, transparentcolorless, transparent

td align="center"> Colorless
Table 2

Color change 1%-aqueous solution of prednisolone injection
No.sterilizationThe retention time
 ToAfter2 months6 months1 year3 years
1ColorlessColorlessColorlessColorlessColorless
prednisolone hemisuccinateColorlessColorlessColorlessColorlessSt. Yellowyellow

Table 3

The change of the pH value and the content of prednisolone in solution
No.pHThe content of prednisolone
 Before after sterilizationAfter 1 and 3 years storageBefore after sterilizationAfter 1 and 3 years storage
17,5 7,57,5 7,451,00 1,011,01 1,00
prednisolone hemisuccinate7,5 7,57,45 7,101,00 1,021,01 1,04

The solution for injection on the basis of water-soluble forms of prednisolone containing a salt of sodium and auxiliary additive, characterized in that a water-soluble form of prednisolone is prednisolone sodium phosphate, and as the sodium salt using sodium phosphate disubstituted anhydrous and one-deputizing 2-water, taken when the ratio (1,375 to 1.5):1, respectively, as the sub is Oh additives use propylene glycol in the following ratio of ingredients, wt.%:

Prednisolone sodium phosphate (in terms of prednisolone) of 2.5-3.5

Sodium phosphate disubstituted anhydrous 0,045-0,055

Sodium phosphate one-deputizing dowolny 0,03-0,04

Propylene glycol 12-17

Water for injections the Rest up to 100%



 

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