Pharmaceutical composition eliciting anesthetic activity

FIELD: medicine, pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition used in stomatology in the topical anesthesia. The pharmaceutical composition comprising articaine hydrochloride and epinephrine hydrochloride and accessory substances, such as sodium metabisulfite, sodium chloride and water for injection involves additionally glycine and pH-regulating substance taken in the definite ratio of components. Invention provides preparing the preparation that is stable, non-toxic and doesn't cause allergic response reactions and elicits highly expressed infiltration and conducting anesthetic activity, good tissue tolerance and activity promoting to accelerated wound-healing in the post-operative period.

EFFECT: improved and valuable medicinal properties of composition.

3 cl, 3 ex

 

The invention relates to the pharmaceutical industry, namely pharmaceutical compositions used in dentistry for local anesthesia.

Known drug called "Xylonor" [1], which is an anesthetic locally-regional actions, manufactured by CJSC "world of the health care system (WHS), Russia. The medication comes in the form of a solution for injection and contains one to carpool 1.8 ml as the primary active ingredient hydrochloride lidocaine mnogoyarusnyi 36 mg, norepinephrine tartrate, expressed in norepinephrine basis 0.036 mg, epinephrine is the basis of 0.036 mg, sodium chloride 11,70 mg, disulfate potassium (corresponding to Sox2) 1.24 mg, edetate sodium 0.45 mg, parahydroxybenzoate bromide of 1.44 mg, parahydroxybenzoate cut 0.36 mg, hydrochloric acid 0,388 Ml solution of sodium hydroxide as a pH regulating substance pH 5,00±0.20 and water for injection. Introduced into the oral cavity by means of local infiltration anesthesia lidocaine reaches its peak concentration in the blood after about 10-15 minutes after injection. Anesthesia occurs within 2-3 minutes and lasts 90-120 minutes on the level of the soft tissues and 5-10 minutes on the level of the pulp. The half long and is approximately 90 minutes. The drug is an effective anesthetic tool is for any kind of classical intervention in dentistry. However, the drug has disadvantages, which include a long half-life, various allergic reactions due to the high systemic toxicity, adverse effects on wound healing due to low tissue tolerance.

Renowned pharmaceutical composition used in dentistry, entitled "Septanest with adrenaline produced in the form of solution for injection [2]. The product contains in the carpool 1.8 ml hydrochloride artikaina 72,0 mg tartrate adrenaline: bitartrate of ephedrine 0,033 mg, epinephrine basis 0.18 mg and excipients, such as sodium chloride is 2.88 mg, disulfit sodium (sodium metabisulfite) 1.8 mg, edetate sodium 1.8 mg, the solution of sodium hydroxide as a pH regulating substance to a pH of 6.0+0.2 and water for injection of 1.8 ml of the drug reaches its peak after 17 minutes after the injection, the half-life of approximately 25 minutes, which reduces its toxicity and reduces allergic reactions are possible. However, the drug can cause in an individual patient serious allergic reactions due to the presence in its composition of edetate sodium and a large number of disulfit sodium. In addition, the pharmaceutical composition does not have a pronounced infiltration and block anaesthetic activity.

Closest to the claimed farmacevticheskoi composition is a pharmaceutical composition for injection, with anaesthetic activity, called "Ultracain D - s Forte" on the basis of artikaina and epinephrine [3]. Components 1 ml of the following: artikaina hydrochloride 40 mg of epinephrine hydrochloride 12 mg, excipients, such as sodium metabisulfite 0.55 mg, sodium chloride, water for injections. The effect of the drug "Ultracain D - s Forte starts in 1-3 minutes, and the duration of anesthesia is 75 minutes. The drug is 2 times more powerful than lidocaine, 6 times stronger than Novacaine and has a high diffusion capacity, low toxicity and small vasoconstrictor effect, which is more positive effect on wound healing, shows less side effects due to the absence in the composition of edetate sodium. The half-life of 25.3 minutes. The disadvantages of the drug is some toxicity resulting from the presence of the drug sulfites, still resulting in individual patients with serious allergic reactions.

The basis of the invention is the task to create such a pharmaceutical composition in which through the use of major components and auxiliary components, taken in a certain ratio, but also due to the introduction of an additional component achieved a significant reduction of toxicity, increase infiltration and provodnikovoj anaesthetic activity, improving tissue tolerance and accelerate wound healing.

The problem is solved in that in the known pharmaceutical composition having anaesthetic activity, containing articaine and epinephrine and excipients, such as sodium metabisulfite, sodium chloride, pH regulating substance and water for injection, according to the invention additionally contains a glycine at the following ratio of components, g:

Artikaina hydrochloride38,0-42,0
Epinephrine base0,005-0,12
(in the form of hydrochloride)
Metabisulphite sodium0,25-0,55
Glycine4,0-20,0
Sodium chloride0,36-0,8
PH regulating substance8,5-12,5
Water for injectionto 1 l

Preferably the pharmaceutical composition has a content of components was:

Artikaina hydrochloride40,0
Epinephrine base0,01
(in the form of hydrochloride)
Metabisulphite sodium0,3
Glits is n 8,0
Sodium chloride0,4
PH regulating substance10,0
Water for injectionto 1 l

In addition, as the pH regulating substance use 1 M solution of hydrochloric acid.

In this pharmaceutical composition as the active substance is applied artikaina hydrochloride - anesthetic amide type belonging to the group of thiophenol. In tissues subjected to hydrolysis and releases the basis of having lipophilic properties, and easily penetrates through the membrane inside the nerve fibres. Ionized and transformed into a cation. Interacting with receptors, inhibits the entry of sodium ions into the cell in the phase of depolarization and blocking conduction of impulses in the nerve fiber. A high percentage of zwiazane with plasma proteins in articaine svidetelstvuet that 95% of the drug reaches the blood stream in the form of a pharmacologically inactive substance and shows about low systemic toxicity and high efficiency anesthesia. The composition of the pharmaceutical composition includes a vasoconstrictor is epinephrine (in the form of hydrochloride), which is providing sosudosuzhayushcheye action, and prevents systemic absorption artikaina and development of its side effects, and prolong longer the time, the action of the main active substances - artikaina to 360 minutes.

With the introduction in the pharmaceutical composition of amino acids such as glycine (aminouksusnoy acid), amplification of the action of the vasoconstrictor is epinephrine and prolonged for a longer time, the basic active substance - artikaina. Glycine enhances the action of the main active substances - artikaina, which allows to use the smallest dose of a solution of the drug. Anesthesia occurs within 0.5 to 3 minutes and lasts for at least 75 minutes. In addition, the glycine in aqueous solutions articaine with epinephrine binds heavy metal ions, which are present in the sodium metabisulfite, injection water, raw materials, and thus glycine performs the function of the complexing agents and contributes to the stability of the drug during storage for two years. Glycine also strengthens the cell, protects, nourishes her in a stressful situation, has a sedative effect, which is very important when operational stomatologicheska intervention. The use of glycine slows the passage of artikaina in General circulation and provides thus saving active tissue concentration, which in turn promotes good wound-healing in the postoperative period. In addition, the introduction of glycine reduces the presence in the composition of tachogenerator (antioxidant), as sodium metabisulfite, which in turn reduces the amount of sulfites. As the medical practice, the amount of sulfites in anestasiaweb solution should be minimal, because the sulfites can cause allergies and trigger an bronchial asthma attack. Thus, the introduction of glycine reduces the risk of allergic reactions. In the preclinical and clinical studies have established the optimal amount of glycine in the pharmaceutical composition, which is 4,0-20,0 g on 1 l. the half-life of 21.9 minutes. Low systemic toxicity of the drug is ensured by the fact that the glycine it binds to plasma proteins (95%), and also due to the rapid half-life. This allows you to safely apply the pharmaceutical composition for children, pregnant women, nursing mothers and the elderly. Stability of the finished product is ensured by the introduction into the composition of a stabilizer (antioxidant), sodium metabisulfite and safe for patients, the dose and complexing agents - glycine, and bringing the pH to a certain level by introducing into the composition a pH regulating substances, which use a 1 M solution of hydrochloric acid in the amount of 8.5 to 12.5 g per 1 l of the Optimal pH, the ri which ensures maximum durability of the pharmaceutical composition, determined within the range of 3.5 to 4.5.

Thus, the obtained stable and non-toxic pharmaceutical composition having a pronounced infiltration and block anaesthetic activity, good tissue tolerance and promoting accelerated wound-healing.

The pharmaceutical composition was prepared in this way.

Example 1.

Preparation of the solution is carried out in a glass programmirovanie reactor with a capacity of 30 liters, equipped with an anchor stirrer. Chilled water for injection with a temperature of 18°served in the reactor by passing it through a sterilizing filter, and saturated with filtered nitrogen under pressure of 0.003 MPa for 20 minutes.

Then manually through the loading hatch download metabisulfite sodium in the number 0,01705 kg and pre-calcined sodium chloride in the amount of 0,0108 kg and thoroughly stirred for 10 minutes. Then add in the reactor 0.6 kg of glycine and again stirred solution for 15 minutes.

Then into the reactor through a hatch upload 1.14 kg artikaina hydrochloride and stirred until complete dissolution within 15 minutes.

Then in a separate container made of glass with a capacity of 1 l pour 900 ml of water for injection at room temperature, pre-saturated with nitrogen in the reactor, add 0,255 kg 1 M solution of hydrochloric acid and add Aut 0,00036 kg epinephrine basis. The solution is stirred until complete dissolution of epinephrine for 10 minutes. The resulting solution of epinephrine hydrochloride quantitatively transferred into a reactor and then the reactor is stirred for 10 minutes. Conduct sampling through the hatch and determine the pH of the solution, which should be in the range of 3.5 to 4.5. Adjustment of the solution pH spend 1 M solution of hydrochloric acid to the required limits.

After adjusting the pH of the solution to stop the stirrer and bring its contents on the label up to 25 litres, adding water for injection pre-saturated nitrogen. The solution is stirred for 15 minutes.

At the end of the cooking process solution to produce a sample for analysis according to the method of sequential control and define the appearance of the solution, the solution pH in the range 3.5 to 4.5, the content artikaina hydrochloride in 1 ml of a solution of 0.038 g, the content of epinephrine hydrochloride from 0,000012 g, the content of sodium metabisulfite 0,00055 g, glycine content is from 0.02,

When the deviation of the quantitative content components are adjusting the concentration of the solution by adding calculated amounts of the substance or water for injection, pre-saturated with nitrogen.

Then carry out a sterilizing filtration of the solution artikaina with epinephrine. Solution implement the Torah by means of a pump serves on filters pressure of 0.10-0.12 MPa, passed through the pre-filter with a pore size of 0.45 μm and finish sterilizing filter with a pore size of 0.2 μm.

Then the filtered solution artikaina with epinephrine served in a sterile collection of filtered solution.

Then carry out the filling of the capsules and their closure on a special machine for filling solution and capping the carpool CFV AA company N. STRUNCK+CO (GF-25) 1.8 ml.

In the preparation of the solution and filtering all equipment zacherley from the light and the whole process is carried out in aseptic conditions, including filling and sealing capsules.

Example 2.

Preparation of the solution is carried out in a glass programmirovanie reactor with a capacity of 30 liters, equipped with an anchor stirrer. Chilled water for injection with a temperature of 19°served in the reactor by passing it through a sterilizing filter, and saturated with filtered nitrogen under pressure of 0.003 MPa for 20 minutes.

Then manually through the loading hatch download metabisulfite sodium in the number 0,0093 kg and pre-calcined sodium chloride in the amount of 0,012 kg and thoroughly stirred for 10 minutes. Then add in the reactor 0.24 kg of glycine and again stirred solution for 15 minutes.

Then into the reactor through a hatch load of 1.2 kg artikaina hydrochloride and stirred until complete dissolution within 15 minutes.

The village is E. this in a separate container made of glass with a capacity of 1 l pour 900 ml of water for injection at room temperature, pre-saturated with nitrogen in the reactor, add 0.3 kg 1 M solution of hydrochloric acid and add 0,00003 kg epinephrine basis. The solution is stirred until complete dissolution of epinephrine for 10 minutes. The resulting solution of epinephrine hydrochloride quantitatively transferred into a reactor and then the reactor is stirred for 10 minutes.

Conduct sampling through the hatch and determine the pH of the solution, which should be in the range of 3.5 to 4.5. Adjustment of the solution pH spend 1 M solution of hydrochloric acid to the required limits.

After adjusting the pH of the solution to stop the stirrer and bring its contents on the label up to 25 litres, adding water for injection, pre-saturated with nitrogen. The solution is stirred for 15 minutes.

At the end of the cooking process solution to produce a sample for analysis according to the method of sequential control and define the appearance of the solution, the solution pH in the range 3.5 to 4.5, the content artikaina hydrochloride in 1 ml 0,040 g, the content of epinephrine hydrochloride 0,000008 g, the content of sodium metabisulfite 0.0003 g, the content of glycine 0,008,

When the deviation of the quantitative content components are adjusting the concentration of the solution by adding calculated amounts of substances or water for inye the Nations, pre-saturated with nitrogen.

Then carry out a sterilizing filtration of the solution artikaina with epinephrine. The solution from the reactor by means of a pump serves on filters pressure of 0.10-0.12 MPa, is passed through a pre-filter with a pore size of 0.45 μm and finish sterilizing filter with a pore size of 0.2 μm.

Then the filtered solution artikaina with epinephrine served in a sterile collection of filtered solution.

Then carry out the filling of the capsules and their closure on a special machine for filling solution and capping the carpool CFV AA company .STRUNCK+CO (GF-25) 1.8 ml.

In the preparation of the solution and filtering all equipment zacherley from the light and the whole process is carried out in aseptic conditions, including filling and sealing capsules.

Example 3.

Preparation of the solution is carried out in a glass programmirovanie reactor with a capacity of 30 liters, equipped with an anchor stirrer. Chilled water for injection to a temperature of 20°served in the reactor by passing it through a sterilizing filter, and saturated with filtered nitrogen under pressure of 0.003 MPa for 20 minutes.

Then manually through the loading hatch download metabisulfite sodium in the number 0,0775 kg and pre-calcined sodium chloride in the amount of 0,024 kg and thoroughly stirred for 10 minutes. Then add in the reaction is the PR 0.12 kg of glycine and again stirred solution for 15 minutes.

Then into the reactor through a hatch load of 1.26 kg artikaina hydrochloride and stirred until complete dissolution within 15 minutes.

Then in a separate container made of glass with a capacity of 1 l pour 900 ml of water for injection at room temperature, pre-saturated with nitrogen in the reactor, add 0,375 kg 1 M solution of hydrochloric acid and add 0,000015 kg epinephrine basis. The solution is stirred until complete dissolution of epinephrine for 10 minutes. The resulting solution of epinephrine hydrochloride quantitatively transferred into a reactor and then the reactor is stirred for 10 minutes. Conduct sampling through the hatch and determine the pH of the solution, which should be in the range of 3.5 to 4.5. Adjustment of the solution pH spend 1 M solution of hydrochloric acid to the required limits.

After adjusting the pH of the solution to stop the stirrer and bring its contents on the label up to 25 litres, adding water for injection, pre-saturated with nitrogen. The solution is stirred for 15 minutes.

At the end of the cooking process solution to produce a sample for analysis according to the method of sequential control and define the appearance of the solution, the solution pH in the range 3.5 to 4.5, the content artikaina hydrochloride in 1 ml 0,042 g, the content of epinephrine hydrochloride 0,000012 g,the content of sodium metabisulfite 0.00025 grams, the content of glycine from 0.004,

When the deviation of the quantitative content components are adjusting the concentration of the solution by adding calculated amounts of the substance or water for injection, pre-saturated with nitrogen.

Then carry out a sterilizing filtration of the solution artikaina with epinephrine. The solution from the reactor by means of a pump serves on filters pressure of 0.10-0.12 MPa, is passed through a pre-filter with a pore size of 0.45 μm and finish sterilizing filter with a pore size of 0.2 μm.

Then the filtered solution artikaina with epinephrine served in a sterile collection of filtered solution.

Then carry out the filling of the capsules and their closure on a special machine for filling solution and capping the carpool CFV AA company .STRUNCK+CO (GF-25) 1.8 ml.

In the preparation of the solution and filtering all equipment zacherley from the light and the whole process is carried out in aseptic conditions, including filling and sealing capsules.

The resulting preparation has anaesthetic activity and meets the requirements of the analytical normative documentation.

Thus, receive pharmaceutical composition in the form of a medicinal product artikaina with epinephrine, which is stable, less toxic and does not cause allergic reactions, pharmaceutical is eskay composition, possessing a pronounced infiltration and block anaesthetic activity, good tissue tolerance and promoting accelerated wound-healing.

Sources of information

1. Anesthetic drug "Xylonor" CJSC world of the health care system (WHS), www.stomat.ru

2. Anesthetic drug "Septanest with adrenaline, the company's catalog "Septodont", 2003, s-128.

3. Anesthetic drug "Ultracain D-s Forte" pharmaceutical company Hoechst Marion Roussel", http://medi.ru/doc/f5644.htm

1. Pharmaceutical composition having anaesthetic activity, containing articaine hydrochloride and epinephrine hydrochloride and excipients, such as sodium metabisulfite, sodium chloride and water for injection, characterized in that it further comprises glycine and pH regulating substances in the following ratio of components, g:

Artikaina hydrochloride38,0-42,0
Epinephrine hydrochlorideof 0,005 0,012
Metabisulphite sodium0,25-0,55
Glycine4,0-20,0
Sodium chloride0,36-0,8
pH Regulating substance8,5-12,5
Water for injectionTo 1 l

2. The pharmaceutical composition according to claim 1, characterized in that component, g:

Artikaina hydrochloride40,0
Epinephrine hydrochloride0,01
Metabisulphite sodium0,3
Glycine8,0
Sodium chloride0,4
pH Regulating substance10,0
Water for injectionTo 1 l

3. The pharmaceutical composition according to claims 1 and 2, characterized in that as the pH regulating substance use 1 M solution of hydrochloric acid.



 

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FIELD: organic chemistry, pharmaceutical industry, medicine.

SUBSTANCE: invention relates to new derivatives of S-substituted N-1-[(hetero)aryl]alkyl-N'-1-[(hetero)aryl]alkylisothioureas of general formula I

in form of free base and salts with pharmaceutically accepted acids, as well as racemate, individual optical isomers or mixture thereof. In formula R1, R2, R3, R4, Y and Z are as described in specification. Compounds of present invention are capable to potentiate (positively modulate) AMPA/KA glutamate receptors and simultaneously to block transmembrane currents induced by activation of NMDA glutamate receptors. Also disclosed are method for production of said compounds, including optical isomers; pharmaceutical composition; method for investigation of glutamatergic system, and method for Alzheimer's disease, treatment; as well as method for extreme retentiveness of memory by administering of effective amount of claimed compounds.

EFFECT: new pharmaceutically active compounds for Alzheimer's disease treatment.

23 cl, 1 tbl, 11 ex

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