UA146864U - MEDICINAL PRODUCT FOR SYSTEMATIC TREATMENT OF BACTERIAL INFECTIONS - Google Patents

Abstract

A medicament for the systemic treatment of bacterial infections caused by gram-positive, gram-negative, aerobic and / or anaerobic bacteria comprises at least one dosage form of a medicament containing an antimicrobial component and at least one pharmaceutically acceptable excipient. As an antimicrobial component contains the active pharmaceutical ingredient of formula (I) (I). The drug is made in a dosage form for parenteral administration in solid dosage form in the form of powder for infusion or lyophilized powder for infusion.

Description

A useful model relates to medicine, namely antimicrobial drugs for the treatment of bacterial infections.

Infectious diseases are a group of diseases caused by the penetration of microorganisms, viruses or prions into the patient's body. Depending on the type of pathogen, infectious diseases are divided into prion, viral, bacterial, protozoan and fungal. Therefore, depending on the type of infectious agent, antimicrobial or antiviral drugs are used to treat the patient.

Antimicrobial drugs are used for the prevention and/or treatment of inflammatory processes caused by bacterial microflora. According to the effect of drugs on bacterial microorganisms, bactericidal antimicrobial drugs (those that destroy bacteria due to, for example, destruction of their outer membrane) and bacteriostatic antimicrobial drugs (which inhibit the reproduction of microorganisms) are distinguished.

For example, the well-known antimicrobial agent LINCOMYCIN (web page with the address: por//kvipiv2.gy/saiaiod/geyseriigpue-rgeragagulLipkotiivipg/), which is a ready-made solution for intravenous and intramuscular injections and contains lincomycin hydrochloride (which is equivalent to 300 mg lincomycin base) and such excipients as disodium edetate, sodium hydroxide solution and water for injections. The medicine is packed in ampoules, 10 ampoules each, together with instructions for use and an ampoule scarifier in a cardboard box, 5 or 10 ampoules in open contour packages.

The main disadvantage of this known antimicrobial agent is its limited spectrum of action, namely, the known antimicrobial agent is effective mainly against gram-positive bacteria and ineffective against most gram-negative bacteria. That is, a known antimicrobial drug should be prescribed only in a hospital after obtaining the results of a microbiological study, and it is not suitable for outpatient practice, where treatment is always carried out empirically. In addition, the known antimicrobial suppresses the bifido- and lactoflora of the infected patient.

The correct choice of an antimicrobial agent by the doctor determines the effectiveness of the treatment, the effectiveness of the elimination of the pathogen and the speed of the patient's recovery. An antimicrobial agent is most effective when prescribed at the beginning of the disease, so it is most often used

Zo is chosen empirically, without relying on the results of a microbiological study. The effect of treatment with an antimicrobial agent depends on the spectrum of activity of the antimicrobial agent and its compliance with the characteristics of the causative agent of the infection. With an irrational choice of the initial antimicrobial agent, the treatment of an infected patient is delayed, complications may develop and repeated courses of treatment or hospitalization may be required. This determines the urgent need of modern medicine for highly effective antimicrobial agents with a broad spectrum of action, which successfully treat infections caused by both gram-positive and gram-negative bacteria, as well as both aerobic and anaerobic bacteria.

The useful model is based on the task of creating a highly effective and safe antimicrobial agent with a wide spectrum of action, which contributes to improving the quality and standard of living of patients and reducing the financial burden on patients, characterized by optimal physical properties and shelf life.

The problem is solved by the fact that a drug for the systemic treatment of bacterial infections caused by gram-positive, gram-negative, aerobic and/or anaerobic bacteria, which contains at least one dosage form of a drug containing an antimicrobial component and at least one pharmaceutically acceptable excipient , according to a useful model, as an antimicrobial component contains an active pharmaceutical ingredient of formula (I) but

Me i om NI o 9) kosh) (0,

and the drug is made in a dosage form for parenteral administration in a solid dosage form in the form of a powder for infusion or a lyophilized powder for infusion.

In addition, according to one of the variants of the implementation of the useful model, as pharmaceutically acceptable excipients, it contains form-forming substances, pH regulators, stabilizers.

In addition, according to one of the variants of the implementation of the useful model, the dosage form of the drug is a dosage form for parenteral administration.

In addition, according to one of the variants of the implementation of the useful model, one dosage form of the medicinal product contains from 50 mg to 700 mg of the active pharmaceutical ingredient of the formula ().

In addition, according to one of the variants of the implementation of the useful model, one dosage form of the medicinal product contains 300 mg of the active pharmaceutical ingredient of the formula (1).

In addition, according to one of the variants of the implementation of the useful model, one dosage form of the medicinal product contains 600 mg of the active pharmaceutical ingredient of the formula (1).

Medicinal product - a substance or a combination of substances (one or more active pharmaceutical ingredients (APIs) and excipients) that has properties and is intended for the treatment or prevention of diseases in humans. The medicinal product may contain at least one compound, namely AFiI. According to the useful model, AFI is an active pharmaceutical ingredient of the formula (I) no mia NN E ek I tat - M ho oo ().

The active pharmaceutical ingredient of formula (I) belongs to antimicrobial agents for systemic use. The active pharmaceutical ingredient of formula (I) inhibits the synthesis of the cell wall of bacteria, while it is stable to human dehydropeptidase 1. After intravenous administration, the active pharmaceutical ingredient of formula (I) is well distributed in human tissues and organs, is characterized by linear pharmacokinetics and is excreted mainly by the kidneys with urine. The active pharmaceutical ingredient of formula (1) is characterized by a wide spectrum of antimicrobial action against aerobic gram-positive and gram-negative bacteria, as well as against anaerobic bacteria.

In addition, the medicinal product may contain at least one pharmaceutically acceptable excipient. Use of pharmaceutically acceptable excipients for

From the production of means according to a useful model, it is possible to ensure the receipt of medicines in a dosage form, characterized by acceptable physico-chemical indicators and good indicators of shelf life.

Form-forming substances, pH regulators, stabilizers, etc. can be used as auxiliary substances in the composition of the medicinal product in the form for parenteral administration.

According to the essence of the utility model, solvents such as water, isotonic solutions, alcohols, ethers, glycerin, fatty oils, polyethylene oxide, silicone fluids, etc. can be used as mold forming substances.

According to the essence of the utility model, bases, acids, salts, etc. can be used as pH regulators.

According to the essence of the useful model, as stabilizers can be used acids, bases, salts of weak bases and strong acids, salts of strong bases and weak acids, etc. Preferably, inorganic acids can be used as part of the medicinal product in the form for parenteral administration.

A medicinal product containing the active pharmaceutical ingredient of formula (I) can be embodied in a dosage form for parenteral administration. The dosage form for parenteral administration can be powders for infusions, lyophilized masses for infusions, tablets for infusions, etc., which are converted into a solution, suspension, emulsion, etc. immediately before use. The drug can be in the form of powder, granules, nanoparticles, microspheres, etc., which are diluted in an acceptable solvent before use.

Preferably, the drug can be in the form of a lyophilized powder, granules, nanoparticles, microspheres, etc., which are diluted in an acceptable solvent before use.

The medicinal product in the form for oral administration may be packaged in an acceptable sealed primary packaging. Acceptable hermetic primary packaging, which can be a container and/or a container and a means of closure, is made of materials acceptable for injectable dosage forms to ensure effective storage of the medicinal product according to the useful model in the form for parenteral administration throughout the declared shelf life. Acceptable container materials include glass, polymer materials, etc. Glass, polymer materials, rubbers, etc. can be used as acceptable materials for closures, which provide moisture and air tightness, while the primary packaging itself is hermetic and isolates the medicinal product in a useful fashion from contact with the external environment.

Ampoules, vials, glasses, syringes, syringe tubes, dropper tubes, folding bags, etc., made of materials acceptable for injection dosage forms can be used for packaging the medicinal product according to the useful model.

A suitable primary packaging for a utility model in the form of a lyophilized powder for infusion is a glass hermetic ampoule or a plastic hermetic ampoule.

A particularly suitable primary packaging for a utility model in the form of a lyophilized powder for infusion is a glass vial with a rubber stopper and an aluminum cap, or a plastic bottle with a rubber stopper and an aluminum cap.

The medicinal product in the form for parenteral administration in the primary packaging may be packed in the secondary packaging with the booklet of instructions for the use of the medicinal product according to the useful model inside the secondary packaging and, if necessary, a scarifier. Any pharmaceutical acceptable secondary packaging may be used. Secondary packaging such as a cardboard box is especially suitable.

Before use, the antimicrobial drug is diluted in an appropriate amount of any solvent that is pharmaceutically acceptable and compatible with the antimicrobial drug. Such solvents as water, sodium chloride solution, solution can be used

From dextrose, potassium chloride solution, mannitol solution or their combinations.

A useful model is explained by examples.

Example 1

Stage 1. 13763 g of water for injections are loaded into the reactor. 1125 g of the active pharmaceutical ingredient of formula (I), 75 g of methylcellulose, 7.5 g of povidone, 15 g of methyl-p-oxybenzoate, 15 g of polysolvate are sequentially added to the water and mixed until the solid phase is completely dissolved and a homogeneous solution is obtained.

Stage 2. The solution obtained in Stage 1 is filtered through a sterilizing membrane filter into a sterile container.

Stage 3. On the automatic packaging line, 2.0 ml of the solution obtained at Stage 2 is packed into glass ampoules. Glass ampoules are placed in a lyophilizer and lyophilized for 14 hours, slowly raising the temperature from -45 "C to 40 "C.

Stage 4. After lyophilization, glass ampoules are sealed and packed in 5 blisters on a blister machine, and each blister is packed in a cardboard box with a booklet of instructions for use.

Thus, the obtained product is a lyophilized powder packed in a transparent glass ampoule containing 150 mg of the compound of Formula 1, 5 ampoules in a blister and 1 blister in a cardboard box with a booklet of instructions for use.

Example 2

Stage 1. 14513 g of water for injections are loaded into the reactor. 375 g of the active pharmaceutical ingredient of formula (I), 75 g of methylcellulose, 7.5 g of povidone, 15 g of methyl-p-oxybenzoate, 15 g of polysolvate are successively added to the water and mixed until the solid phase is completely dissolved and a homogeneous solution is obtained.

Stage 2. The solution obtained in Stage 1 is filtered through a sterilizing membrane filter into a sterile container.

Stage 3. On the automatic packaging line, 2.0 ml of the solution obtained at Stage 2 is packed into plastic vials. Plastic vials are loosely closed and placed in a lyophilizer and lyophilized for 14 hours, slowly raising the temperature from -45 "C to 40 "C.

Stage 4. After lyophilization, plastic vials are tightly closed with rubber stoppers, aluminum lids and packed 1 piece in a cardboard box with a booklet of instructions for (516) use.

Thus, the resulting product is a lyophilized powder packed in a transparent glass bottle with a rubber stopper, rolled up with an aluminum cap, which contains

300 mg of the Formula 71 compound, 1 vial in a cardboard box with a booklet of instructions for use.

Example C

Stage 1. 12638 g of water for injections are loaded into the reactor. 2250 g of the active pharmaceutical ingredient of formula (I), 75 g of methylcellulose, 7.5 g of povidone, 15 g of methyl-p-oxybenzoate, 15 g of polysolvate are successively added to the water and mixed until the solid phase is completely dissolved and a homogeneous solution is obtained.

Stage 2. The solution obtained in Stage 1 is filtered through a sterilizing membrane filter into a sterile container.

Stage 3. On the automatic packaging line, 2.0 ml of the solution obtained in Stage 2 is packed into glass vials. Glass vials are loosely closed and placed in a lyophilizer and lyophilized for 14 hours, slowly raising the temperature from -45 "C to 40 "B.

Stage 4. After lyophilization, glass vials are tightly closed with rubber stoppers, aluminum lids and packed 1 piece each in a cardboard box with a booklet of instructions for use.

Thus, the obtained product is a lyophilized powder, packed in a transparent glass bottle with a rubber stopper, rolled up with an aluminum cap, which contains 300 mg of the compound of Formula 1, 1 bottle in a cardboard box with a booklet of instructions for use.

Example 4

Stage 1. 10388 g of water for injections are loaded into the reactor. 4500 g of the active pharmaceutical ingredient of formula (I), 75 g of methylcellulose, 7.5 g of povidone, 15 g of methyl-p-oxybenzoate, 15 g of polysolvate are sequentially added to the water and mixed until the solid phase is completely dissolved and a homogeneous solution is obtained.

Stage 2. The solution obtained in Stage 1 is filtered through a sterilizing membrane filter into a sterile container.

Stage 3. On the automatic packaging line, 2.0 ml of the solution obtained in Stage 2 is packaged in

From glass vials. Glass vials are loosely closed and placed in a lyophilizer and lyophilized for 14 hours, slowly raising the temperature from -45 "C to 40 "B.

Stage 4. After lyophilization, glass vials are tightly closed with rubber stoppers, aluminum lids and packed 1 piece each in a cardboard box with a booklet of instructions for use.

Thus, the resulting product is a lyophilized powder, packed in a transparent glass bottle with a rubber stopper, rolled up with an aluminum cap, which contains 600 mg of the compound of Formula 71, 1 bottle in a cardboard box with a booklet of instructions for use.

Example 5

Stage 1. 9638 g of water for injections are loaded into the reactor. 5250 g of the active pharmaceutical ingredient of formula (I), 75 g of methylcellulose, 7.5 g of povidone, 15 g of methyl-p-oxybenzoate, 15 g of polysolvate are successively added to the water and mixed until the solid phase is completely dissolved and a homogeneous solution is obtained.

Stage 2. The solution obtained in Stage 1 is filtered through a sterilizing membrane filter into a sterile container.

Stage 3. On the automatic packaging line, 2.0 ml of the solution obtained at Stage 2 is packed into glass ampoules. Glass ampoules are placed in a lyophilizer and lyophilized for 14 hours, slowly raising the temperature from -45 "C to 40 "C.

Stage 4. After lyophilization, the glass ampoules are sealed and packed 3 pieces in a blister on a blister machine, and each blister is packed in a cardboard box with a booklet of instructions for use.

Thus, the obtained product is a lyophilized powder packed in a transparent glass ampoule containing 700 mg of the compound of Formula 1, 3 ampoules in a blister and 1 blister in a cardboard box with a booklet of instructions for use.

Example 6

A study was conducted with the participation of 132 people who were diagnosed with an infectious disease of the lower respiratory tract or an infectious disease of the urinary tract of bacterial etiology.

The treatment regimen included a drip infusion of 300 mg to 600 mg of an antimicrobial drug in a useful pattern every 12 hours for 7 to 14 days, depending on the severity of the disease. The duration of the infusion was 1 hour.

The overall clinical effectiveness of the antimicrobial drug according to the utility model was 94.7095 (i.e. 125 out of 132 people successfully recovered after treatment), the clinical effectiveness against lower respiratory tract disease was 92.65 95 (i.e. 63 out of 68 people successfully recovered after treatment), the clinical the effectiveness against urinary tract disease was 96.88 95 (i.e. 62 out of 64 people successfully recovered after treatment).

Side effects were observed in 12 95 people, among side effects the most frequent were rash (2.2 o) and gastrointestinal disorders (1.5 95).

Thus, the antimicrobial drug is effective in the treatment of infectious diseases of the lower respiratory tract and urinary tract of bacterial etiology.

The technical result achieved when using the tool according to the useful model:

Efficiency. The results of clinical studies show that the antimicrobial agent is highly effective against infectious diseases of various bacteriological etiology. In addition, the dosage form for parenteral administration is absorbed and acts very quickly.

Safety. The dosage form of the antimicrobial agent according to the useful model, namely the lyophilized powder for infusion, ensures high stability of the drug and the active pharmaceutical ingredient, and safety of use. When using the tool according to the useful model, no side effects were observed.

Improving the quality and standard of living of patients, and reducing the financial burden on the patient. The effectiveness of the tool based on a useful model, combined with a reduced risk of developing serious side effects, allows to reduce the negative symptoms of infectious diseases and improve the quality and standard of living of patients without the need for the use of additional drugs.

The qualitative and quantitative composition of the drug according to the useful model was selected in such a way as to ensure optimal physical properties of the drug and an acceptable shelf life.

Claims (2)

USEFUL MODEL FORMULA Co.) 1. Medicinal product for the systemic treatment of bacterial infections caused by gram-positive, gram-negative, aerobic and/or anaerobic bacteria, which contains at least one dosage form of a medicinal product containing an antimicrobial component and at least one pharmaceutically acceptable excipient, which is characterized by , which as an antimicrobial component contains an active pharmaceutical ingredient of the formula (I) but SHKA E m - NA o o codes); () and the medicinal product is made in a dosage form for parenteral administration in a solid dosage form in the form of a powder for infusion or a lyophilized powder for infusions 40 2. Medicinal product according to claim 1, which is characterized by the fact that it contains form-forming substances, pH regulators, stabilizers as pharmaceutically acceptable excipients. Q. The medicinal product according to any of claims 1, 2, which is characterized by the fact that the dosage form of the medicinal product is a medicinal form for parenteral administration. 4. Medicinal product according to any one of claims 1-3, which is characterized in that one dosage form 45 of the medicinal product contains from 50 to 700 mg of the active pharmaceutical ingredient of formula (1). 5. Medicinal product according to any one of claims 1-4, which is characterized in that one dosage form of the medicinal product contains 300 mg of the active pharmaceutical ingredient of formula (1). 6. Medicinal product according to any one of claims 1-4, which is characterized in that one dosage form of the medicinal product contains 600 mg of the active pharmaceutical ingredient of formula (1).