Immobilized form of cephasoline for preventing postoperative infectious complications in otolaryngology

FIELD: pharmaceutical industry.

SUBSTANCE: invention provides immobilized form of cephasoline wherein cephasoline is included into polymer matrix made of sodium-carboxymethylcellulose.

EFFECT: reduced (by three days) treatment time.

1 dwg, 5 tbl


The invention relates to medicine, in particular to the pharmacy, surgery, and otolaryngology.

The closest dosage form is Cefazolin powder for preparation of injection solution, which is used intramuscularly or intravenously (bolus or drip). For the prevention of postoperative infectious complications anticipated appointed 1.0 g for 30 min prior to surgery, 0.5-1.0 g during operation, and 0.5-1.0 g every 6-8 hours during the day after surgery. The duration of treatment is 7-10 days. Consumption is anticipated from 3.5 to 42 g [Piskunov GS, Piskunov SZ Medicines used in otorhinolaryngology. - M.: ZAO "Thinstation", 2000. - Pp.33-34; Mashkovsky PPM Medicines: a Manual for physicians: 2 so - 2. - Ed. 14-e, revised and enlarged extra - M.: New wave, 2000. - 608 S.; Belousov SHE, Ushkalov E.A. Formulary system in the antibiotic /Antibiotics and chemotherapy. - 2001. - V.46. No. 11. - P.23-35].

Specified dosage form Cefazolin has disadvantages: side effects from vital systems of the body, nausea, vomiting, diarrhea, epigastric pain, pseudomembranous colitis, candidates, impaired renal function, increased concentrations of liver enzymes (ACT, ALT, alkaline phosphatase, LDH) in the blood, changes in peripheral blood (reversible leukopenia, neutrope what I thrombocytopenia, agranulocytosis, lymphocytosis, hemolytic anemia), allergic reactions (skin rash, pruritus, toxic epidermal necrosis, erythema multiforme, fever; angioedema, arthralgia, anaphylactic shock). Possible pain at the site of intramuscular injection, the formation of infiltrates, abscesses, phlebitis and thrombophlebitis [Piskunov GS, Piskunov SZ Medicines used in otorhinolaryngology. - M.: ZAO "Thinstation", 2000. - Pp.33-34; Mashkovsky PPM Medicines: a Manual for physicians: 2 so - 2. - Ed. 14-e, revised and enlarged extra - M.: New wave, 2000. - 608 S.; Register of medicines of Russia. 8th ed., revised and enlarged supplementary / CH. edit Ufraw. - M.: radar-2001, 2001. - 1503 S.].

Thus, the main disadvantages of a solution of Cefazolin, administered intravenously or intramuscularly, is a side effect and a significant consumption of antibiotic.

Object of the invention is the expansion of the range of dosage forms Cefazolin for prophylaxis of postoperative infectious complications in otolaryngology.

This object is achieved in that the immobilized form, in addition to Cefazolin, contains sodium carboxymethyl cellulose and glycerin in the following ratio, wt.%:

Sodium carboxymethylcellulose2,0-4,0
Glycerin1.5 to 2.5
Purified waterRest

The invention is illustrated in the following tables and drawing.

Table 1. The effect of Cefazolin in polymer matrices on the transport function of ciliated epithelium of the mucous membrane of the nasal cavity.

Table 2. Antimicrobial activity of polymer matrices with Cefazolin.

Table 3. The effect of drying temperature on the stability of polymer matrix with Cefazolin.

Table 4. Stability of immobilized forms of Cefazolin during storage at (4±2)°C.

Table 5. The influence of immobilized forms of Cefazolin on the regression of the symptoms of inflammation of the nasal mucosa in the postoperative period.

A drawing. Release is anticipated from the polymer matrix.

The introduction of the immobilized forms of Cefazolin sodium-carboxymethylcellulose reduces the toxicity is anticipated to increase the time and the degree of release from the dosage form and, consequently, to increase efficiency.

To increase the elasticity of the polymer matrix, they included the glycerin.

Characteristic of interest:

Cefazolin* (Cefazolin*)-(6R-TRANS)-3-[(5-methyl-1,3,4-thiadiazole-2-yl)-thiomethyl]-8-oxo-7-[(1H-tetrazol-1-yl-acetyl)amino]5-thio-1-azabicyclo[4.2.0.]Oct-2-ene-2-carboxylic acid (as sodium salt). Synonyms: Cefazolin sodium salt, Cefazolin sodium (Cefazolinum-natrium) AMOLED (Russia) (FS 42-3477-98), Ancef (Ancef), Vomitin (Vulmizolin), Kefzol (Kefzol), Intrusion (Intrazoline) and other Dried powder of white or white with a yellowish tint. Soluble in water, isotonic sodium chloride solution and 5% glucose solution, very little is soluble in ethyl alcohol. Pharmacological action - antibacterial, bactericidal. Has a wide range of antimicrobial activity: active against both gram-positive (staphylococci, not producing and producing penicillinase; and hemolytic viridans streptococci group a, pneumococci, Bacillus diphtheria, anthrax), and gram-negative microorganisms (meningococci, gonococci, Shigella, Salmonella, E. coli, Klebsiella, Proteus, and others). Cefazolin prevents the formation of bacterial wall by competitive blocking of enzymes involved in the synthesis of peptidoglycan, which is included in the composition of cell membranes. The half-life of 1.8 h at intravenous and 2 h after intramuscular injection, the maximum concentration in blood is reached after 1 h Bound to plasma proteins at 80%, not biotransformed, excreted by the kidneys [Register of medicines of Russia. Encyclopedia of drugs. 8th ed., revised and expanded. / CH. ed Ufraw / M: RLS-2001". - 2001. - 1504 S.; the State register of medicines / health Ministry. - M., 1998. - 1004 S.]. The selected number is anticipated due to the lack of adverse effects on the transport activity of ciliated epithelium of the mucous membrane of the nasal cavity and optimal antimicrobial activity of the local administration (table 1 and 2).

Sodium carboxymethylcellulose (Na-CMC) is a sodium salt of a simple ester of cellulose glycolic acid. It is a white or slightly yellowish powdery product is odorless. In addition to the Na-CMC domestic production currently used Na-CMC production of Dutch firm Hercules Blanose Cellulose Gum Type 7M31CF (Blanose), which is a granulated product. Na-CMC is soluble in hot and cold water, 50% aqueous solution of ethanol, forms a highly viscous aqueous solutions. Na-CMC physiologically inert and does not intrude. Na-CMC in pharmaceutical practice as a prolongator of drugs in eye drops and injectable solutions, emulsifier, binding and loosening means in the production of tablets, fundamentals of medical films [Polymers in pharmacy / Aeencv, Metalysis. - M.: Medicine, 1985. - P.10-20]. Na-CMC and Blanose provide maximum and uniform dissolution and release of Cefazolin from the polymer matrix is about comparison with methylcellulose (MC) and oksipropilmetiltselljulozy (OPMC) (see), stability during storage (table 4), and therefore increase therapeutic effect. In polymer compositions is anticipated with OPMC and MC during drying occurs destruction of the antibiotic, as evidenced by the color change, the shift of the maximum absorption, a significant reduction of the zones of inhibition of growth of the test microorganism and quantitative content (table 3). The selected number of Na-CMC and Blanose due to the fact that at concentrations below 2 wt.% reduced strength of the polymer matrix and the time of contact with the mucous membrane, and when the content is more than 4 wt.% formed by dissolution of the matrix gel reduces transport activity of ciliated epithelium of the mucous membrane of the nasal cavity.

Introduction to polymer matrix 1.5 to 2.5 wt.% glycerin (FS 42-2202-99) provides elasticity and strength matrices (table 4).

Thus, the optimum of immobilized form Cefazolin is a polymeric matrix of 2-4 wt.% sodium-carboxymethylcellulose containing 0.5-2.0 wt.% Cefazolin and 1.5 to 2.5 wt.% glycerol.

For the proposed structure based on the properties of incoming ingredients optimal drying temperature of the polymer composition (30°C), which allows you to save the antimicrobial activity, the quantitative content of the antibiotic within the normal range, and developed manufacturing technology (postage the essential quality control), which consists of the following steps.

1. Sanitization of production. Training facilities, personnel, supplies, equipment, raw materials.

2. Obtaining pharmaceutical compositions.

2.1. Preparation of a solution of sodium-carboxymethyl cellulose and glycerin in parts of purified water.

2.2. Dissolution is anticipated in the remaining part of the purified water.

2.3. Mixing the polymer solution with a solution of the antibiotic.

2.4. Deaeration.

3. Obtaining the polymer matrix.

3.1. Bottling of medicinal composition on the substrate.

3.2. The drying.

3.3. The dosage.

4. Packing of the polymer matrix.

Example by way of receipt.

To improve the stability of the polymer matrix is prepared under aseptic conditions in accordance with the requirements of normative documents using sterile utensils. A portion of Na-CMC (or Blanose) pour part of sterile purified water heated to 50-70°and periodically stirred to dissolve the polymer, add the glycerin. Cefazolin is dissolved in the remaining amount of sterile water and thoroughly mix with cooled to (20±2)°With the polymer solution until smooth. After deaeration homogeneous polymer pharmaceutical composition is poured onto the substrate and dried at a temperature of (30±3)°C for 5-6 hours. Dried Polym rye matrix is removed from the substrate, metered and placed in sterile glass bottles from data for medicines (THE 62-2-1077) (glass NS-1), sealed with rubber stamps IL-119 (TU 38-006108-90) and metal caps "running". The vials are placed in cardboard boxes. Stored at a temperature of (4±2)°protected from light (in the refrigerator) for 12 (24) months (table 4).

Reducing the toxicity and increasing the efficacy of Cefazolin in immobilized form in the prevention of postoperative infectious complications was confirmed by results of application (table 5).

The use of immobilized forms of Cefazolin.

On the mucosal surface of the lower turbinate and septum of the nose was Packed polymer matrix with the anticipated size of 2×1 cm on average nasal sink - matrix 1.5×1 see the First introduction of polymer matrices with Cefazolin was carried out for 2 hours before surgery. After removal of tampons a day after the operation, the introduction of immobilized forms of Cefazolin produced daily once a day for 5-6 days. Not identified allergic reactions, inflammation and ulceration of the mucous membranes of the nasal cavity.

Example usage.

Patient M., 25 years old, medical history, No. 1348 18.02.04, made submucous resection of nasal septum, dfugstore the inner submucosal vasotomy. After removal of the swab from the nasal cavity on the following day entered immobilized form anticipated by the above method. The introduction of Cefazolin was carried out for 4 days. Within a day the patient when rhinomanometry noted a sufficient degree of nasal breathing, there was no inflammation, there was no excess production of nasal secretions, surface temperature of the mucosa was close to the benchmark, there was no need for the use of decongestants.

To determine the effect of polymer carrier for therapeutic activity of immobilized forms of Cefazolin group of patients after surgery in the left half of the nose was injected polymer matrix Cefazolin of Blanose, in the right - of Na-CMC. Differences in the postoperative period is not installed. Regression of symptoms of inflammation was similar in both halves of the nose, which testifies to the same activity of the polymer matrices of Na-CMC and Blanose.

Thus, the proposed immobilized form Cefazolin has a high therapeutic efficacy, low toxicity to tissues of the mucous membrane of the nasal cavity and efficiency. The consumption of antibiotic treatment 0.2 to 0.8, Developed an optimal method of making an immobilized form Cefazolin, drop the speaker changes in the structure and physico-chemical properties of drug substances.

Offer immobilized form Cefazolin allows you to extend the range of available drugs for the prevention of postoperative infectious complications.

Table 1
The content of Cefazolin

in the polymeric matrix, wt.%
During transport, minutes
Before the introduction ofAfter removing
Note: each average value obtained in 6 subjects.

Table 2
Test microorganismsThe diameter of zones of inhibition of growth of test microorganisms (mm) for the content of Cefazolin, wt.%
Staphylococcus aureus was ATSS-653830,5±0,335,5±1,5 39,8±1,241,5±1,4
Bacillus subtilis was ATSS 663334,1±0,738,5±1,844,3±1,247,5±1,7

Table 3
The quality indicatorsDrying temperature, °Shelf lifePolymers-media
6 monthsWhiteYellowWhiteYellow
6 monthsYellowLight yellowYellowLight yellow
Quantitative content, Rel. %(30±2)Fresh100,04100,3097,33100,67
6 months98,7098,3389,33(45±2)Fresh95,6798,67100,2097,67
6 months86,3390,3358,0050,33
The maximum adsorption wavelength, nm(30+2)Fresh272274274274
6 months272280295295
6 months295295300300
Zone of inhibition of growth of Bacillus subtilis, mm(30+2)Fresh37,037,036,5a 38.5
6 months36,534,034,528,5
6 months32,030,028,725,7

Table 4
The quality indicators Polymers-media
Freshly prepared matrixAfter storageFreshly prepared matrixAfter storage for 12 months. if 4°
12 months. if 4°24 months. if 4°
ColorWhiteWhiteWhiteWhiteLight yellow
Average weight, g0,0409±0,00150,0416+0,00420,0411±0,00310,0399±0,00170,0408±0,0028
Solubility, minutes10±320±322±512±420±6
Quantitative content, Rel.%98,67±1,2794,99±1,7090,76±0,7499,83+1,4790,60±1,37
The maximum adsorption wavelength, nm272272272272272
The Rf-value0,67+0,020,68+0,030,67±0,010,68+0,02
The diameter of zones of inhibition of growth Bac.subtilis ATCC 6633, mm37,0±1,035,0±1,034,0±0,837,0±1,035,0±1,5

Table 5
The symptoms of inflammation

the mucous membrane of the nasal cavity
The first day after removal of tamponsThe third day after removal of tampons
The traditional method of prophylaxisUsing immobilized form CefazolinThe traditional method of prophylaxisUsing immobilized form Cefazolin
The exudationRichModerateModerateMissing or weak
surface temperature35,4±0,335,4±0,434,9±0,534,0±0,3

The remedy for the prevention of postoperative infectious complications in otolaryngology, containing Cefazolin, polymer and glycerol, wherein the anticipated enclosed in a polymeric matrix of sodium carboxymethylcellulose in the following ratio, wt.%:

Sodium carboxymethylcellulose2,0-4,0
Glycerin1.5 to 2.5
Purified waterRest


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