Injection dissolvent of prolonged action

FIELD: medicine.

SUBSTANCE: invention concerns medicine area, namely to pharmacy and concerns a composition of ingredients of a dissolvent for reception of a medicinal injection solution. The offered agent contains water for injections, low-molecular polyethylene, T-2 emulgent, microcrystallic gelatin, olive oil at a certain parity of components. The offered agent provides reliable fixation of a medical product in tissues at an injection way of introduction, raises its pharmaceutical availability at the expense of incoming auxiliary substances, possesses prolonged action, is convenient and hygienic in use.

EFFECT: provision of reliable fixation of a medical product which possesses prolonged action, is convenient and hygienic in use, in tissues at an injection way of introduction, rising of its pharmaceutical availability at the expense of entering incoming substances.

4 ex

 

The present invention relates to medicine, namely to the pharmacy, and relates to the composition of ingredients of the solvent to obtain the injection solution, it can be used for the preparation of liquid dosage forms.

It is known the use of water for injection as solvent included in the composition of many injectable drugs / Requirements for "Water for injection" Russian (FS 42-2620-97) and European (EP IV 2002) Pharmacopoeia./.

This injection solvent is the closest analogue of the present invention to the technical essence and the achieved result.

Object of the invention is the expansion of the means to obtain drugs in the form of solution for injection prolonged action.

The technical result - the creation of new injection solvent domestic production for the preparation of dosage forms in the form of an injection solution with efficiency in injecting routes of administration, with a uniform distribution in the tissues, severe and prolonged action of the active substance due to the composition of the injection solvent.

This technical result is achieved due to the fact that the solvent to obtain the drug injection solution containing the th water for injection, further comprises a low molecular weight polyethylene, emulsifier T-2, gelatin, microcrystalline, olive oil in the following ratio, wt.%:

Water for injection1,841
Low-molecular-weight polyethylene67,114
Emulsifier T-216,778
Gelatin, microcrystalline6,717
Olive oil100

All components included in the composition of the funds authorized for medical use.

Low-molecular-weight polyethylene (NMPA) molecular weight 1500-5000 (TU 6-05-1837-82) is a viscous waxy, oily and sticky to the touch a lot in a thick layer of greyish odourless. NMPA is a mixture of polymer molecules of different lengths, which is characterized by the supramolecular structure consisting of alternating amorphous and crystalline regions having a net structure, contributes to the prolongation of the active substance in the composition.

Gelatin medical microcrystalline (GF X) as an auxiliary substance - limited swelling high the molecular connection, affecting the pharmaceutical availability of the active substance.

Olive oil (GF X) improves the structure of the composition, lowers the viscosity, fluidity.

Emulsifier T-2 (TU 18-17-05-76) gives the mass a sufficient elasticity, used as a stabilizer, plasticizer and emulsifier.

The proposed composition of the injection of the solvent provides the convenience and hygiene applications, the storage stability. As a result of experimental studies, it was found that the composition of the solvent for injection provides reliable fixation of the drug in the tissue at the injection route of administration using a syringe with a diameter of needle 1.5 mm, helps dissolve in the claimed composition of the existing medicinal substances, has a prolonged action and increases their pharmaceutical availability due to the incoming auxiliary substances.

Example 1. The composition 100,0 injection solvent: water for injection - 1,841; NMPA - 67,114; emulsifier T-2 - 16,778; gelatin microcrystalline - 6,717; olive oil - from 6.0 to 7,550.

Get injectable solution as follows.

In a water bath melt the emulsifier T-2 at 70C in varicellae Cup. The alloy add 5% water for injection. The aqueous phase emuleret. To the resulting mixture is added the calculated amount of pre-melted, NMPA. The mixture was thoroughly stirred. To the resulting mixture add shredded gelatin microcrystalline and olive oil. The resulting composition is thoroughly mixed, filtered, filled into sterile vials under tested and sterilized at 100C for 30 minutes.

Received the injection solvent is a homogeneous viscous mass of white with a yellowish tinge, with a density of 1.3 g/cm3pH to 6.0, has a viscous consistency. Due to the consistency and physico-chemical properties of the composition of the injection solvent is firmly held in the tissues while injecting, at the expense of those excipients has prolonged action of active substances introduced into the inventive composition, as well as convenient and hygienic to use, because the proposed composition of the ingredients.

Example 2. Made of injection solvent prolonged action in the same way. As the active substance introduced 5-fluorouracil - 5% aqueous solution of 5-fluorouracil (5-fu was dissolved in water for injection). The composition 100,0 funds for cancer treatment in the form of solution for injection: 5-fluorouracil - 0,087; water for injection - 1,754; NMPA - 67,114; emulsifier T-2 - 16,778; gelatin microcrystalline - 6,717; olive oil - 7,550. The resulting tool, etc is made using injection solvent, is a homogeneous viscous mass of white with a yellowish tinge, with a density of 1.3 g/cm3pH to 6.0, has a viscous consistency. Due to the consistency and physico-chemical properties of the composition tool is firmly held in the tissues while injecting, at the expense of those excipients has prolonged action of active substances introduced into the inventive composition, as well as convenient and hygienic to use, because the proposed composition of the ingredients. Received the drug is securely held in the tissues, due to the composition of the injection of the solvent provides a prolonged effect of the cytostatic agent.

Example 3. Made of injection solvent prolonged action in the same way. As the active substance entered monomitsin from the calculation of 0.25 or 0.5, which is dissolved in water for injection. The resulting tool, made using injection solvent is a homogeneous viscous mass of white with a yellowish tinge, with a density of 1.3 g/cm3pH to 6.0, has a viscous consistency. Due to the consistency and physico-chemical properties of the composition tool is firmly held in the tissues while injecting, at the expense of those excipients has prolong the automatic action of active substances, entered in the inventive composition, as well as convenient and hygienic to use, because the proposed composition of the ingredients. Received the drug is securely held in the tissues, due to the composition of the injection of the solvent provides a prolonged effect of the antibiotic.

Example 4. Made of injection solvent prolonged action in the same way. As the active substance entered kanamycin sulfate for parenteral use of the calculation of 0.25 or 0.5, which is dissolved in water for injection. The resulting tool, made using injection solvent is a homogeneous viscous mass of white with a yellowish tinge, with a density of 1.3 g/cm3pH 6,0 has a viscous consistency. Due to the consistency and physico-chemical properties of the composition tool is firmly held in the tissues while injecting, at the expense of those excipients has prolonged action of active substances introduced into the inventive composition, as well as convenient and hygienic to use, because the proposed composition of the ingredients. Received the drug is securely held in the tissues, due to the composition of the injection of the solvent provides a prolonged effect Antibes is of Otik.

The solvent to obtain the drug injection solution containing water for injection, characterized in that it further comprises a low molecular weight polyethylene, emulsifier T-2, gelatin, microcrystalline, olive oil in the following ratio, wt.%:

Water for injection1,841
Low-molecular-weight polyethylene67,114
Emulsifier T-216,778
Gelatin, microcrystalline6,717
Olive oil100



 

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