The aerosol product and method thereof

 

(57) Abstract:

Application: aerosol products in various areas, as inhalers and medicines for nose, as external agents. The inventive aerosol suspension preparation contains, wt%: disperse the active substance (cromoglicate sodium or chloride, Bromhexine) 1 4 aerolef 0.5 to 1.5 and the propellant (chloro-, fluoro-hydrocarbon) - rest; optionally, it can contain up to 0.1 wt.% polyoxyethylenesorbitan monooleate or up to 0.05 wt. % sarbatorile to 0.1 wt.% aromatic substances. The method involves dissolution of the propellant 0.1 to 1.5 wt.% aerolate and subsequent mixing with a solution of 1 to 4 wt.% dispersion of the active substance. 2 S. and 3 C.p. f-crystals, 1 Il., table 4.

The invention relates to an aerosol of the drug in a state of suspension. In addition, the invention concerns a method of manufacturing such preparations used in various fields, primarily as inhalers and medicines for nose, as well as outdoor products.

The dispersion medium (propellant) when using aerosol products evaporates, and under its vapor surfactants and Vara/P> The closest technical solution is an aerosol product containing up to 15 wt. dispersion of the active substance (talc, metal compounds), suspended in a propellant, surface-active substances to 0.5 wt. (1). A method of obtaining a known aerosol formulation comprises mixing components (2). Known aerosol drug may not provide the improved properties of drugs to the body.

The aim of the invention is a significant improvement in the properties characterizing the stability of the aerosol product.

The aerosol product according to the invention contains, by weight. dispersed active substance 1-4; aerolef 0.5 to 1.5 and the propellant else; additionally it contains polyoxyethylenesorbitan, monooleate to 0.1 wt. or sorbitan trioleate to 0.05 wt. aromatic substances to 0.1 wt.

The method of obtaining aerosol formulation involves the dissolution of the propellant 0.1 to 1.5 wt. aerolate and subsequent mixing of the solution with 1-4 wt. dispersion of the active substance; in addition to the drug mix to 0.1 wt. polyoxyethylenesorbitan of monooleate or up to 0.05 and Mac. sorbitan of trioleate, up to 0.1 wt. aromatic substances, in the amount of dispersant (surfactant) tool is a component of the emulsion system, used in cosmetics and medicine.

Particularly preferred as active substances for drugs with anti-asthma effect can be cromoglicate sodium, which according to the invention are preferably used in nepodelajesh drying preparations in the form of a 9% aqueous solution.

As the active substance is preferably used also Bromhexine.

An important factor is the size of the particles used active substances. For aerosol products you want an active substance had a microcrystalline structure, that is, certain particle sizes.

The desired particle sizes change depending on the applied active substances. In the General case the active substance is used with the particle sizes that are desirable for a given area. Therefore: for inhalation drugs at least 90% of the cases, the particle size should be less than 10 μm (preferably 5 μm), for drugs in the nose at least 90% of the cases, the particle size should be less than 20 μm, while the size of the particles in preparations intended for external use.

The active substance with the correct portion sizes is>As a dispersing medium (propellant) must use non-toxic substances that evaporate easily at room temperature and atmospheric pressure. These include various alkane derivatives, in particular, various chlorine - fluorine alkanes. Can also be used a mixture of them and nitrogen.

You can use monitor-trichlorethane (working gas 11), debtor-dichloromethane (working gas 12), trifluorotrichloroethane (working gas 13), titrettor-dichloroethane (working gas 114). The quantity of the working gas in wt. in the range of 60-99 (preferably 85-98).

In the proposed medicines, in particular for outdoor applications and nose, can be used and other auxiliary substances and substances-media. These include, for example, a buffering agent to establish the appropriate pH-indicator (phosphate buffer), anti-oxidation means (ascorbic acid, bisulfite), preservatives (benzalkonium chloride) and/or water.

Blending components are produced alternately and so that in the liquid dispersion medium (optionally pre-cooled) was added first to dissolve the surfactant,th rotation of more than 1000 rpm, used in the manufacture of suspensions.

Cylinders should be fitted with a metering device, guaranteeing the issuance of the appropriate area.

Particularly preferred according to the results of their experiments were the preparations of the following composition, wt. Sodium chromoglycate 1-2 Aerolef 0.3 To 2 Sorbitan-trioleate 0-0,2 working gas (dis - dispersed environment) to 100.

As the working gas mixture, it is preferable to use a mixture of the following composition: working gas 11 55-75 working gas 12 10-25 working gas 114 10-25.

Below is a comparative analysis of the properties proposed in the invention of the drug with properties of the drug known composition.

The drawing shows a diagram of dialysator of Muhlemann, in vitro which was measured absorption of the biocatalyst from the drug proposed in the invention and compared drug where 1 trial Supplement; 2 glass tube; 3 receptor phase (pH 7.4, phosphate buffer); 4 tube from thermostat (not shown); 5 double-walled dialysis vessel; 6 pipe to thermostat (not shown); 7 membrane dialysator; 8 magnetic stirrer; 9 device magnetic stirrer (CAMAS PCT).

As the membrane used, the so-called the of 17-18 h pre-processed in phosphate buffer with pH-indicator, equal to 7.4. For measurements in the device was filled with 50 ml of buffer solution. The measuring system worked at 37aboutC and the stirrer at a rotational speed of 100 rpm Measurements were made on three "doses" of various crafted aerosol products formed on the membrane. (VI dose equal to the number of substances released from shook cylinder by clicking once its metering valve, which is approximately 1 mg of sodium chromoglycate). Before raspryskivanii cylinder with an analytical precision was suspended after raspryskivanii he was again weighed, therefore, by accurately defined amount of the active substance, trapped on the membrane. From the receptor phase of the system at certain time intervals were sampled, and the number of disodium-chromoglycate, re-dissolved in the donor phase was measured spektrometricheskim way.

P R I m e R 1. The drug composition, wt.

Disodium-chromoglycate (water content 9%) 1.7 Aerolef 1,3 Monitorthread 70,7 Debtor-dichloromethane 13,15 Tetraphenylborate 13,15.

Monitor-trichlormethane cooled to 10 1aboutC. it dissolves aerolef, then in a mixture of parts and at a constant peremeshivaniya stirred 45 min (when the rotational speed of the stirrer 2800 rpm). Prepared suspension with continuous stirring on the stirrer speed of about 1400 rpm and the cooling is pumped in aerosol containers. The cylinders are closed by appropriate metering valves. Then through the valves of the cylinders in them under pressure pumped two other gas components (in the form of a mixture or separately).

P R I m m e R 2. The drug composition, wt. Disodium-chromoglycate (water content 9% ) 3.3 Aerolef 0.6 Policitian-SOR - Binet-monooleate 0.1 Monitor-trichlormethane 67,0 Dipertahankan 14,5 Tetraphenylmethane 14,5.

Monitor-trichlormethane cooled to 5 1aboutC. it dissolves aerolef, and then polyoxyethylene-sorbent-monooleate. To this solution is added to cooled to -45aboutWith a mixture of difenilamina and tetrafluorodichloroethane. At this temperature parts with constant stirring (speed stirrer 2500 rpm) the mixture is added to disperse the active ingredient disodium-chromoglycate. Then the suspension under continuous stirring and cooling is pumped in aerosol containers, which are closed with respective metering valves.

P R I m e R 3. The composition shown in table. 1.

Made serve sorbent-trioleate.

P R I m e R 4. The drug composition, wt. Chloride, Bromhexine 2.04 Aerolef 0,68 Sorbent-trioleate 0.17 Trifter-trichloroethane 35,74 Debtor-dichloromethane, 30,65 Titrator-dichloroethane 30,65 Aromatic substances 0,068.

Trifter-trichloroethane is cooled to 10 1aboutC. it dissolves aerolef, and then sorbent-trillat. Then in a mixture of parts with continuous stirring (speed stirrer 1500 rpm) is added Bromhexine, and then the whole system for 50 min mix (when the rotational speed of the stirrer 2500 rpm). Prepared suspension with continuous stirring (speed mixer 1400 rpm) and cooling is pumped in aerosol containers. The cylinders are closed by appropriate metering valves. Then into the cylinders through the valve under pressure introduced two other gas components (in the form of a mixture or separately).

P R I m e R 5. The drug composition, wt. Sodium-cromoglycate 1.70 Aerolef 0,66 working gas 11 69,74 working gas accounted for 14.45 12 working gas 114 accounted for 14.45.

The drug is manufactured in the same manner as in example 1.

Drugs I. IV.

Drugs (II-IV) in accordance with the conditions of equipment and sample preparation (I) produce the oleate dissolving the appropriate amount of sorbent-trioleate.

The data are given in table. 2.

In table. 3 shows the change in concentration diffentiating active substances depending on the time.

From table. 2 shows that the active ingredient of preparations containing aerolef (example 1, 3A and 5), rastreskivaetsja much more effective than the active substance of the compared drugs (examples I-IV).

Table 4 summarizes the characteristic physical properties of various mixtures (the investigated mixtures are numbered according to table. 3). Were investigated parameters indicated in the table as follows:

residual sediment (in.) SV,

the ability to redispersion (number needed shaking of the container, one shake of the container means its turning 180about) RD,

the nature of the sediment HR,

adhering to the aerosol container material (in mg) VHM,

adhering to the valve of the aerosol container material (in mg) VH

the average particle size, the distribution of values of the granules was measured by the instrument NAIS CR 420).

According to these data the aerosol product obtained by the proposed method has superior physical properties that determine their consumer properties.

1. Aero is, he further comprises aerolef in the following ratio, wt.

Dispersed active substance 1 4

Aerolef 0,5 1,5

Propellant Else

2. The drug under item 1, characterized in that it further comprises politicalisation monooleate to 0.1 wt. or sorbitan trioleate to 0.05 wt. aromatic substances to 0.1 wt.

3. The method of obtaining aerosol formulation, comprising mixing the dispersed active substance and propellant, characterized in that before the introduction of 1-4 wt. disperse active ingredients in the propellant is dissolved 0.1 to 1.5 wt. aerolate.

4. The method according to p. 3, characterized in that the drug is admixed to 0.1 wt. polyoxyethylenesorbitan of monooleate or up to 0.05 wt. sorbitan of trioleate until 01 wt. aromatic substances.

5. The method according to p. 3, characterized in that the active substance applied cromoglicate sodium or chloride, Bromhexine.

 

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