Compound for capsules

FIELD: medicine.

SUBSTANCE: invention concerns pharmaceutical technology and medicine and concerns a compound for capsules. An antimicrobial and interferon inducing agent includes a γ-modification of aminobenzenesulphamide as active substance. It also contains talc, calcium stearate and sucrose at a certain parity of components.

EFFECT: invention provides maximum therapeutic concentration of the preparation in blood.

3 ex

 

The invention relates to pharmaceutical technology and medicine, and more specifically to a composition for capsules.

When using capsules drug is protected from the external environment, the actions of the gastrointestinal tract excluded the possibility of penetration into the respiratory tract. Capsules are convenient in use, easily ingested. In addition, by adjusting the composition of the capsule's shell, it can extend the action of medicinal substances. In some cases, oral administration of certain drugs using capsules is the most preferred. Such substances include fine "dusty" substance, some of which are exposed to the medium already in the mouth, losing its therapeutic effect. Such substances include, in particular, the γ-modification of paraaminobenzoic.

It is known that the γ-modification of paraaminobenzoic has antimicrobial and interferon-inducing effect (patent RF №2033153).

However, this substance is a highly dispersed substance and belongs to the category of dusty, so use it orally is extremely difficult. In addition, it has a bitter taste, irritating effect on the mucous membrane of the gastrointestinal tract and with the passage of the gastrointestinal tract, starting with ro the new cavity, it is partially metabolized, turning in acetylated form, which does not has an antibacterial effect. Therefore, the number of active (deacetylating) form is reduced, resulting in not ensured maximum therapeutic concentration of drug in the blood.

One of the most convenient dosage forms γ-modification of paraaminobenzoic oral its application can serve capsules.

However, the γ-modification of paraaminobenzoic has a low flowability and bulk mass and, in addition, the powder is strongly electrified. All this requires the use of auxiliary substances for the introduction of this drug in capsules. Such auxiliary substances, as a rule, are substances that are functional are diluents, disintegrating agents, and slip agents, approved for medical use: lactose, saccharose, flour, talc, corn starch or potato, calcium phosphate one-deputizing etc.

The basis of the invention is to create such a composition for capsules, which would be convenient for encapsulation and would have a high bioavailability of the active substance γ-modification of paraaminobenzoic, and would preserve the physico-chemical and technological properties of the each of the selected excipients, providing flowability of the mass composition.

This problem is solved by the fact that features such a composition for capsules containing talc, calcium stearate, sucrose, which according to the invention also includes γ-modification of paraaminobenzoic, in the following ratio, wt.%:

γ-Modification of paraaminobenzoicof 9.30-19,95
Talc3,00
Calcium stearate1,00
Sucrose82,05-86,70

Depending on the desired dose of the medicinal substance can be obtained capsule mixture of different sizes of capsules. For this it is necessary to vary the number of components while preserving their chosen correlations between them.

In this song, sucrose, talc and calcium stearate eliminate the effect of the electrification of the γ-modification of paraaminobenzoic. Calcium stearate and talc reduce internal friction between the particles of the composition and external friction between the particles of the composition and surface equipment.

The main characteristic of the bioavailability of oral dosage forms is the rate of dissolution.

<> The rate of dissolution of γ-modification of paraaminobenzoic enclosed in capsules of the composition, determine the device "Rotary basket" by well-known methods (the State Pharmacopoeia of the USSR, eleventh edition (release 2), Westergeest, 1991, str). Environment dilution water is purified, the rotation speed of the basket is 80 rpm, volume environment dissolving 250 ml, temperature 37°C. the Content of γ-modification of paraaminobenzoic in solution determined by a spectrophotometric method for the optical density of the solution at a wavelength of 258 nm in a cell with a layer thickness of 10 mm

In the result, it was found that after 30 minutes, there is an almost complete transition of medicinal substances in the water (97,89%). After a 30-minute study is the decrease in optical density of the solution, indicating no accumulation amount of drug. Thus, the proposed structure provides high bioavailability of γ-modification of paraaminobenzoic.

Also determine the bioavailability of γ-modification of paraaminobenzoic and the proposed composition of the "in vivo".

The study of the biological availability of the medicinal substance in the capsule composition of the mixture was carried out in comparison with the substance of this matter on 4 rabbits sa is Zach breed chinchilla weight of 3,350-3,600 kg For 14 hours before the start of the experiment, animals were deprived of food. At the 1st stage of the study, the rabbits injected only γ-modification of paraaminobenzoic. At the 2nd stage after a 3-week break rabbits injected with the proposed structure. Pure substance and the composition is taken at the rate of 100 mg of the active substance (γ-modification of paraaminobenzoic) per 1 kg of body weight of the animal and before the introduction of the substance and the composition is pre-mixed with 10 ml of water to obtain a homogeneous suspension. The introduction is carried out in the esophagus using a syringe and probe. Then after 0.5, 1, 2, 4 and 6 hours after administration in each group determine the concentration of γ-modification of paraaminobenzoic in the blood. Blood samples (1 ml taken from the marginal ear vein of rabbits in a test tube with 15 ml of purified water, mix, and then add 4 ml of 15%trichloroacetic acid, and again thoroughly mixed and filtered through a paper filter.

The concentration of γ-modification of paraaminobenzoic in the blood is performed by the method of Prestige-Gavrilova.

In the result, it was found that the introduction of capsule mixture of γ-modification of paraaminobenzoic in the blood is higher than the introduction of one substance γ-modification of paraaminobenzoic, namely: after 0.5 hour after administration 1.69 times, 1 hour later - is 1.21 times.

The maximum concentration of γ-modification of paraaminobenzoic after the introduction of a pure substance is 15,16±1,64, and after the introduction of capsule mix - 18,31±1,04 g/ml, respectively.

As a result of the research it was revealed that the maximum concentration in the blood and the degree of bioavailability of γ-modification of paraaminobenzoic in the capsule composition of the mixture is considerably superior than when using a single substance.

The selected auxiliary ingredients and their quantities provide the necessary technological characteristics composition: flowability, bulk weight, bulk density while providing maximum bioavailability of the active substance. We offer capsule composition has the following technological features:

The flowability of the composition1.5-2.5 g/s
Bulk density0,8569 g/cm3
Bulk density0,5592 g/cm3.

Thus, the proposed capsule composition containing γ-modification of paraaminobenzoic, provides high technological characteristics of the drug substance, as well as what its biological availability. The latter even exceeds the value of the biological availability of pure γ-modification of paraaminobenzoic.

Capsule composition has a low flowability, not electrified, which makes it easy to measure with great precision.

The mass of the proposed composition completely fills the capsule volume, in particular of 0.50 cm3, thus eliminating the phenomenon of "flotation", resulting from the free air space capsules. This is quite an important factor, since otherwise there is a reduction in contact area of the medicinal substance in the gastrointestinal tract, which in turn slows down the dissolution rate of a drug and, consequently, reducing the bioavailability of the dosage form.

If you want to use composition with greater or lesser content of γ-modification of paraaminobenzoic accordingly, it is necessary to use capsules of larger or smaller size. For this purpose it is only necessary to change the number of selected components, saving them the specified value.

The method of obtaining the proposed composition for capsules containing γ-modification of paraaminobenzoic, simple in technological performance and is as follows.

Prepare gelatin mass. Its preparation, the tion carried out in the traditional way, namely, after the preliminary swelling of gelatin at room temperature it is heated to complete dissolution. Then, the resulting gelatinous mass is formed into a gelatinous membrane by immersion, vacuum and thermostatic.

Composition for capsules prepared by mixing γ-modification of paraaminobenzoic and sucrose in selected quantities in round bottom flask for 10-15 min, followed by "dusting" sliding agents (talc, calcium stearate), for example, in the mixer type "turbula".

After this hard gelatin capsules filled the received contents using the capsule machine and close the lid.

For a better understanding of the present invention are the following specific examples.

Example 1. Prepare capsule mixture of the following composition, g:

γ-Modification of paraaminobenzoic0,04
Talc0,0129
Calcium stearate0,0043
Sucrose0,3728

For this mix 0.04 g of γ-modification of paraaminobenzoic and 0,3728 g of sucrose in a round bottom flask for 10 minutes the mixture is podryvayut mixture 0,0129 g of talc and 0,0043 g of calcium stearate in "turbula".

The resulting composition has a flowability 2.5 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/ cm3.

Example 2. Prepare capsule mixture of the following composition, g:

γ-Modification of paraaminobenzoic0,005
Talc0,0129
Calcium stearate0,0043
Sucrose0,3628

The mixture is prepared as described in example 1.

The resulting composition has a flowability 2.0 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/ cm3.

Example 3. Prepare capsule mixture of the following composition, g:

γ-Modification of paraaminobenzoic0,06
Talc0,0129
Calcium stearate0,0043
Sucrose0,3528

The mixture is prepared as in example 1.

The resulting composition has a flowability of 1.5 g/s, bulk mass 0,8569 g/cm3, bulk density 0,5592 g/cm3.

Antimicrobial and online is hereinafterbe means on the basis of the γ-modification of paraaminobenzoic, characterized in that it is made in the form of capsules and additionally contains talc, calcium stearate and sucrose in the following ratio, wt.%:

γ-modification
paraaminobenzoic9,3-19,95
talc3,0
calcium stearate1,0
sucrose82,05 to 86.7



 

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