RU2503445C1 - Pharmaceutical composition in form of skin protection paste - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical composition in the form of a skin protection paste. The composition contains a film-forming agent representing poly(butyl methacrylate-co-methyl methacrylate), hydrocolloid, a filling agent, a softening agent and an alcoholic diluent in the certain proportions.

EFFECT: pharmaceutical composition has a prolonged shelf life and is able to ensure a uniform skin coverage which is characterised by the balanced characteristics of durability and flexibility.

3 cl, 2 tbl, 5 ex

Description

FIELD OF THE INVENTION

The invention relates to medical supplies, namely, to compositions in the form of a paste for treating human skin in order to protect it from physiological and pathological secretions, such as discharge from a colostomy or ileostomy and exudates from wounds and fistulas.

State of the art

As the closest analogue of the present invention, the authors consider the composition in the form of a paste for medical purposes, disclosed in patent RU 2155029 (publ. 27.08.2000). The specified composition includes a film former, hydrocolloid, plasticizers and alcohol, and is characterized in that the film former contains a copolymer of butyl methacrylate with methacrylic acid and, in addition, a filler is introduced into its composition. The composition has the following quantitative composition (in wt.%):

film former 15.2-30.2 filler 11.2-22.8 hydrocolloid 14.9-27.3 plasticizers 12.6-25.2 ethanol 12.7-25.2

In preferred embodiments of the closest analogue, the film-forming agent is a copolymer of butyl methacrylate with methacrylic acid, sold under the brand name BMK-5, kaolin is used as a filler, sodium carboxymethyl cellulose, sodium alginate or a mixture thereof is added to the composition as a hydrocolloid, and it contains a mixture as plasticizers castor oil and dioctyl phthalate.

In other preferred embodiments, the paste composition further comprises a superabsorbent — a rare crosslinked polyacrylic acid, a bismuth salt, or a sticky agent — Harpius ester, as well as polyethylene glycol to improve wettability.

The main disadvantage of the paste is its tendency to sedimentation due to the use of the film former BMK-5. The specified copolymer does not differ in the stability of characteristics over time, which leads to sedimentation in the tubes during storage, makes it difficult to squeeze out a portion of the paste for application to the skin until the tube outlet is blocked. This reduces the warranty period of storage of the drug, creates inconvenience for users and necessitates a more frequent purchase of the drug, leading to unreasonable costs. In addition, the resulting coating on the skin is heterogeneous and has an unreasonably high elasticity, as a result of which microcracks often occur, leading to its detachment.

Thus, there is a need to expand the arsenal of funds devoid of this drawback.

Disclosure of invention

As a result of extensive research, the authors of the present invention concluded that it is unpromising to improve the paste containing the BMK-5 film former, and found that the disadvantages of the closest analogue can be overcome by creating a pharmaceutical composition in the form of a paste to protect the skin, including a film former, a hydrocolloid, a filler, a plasticizer and an alcohol diluent which, as a film former, contains a copolymer of butyl methacrylate with methyl methacrylate in the following component content (In wt.%):

film former 18-22 filler 19-21 hydrocolloid 22-30 plasticizer 7-10 alcohol diluent 24-27

provided that the content of all components is 100 wt.%.

Suitable fillers for the purposes of the present invention are kaolin or bentonite, the hydrocolloid is sodium carboxymethyl cellulose, sodium alginate or a mixture thereof, castor oil is a plasticizer, and ethyl or isopropyl alcohol is the alcohol diluent.

Preferably, the pharmaceutical composition contains kaolin as an excipient and ethyl alcohol as an alcohol solvent.

Also preferably, the pharmaceutical composition contains bentonite as an excipient, and contains isopropyl alcohol as an alcohol solvent.

One technical result of the invention is to increase the shelf life of the paste before use due to the almost complete exclusion of sedimentation. The pastes stored in the storage batch satisfy all the requirements for them even after 4 years from the date of their production.

Another technical result is to obtain a uniform coating thickness on the patient’s skin, characterized by balanced properties of strength and elasticity by reducing viscosity and increasing the uniformity of the finished product.

Most preferably, the technical results of the present invention can be achieved using a hydrocolloid in which the weight ratio of sodium carboxymethyl cellulose to sodium alginate is from 4.5: 1 to 5: 1.

The implementation of the invention

Further, the present invention will be illustrated by examples of preferred implementation, confirming the achievement of the technical result and characterizing its advantages compared with the closest analogue.

Examples 1-4. Cooking pasta

Dry components are loaded into the mixer at room temperature in the amounts indicated in Table 1: a copolymer of butyl methacrylate with methyl methacrylate, sodium carboxymethyl cellulose (NaKMC), sodium alginate and kaolin or bentonite, mixed for 30-45 minutes until a homogeneous mixture is obtained.

In a separate container equipped with a frame stirrer, a mixture of liquid components is prepared, taken in the amounts indicated in table 1: castor oil and ethyl or isopropyl alcohol.

The mixture of liquid components is added to the mixer with stirring, the mixer is sealed and stirring is continued for 20-30 minutes. The finished paste is packed in tubes of 30.0 g. A part of the product is put into storage to determine the expiration date.

Table 1 Composition The content of components (wt.%): Example 1 Example 2 Example 3 Example 4 Butyl methacrylate copolymer with methyl methacrylate twenty 19 22 eighteen Hydrocolloid: NaKMTS twenty twenty eighteen 25 Sodium Alginate four four four 5 Kaolin (white clay) 21 0 twenty 19 Bentoite 0 21 0 0 Castor oil 8 7 10 9 Ethanol 27 0 26 24 Isopropyl alcohol 0 27 0 0

Example 5. Evaluation of the properties of the paste

The adhesive ability of the material was evaluated by volunteers as follows: the paste was squeezed onto a sticky bandage or adhesive plaster, smeared to obtain a strip 10x100 mm in size, 1-1.5 mm thick. The prepared sample was dried, then glued onto the skin of the volunteer's hands, kept for 1 hour, and then peeled off using a tensile testing machine. The adhesion ability of the paste was determined by the magnitude of the peeling force.

The water absorption of the paste was evaluated by the gravimetric method, determining the amount of water absorbed by the paste sample upon contact with water for 6 hours at 30 ° C.

The fluidity of the paste was evaluated on a Heppler consistometer. The technique is based on determining the diameter of the spot formed by 2 ml of paste when exposed to a load of 35 N for 5 minutes.

The ease of removing paste from the skin was evaluated by volunteers. The assessment was carried out according to a five-point system: 5 points - easy and complete removal, 4 points - easy removal, there are minor residues, 3 points - removal is difficult or there are significant residues, 2 points - removal is difficult or most of the film remains, 1 point - application is required solvents to remove.

Sedimentation of paste in tubes was evaluated qualitatively on a five-point scale. The control was carried out by squeezing the paste from the tube after 3-30 days. The presence of solid sediment in the lower part of the tube or blockage of the outlet was recorded.

Samples stored in storage have been tested positively for 4 years.

The results are presented in table 2.

table 2 Property Example one 2 3 four "P" Adhesive ability, N / m 130 150 180 160 100-180 Water absorption,% 180 160 200 170 150-200 Fluidity, mm fifty 55 45 60 42-55 Ease of removal from the skin, points four four 3 5 5-2 Sedimentation, points 5 four 5 5 2-1 "P" is an invention in accordance with patent RU 2155029.

The data obtained indicate greater stability of consumer properties of pastes in accordance with the present invention, which is its advantage over the known technical solution. The data also confirm the achievement of the technical result, which consists in obtaining a paste with a long shelf life, capable of giving a uniform coating on the patient’s skin, which is characterized by balanced properties of strength and elasticity, as measured by the adhesive ability and ease of removal from the skin.

Claims (3)

1. A pharmaceutical composition in the form of a paste for skin protection, including a film former, a hydrocolloid, a filler, a plasticizer and an alcohol diluent, characterized in that the film contains a butyl methacrylate / methyl methacrylate copolymer in the following components, wt.%:
film former 18-22 filler 19-21 hydrocolloid 22-30 plasticizer 7-10 alcohol diluent 24-27,
provided that the content of all components is 100 wt.%. 2. The pharmaceutical composition according to claim 1, characterized in that it contains kaolin as a filler, and contains ethyl alcohol as an alcohol solvent. 3. The pharmaceutical composition according to claim 1, characterized in that it contains bentonite as an excipient, and contains isopropyl alcohol as an alcohol solvent.