Ocular drug and method thereof

 

(57) Abstract:

The invention relates to the field of medicine. Ocular drug consists of Riboflavin, ascorbic acid, boric acid, collagen, nipagina, water svezheprokipyachennoy purified. Sterile ophthalmic solution means is subjected to lyophilization. The method is as follows: dissolve in water svezheprokipyachennoy purified by heating Riboflavin, add to a hot solution of boric acid, nipagin; stirred and cooled, add ascorbic acid, stirred and dissolved, and then, on the surface of the solution add collagen, leave to dissolve, mix and bring the volume svezheprokipyachennoy purified water, and then lyophilizer. The invention provides a prolonged drug action and long shelf-life. 2 S. p. f-crystals, 1 table.

The invention relates to medicine, namely to ophthalmology products used as eye product containing water-soluble vitamins in combination with drugs and auxiliary substances involved in carbohydrate, protein and fat metabolism and maintain normal visual function, the individual recipes /Ministry of health of the Russian Federation 214 from 16.07.97, "Control the quality of drugs manufactured in pharmacies", Markov M. D. "Drug". Kharkiv "Torgsin", 1998. 2. - 590 C./.

The disadvantage of these drops is the following: shelf life is 2 days when stored at a temperature of 25oC, 7 days at 3-5oWith; the drops do not enter excipients that ensure their sterility and stability for a longer period than 2-7 days; drops used 2-3 times a day, i.e. not provided with prolonged action of medicinal substances by increasing the viscosity of the solution, it was found that viscous solutions less easy on the eye, allow you to better withstand instillation, provide prolonged contact of medicinal substances from conjunctiva /Novikova L. C. Theoretical foundations and development of a stable ocular drug plant production; abstract. dis....Prof. formats. Sciences. - M., 1994. - 52 S. , Centralis A. A. Ocular dosage forms in pharmacy. - M.: Medicine, 1988. - 255 S./.

Known tools do not provide prolonged action of medicinal substances, have a limited shelf life, i.e., to produce in an industrial environment and in mass quantity cannot.

This objective is achieved in that the proposed facility in addition to drugs /Riboflavin, ascorbic acid, boric acid/ contains excipients /nipagin, collagen/ in the following ratio of components /wt.%/:

Riboflavin - 0,01 - 0,02

Ascorbic acid is 0.1 to 0.6

Boric acid - 1,0 - 3,0

Collagen - 0,7 - 1,0

Nipagin - 0,01 - 0,06

Water svezheprokipyachennoy purified - 98,18 - 95,32

The tool with the purpose of prolonged action and increase its stability in solution additionally contains collagen in the amount of 0.7-1.0%; nipagin 0,01-0,06%; and dried by sublimation /lyophilization/.

1. Feature lenses

Collagen - biopolymer is the main protein of connective tissue, white fibrous powder, able to swell and dissolve in water. Molecular weight average of 300,000 /Ivanov, L. A., Bychenkov I. A., Kondratyev ie Collagen in the technology of medicinal forms. M.: Medicine, 1984. - 111 S./ In ocular drug lyophilized collagen was introduced to prolong therapeutic effect of drugs /Riboflavin, ascorbic acid, boric acid/. The optimal concentration is of medicinal substances /Polonskaya M. C., Novikov HP, Shormanov Century as the Study of the release of Riboflavin eye drops based on collagen. In the book: Actual problems of medicine and pharmacy/. Materials 64th final scientific conference. - Kursk, 1999. - S. 335-337/.

Collagen as an auxiliary substance is characterized by a number of valuable properties. Unlike synthetic Navy collagen completely resorbed and utilized by the body. He has the ability to stimulate the regeneration of damaged tissue has a higher sorption capacity, weak antigenicity, non-toxic, has no carcinogenic properties /Nikolaev A. C., Schechter A. B. Collagen and regeneration /Main mechanisms of therapeutic action of drugs of collagen/. - In the book: Experimental and clinical aspects of biological polymers in medicine. M., 1981. -S. 11-13/.

Nipagin - methyl ester p-oksibenzoynoy acid, a white crystalline powder, slightly soluble in water, soluble in chloroform, hydrochloric acid /FS 42-1460-80/. Widely used as a preservative in the preparation of injection solutions, medicines, eye drops, emulsions /Yevtushenko Acting , Pakhomov, I. C. control Methods preservatives used in the manufacture of organo is the first tool nipagin introduced as a preservative, contributing to the preservation of the sterility of money, and after its dissolution and preparation of the droplets during their use. Optimal concentrations of nipagin in which it exerts its antimicrobial activity, are 0.01 to 0.05 wt.% /Khokhlova L. N. Study of antimicrobial activity of preservatives in heterogeneous dosage forms /suspensions, emulsions/ and solution of polyethylene oxide: author. dis.... Kida. formats. Sciences. -Kharkov, 1985. - 23 S./.

2. Comparative analysis of the prototype shows the presence of novelty, because there are two additional components, and a significant difference is the method of obtaining, because of the sterile solution is subjected to lyophilization.

A preparation containing vitamins in combination with drugs and auxiliary substances involved in carbohydrate, protein and fat metabolism and maintain normal visual function of the eye, is prepared as follows in aseptic conditions: 1. Riboflavin is dissolved in water svezheprokipyachennoy purified by heating in a hot solution add boric acid, mix until dissolved; add nipagin; in the cooled solution is diluted acid asmodai svezheprokipyachennoy volume was adjusted to the calculated. 3. The resulting solution was poured into vials and freeze-dried method.

The invention is evidenced by the following specific examples, given in the table.

When conducting experimental studies prepared eye drops according to the formulations shown in the table. Held biopharmaceutical research and studied their biopharmaceutical properties. Experiments were performed on adult rabbits, studied local irritating action /tolerance/ eye drops on the ocular tissue, the General condition of the animal, effect on the function of blood, acute toxicity, pharmacodynamics of drugs into the eye tissues, specific and General pharmacological activity.

We studied experimental and control groups of 6 rabbits. The first experimental group rabbits were administered the investigational eye drops 3 times a day 2 drops in 2 months. The other experimental group rabbits were administered the investigational eye drops 2 times a day. Experimental studies conducted by well-known methods, showed that the concentration of active substances in the tissues of the eye is maintained at levels that ensure therapeutic efficacy of drugs.

And the non-therapeutic effectiveness of the proposed tools.

Example 1 method of preparation: in aseptic conditions, 0.5 g of Riboflavin was dissolved by heating in 1 l of water svezheprokipyachennoy cleaned in hot solution was placed 50.0 g of boric acid, was stirred to dissolve; to the resulting solution was sequentially added nipagin 2.5 g, was stirred until dissolved and leave to cool. To the cooled solution was dissolved ascorbic acid 15,0. On the surface of the solution was placed in an even layer of collagen and left to dissolve. The resulting solution was stirred and the water purified svezheprokipyachennoy brought the volume up to 1.5 l

The prepared solution was filtered on a prepared sterile filter Pilot type Seitz pressure of 0.42-0,53105PA sterile air. The sterile solution was poured into 1.5 ml per 1,000 vials of 5 ml

The vial containing the solution was placed in the freezer and froze 5 hours, conducted training for 5 hours and transferred into the chamber of the freeze dryer TG 5.2 /DDR/. The chamber is hermetically closed and were drying for 32-40 hours at a temperature of 255-268,0 K, i.e. close to the eutectic. At the end of the drying temperature did not exceed 296,0, working pressure of 13 PA. Drying was carried out before the wound humidity 4-5%, easily dissolved in water.

Thus, the resulting tool in comparison with analogues and the prototype has a shelf life of three years, has a prolonged effect by the addition of dry collagen, which leads to a reduction in the number of instillations up to 2 times per day, maintains sterility during use in a month, as it contains a preservative - nipagin, easily prepared yourself at home by dissolving the dry content of the vial in the water purified svezheprokipyachennoy. Convenient and efficient packaging - bottle cap-dropper excludes use the eye dropper that patients do not always wash thoroughly, which can lead to eye infections. Expanding range of domestic ophthalmic drugs.

1. Ocular drug consisting of Riboflavin, ascorbic acid, boric acid, characterized in that it further introduces the collagen in the following ratio, wt. %:

Riboflavin - 0,01-0,02

Ascorbic acid is 0.1 to 0.6

Boric acid - 1,0-3,0

Collagen - 0,7-1,0

Nipagina - 0,01-0,06

Water svezheprokipyachennoy purified - 98,18-95,32

2. The method of obtaining ocular drug under item 1, otlichayuschij Riboflavin 0.01 to 0.02, to the hot solution add boric acid 1.0 to 3.0, and dissolve, then nipagin 0,01-0,06, stirred and cooled, add ascorbic acid, stirred and dissolved, and then, on the surface of the solution add collagen 0,7-1,0, leave for complete dissolution, and then mixed and the volume was adjusted to 1.5 l water svezheprokipyachennoy purified, then lyophilizer.

 

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