Pharmaceutical composition having spasmolytic and analgesic effect

 

(57) Abstract:

The invention relates to medicine, specifically to medicines antispasmodic and analgesic actions. The pharmaceutical composition contains components at the ratio of active components, wt.%: bromizoval 20-40, paracetamol 10-25, caffeine 5-10, phenobarbital 1-5, papaverine hydrochloride 2-10, ephedrine hydrochloride 0.5 to 2, codeine phosphate 0.5 to 5, atropine sulfate 0,02-0,05, pharmaceutically acceptable fillers - the rest. The proposed composition exhibits a wider range of analgesic activity and has high stability. 2 C.p. f-crystals, 3 tables.

The invention relates to medicine, specifically to medicines antispasmodic and analgesic actions.

Known means, analgesic and antipyretic action, containing as active ingredients acetylsalicylic acid, paracetamol, caffeine and pharmaceutically acceptable excipients (RF Patent 2101014). The specified tool does not possess antispasmodic effect and, in addition, the presence of acetylsalicylic acid may cause side effects.

Known means (cafein) containing mg, codeine phosphate is 0.01 mg (drugs of foreign firms in Russia. Handbook, Moscow, "Attraversare", 1993, page 321). This tool has antipyretic, analgesic and mild anti-inflammatory action. Its antispasmodic action is not specified. When using the tool can cause side effects associated with high concentrations of paracetamol and propifenazona.

Known composition (spasmodically), have antispasmodic and analgesic action, containing the following components per 1 tablet in the year:

The propifenazona - 0,15

Phenobarbital - 0.02

Papaverine hydrochloride - 0,03

Codeine phosphate - 0,015

Ephedrine chloride - 0,005

Atropine methobromide - 0,005

(Drugs of foreign firms in Russia. Handbook, Moscow, "Attraversare", 1993, page 511).

The specified composition at a sufficiently pronounced spasmolytic effect has a fairly moderate analgesic action, which narrows therapeutic possibilities of its application. The drug has a narrow range of analgesic activity, because it removes basically spasmodic pain of origin. In addition, the drug is not sufficiently stable, the fast pharmaceutical composition, described in the patent of the Russian Federation 2138252 (a 61 K 9/20).

This composition contains aspirin, caffeine, phenobarbital, codeine and pharmaceutically acceptable excipients. The main disadvantage of this tool is the presence in the composition of dipyrone (INN-metamizol), the use of which is prohibited in more than 50 countries around the world. Meanwhile, thanks to dipyrone specified drug has high analgesic effect.

The objective of the invention is to provide a pharmaceutical composition having a set of positive properties, advanced range of therapeutic applications and high analgesic and spasmolytic activity. This task is solved by the selection of ingredients in certain proportions.

Combination of drugs with antispasmodic, analgesic and sedative effect allows the use of the drug in spasm of the gastrointestinal tract, biliary and renal colic, pain in the bladder, spasms of migraines and pain of other origin.

The basis of the invention is the concept of creating a new composition, analgesic and antispasmodic effect with a wider, the pharmaceutical composition having spasmolytic and analgesic effect, containing caffeine, phenobarbital, codeine phosphate and pharmaceutically acceptable excipients, optionally contains bromizoval, paracetamol, papaverine hydrochloride, ephedrine hydrochloride and atropine sulfate in the following quantitative ratio of components,wt.%:

Bromizoval - 20-45

Paracetamol - 10-25

Caffeine - 5-10

Phenobarbital - 1-5

Papaverine hydrochloride - 2-5

Ephedrine hydrochloride and 0.5-2

Codeine phosphate is 0.5 - 5

Atropine sulfate - 0,02-0,05

Pharmaceutically acceptable excipients - Rest

Preferably the pharmaceutical composition comprises the following proportion of components, wt.%:

Bromizoval to 39.4

Paracetamol - 23,6

Caffeine - 8,0

Phenobarbital - 3,13

Papaverine hydrochloride - 4,7

Ephedrine hydrochloride - 0,78

Codeine phosphate - 1,26

Atropine sulfate 0,0394

Pharmaceutically acceptable excipients - Rest

Analgesic and spasmolytic effect of the composition according to the invention due to the presence of the corresponding components. However, the qualitative and quantitative composition is chosen such abrazado in turn will allow you to use the composition and spasmodic pain and pain of other origin. In addition, the exclusion of dipyrone in pharmaceutical compositions allows you to make the structure more secure (by reducing the likelihood of side effects) while increasing analgesic effect. In addition, the composition according to the invention showed a higher stability.

Based on the proposed structure can be obtained in various dosage forms, including tablets, capsules, etc. Tablets and capsules are prepared the traditional way with the addition of pharmaceutically acceptable fillers.

The greatest stability is manifested in the application as fillers of potato starch, talc medical, calcium stearate. The dosage form is formed with the use of ethyl alcohol and water.

The invention is illustrated by the following examples,

Example 1

An example of retrieving tablets

To obtain 10 kg of tablets weigh, kg:

Bromizoval - 3,94

Paracetamol - 2,36

Caffeine - 0,80

Phenobarbital - 0,313

Papaverine hydrochloride - 0,47

Ephedrine hydrochloride - 0,078

Codeine phosphate 0,126

Atropine sulfate 0,00394

Potato starch (moisture content 8-10%) of 1.46

Talc IU the 240

0.8 kg of caffeine pure crushed in a mortar and sieved through a nylon sieve 32. The output of crushed caffeine should be 0,79 kg

3.94 g of atropine sulfate is placed in the beaker, add 0.1 kg ethanol 95% and 0.4 kg of purified water. Stirred until complete dissolution of atropine sulfate.

All listed below raw materials intended for mixing, previously sieved through a metal sieve.

0,078 kg of ephedrine hydrochloride (if necessary pre-ground) and ~ 0.1 kg breezevale placed in a mortar, thoroughly mixed, add 0,126 kg of codeine phosphate, mix again and then in the following sequence type: 0,313 kg phenobarbital, 0,470 kg papaverine hydrochloride, 0,79 kg of crushed caffeine, 2.36 kg of paracetamol and the remaining number of breezevale. Each subsequent ingredient added after thorough mixing of the previous.

Then the resulting mixture of powders moisturize with a water-alcohol solution of atropine sulfate. Again stirred until a homogeneous hydrated mass.

The wet mass is passed through a granulator using a perforated drum with a hole diameter of 3 mm

The manufacture of pellets produced on a tablet press. The weight of the tablets is 10 kg.

The weight of one tablet of 0.65 G5%. The quantitative content of caffeine, paracetamol, brasavola, phenobarbital, codeine phosphate, papaverine hydrochloride per tablet was determined by HPLC, ephedrine hydrochloride - TLC. The content of active compounds in freshly prepared tablets is (in g per tablet):

Caffeine - 0,0462 - 0,0538

Paracetamol - 0,142 - 0,158

Bromizoval - 0,237 - to 0.263

Phenobarbital - 0,0185 - 0,0215

Codeine phosphate 0,0072 - 0,0088

Papaverine - 0,0277 - 0,0323

Ephedrine hydrochloride - 0,004 - 0,006

The prepared tablets were stored at room temperature in a dry place protected from light for 3 years (observation period).

After 3 years of storage tablets were checked for authenticity. Methods HPLC and TLC were determined by quantitative composition of active substances. Studies have shown that the number of active ingredients remained the same (differences in numbers within the errors of determination). Thus, it was shown that the stability of the proposed high - 3 years (observation period).

Example 2

Other examples of specific embodiments of the claimed Ipolzovanie in the ratios similar to example 1.

Analgesic effect of the proposed composition of the experimentally studied on standardized tests and compared with a strong analgesic for the patent of the Russian Federation 2138252. Analgesic effect was studied by tests "hot plate" (table 2) and model acetic cramps (table 3). The test results are presented respectively in tables 2 and 3. Analysis of the data presented in tables 2 and 3 suggests that the proposed composition possesses analgesic activity comparable with the activity of the potent analgesic wide spectrum of action.

The inventive composition has high analgesic and antispasmodic effect and increased stability and can find application in medicine.

1. Pharmaceutical composition having spasmolytic and analgesic effect, containing caffeine, phenobarbital, codeine phosphate and pharmaceutically acceptable excipients, characterized in that it further comprises bromizoval, paracetamol, papaverine hydrochloride, ephedrine hydrochloride and atropine sulfate in the following quantitative ratio of components, wt.%:

Bromizoval - 20-45

Paracetamol - 10-25

Caffeine - 5-10
,5-5

Atropine sulfate - 0,02-0,05

Pharmaceutically acceptable excipients - Rest

2. The pharmaceutical composition under item 1, characterized in that it contains the following proportion of components, wt.%:

Bromizoval to 39.4

Paracetamol - 23,6

Caffeine - 8,0

Phenobarbital - 3,13

Papaverine hydrochloride - 4,7

Ephedrine hydrochloride - 0,78

Codeine phosphate - 1,26

Atropine sulfate 0,0394

Pharmaceutically acceptable excipients - Rest

3. The pharmaceutical composition according to paragraphs.1 and 2, characterized in that as pharmaceutically acceptable excipients contains potato starch, talc medical and calcium Seurat sufficient for the formation of the dosage form.

 

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