Combination analgesics

 

(57) Abstract:

The invention relates to pharmacy. The proposed new oral analgesic agent with action for 2 min to 12 h, containing a single dosage form non-steroidal anti-inflammatory agent (for example, a derivative of propionic acid or derivative of salicylic acid) and locally acting analgesic (in particular, benzocaine or lidocaine), and locally acting analgesic is released first. The invention allows to combine quick and lasting analgesic action and expands the Arsenal of analgesics. 1 C.p. f-crystals.

The present invention relates to the use of oral compositions containing a combination of at least one locally acting analgesic with a rapid action and at least one somatically acting analgesic with a long action.

Currently known locally acting analgesic with a rapid onset of action (fast-acting analgesics), which can be used, for example, in the form of sprays or sucking tablets. Such local anesthetic drugs exert their effects less to subsequent therapy that means reducing the guarantees and facilities for patients.

As a particularly interesting locally acting analgesic should be called, for example, benzocaine. This drug prevents the formation and conduction of excitation in nerves by blocking sodium flow.

Somatically acting analgesics, such as NSAIDs, in particular acetylsalicylic acid, are another type of drug used to relieve the pain. When using this reduced analgesic sensitivity nociception, and easing the pain should be attributed to inhibition of prostaglandin synthesis. When using most of these somatically acting analgesics maximum effect is reached only after about 1-2 hours.

The present invention is to provide orally applied the drug to meet the needs for which it is necessary for a long time, which is simple and reliable way links fast analgesic effect with long-lasting effects.

As a locally acting analgesics (item A) can be used by all active substances, which are beginning to have a significant effect in the interval of 30 seconds.

Locally acting analgesics (in combination item A) should be used in quantities of from 0.5 to 100 mg, preferably from 1 to 60 mg, and particularly preferably from 2 to 30 mg per single dosage form.

The claimed combination as an element And can contain one or more locally anesthetic components, for example 1, 2 or 3. Of particular interest are combinations with only one connection element A.

Active ingredients as As well known. As particularly suitable should, for example, to call afrophobia local anasthesiologie tools, such as benzocaine, amatokin, amylocaine, butagain, butokukan, butylaminoethyl, chloroprocaine, chloroquin, cyclomethycaine, isobutane, marilyin, oxybuprocaine, procaine, propipocaine, proxymetacaine, Tremain and others. It also should be numbered religovedenie local anesthetics, such as lidocaine, bupivacaine, butanilicaine, kartikay, cinchocaine, Libyan, etidocaine, mepivacaine, oxethazaine, prilocaine, ropivacaine, ethyl-n-piperidineacetic-aminobenzoate, Tolochin, trimekain, vadakan and others.

Used other l the words.

Somatically acting analgesics, is used as the element, also known for a long time. As the preferred should be called non-steroidal anti-inflammatory drugs (NSAIDs), such as a derivative of phenylacetic acid, such as aceclofenac, alclofenac, bromfenac, diclofenac, fenclofenac and other derivatives akriluksusnoy acid, such as acemetacin, amfenac-sodium, bendazac, glucometry, oxiplatin and other derivatives of n-aminophenol, such as acetanilide and other propionic acid derivatives, such as alminoprofen, ibuprofen, Ketoprofen, flurbiprofen, naproxen, oxaprozin, salicylic acid derivatives, such as acetylsalicylic acid (ASA), aluminum-ASA and other salts, diflunisal, Etisalat, posposil, salol, salsalate, saleclomid and others, pyrazolone derivatives, such as amidopyrine, dipiro and other derivatives of oxicam, such as droxicam, isoxicam, piroxicam and other derivative of phenylbutazone, such as azapropazone, butadion, Caltex, oxyphenbutazone and other derivatives pyranoindoleacetic acid, such as etodolac and other derivatives of Anthranilic acid, such as glutenin, sodium meclofenamate, mefenamicacid, mornel the other NSAIDs, such as aniolek, benzoperylene, benzydamine hydrochloride, sodium-butibufen, chlorination, cinmetacin, clonixin, chloracetate, divinename, diprovan, ethenzamide, famprofazone, flupirtine, ibuproxam, indoprofen, Sambazon, meloxicam, medicinova acid, mattenson, rivenson, niflumova acid, nimesulide, pyrazolo, pranoprofen, proquazone, protazanova acid, ramification and others.

Somatically acting analgesics element In accordance with the present invention are used in quantities of from 5 to 1500 mg, preferably from 8 to 1000 mg, particularly preferably from 10 to 800 mg at the final dosage form.

As element And preferably use high-speed local analgesics, the optimal duration of which ranges from 0.5 to 120 minutes, preferably from 2 to 60 minutes, particularly preferably from 5 to 30 minutes. As element preferably used In somatically acting analgesics, significant action which occurs within 15 minutes and lasts up to 24 hours, preferably such action which occurs within 20 minutes and lasts up to 12 hours, especially up to 8 hours.

Oceaniacruises substance, in particular, benzocaine, and as an element contain a derivative of propionic acid or derivative of salicylic acid, in particular ASA.

Preferred somatic analgesics are those that have a duration of at least 3 hours.

The claimed combination is particularly suitable for the treatment of inflammatory and/or associated with pain diseases, especially for the treatment of pharyngitis, laryngitis, tonsillitis, stomatitis, gingivitis various etiologies. Reception claimed combined drug it is advisable to perform oral. The combination can be used in conventional compositions, while the local anesthetic agent should be released first, and somatically acting analgesic in some cases, you may also be in the form of a slow-acting (depot form). As examples of these compounds include: coated tablets, sucking tablets, chewing gum, hard candies with liquid, semi-solid or solid core. Obtaining them is by conventional methods using conventional excipients.

Example 1

As an example, provides a tablet with the roses, 47 mg of microcrystalline cellulose, 2 mg of saccharin (550 parts) and 6 ml of orange juice as a flavoring in a tablet with a total weight of 660 mg of the Obtained tablets-kernel dragonaut with syrup (pills), containing benzocaine, in total, is applied approximately 5 mg of benzocaine and 602 mg syrup for drops. The above tablets are already after 2 minutes after taking my distinct analgesic effect that lasts more than 3 hours.

Example 2

By analogy with example 1 tablets-kernel envelop syrup for drops, which contains 500 mg of lidocaine. This combined structure starts to show its effect after 2 minutes and saves it in more than 6 hours.

1. Pharmaceutical preparation for oral administration with analgesic effect for 2 min to 12 h, containing a single dosage form non-steroidal anti-inflammatory and locally acting analgesic, and locally acting analgesic is released first.

2. Pharmaceutical drug under item 1, characterized in that it additionally contains conventional auxiliary substances and carriers.

 

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