Pharmaceutical composition with anti-inflammatory, analgesic and antipyretic action

 

(57) Abstract:

The invention relates to medicine, specifically to a pharmaceutical composition for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute gout, back pain, neuralgia, myalgia, traumatic inflammation of soft tissues and musculoskeletal system, acute infectious-inflammatory diseases of the upper respiratory tract, dysmenorrhea. The composition contains, wt%: as the active substance - piroxicam - 5,0-20,0; as auxiliary substances Aerosil - 0,1-5,0; starch - 10,1-40,0; talc and 0.1 - 3.0 and microcrystalline cellulose rest. The composition may be in the form of hard capsules. The new composition with piroxicam easily releases the active substance, stable during storage, has a shelf life of at least 2 years and meets the requirements of the State Pharmacopoeia. 1 C.p. f-crystals.

The invention relates to medicine, specifically to a pharmaceutical composition for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute gout, back pain, neuralgia, myalgia, traumatic inflammation of soft tissue and musculoskeletal Piroxicam (4-hydroxy-2-methyl-3-(N-pyridyl-2)carboxamido-[2H] -1,2-benzothiazine-1,1-dioxide) is used in medical practice as anti-inflammatory, analgesic and febrifuge [Mashkovsky M. D. Medicines, T. 1, ed. 13th, Kharkov: Torsing, 1997, S. 174]. The mechanism of action of the drug is associated with inhibition of prostaglandin synthesis by inhibiting the enzyme cyclo-oxygenase. Piroxicam reduces or completely eliminates the pain of moderate intensity, reduces the severity of the inflammatory response, reduces morning stiffness of the joints, helps to increase range of motion. The half-life of piroxicam is 36-45 h, which determines its long-term effects and the possibility of applying 1 times a day in a relatively small dose. In this regard, the development of pharmaceutical compounds with piroxicam special attention should be paid to the problem of increasing the bioavailability of the active substance, one of the solutions is to improve release of piroxicam from the dosage form.

In U.S. patent 4434164, 1984, describes an anti-inflammatory composition in the form of hard gelatin capsules with the following composition of ingredients, wt. %: active substance - 18,2; dicalcium phosphate and 70.8; corn starch - 10,0; sodium lauryl - 0.1; stearate - 0,9.

As deistvuuschaia in this composition leads to deterioration of quality (the new composition does not meet the requirements of Gosfarmakapei XI edition (GF XI) in terms of release of the active substance").

In U.S. patent 4564614, 1986 proposed anti-inflammatory pharmaceutical composition containing a combination of piroxicam and pyridoxine and auxiliary substances, wt.%: piroxicam - 2,9; pyridoxine (hydrochloride) - 3,5; corn starch - 93,2; magnesium stearate is 0.4.

The composition are in the form of hard gelatin capsules. As auxiliary ingredients can also be used lactose and high molecular weight polyethylene glycol. However, the application of the latter, as above additional ingredients, for producing solid dosage forms of piroxicam without other active ingredients can not achieve satisfactory performance for the release of the active substance. The purpose of this invention is to provide a pharmaceutical composition with an optimal combination of excipients for solid dosage forms of piroxicam - capsules.

The technical result to be obtained by the solution of the stated problem, is that a new pharmaceutical composition easily releases the active substance and stable during storage.

This technical result is achieved by the fact that the proposed pharmaceutical is setoudeh substances piroxicam and as excipients starch, additionally contains Aerosil, microcrystalline cellulose and talc in the following ingredients, by weight. %: piroxicam - 5,0-20,0; Aerosil-0,1-5,0; starch-10,1-40,0; talc-0,1-3,0; microcrystalline cellulose rest.

The claimed ratio of ingredients is best found experimentally.

Thanks to the invention, dosage form can easily release the active substance. So, raspadaemost new composition is 3-4 min and Wednesday dissolution passes for 45 minutes more than 85% of piroxicam. The use of the claimed ratio of excipients also provides flowability and nasleduemoe new members without the use of wetting agents and, accordingly, the exceptions under granulation. At the same time the inventive composition has a high stability after 2 years of storage the content of impurities is not more than 1.5% (by weight of active substance) and other quality indicators meet the requirements of normative documents.

The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in capsule form that provides a simple and practical composition can be carried out in accordance with known methods, for example by mixing the active substance with ancillary ingredients in the specified ratio to bulk homogeneous and subsequent kapsulirovaniem mixture.

The obtained pharmaceutical composition complies with the requirements of the global Fund XI (in appearance, raspadaemosti, dissolution, uniformity of dosage, microbiological purity and other parameters), stable in storage and has a shelf life of at least 2 years.

The invention is illustrated by the following examples:

Example 1. In a clean, dry mixer sequentially load the previously sifted powders piroxicam (10.4 g; 10.0 wt. %), microcrystalline cellulose (66.5 g; 64,0 wt. %), Aerosil (1,05 g; 1.0 wt. %), dry potato starch (24.4 g; 23.5 wt.%) and talc (1.6 g; 1.5 wt. %) and mix thoroughly until smooth, then capsulebuy in hard gelatin capsules. The obtained capsules meet the requirements of the pharmaceutical agent. The average weight of the contents of capsules, 0,100, Raspadaemost - 3 min (GF XI - not more than 20 min), dissolved in 0.1 M Hcl after 45 min of 98.2% (GF XI - not less than 75%), uniformity of dosage - meets the requirements of the global Fund XI, impurities - less than 0.2%, microbiological load pre-sifted powders piroxicam (5,2 g; 5.0 wt. %), Aerosil (0.1 g; 0.1 wt.%), dry corn starch (10,5 g; 10.1 wt. %), talc (3.1 g; 3.0 wt. %) and microcrystalline cellulose (85,0 g) and mix thoroughly until smooth, then capsulebuy in hard gelatin capsules. Received capsules with an average weight content 0,099 g satisfy the requirements of the pharmaceutical agent.

Example 3. In a clean, dry mixer sequentially loaded into the form of pre-sifted powders or 50.8 g of microcrystalline cellulose (34,9 wt. %), 29,1 g piroxicam (20.0 wt. %), to 58.2 g of dry starch (40.0 wt. %), 0.14 g of talc (0.1 wt. %) and 7.3 g of Aerosil (5.0 wt.%) and mix thoroughly until smooth, then capsulebuy in hard gelatin capsules. Received capsules with an average weight content 0,140 g satisfy the requirements of the pharmaceutical agent.

1. Pharmaceutical composition with anti-inflammatory, analgesic and antipyretic action, comprising as active ingredient piroxicam, and as excipients starch, characterized in that it further comprises Aerosil, microcrystalline cellulose and talc in the following ingredients, by weight. %:

Plumosa - Else

2. The pharmaceutical composition according to p. 1, characterized in that it is made in the form of hard capsules.

 

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