TR201502081A2 - Antiulcerative pharmaceutical preparations. - Google Patents
Antiulcerative pharmaceutical preparations. Download PDFInfo
- Publication number
- TR201502081A2 TR201502081A2 TR2015/02081A TR201502081A TR201502081A2 TR 201502081 A2 TR201502081 A2 TR 201502081A2 TR 2015/02081 A TR2015/02081 A TR 2015/02081A TR 201502081 A TR201502081 A TR 201502081A TR 201502081 A2 TR201502081 A2 TR 201502081A2
- Authority
- TR
- Turkey
- Prior art keywords
- sodium
- pharmaceutical composition
- gastric
- ulcers
- feature
- Prior art date
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- 230000000767 anti-ulcer Effects 0.000 title claims description 9
- 239000000825 pharmaceutical preparation Substances 0.000 title description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims abstract description 28
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 24
- 201000006549 dyspepsia Diseases 0.000 claims abstract description 19
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- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims abstract description 14
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- 229940126409 proton pump inhibitor Drugs 0.000 claims abstract description 13
- 239000000612 proton pump inhibitor Substances 0.000 claims abstract description 13
- 238000011282 treatment Methods 0.000 claims abstract description 12
- 241000590002 Helicobacter pylori Species 0.000 claims abstract description 10
- 229940037467 helicobacter pylori Drugs 0.000 claims abstract description 10
- 230000002496 gastric effect Effects 0.000 claims abstract description 9
- 208000024798 heartburn Diseases 0.000 claims abstract description 9
- 208000000689 peptic esophagitis Diseases 0.000 claims abstract description 9
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- 206010000060 Abdominal distension Diseases 0.000 claims abstract description 4
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- 230000008029 eradication Effects 0.000 claims abstract description 4
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Abstract
Mevcut buluş; Gastro-özofajiyal reflü hastalığının (GÖRH), eroziv reflü özofajitin, nükslerin, iyileşmiş reflü özofajitin, dispepsinin, nefropatik sistinozisin, pirozisin, yüksek asit salgısı ile kendini gösteren mide rahatsızlıklarının (mide yanması, ekşime, şişkinlik, hazımsızlık), uygun bir antibiyotik kombinasyonu ile birlikte Helicobacter pylori eradikasyonunun, Helicobacter pylori ile ilişkili duodenum ülserlerinin, Helicobacter pylori ile ilişkili peptik ülserlerde nükslerin, sürekli NSAİİ (non-steroidal anti-inflamatuvar ilaçlar) tedavisi gereken hastalarda NSAİİ kullanımı ile ilişkili gastrik ülserlerinin, risk altındaki hastalarda NSAİİ kullanımı ile ilişkili gastrik ve duodenal ülserlerinin, Zollinger Ellison Sendromu?nun, gastrik veya duodenal ülserlerde hemostazın kısa süreli sürdürülmesi ve tekrar kanamanın profilaktik, semptomatik veya terapötik tedavisinde kullanılmak üzere proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki uygun etken maddenin ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bileşim/ler ile ilgilidir.The present invention; Gastro-oesophageal reflux disease (GERD), erosive reflux esophagitis, relapses, healed reflux esophagitis, dyspepsia, nephropathic cystinosis, pyrosis, stomach ailments (heartburn, heartburn, bloating, indigestion) manifested by high acid secretion, with an appropriate antibiotic combination. Helicobacter pylori eradication, Helicobacter pylori associated duodenal ulcers, Helicobacter pylori associated peptic ulcers recurrence, continuous NSAID (non-steroidal anti-inflammatory drugs) treatment in patients requiring NSAID use associated gastric ulcers associated with NSAID use in patients at risk Duodenal ulcers, Zollinger-Ellison Syndrome, gastric or duodenal ulcers, gastric or duodenal ulcers for the short-term maintenance of hemostasis and proton pump inhibitors in the group of proton pump inhibitors for use in the prophylactic, symptomatic or therapeutic treatment of recurrent bleeding. relates to pharmaceutical composition / s containing acceptable derivatives.
Description
TARIFNAME ANTIÜLSERATIF FARMASÖTIK TERKIPLER BULUSUN ILGILI OLDUGU ALAN Mevcut bulus; Gastro-özofajiyal reflü hastaliginin (GÖRH), eroziv retlü özofajitin, nükslerin, iyilesmis reflü özofajitin, dispepsinin, nefropatik sistinozisin, pirozisin, yüksek asit salgisi ile kendini gösteren mide rahatsizliklarinin (mide yanmasi, eksime, siskinlik, hazimsizlik), uygun bir antibiyotik kombinasyonu ile birlikte Helicobacter pylori eradikasyonunun, Helicobacter pylori ile iliskili duodenum ülserlerinin, Helicobaoter pylori ile iliskili peptik ülserlerde nükslerin, sürekli NSAII (non-steroidal anti-inflamatuvar ilaçlar) tedavisi gereken hastalarda NSAII kullaniini ile iliskili gastrik ülserlerinin, risk altindaki hastalarda NSAII kullanimi ile iliskili gastrik ve duodenal ülserlerinin, Zollinger Ellison Sendromu”nun, gastrik veya duodenal ülserlerde hemostazin kisa süreli sürdürülmesi ve tekrar kanamanin protîlaktik, semptomatik veya terapötik tedavisinde kullanilmak üzere proton pompa inhibitörleri grubunda yer alan antiülseratit` Özellikteki uygun etken maddenin ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farinasötik bilesim/ler ile ilgilidir. DESCRIPTION ANTIULCERATIVE PHARMACEUTICAL COMPOSITIONS FIELD OF THE INVENTION The present invention; Gastro-esophageal reflux disease (GERD), erosive reflux esophagitis, relapses, healed reflux esophagitis, dyspepsia, nephropathic cystinosis, pyrosis, high stomach ailments manifested by acid secretion (heartburn, vomiting, bloating, indigestion), with an appropriate combination of antibiotics, Helicobacter pylori eradication of Helicobacter pylori-associated duodenal ulcers, Helicobacter pylori pylori-associated peptic ulcers, relapses are associated with sustained NSAID (non-steroidal anti-inflammatory risk of gastric ulcers associated with the use of NSAIDs in patients requiring treatment Gastric and duodenal ulcers associated with NSAID use in patients under Zollinger Hemostasis in gastric or duodenal ulcers in Ellison's Syndrome, short-term maintenance and prophylactic, symptomatic or therapeutic treatment of rebleeding. It is an antiulceratitis in the group of proton pump inhibitors for use. containing the appropriate active ingredient and/or pharmaceutically acceptable derivatives relates to pharmaceutical composition(s).
Mevcut bulus; proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki uygun etken maddenin Esomeprazol, bis-(5-metoksi-Z-[(S)[(4-metoksi-3,5-dimetil-2-piridinil) metil]sulfinil]-lH-benzimidazol l-il) (Formül I) ve/veya farmasötik olarak kabul edilebilir türevleri oldugu farmasötik bilesim/ler ile ilgilidir. The present invention; Appropriate antiulcerative properties in the proton pump inhibitors group active ingredient Esomeprazole, bis-(5-methoxy-Z-[(S)[(4-methoxy-3,5-dimethyl-2-pyridinyl) methyl]sulfinyl]-1H-benzimidazol 1-yl) (Formula I) and/or pharmaceutically acceptable relates to the pharmaceutical composition(s) of which it is derivative.
Formül I Ayrica bulus, Esomeprazol ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bilesimlerin oral ve parenteral uygulama için uygun olan formülasyonlarini ve profilaktik, semptomatik veya terapötik kullanimlarini da kapsamaktadir. ÖNCEKI TEKNIK (TEKNIGIN BILINEN DURUMU) Mide asitinin mideden özefagusa (yemek borusu) kaçmasina reflü denir. Hastaligin gerçek adi Gastro Özofageal Reflü (GÖR) 'dür. Genelde yemek borusundaki bir fitik veya kapakçigin zayifligi reflüye neden olur. Stres, gazli içecekler, çay ve kahve türü içecekler reflüyü arttirir. Formula I In addition, the invention includes Esomeprazole and/or its pharmaceutically acceptable derivatives. formulations of pharmaceutical compositions suitable for oral and parenteral administration and includes prophylactic, symptomatic or therapeutic uses. PRIOR ART (KNOWN STATE OF THE ART) Reflux is the escape of stomach acid from the stomach to the esophagus (esophagus). Your disease is real Its name is Gastro Esophageal Reflux (GER). Usually a hernia in the esophagus or Weak valve causes reflux. Stress, carbonated drinks, tea and coffee type drinks increases reflux.
Mide içeriklerinin yemek borusuna dogru geri akisi, yemek borusunun skuamöz epitelyumuna zarar verebilir ve yemek borusu mukozasini, Baret özofagusu ve yemek borusu karsinomuna yatkin hale getirebilir. Gastrik refluksatin temel kiskirticilari, pepsin ve hidroklorik asittir. Asit, sodyum bikarbonat ile hizli bir sekilde nötralize olabilir, ancak pepsin, 5”e kadar olan pH”larda aktif kalabilir ve sadece 7”nin üzerindeki pH°larda geri çevrilemez sekilde inhibe olur. Pepsin, peptid baglarinin belirli aminoasitler arasinda bölünmesini katalize eden proteolitik bir enzimdir. Sonuç olarak pepsin, yemek borusu üzerinde sürekli zarar verici bir etkiye sahip olabilir. The reflux of stomach contents into the esophagus, the squamous esophagus epithelium and esophageal mucosa, Baret's esophagus and food may predispose to tuberculous carcinoma. Main provocateurs of gastric refluxate, pepsin and hydrochloric acid. Acid can be quickly neutralized with sodium bicarbonate, but Pepsin can remain active at pHs up to 5” and only recover at pH above 7” is irreversibly inhibited. Pepsin is a link between peptide bonds and certain amino acids. It is a proteolytic enzyme that catalyzes the cleavage of As a result, pepsin can have a permanent detrimental effect on
Aslinda gastroözofagial reflü özellikle yemek sonrasindaki dönemlerde ve uykunun REM fazinda (rapid eye movement) olmak üzere gün içinde 10-50 kez kadar olabilen fizyolojik bir olaydir. Fizyolojik gastroözofagial reflü kisa sürdügünden farkina varilmaz veya çok hafif semptomlar olusturabilir. Ancak gastroözofagial reflü gün içinde sik araliklarla tekrarladiginda, uzun sürdügünde ve özellikle uyku sirasinda olustugunda artik patolojik gastroözofagial reflü söz konusudur ki bu tablo genellikle özefagus mukozasinda degisik derecelerde olabilen hasarlanma ve çesitli semptomlarla birliktedir. In fact, gastroesophageal reflux, especially in the postprandial periods and REM sleep Physiological, which can be up to 10-50 times a day, especially in the phase (rapid eye movement) is an event. Physiological gastroesophageal reflux may not be noticed because it lasts for a short time or it is very may produce mild symptoms. However, gastroesophageal reflux occurs frequently during the day. When it recurs, lasts for a long time and especially occurs during sleep, it is no longer pathological. there is gastroesophageal reflux, which is usually different in the esophageal mucosa. It is associated with various degrees of damage and symptoms.
Bu durumda gastroözofagîal reflü hastaligindan bahsedilir. Özefagusda endoskopik ve/veya histopatolojik yöntemlerle saptanabilen bir hasarlanmanin varligi ise reflü özofajiti olarak adlandirilir, Yemek borusundaki geri akis az miktarda mide suyunun, yiyecek ve/veya safra asidinin yemek borusunun alçak bölümlerine girmesi ile ortaya çikmakta ve kendisini mide eksimesi seklinde gösterebilen agri ile birlikte olusan yemek borusu iltihabina neden olmaktadir. In this case, gastroesophageal reflux disease is mentioned. Endoscopic in the esophagus and/or reflux esophagitis if there is damage that can be detected by histopathological methods. is called, The reflux in the esophagus results in a small amount of gastric juice, food, and/or bile acid. occurs when it enters the lower parts of the esophagus and Causes inflammation of the esophagus with pain, which can show in the form of respiration. is happening.
Tedavide en çok tercih edilen ilaçlar antiasitler, aljinik asit içeren ilaçlar, H2 Reseptörleri ve proton pompasi inhibitörleridir. Ileri durumlarda cerrahi tedavi tercih edilebilir. The most preferred drugs in treatment are antacids, drugs containing alginic acid, H2 Receptors and proton pump inhibitors. In advanced cases, surgical treatment may be preferred.
Semptomlari az olan hastalarda antiasitler (aljinik asit-antiasit kombinasyonlari), daha ciddi veya antiasite yeterince cevap alinamayan hastalarda H2-reseptör antagonistleri (Simetidin, Ranitidin, Famotidin ve Nizatidin) veya hidrojen pompa blokerleri (Omeprazol, Lansoprozol, Pantaprozol ve Esomeprazol) verilebilir. Tedavide kullanilan asit azaltici ilaçlara ek olarak prokinetik ilaçlar (betanekol, metoklopramid ) kullanilabilir. Antacids (alginic acid-antacid combinations) in patients with less symptoms H2-receptor antagonists in severe or unresponsive patients (Cymetidine, Ranitidine, Famotidine and Nizatidine) or hydrogen pump blockers (Omeprazole, Lansoprozole, Pantaprozole and Esomeprazole) can be given. used in treatment In addition to acid-reducing drugs, prokinetic drugs (betanecol, metoclopramide) can be used.
Proton pompa inhibitörlerinin klinik deneylerde mide ülseri, onikiparmak bagirsagi ülseri, yemek borusu geri akisi ve yemek borusu olmadan gastro yemek borusu geri akisi ile ilgili hazimsizlik rahatsizligi olan hastalarda semptomlarin giderilmesinde etkili oldugu kanitlanmistir. Örnek olarak omeprazolün mide-onikiparmak bagirsagi ve yemek borusu lezyonlarinin tedavisi ve bu sartlardaki hazimsizlik semptomlarinin ortadan kaldirilmasi açisindan H2 reseptör antagonistlere nazaran üstün oldugu bulunmustur (Eriksson S., Euro J ourn of Gastroenterology, 1995). In clinical trials of proton pump inhibitors, gastric ulcer, duodenal ulcer, pertaining to gastro-esophageal reflux with and without esophageal reflux It is effective in relieving symptoms in patients with indigestion. has been proven. For example, omeprazole in the gastrointestinal tract and esophagus treatment of the lesions and elimination of the symptoms of indigestion in these conditions It was found to be superior to H2 receptor antagonists in terms of Journal of Gastroenterology, 1995).
Esomeprazol, omeprazolün S-izomeridir ve mide asit sekresyonunu özgün bir etki mekanizmasiyla azaltir. Gastroözofageal retluks hastaliginda (GÖRH); erosif retluks özofajitinin tedavisinde; nükslerin önlenmesi için, iyilesmis retluks özofajitinin uzun süreli idame tedavisinde ve gastroözofageal refluks hastaliginin semptomatik tedavisinde endikedir. Oral yoldan tedavinin uygun olmadigi durumlarda parenteral tedavi uygulanir. Esomeprazole is the S-isomer of omeprazole and has a specific effect on gastric acid secretion. reduces by the mechanism. In gastroesophageal retlux disease (GERD); erosive retlux in the treatment of esophagitis; long-term treatment of healed retlux esophagitis to prevent recurrences maintenance therapy and symptomatic treatment of gastroesophageal reflux disease. is indicated. In cases where oral treatment is not appropriate, parenteral treatment is applied.
Omeprazol, asit salgilama mekanizmasinin son asamasinda mide asidi salgilanmasinin kontrol edilmesi vasitasiyla insanin da dahil oldugu memeli canlilarda mide asidinin önlenmesi için yararlidir ve bu sayede uyarici nedene bakmaksizin temel ve uyarilmis mide asidi salgilanmasini azaltir. Omeprazole inhibits gastric acid secretion in the final stage of the acid secreting mechanism. stomach acid in mammals, including humans, by controlling It is useful for the prevention of basic and stimulated stomach regardless of the stimulant cause. reduces acid secretion.
Teknikte bilindigi gibi, omeprazol asitlere karsi hassastir, fakat bazik çözeltilerde çok, suda çok az çözünmektedir. Ayrica, omeprazolün neme, isiya, isiga ve organik çözücülere hassas oldugu bilinmektedir. As is known in the art, omeprazole is sensitive to acids, but very much in basic solutions, in water. It dissolves very little. In addition, omeprazole is resistant to moisture, heat, light and organic solvents. It is known to be sensitive.
Mide asidi bastirici özellikteki proton pompa inhibitörlerinin asit ortaminda kararsiz bir yapiya sahip olmasi büyük ölçüde asidik bir ortam olan mide içerigine temas ederek parçalanmasina neden olur, bu yüzden oral yoldan uygulamaya yönelik farmasötik bilesimlerin gelistirilmesi gerekmektedir. Bundan yola çikarak; etken maddenin midedeki gastrik asitten dolayi bozulmasini önlemek ve ince bagirsagin yakin bölümünde serbest kalmasini saglamak için bilesim bir enterik kaplama ile kaplanabilir. çoklu tablet seklinde sikistirilmis dozaj biçimleri açiklanmaktadir. parenteral forrnülasyonu ve ömeklerinden bahsedilmektedir. Proton pump inhibitors with gastric acid suppressing properties are unstable in the acid environment. having a structure by contacting the stomach contents, which is a highly acidic environment causes degradation, therefore pharmaceuticals for oral administration compositions need to be developed. Based on this; active ingredient in stomach to prevent deterioration due to gastric acid and free in the proximal part of the small intestine. The composition may be coated with an enteric coating to ensure retention. Compressed dosage forms in the form of multiple tablets are disclosed. parenteral formulation and examples are mentioned.
BULUSUN AÇIKLAMASI Mevcut bulus; Gastro-özofajiyal reflü hastaliginin (GÖRH), eroziv reflü özofajitin, nükslerin, iyilesmis reflü özofajitin, dispepsinin, nefropatik sistinozisin, pirozisin, yüksek asit salgisi ile kendini gösteren mide rahatsizliklarinin (mide yanmasi, eksime, siskinlik, hazimsizlik), uygun bir antibiyotik kombinasyonu ile birlikte Helicobacter pylori eradikasyonunun, Helicobacter pylori ile iliskili duodenum ülserlerinin, Helioobacter pylori ile iliskili peptik ülserlerde nükslerin, sürekli NSAII (non-steroidal anti-intlamatuvar ilaçlar) tedavisi gereken hastalarda NSAII kullanimi ile iliskili gastrik ülserlerinin, risk altindaki hastalarda NSAII kullanimi ile iliskili gastrik ve duodenal ülserlerinin, Zollinger Ellison Sendromu”nun, gastrik veya duodenal ülserlerde hemostazin kisa süreli sürdürülmesi ve tekrar kanamanin profilaktik, semptomatik veya terapötik tedavisinde kullanilmak üzere proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki uygun etken maddenin ve/veya farmasötik olarak kabul edilebilir türevlerini içeren farmasötik bilesim/ler ile ilgilidir. DESCRIPTION OF THE INVENTION The present invention; Gastro-esophageal reflux disease (GERD), erosive reflux esophagitis, relapses, healed reflux esophagitis, dyspepsia, nephropathic cystinosis, pyrosis, high stomach ailments manifested by acid secretion (heartburn, vomiting, bloating, indigestion), with an appropriate combination of antibiotics, Helicobacter pylori eradication of Helicobacter pylori-associated duodenal ulcers, Helioobacter pylori-associated peptic ulcers, relapses are associated with persistent NSAIDs (non-steroidal anti-inflammatory risk of gastric ulcers associated with the use of NSAIDs in patients requiring Gastric and duodenal ulcers associated with NSAID use in patients under Zollinger Hemostasis in gastric or duodenal ulcers in Ellison's Syndrome, short-term maintenance and prophylactic, symptomatic or therapeutic treatment of rebleeding Antiulcerative properties in the group of proton pump inhibitors for use containing the appropriate active ingredient and/or pharmaceutically acceptable derivatives relates to pharmaceutical composition(s).
Mevcut bulusun bir diger yönü; parenteral uygulamaya yönelik proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki uygun etken madde ve/veya farmasötik olarak kabul edilebilir türevlerini ve farmasötik olarak kabul edilebilir uygun yardimci maddeleri içeren farmasötik bilesim/lerin hazirlanmasi ile ilgilidir. Another aspect of the present invention is; proton pump inhibitors for parenteral administration as the appropriate active substance and/or pharmaceutical with antiulcerative properties in the group acceptable derivatives and suitable pharmaceutically acceptable excipients It relates to the preparation of pharmaceutical composition(s) containing
Bulusta kullanilan proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki uygun etken madde; oiiieprazol, lansoprazol, pantoprazol, esomeprazol, timoprazol, leminoprazol, rabeprazol ve/veya farmasötik olarak kabul edilebilir türevleri arasindan tercihen esomeprazol sodyum olarak seçilir. It is an antiulcerative agent in the group of proton pump inhibitors used in the invention. suitable active ingredient; oiiieprazole, lansoprazole, pantoprazole, esomeprazole, timoprazole, leminoprazole, rabeprazole and/or pharmaceutically acceptable derivatives preferably esomeprazole sodium is selected.
Bulusta “farmasötik olarak kabul edilebilir türevleri” terimi ile farmasötik olarak kabul edilebilir uygun tuzlar, esterler, solvatlar, hidratlar, kompleksler, polimorflar, enantiyomerler, önilaçlar, asit adisyon tuzlari, analoglar, izomerler, rasematlar, amidler, enantiyomer tuzlari, bazik tuzlar, konjugeler, tautomerler, anhidratlar, anhidritler, bazlar, asitler, eterler, kristal ve amorf formlar veya serbest formlarindan bir veya daha fazlasi ifade edilmektedir. In the invention, the term "pharmaceutically acceptable derivatives" is defined as pharmaceutically acceptable. Suitable salts, esters, solvates, hydrates, complexes, polymorphs, enantiomers, prodrugs, acid addition salts, analogs, isomers, racemates, amides, enantiomer salts, basic salts, conjugates, tautomers, anhydrates, anhydrides, bases, one or more of acids, ethers, crystalline and amorphous forms or free forms is expressed.
Oral uygulama için hazirlanan farmasötik bilesim/ler kati ya da sivi dozaj formlarinda olabilir. Bu dozaj formlari; tablet (çignenebilir tablet, agizda çözünen tablet, dagilabilen tablet, suda dagilabilen tablet, film kapli tablet, barsakta açilan kaplamali (enterik) tablet, mini tablet, kontrollü salimli tablet (sürekli salimli tablet, hemen salimli tablet, uzatilmis salimli tablet, geciktirilmis salimli tablet vb.), kapsül (sert, yumusak, enterik kapli, film kapli), kontrollü salimli kapsül (sürekli salimli kapsül, hemen salimli kapsül, uzatilmis salimli kapsül, geciktirilmis salimli kapsül), toz, granül, kaplet, disk, agizda çözünen film, yigin toz (çok dozlu), pellet, sase, suda dagilabilen toz, suda dagilabilen granül, efervesan tablet, efervesan granül, efervesan toz, jelül, pilül, surup, solüsyon, süspansiyon, eliksir, damla, posyon, emülsiyon veya sprey gibi bir dozaj sekli halinde formüle edilebilir. Pharmaceutical composition/s prepared for oral administration in solid or liquid dosage forms it could be. These dosage forms are; tablet (chewable tablet, mouth soluble tablet, dispersible tablet, dispersible tablet, film-coated tablet, coated (enteric) tablet that opens in the intestine, mini tablet, controlled-release tablet (sustained-release tablet, immediate-release tablet, extended-release tablet) release tablet, delayed release tablet, etc.), capsule (hard, soft, enteric-coated, film coated), controlled-release capsule (sustained-release capsule, immediate-release capsule, extended-release capsule) release capsule, delayed release capsule), powder, granule, caplet, disc, oral film, bulk powder (multidose), pellet, sachet, water-dispersible powder, water-dispersible granule, effervescent tablet, effervescent granule, effervescent powder, gel, pill, syrup, solution, suspension, elixir, It may be formulated in a dosage form such as drops, position, emulsion or spray.
Bulusta kullanilan parenteral uygulamaya yönelik farmasötik enjektabl çözelti için liyofilize toz içeren flakon formülasyonu; uygun etken maddelerin yaninda en az bir pH ayarlayici ajan, en az bir çözücünün ve gerekli görüldügü durumda en az bir selat yapici ajanin da dahil oldugu gruptan seçilen bir veya daha fazla farmasötik olarak kabul edilebilir yardimci madde içerebilen bir bilesimi tanimlar. For the pharmaceutical injectable solution for parenteral administration used in the invention vial formulation containing lyophilized powder; at least a pH in addition to suitable active ingredients setting agent, at least one solvent and, if necessary, at least one chelator one or more pharmaceuticals selected from the group that includes the agent Defines a composition that may contain an excipient.
Parenteral enjeksiyon intraperitonal, intravenöz, infîjzyon, intramüsküler, subkutan veya intraderinal yollarla uygulanabilir. Mevcut bulus, intravenöz yolla kullanilmak üzere hazirlanmis enjektabl çözelti için liyofilize toz içeren flakon formunda farmasötik bir bilesimdir. Parenteral injection is intraperitoneal, intravenous, infusion, intramuscular, subcutaneous or can be administered intradermally. The present invention is intended for intravenous use. a pharmaceutical product in the form of a vial containing a lyophilized powder for a prepared injectable solution. is the composition.
Bulusta “pH ayarlayici ajan” terimi, kompozisyonun asitlik ve bazligini düzenleyen maddeler olarak ifade edilmektedir. pH ayarlayici ajan olarak; sitrik asit anhidrus, sodyum sitrat dihidrat, sodyum fosfat, sodyum dihidrojen fosfat, potasyum sitrat, fosforik asit, amonyum hidroksit, sitrik asit, diizopropanolamin, sodyum karbonat, sodyum silikat, disodyum ortofosfat, kalsiyum karbonat, magnezyum karbonat, magnezyum hidroksit, magnezyum alüminat, dietanol amin, sodyum aljinat, etilendiamin, meglümin, hidroklorik asit, laktik asit, sodyum sitrat, sodyum hidroksit, sodyum klorür, trietanolamin, trolamine, sodyum benzoat, sodyum hidrojen karbonat, potasyum/sodyum asetat veya bunlarin karisimlari kullanilabilir. Bulusta tercihen sodyum hidroksit kullanilmaktadir. Çözücü olarak saflastirilmis su, enjeksiyonluk su, deiyonize su veya bunlarin karisimlari kullanilabilir. Bulusta tercihen enjeksiyonluk su kullanilmaktadir. In the invention, the term "pH adjusting agent" is used to regulate the acidity and basicity of the composition. referred to as items. As a pH adjusting agent; citric acid anhydrous, sodium citrate dihydrate, sodium phosphate, sodium dihydrogen phosphate, potassium citrate, phosphoric acid, ammonium hydroxide, citric acid, diisopropanolamine, sodium carbonate, sodium silicate, disodium orthophosphate, calcium carbonate, magnesium carbonate, magnesium hydroxide, magnesium aluminate, diethanol amine, sodium alginate, ethylenediamine, meglumine, hydrochloric acid, lactic acid, sodium citrate, sodium hydroxide, sodium chloride, triethanolamine, trolamine, sodium benzoate, sodium hydrogen carbonate, potassium/sodium acetate or their mixes can be used. Sodium hydroxide is preferably used in the invention. Solvent purified water, water for injection, deionized water or mixtures thereof can be used. Water for injection is preferably used in the invention.
Bulusta selat yapici ajan olarak EDTA (etilen diamin tetraasetik asit), disodyum EDTA (disodyum etilen diamin tetraasetik asit) veya kalsiyum EDTA (kalsiyum etilen diainin tetraasetik asit) veya bunlarin karisimlari kullanilabilir. Bulusta tercihen disodyum EDTA kullanilmaktadir. Bulusta kullanilan selat yapici ajan miktari %0.01-10 agirlik oranindadir. EDTA (ethylene diamine tetraacetic acid), disodium EDTA as chelating agent in the invention (disodium ethylene diamine tetraacetic acid) or calcium EDTA (calcium ethylene diamine tetraacetic acid) or mixtures thereof can be used. In the invention, preferably disodium EDTA is used. The amount of chelating agent used in the invention is 0.01-10% by weight.
Mevcut bulustaki Esomeprazol ve/veya farrnasötik olarak kabul edilebilir türevlerini içeren farrnasötik bilesimlerin uygun olan forrnülasyonlarina ait doz araligi; 4-1601ng tercihen; Sing, ZOmg, 40mg ve 80mg olup hastanin bireysel ihtiyaçlarina ve uzmanin degerlendirmesine göre ayarlanmaktadir. containing Esomeprazole and/or pharmaceutically acceptable derivatives of the present invention. dose range of suitable formulations of pharmaceutical compositions; 4-1601ng preferably; Sing, ZOmg, 40mg and 80mg are available depending on the individual needs of the patient and the specialist. adjusted according to its assessment.
Bulusta, Esomeprazol ve/Veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin parenteral uygulamasina yönelik farmasötik enjektabl çözelti için liyofilize toz içeren flakon formülasyonu asagidakileri içermektedir; - yaklasik %10-100 agirlik oraninda Esomeprazol sodyum (mannitol ile karisim halinde) - kafi miktar bir veya daha fazla pH ayarlayici ajan - gerekli görüldügü durumda yaklasik %0.0l-lO agirlik oraninda bir veya daha fazla selat yapici ajan Bulus esas olarak parenteral uygulamaya yönelik proton pompa inhibitörleri grubunda yer alan antiülseratif özellikteki etken maddeyi ve/veya farrnasötik olarak kabul edilebilir türevlerini ve farmasötik olarak kabul edilebilir uygun yardimci maddeleri içeren farmasötik bilesimlerin hazirlanmasiyla ile ilgilidir. Bulusun farmasötik bilesimlerinin enjektabl çözelti için liyofilize toz içeren flakon formunda olmasi temeldir. Elde edilen liyofilize toz içeren Ilakon dozaj formunun parenteral yolla uygulanmasinin çabuk etki saglamasi, oral yoldan ilaç alinamayan durumlarda hastanin kolay ilaç alimini saglamasi, gastro-intestinal sivilar tarafindan ilacin tahrip edilmesinin önlenmesi, lokal ve sistemik etki saglamasi, biyoyararlanim yüksek olmasi gibi avantajlari söz konusudur. Bahsi geçen parenteral uygulamaya yönelik liyofilize toz içeren Ilakon dozaj formu intravenöz olarak uygulanabilmektedir. Böylece elde edilen liyofilize toz içeren flakon sasirtici bir sekilde fiziksel ve kimyasal kararlilik açisindan oldukça stabil bir davranis sergilemistir. Ayrica yeterli terapötik etkiyi saglamak ve yan etkileri minimuma indirmek için sasirtici bir sekilde etkili olduklari belirlenmistir, Bulusun özellikleri asagidakilerle sinirli kalmamak üzere örnekler asagida verilmistir: Esomeprazol ve/veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin parenteral uygulamasina yönelik farmasötik enjektabl çözelti için liyofilize toz içeren flakon forrnülasyonu asagidakileri içerrnektedir; - yaklasik %10-100 agirlik oraninda Esomeprazol sodyuin (mannitol ile karisim halinde) - gerekli görüldügü durumda yaklasik %0.0 l -10 agirlik oraninda disodyum EDTA Esomeprazol ve/veya farmasötik olarak kabul edilebilir türevlerinin kullanildigi farmasötik bilesimlerin parenteral uygulamasina yönelik farmasötik enjektabl çözelti için liyofilize toz içeren flakon formülasyonu asagidakileri içermektedir; - yaklasik 4-]60mg Esomeprazol sodyum (mannitol ile karisim halinde) - gerekli görüldügü 0.01-20mg disodyum EDTA Üretim prosesi: Liyofilizasyon: Esomeprazol Sodyum enjeksiyonluk su içerisinde, berrak bir çözelti elde edinceye kadar karistirarak çözülür. Gerekli görüldügü durumda enjeksiyonluk su içerisinde çözülmüs Disodyum EDTA, berrak bir çözelti elde edinceye kadar karistirilarak eklenir. pH kontrol edilir. pH istenilen aralikta olmalidir. Eger pH uygun degilse, Sodyum Hidroksit ile pH ayarlanir. Hacim tamamlanir. Çözelti uygun filtreden geçirilerek filtre edilir. Flakonlar istenilen miktarda doldurulur. Istenilen parametrelerde uygun liyofilizasyon islemi yapilir, final kurutmadan sonra azot geçirilir ve flakonlar kapatilir. Esomeprazole and/or pharmaceutically acceptable derivatives are used in the invention. for pharmaceutical injectable solution for parenteral administration of pharmaceutical compositions The vial formulation containing lyophilized powder contains the following; - approximately 10-100% by weight of Esomeprazole sodium (as mixed with mannitol) - sufficient amount of one or more pH adjusting agents - one or more chelates at a rate of approximately 0.01-10% by weight, if deemed necessary builder agent The invention is mainly in the group of proton pump inhibitors for parenteral administration. active substance with antiulcerative properties and/or pharmaceutical acceptable derivatives and suitable pharmaceutically acceptable excipients. relates to the preparation of pharmaceutical compositions. Pharmaceutical compositions of the invention For injectable solution, it is essential that it is in the form of vials containing lyophilized powder. Obtained The rapid effect of parenteral administration of the Ilakon dosage form containing lyophilized powder to provide easy medication for the patient in cases where oral medication cannot be taken, prevention of drug destruction by gastrointestinal fluids, local and systemic It has advantages such as effective effect and high bioavailability. Aforementioned Ilakon dosage form containing lyophilized powder for parenteral administration is administered intravenously applicable. Surprisingly, the vial containing the lyophilized powder thus obtained showed a very stable behavior in terms of physical and chemical stability. Moreover an astonishing approach to ensure adequate therapeutic effect and minimize side effects. It has been determined that they are effective in this way, Examples of the features of the invention are given below, but not limited to the following: Pharmaceutical use of esomeprazole and/or pharmaceutically acceptable derivatives Lyophilized powder for pharmaceutical injectable solution for parenteral administration of compositions Containing vial formulation contains the following; - approximately 10-100% by weight of Esomeprazole sodium (as mixed with mannitol) - disodium EDTA approx. 0.0 % l -10 wt% if deemed necessary Pharmaceutical use of esomeprazole and/or pharmaceutically acceptable derivatives Lyophilized powder for pharmaceutical injectable solution for parenteral administration of compositions Containing vial formulation contains the following; - approx. 4-]60mg Esomeprazole sodium (as a mixture with mannitol) - 0.01-20mg disodium EDTA as needed Production process: Lyophilization: Esomeprazole Sodium in water for injection until a clear solution is obtained. solved by mixing. If necessary, dissolved in water for injections. Disodium EDTA is added with stirring until a clear solution is obtained. pH control is done. The pH should be in the desired range. If pH is not appropriate, pH with Sodium Hydroxide is set. The volume is complete. The solution is filtered by passing through the appropriate filter. vials filled in the desired amount. Appropriate lyophilization process is performed in the desired parameters, After final drying, nitrogen is passed through and the vials are closed.
Claims (6)
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| TR2015/02081A TR201502081A2 (en) | 2015-02-21 | 2015-02-21 | Antiulcerative pharmaceutical preparations. |
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| TR2015/02081A TR201502081A2 (en) | 2015-02-21 | 2015-02-21 | Antiulcerative pharmaceutical preparations. |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US11891588B2 (en) | 2019-07-31 | 2024-02-06 | Ecolab Usa Inc. | Personal protective equipment free delimer compositions o |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US11891588B2 (en) | 2019-07-31 | 2024-02-06 | Ecolab Usa Inc. | Personal protective equipment free delimer compositions o |
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