TR202022087A2 - Inhalation Powder for SARS Cov-2 Infections - Google Patents

Inhalation Powder for SARS Cov-2 Infections Download PDF

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Publication number
TR202022087A2
TR202022087A2 TR2020/22087A TR202022087A TR202022087A2 TR 202022087 A2 TR202022087 A2 TR 202022087A2 TR 2020/22087 A TR2020/22087 A TR 2020/22087A TR 202022087 A TR202022087 A TR 202022087A TR 202022087 A2 TR202022087 A2 TR 202022087A2
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TR
Turkey
Prior art keywords
infections
carvacrol
essential oil
inhalation
capsule
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TR2020/22087A
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Turkish (tr)
Inventor
Ercan Canbay İsmet
Canbay Torun Bahar
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Canbay Torun Bahar
Ismet Ercan Canbay
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Priority to TR2020/22087A priority Critical patent/TR202022087A2/en
Publication of TR202022087A2 publication Critical patent/TR202022087A2/en

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Abstract

Bu buluşta SARS Cov-2 enfeksiyonlarında karvakrol ve eucalyptus uçucu yağı kombine edilerek doğrudan toz halde akciğere verilmek için formüle edilmiştir. Kısaca SARS Cov-2 enfeksiyonlarının önlenmesinde ve tedavisinde kullanılabilecek kombine inhalasyon tozu ve hazırlanmasını açıklamaktadır.In this invention, in SARS Cov-2 infections, carvacrol and eucalyptus essential oil are combined and formulated to be administered directly to the lungs in powder form. Briefly describes the combined inhalation powder and its preparation that can be used in the prevention and treatment of SARS Cov-2 infections.

Description

TARIFNAME SARS Cov-2 Enfeksiyonlari Için Inhalasyon Tozu Teknik Alan Bu bulus inhalasyon yoluyla hastalara verilmek üzere gelistirilmis eucalyptus uçucu yagi ve karvakrol içeren tercihen bomeolunde kullanildigi kum toz formülü hakkindadir. Önceki Teknik Su anda COVlD-l9'a neden olan koronavirüs olan SARS-COV-Z'yi tedavi etmek için antiviral olarak remdesivir ve favipiravir kullanilmaktadir. Ancak bunlarin hastaya uygulanmasi invaziv ve zordur. Bu ilaçlari içeren inhalasyon yolu ile verilebilecek kuru toz formülü mevcut degildir. Remdesivir SARS-CoV-Z'yi tedavi etmek için genellikle intravenöz uygulama ile infüzyon halinde verilir. DESCRIPTION Inhalation Powder for SARS Cov-2 Infections Technical Area This invention was developed to be administered to patients by inhalation eucalyptus. Sand powder formula containing essential oil and carvacrol, preferably used in bomeol. is about. Prior Art Treating SARS-COV-Z, the coronavirus that currently causes COVID-19 Remdesivir and favipiravir are used as antivirals. However, these It is invasive and difficult to administer to the patient. By inhalation containing these drugs There is no dry powder formula that can be given. Remdesivir SARS-CoV-Z It is usually given as an infusion by intravenous administration to treat

Remdesivir, agir hastalik nedeniyle hastaneye yatirilan yetiskin ve pediatrik hastalarda acil durumlarda kullanilmaktadir. Ilk önceleri Ebola virüsü hastaligini tedavi etmek için gelistirilen remdesivir, insan hava yolu epitel hücrelerinde COVlD-19'u tedavi etmek için umut verici sonuçlar göstermistir. Bununla birlikte, sinirli etkili uygulama yöntemleri, yasami tehdit eden semptomlar sergileyen hastalara yaygin tedavi uygulama çabalarini engellemistir. Remdesivir is used in adult and pediatric hospitalized patients with severe illness. used in emergencies. First, the Ebola virus disease Remdesivir, developed to treat human airway epithelial cells It has shown promising results for treating COVID-19. With this However, limited effective methods of administration, life-threatening symptoms This has hindered efforts to apply widespread treatment to patients with

SARS-COV-2 virüsünün ilk yerlestigi bölge üst solunum yoludur. Bu nedenle günlük hayatin içinde virüsün yerlesmesini engelleyecek virüsün ilk yerlesim bölgesinde çogalmasini önleyecek formülasyonlara ihtiyaç bulunmaktadir. The first location of the SARS-COV-2 virus is the upper respiratory tract. Because the first settlement of the virus that will prevent the virus from settling in daily life. There is a need for formulations to prevent proliferation in the region.

Bogaz pastilleri bu nedenle sikça tercih edilen ürünler olmakla beraber seker içerikleri nedeni ile bazen kullanimlari tercih edilmemektedir. For this reason, throat lozenges are frequently preferred products. Sometimes their use is not preferred due to their content.

Antimikrobiyal etkinligi bilinen çok sayida bitki ve bitkisel madde bulunmaktadir. There are many plants and herbal substances with known antimicrobial activity.

Bunlarin çok farkli kombinasyonlarinin yapilmasi mümkündür. Bu antimikrobiyal ajanlarda daha çok bakteriyel enfeksiyonlar için kombine edilmis olup viral enfeksiyonlar için gelistirilmis ürünlerin sayisi sinirlidir. ekstresini benzalkonyum klorür ile birlikte içeren antiviral kombinasyonlar hakkindadir. içeren ürünler hakkindadir. It is possible to make many different combinations of these. This antimicrobial agents are mostly combined for bacterial infections and viral The number of products developed for infections is limited. antiviral combinations containing the extract together with benzalkonium chloride is about. about products containing

USZOO4/007l757 numarali patent basvurusu solunum yolu enfeksiyonlarinda intranasal yama kullanilmasi hakkindadir. Bu basvuru kombinasyonda kullanilan bilesiklerden çok uygulama metodu hakkindadir. Patent application numbered USZOO4/007l757 on respiratory tract infections It is about using an intranasal patch. This reference is used in combination it is more about the method of application than about the compounds.

EP1748769 numarali patent basvurusu daha önce antiseptik antifungal antibakteriyel etkisi gösterilmis p-mentan-3,8-diol bilesiklerinin antiviral olarak kullanilmasi hakkindadir. Patent application number EP1748769 was previously applied to antiseptic antifungal Antiviral use of p-menthane-3,8-diol compounds with antibacterial effects it is about to be used.

Bu buluslarin hiçbirisi Viral enfeksiyonlarda kullanilacak hizli ve etkili kombinasyonlar ve bunlarin formülasyonlari hakkinda degildir. Yine bu buluslarin hiçbiri SARS CoV-2 enfeksiyonlarindan korunma metodu hakkinda degildir. None of these inventions are quick and effective for use in viral infections. It is not about combinations and their formulations. again this none of the inventions about the method of protection from SARS CoV-2 infections is not.

Uygulamasi kolay etkili ve güvenilir antiviral kompozisyonlarinin gelistirilmesine ihtiyaç vardir. To develop effective and safe antiviral compositions that are easy to apply. there is a need.

Bu bulus SARS CoV-Z viral enfeksiyonlardan korunmada ve viral enfeksiyon tedavisine yardimci, uygulamasi kolay, güvenilir kombinasyonlar ve bu kombinasyonlarin hazirlanma metodu hakkindadir. This invention provides protection from SARS CoV-Z viral infections and viral infection. easy to apply, reliable combinations that help in the treatment of It is about the method of preparation of combinations.

Bulusun çözümünü amaçladigi teknik problemler Bu bulus eucalyptus uçucu yagi ve karvakrol içeren inhalasyon yoluyla hastalara verilmek üzere gelistirilmis kuru toz formülüdür. Bu bulus COVlD-l9 hastalarini tedavi etmek için inhalasyon yoluyla dogrudan akcigerlere verilebilecek toz formülasyonunu ve bunun nasil hazirlanacagini anlatir. Bugüne kadar Eucalyptus uçucu yagi ve Karvakrolü bir arada içeren ve inhalasyon yoluyla kullanilabilecek bir toz formülü gelistirilmemistir. Technical problems that the invention aims to solve This invention is administered to patients via inhalation containing eucalyptus essential oil and carvacrol. It is a dry powder formula developed for administration. This invention treats COVID-19 patients powder that can be inhaled directly into the lungs to treat explains its formulation and how to prepare it. Eucalyptus to date It contains essential oil and Carvacrol together and can be used by inhalation. a powder formula has not been developed.

COVID-l9 hastaligi tedavisi zor bir hastaliktir. COVID-l9 hastaliginda yan etkisi çok fazla olan ilaçlarin yerine eucalyptus uçucu yagi ve karvakrolun hedef dokulara dogrudan ulasmasini saglayan ürünler etkin bir tedavi saglayacaktir. COVID-19 is a difficult disease to treat. Side effect in COVID-19 disease target of eucalyptus essential oil and carvacrol instead of drugs that are too much Products that allow it to reach the tissues directly will provide an effective treatment.

Tedavisi zor olan bu hastalikta uygulama kolayligi olan ürün gelistirilerek hem hastane yükü azaltilacak hem de özellikle yasli hastalarda ölüm risklerini artiran yan etki insidansinin azaltilmasi amaçlanmistir. In this disease, which is difficult to treat, a product that is easy to apply has been developed and both the hospital burden will be reduced and the risk of death will increase, especially in elderly patients. It is aimed to reduce the incidence of side effects.

Yine bu bulusta antiviral etkinin güçlendirilmesi için ayni formülasyon içerisine diger antiviral ajanlar katilabilir. Diger antiviral ajanlar arasinda borneol, epigallokatesin galat sayilabilir. Diger antiviral ajanlarin sayisi burada anlatilanlarla sinirli degildir. Again, in this invention, it is included in the same formulation to strengthen the antiviral effect. Other antiviral agents may be added. Other antiviral agents include borneol, epigallocatecin can be considered gallate. Number of other antiviral agents here is not limited by what is told.

SARS CoV-Z enfeksiyonun tedavisinde eucalyptus uçucu yagi ve karvakrolun bir arada veya gerektiginde bir baska antiviral ajanla kullanilmasi, dozlari ve hazirlama teknigi belli degildir, bu bulus bunlari açiklamaktadir. A combination of eucalyptus essential oil and carvacrol in the treatment of SARS CoV-Z infection. its use with another antiviral agent in between or when necessary, its doses and preparation technique is unclear, which this invention explains.

Bulusun Açiklamasi Bu bulusta antiviral ajanin inhalasyona uygun toz formülü hazirlanmistir. Bunun için antiviral ajan etanolde çözülür ve laktoza püskürtülerek kaplanir. Antiviral ajanin etanoldeki çözeltisi 10 mg/ml olmalidir. Laktoz olarak %50-75 oranda 1-3 mikrometre inhalasyona uygun laktoz tozuna etanolde çözülmüs lÜmg/ml antiviral bilesik püskürtülür. Akiskan yatak Cihazinda 50°C”yi geçmeyen isida kaplama yapilir. Sert jelatin kapsüle dolum yapilarak inhalasyon yolu ile hastaya verilir. Inhalasyon cihazi olarak herhangi bir inhalasyon cihazi kullanilabilir. Description of the Invention In this invention, powder formula of antiviral agent suitable for inhalation is prepared. This The antiviral agent is dissolved in ethanol and spray coated with lactose. antiviral The solution of the agent in ethanol should be 10 mg/ml. 50-75% as lactose 1-3 Micrometer to lactose powder suitable for inhalation dissolved in ethanol IUmg/ml antiviral compound is sprayed. Temperature not exceeding 50°C in the fluidized bed device coating is done. It is filled into a hard gelatin capsule and given to the patient by inhalation. is given. Any inhaler can be used as an inhaler.

Antiviral ajan olarak bu bulusta eucalyptus uçucu yagi ve karvakrol tercih edilmistir. Bu iki antiviral ajan istenirse diger antiviral ajanlarla, antienflamatuvar ajanlarla kombine edilebilir. Kombine edilecek diger ajanlar arasinda borneol ve epigallokatesin gallat tercih edilir. Eucalyptus essential oil and carvacrol were preferred in this invention as antiviral agents. has been made. These two antiviral agents can be combined with other antiviral agents if desired. Can be combined with agents. Other agents to be combined include borneol and epigallocatecin gallate is preferred.

Bu bulustaki kombinasyon asagidaki sekilde hazirlanabilir. Eucalyptus uçucu yagi ve karvakrol 0.5-1 mg/ml olacak sekilde etanolde çözülür ve inhalasyona uygun laktoz tozuna püskürtülerek fludized bed (Akiskan yatak) Cihazinda kaplanir ve 50°C”yi geçmeyen sicakliklar kullanilarak kaplanir. Kaplama sonunda miktar tayini yapildiginda 1 doz tozda yaklasik 0.5 -1 mg eucalyptus uçucu yagi ve 0.5 -1 mg karvakrol olmalidir. Bu sekilde hazirlanan toz dogrudan nefesle akcigerlere alinmak üzere sert jelatin veya benzeri kapsüllere doldurulup inhalasyonla hastalara verilir. Inhalasyonla verilecek cihaz herhangi bir toz inhalasyon cihazi olabilir. The combination in this invention can be prepared as follows. Eucalyptus essential oil and carvacrol are dissolved in ethanol as 0.5-1 mg/ml and suitable for inhalation. It is sprayed on lactose powder and coated in a fludized bed device and It is coated using temperatures not exceeding 50°C. Quantity at the end of coating When the determination is made, approximately 0.5 -1 mg of eucalyptus essential oil and 0.5 -1 mg of eucalyptus essential oil in 1 dose of powder mg of carvacrol. The powder prepared in this way is directly breathed into the lungs. It is filled into hard gelatin or similar capsules to be taken and administered by inhalation. given to patients. The device for inhalation is any powder inhaler it could be.

Bu bulusta antiviral kombinasyonuna ek antiviral veya antienflamatuvar etkisi ile bilinen diger ajanlar katilabilir. Diger ajanlar arasinda bomeol, epigallokatesin gallat sayilabilir. Bulusun diger antiviral ve antienflamatuvar ajanlarla kombinasyonu burada anlatilanlarla sinirli degildir. In this invention, it has an antiviral or anti-inflammatory effect in addition to the antiviral combination. Other known agents may be involved. Other agents include bomeol, epigallocatecin gallates. of the invention with other antiviral and anti-inflammatory agents. combination is not limited to what is described here.

Bulusun sanayiye uygulanma biçimi Bu bulusta verilen formül akiskan yatak cihazinda inhalasyona uygun laktoza yüklenir ve kurutulur. Daha sonra kapsül doldurma cihazinda istenen miktarlar sert jelatin kapsüllere doldunilur ve blister ambalaj içine konulur. Sanayide rutinde kullanilan cihaz ve ekipman ile çok kolaylikla üretilebilecek bir formüldür. How the invention is applied to industry The formula given in this invention is lactose suitable for inhalation in a fluidized bed device. loaded and dried. Then the desired quantities in the capsule filling device filled into hard gelatin capsules and placed in blister packs. in industry It is a product that can be produced very easily with the devices and equipment used in the routine. is the formula.

Claims (1)

ISTEMLER . Bu bulus akcigerlere dogrudan inhalasyon ile verilebilecek ve toz formda kombine eucalyptus uçucu yagi ve karvakrol içeren kapsüllerdir. . Bu bulus Istem lide belirtilen kapsül olup, özelligi laktoza yüklemis eucalyptus uçucu yagi ve karvakrol ihtiva etmesi ve bir doz inhalasyon tozunda eucalyptus uçucu yagi ve karvakrolun herbirinin en fazla 1 mg/ml olmasidir. . Bu bulus Istem 2”de belirtilen kapsül olup ayrica bomeol içerir. . Bu bulus Istem 3”de belirtilen kapsül olup, özelligi laktoza yüklemis bomeol ihtiva etmesidir. . Bu bulus Istem 2'de veya Istem 3ide belirtilen kapsül olup ayrica . Bu bulus Istem 5”de belirtilen kapsül olup, Özelligi laktoza yüklemis epigallokatesin gallat ihtiva etmesidir. . Yukaridaki istemlerin herhangi birine göre olan ve SARS COV-2 enfeksiyonlarinin tedavi etme metodu için kullanilan ürün.REQUESTS . This invention is capsules containing combined eucalyptus essential oil and carvacrol in powder form, which can be administered by direct inhalation into the lungs. . This invention is the claimed capsule, its feature is that it contains lactose-loaded eucalyptus essential oil and carvacrol, and each of eucalyptus essential oil and carvacrol in a dose of inhalation powder is maximum 1 mg/ml. . This invention is the capsule as claimed in claim 2 and also contains bomeol. . This invention is the capsule specified in Claim 3, and its feature is that it contains bomeol loaded with lactose. . The invention is the capsule as claimed in claim 2 or claim 3, further comprising . This invention is the capsule specified in Claim 5, and its feature is that it contains lactose-loaded epigallocatecin gallate. . The product according to any of the preceding claims, used for the method of treating SARS COV-2 infections.
TR2020/22087A 2020-12-28 2020-12-28 Inhalation Powder for SARS Cov-2 Infections TR202022087A2 (en)

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