Gabatarwa ga asali kaddarorin da aikace-aikace na Pharmaceutical sa hypromellose (HPMC)

1. Asalin yanayin HPMC
Hypromellose, sunan Ingilishi hydroxypropyl methylcellulose, wanda aka fi sani da HPMC. Tsarin kwayoyin halittarsa ​​shine C8H15O8-(C10Hl8O6)n-C8Hl5O8, kuma nauyin kwayoyin yakai kusan 86,000. Wannan samfurin wani abu ne na semi-synthetic, wanda shine ɓangare na ƙungiyar methyl kuma wani ɓangare na polyhydroxypropyl ether na cellulose. Ana iya ƙera shi ta hanyoyi biyu: ɗaya shine a bi da methyl cellulose na darajar da ta dace tare da NaOH, sa'an nan kuma mayar da martani tare da propylene oxide a ƙarƙashin yanayin zafi da matsa lamba. Dole ne a ci gaba da ɗaukar lokaci don ba da damar ƙungiyoyin methyl da hydroxypropyl su haɗa tare da ether. An haɗa nau'in nau'in zuwa zoben anhydroglucose na cellulose, kuma zai iya kaiwa matakin da ake so; ɗayan kuma shine a yi maganin linter na auduga ko fiber ɓangaren itace tare da soda caustic, sannan a samu ta hanyar amsawa da methane mai chlorinated da propylene oxide a jere, sannan a ƙara tacewa , Pulverize, sanya ta zama foda mai kyau da uniform ko granule. HPMC iri-iri ne na cellulose na tsire-tsire na halitta, kuma yana da kyakkyawan kayan haɓaka magunguna, wanda ke da tushe mai fa'ida. A halin yanzu, ana amfani da shi sosai a gida da waje, kuma yana ɗaya daga cikin abubuwan da ake amfani da su na magunguna waɗanda aka fi amfani da su a cikin magungunan baka.

 

Launin wannan samfurin fari ne zuwa fari mai madara, mara guba kuma maras ɗanɗano, kuma yana da granular ko fibrous, foda mai sauƙi. Yana da ɗan kwanciyar hankali a ƙarƙashin hasken haske da zafi. Yana kumbura a cikin ruwan sanyi don samar da maganin colloidal fari madara mai ɗanɗano kaɗan. Al'amarin sol-gel interconversion na iya faruwa saboda canjin yanayin zafi na wani taro na bayani. Yana da sauƙin narkewa a cikin 70% barasa ko dimethyl ketone, kuma ba zai narke a cikin barasa mai anhydrous, chloroform ko ethoxyethane.

Hypromellose yana da kyakkyawan kwanciyar hankali lokacin da pH ke tsakanin 4.0 da 8.0, kuma yana iya kasancewa a tsaye tsakanin 3.0 da 11.0. Bayan adanawa na kwanaki 10 a zafin jiki na 20 ° C da ƙarancin dangi na 80%, ƙimar shayar da danshi na HPMC shine 6.2%.

Saboda bambance-bambance a cikin abubuwan maye biyu a cikin tsarin hypromellose, methoxy da hydroxypropyl, nau'ikan samfuran sun bayyana. A cikin takamaiman ƙaddamarwa, nau'ikan samfura daban-daban suna da takamaiman danko da zafin jiki na thermal, sabili da haka, yana da kaddarorin daban-daban kuma ana iya amfani dashi don dalilai daban-daban. Pharmacopoeias na ƙasashe daban-daban suna da ƙayyadaddun ƙayyadaddun bayanai da maganganu daban-daban don ƙirar: Tsarin Pharmacopoeia na Turai yana dogara ne akan nau'ikan nau'ikan nau'ikan viscosities daban-daban da digiri daban-daban na maye gurbin samfuran a kasuwa. An bayyana ta da daraja da lamba. Naúrar ita ce mPa•s. Bayan ƙara lambobi 4 don nuna abun ciki da nau'in kowane madaidaicin hypromellose, alal misali, hypromellose 2208, lambobi biyu na farko suna wakiltar kusan kashi na ƙungiyar methoxy, lambobi biyu na ƙarshe suna wakiltar hydroxypropyl Kimanin kaso na lokuta.

2.Hanyar narkar da HPMC a cikin ruwa

2.1 Hanyar ruwan zafi

Tun da hypromellose ba ya narkewa a cikin ruwan zafi, ana iya tarwatsa shi daidai a cikin ruwan zafi a matakin farko, sannan lokacin da aka sanyaya, ana bayyana hanyoyi guda biyu kamar haka:

(1) Sanya adadin ruwan zafi da ake buƙata a cikin akwati da zafi da shi zuwa kusan 70 ℃. A hankali ƙara samfurin a ƙarƙashin jinkirin motsawa. A farkon, samfurin yana iyo a saman ruwa, sa'an nan kuma a hankali ya samar da slurry. Kwantar da slurry.

(2) Ƙara 1/3 ko 2/3 na adadin ruwan da ake buƙata a cikin kwandon kuma zafi shi zuwa 70 ° C don tarwatsa samfurin don shirya ruwan zafi, sannan ƙara sauran adadin ruwan sanyi ko ruwan kankara. zuwa slurry ruwan zafi A cikin slurry, kwantar da cakuda bayan motsawa.

2.2 Hanyar hada foda
Barbashi na foda da sauran sinadaran foda na daidai ko babba ana watse su ta hanyar busassun hadawa, sannan a zuba ruwa ya narke. A wannan lokacin, ana iya narkar da hypromellose ba tare da agglomeration ba.

3. Amfanin HPMC

3.1 Ruwa mai sanyi

Yana narkewa a cikin ruwan sanyi ƙasa da 40 ° C ko 70% ethanol. Yana da m insoluble a cikin ruwan zafi sama da 60 ° C, amma za a iya gelled.

3.2 Rashin kuzarin sinadari

Hypromellose (HPMC) wani nau'in ether ne wanda ba na ionic cellulose ba. Maganin sa ba shi da cajin ionic kuma baya mu'amala da gishirin ƙarfe ko mahaɗan kwayoyin ionic. Sabili da haka, sauran abubuwan haɓaka ba sa amsawa tare da shi yayin tsarin shirye-shiryen.

3.3 Kwanciyar hankali

Yana da ingantacciyar tsayayye ga duka acid da alkali, kuma ana iya adana shi na dogon lokaci tsakanin pH 3 zuwa 1l, kuma dankowar sa ba shi da wani canji na zahiri. Maganin ruwa mai ruwa na hypromellose (HPMC) yana da tasirin anti-mold kuma yana iya kula da kwanciyar hankali mai kyau yayin ajiya na dogon lokaci. Abubuwan da ake amfani da magunguna masu amfani da HPMC suna da ingantacciyar kwanciyar hankali fiye da waɗanda ke amfani da abubuwan haɓaka na gargajiya (kamar dextrin, sitaci, da sauransu).

3.4 Daidaitawar danko

Ana iya haɗa nau'o'in danko daban-daban na HPMC a cikin nau'i daban-daban, kuma dankon sa na iya canzawa bisa ga ƙayyadaddun ƙa'ida, kuma yana da dangantaka mai kyau na layi, don haka za'a iya zaɓar shi bisa ga bukatun.

3.5 Metabolic inertia

HPMC ba a tunawa ko metabolized a cikin jiki, kuma baya samar da adadin kuzari, don haka yana da aminci ga shirye-shiryen magani.

3.6 Tsaro

An yi imani da cewa HPMC abu ne mara guba kuma maras haushi. Matsakaicin kisa ga berayen shine 5g/kg, kuma matsakaicin adadin kisa na berayen shine 5.2g/kg. Adadin yau da kullun ba shi da lahani ga jikin ɗan adam.

4. Aikace-aikacen HPMC a cikin shirye-shirye

4.1 An yi amfani da shi azaman kayan shafa na fim da kayan ƙirƙirar fim

Ana amfani da Hypromellose (HPMC) azaman abun kwamfutar hannu mai rufin fim. Idan aka kwatanta da na gargajiya mai rufi Allunan irin su sugar-rufi Allunan, da rufi Allunan ba su da wani fili abũbuwan amfãni a masking da dandano da kuma bayyanar, amma su taurin da friability , Danshi sha, disintegration, shafi nauyi riba da sauran ingancin Manuniya ne mafi alhẽri. Ana amfani da ƙarancin danko na wannan samfurin azaman kayan shafa na ruwa mai narkewa don allunan da kwaya, kuma ana amfani da madaidaicin madaidaicin azaman kayan shafa na fim don tsarin narkewar ƙwayoyin cuta. Matsakaicin amfani shine yawanci 2.0% -20%.

4.2 a matsayin mai ɗaure da tarwatsewa

Za'a iya amfani da ƙarancin danko na wannan samfurin azaman mai ɗaure da rarrabuwa don allunan, kwaya, da granules, kuma babban ma'aunin danko kawai za'a iya amfani dashi azaman mai ɗaure. Matsakaicin ya bambanta da samfura da buƙatu daban-daban. Gabaɗaya, adadin abin ɗaure da aka yi amfani da shi don busassun allunan granulation shine 5%, kuma adadin abin da ake amfani da shi don rigar granulation shine 2%.

4.3 A matsayin wakili mai dakatarwa

Wakilin dakatarwa wani abu ne na gel danko tare da hydrophilicity. Yin amfani da wakili mai dakatarwa a cikin wakili mai dakatarwa zai iya rage saurin raguwar ƙwayoyin cuta, kuma ana iya haɗa shi zuwa saman ɓangarorin don hana ƙwayoyin daga polymerizing da condensing cikin taro. Wakilan da aka dakatar suna taka muhimmiyar rawa wajen samar da dakatarwa. HPMC shine kyakkyawan nau'ikan wakilai masu dakatarwa. Maganin colloidal da aka narkar da shi zai iya rage tashin hankali na ƙirar ruwa mai ƙarfi da kuma makamashi kyauta akan ƙananan ƙananan ƙwayoyin cuta, don haka inganta kwanciyar hankali na tsarin watsawa daban-daban. Wannan samfurin babban shiri ne na dakatarwar ruwa wanda aka shirya azaman wakili mai dakatarwa. Yana da tasiri mai kyau na dakatarwa, mai sauƙin tarwatsawa, mara ɗorewa, da ƙaƙƙarfan barbashi masu yawo. Adadin da aka saba shine 0.5% zuwa 1.5%.

4.4 An yi amfani da shi azaman mai toshewa, jinkirin da wakili mai sarrafawa da wakili mai haifar da pore

Ana amfani da babban ma'aunin danko na wannan samfurin don shirya allunan ci gaba na hydrophilic gel matrix, masu sakewa da kuma wakilai-saki don allunan ci-gaban-saki-matrix matrix. Yana da tasirin jinkirta sakin miyagun ƙwayoyi. Yawan amfani da shi shine 10% ~ 80% (W / W). Ana amfani da ƙarancin dankowa azaman wakili mai haifar da pore don dorewa ko sarrafa tsarin sakin. Matsakaicin farko da ake buƙata don tasirin warkewa na wannan nau'in kwamfutar hannu za a iya kai shi da sauri, sannan ana aiwatar da sakamako mai dorewa ko sarrafawa, kuma ana kiyaye tasirin magungunan jini mai inganci a cikin jiki. Hypromellose hydrates don samar da gel Layer lokacin da ya hadu da ruwa. Hanyar sakin miyagun ƙwayoyi daga kwamfutar hannu na matrix shine yafi yaduwa na gel Layer da kuma yashwar gel Layer.

4.5 Manne mai kariya da aka yi amfani da shi azaman mai kauri da colloid

Lokacin da aka yi amfani da wannan samfurin azaman thickener, da aka saba maida hankali ne 0.45% ~ 1.0%. Wannan samfurin kuma zai iya ƙara kwanciyar hankali na manne hydrophobic, samar da colloid mai kariya, hana barbashi coalescence da agglomeration, game da shi hana samuwar sediments. Matsayinsa na yau da kullun shine 0.5% ~ 1.5%.

4.6 Ana amfani dashi azaman kayan capsule

Yawancin lokaci, kayan kwalliyar capsule na capsule shine yafi gelatin. Tsarin samar da harsashi na capsule na Ming abu ne mai sauki, amma akwai wasu matsaloli da al'amura kamar rashin kariya daga danshi da magungunan da ke da iskar oxygen, rage narkar da kwayoyi, da jinkirin wargajewar harsashi na capsule yayin ajiya. Sabili da haka, ana amfani da hypromellose a matsayin maye gurbin kayan kwalliya a cikin shirye-shiryen capsules, wanda ke inganta gyare-gyare da amfani da tasirin capsule, kuma an inganta shi sosai a gida da waje.

4.7 A matsayin bioadhesive

Fasahar bioadhesive, aikace-aikacen abubuwan haɓakawa tare da polymers masu haɓakawa, ta hanyar mannewa ga mucosa na ilimin halitta, haɓaka ci gaba da matsawa na hulɗar da ke tsakanin shirye-shiryen da mucosa, don haka ana fitar da miyagun ƙwayoyi a hankali kuma a shayar da mucosa don cimma manufar. magani. An yi amfani da shi sosai a yanzu Ana amfani da shi don magance cututtuka na kogon hanci da kuma mucosa na baki. Fasahar bioadhesion na hanji sabon nau'in tsarin isar da magunguna ne wanda aka haɓaka a cikin 'yan shekarun nan. Ba wai kawai yana tsawaita lokacin zama na shirye-shiryen miyagun ƙwayoyi a cikin ƙwayar gastrointestinal ba, amma kuma yana inganta aikin tuntuɓar miyagun ƙwayoyi tare da ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta. Ƙarfin shigar da miyagun ƙwayoyi zuwa sel na epithelial na ƙananan hanji yana inganta, ta haka yana inganta bioavailability na miyagun ƙwayoyi.

4.8 A matsayin Gel

A matsayin shirye-shiryen m don fata, gel yana da jerin fa'idodi irin su aminci, kyakkyawa, tsaftacewa mai sauƙi, ƙananan farashi, tsari mai sauƙi na shirye-shirye, da kuma dacewa mai kyau tare da kwayoyi. A cikin 'yan shekarun nan, ya sami kulawa mai yawa kuma ya zama ci gaban shirye-shiryen waje na fata. hanya.

4.9 A matsayin mai hana hazo a cikin tsarin emulsification


Lokacin aikawa: Dec-16-2021