1. Nā waiwai kumu o HPMC
Hypromellose, inoa piha hydroxypropyl methylcellulose, alias HPMC. ʻO kona molecular formula C8H15O8-(C10Hl8O6)n-C8Hl5O8, aʻo kona kaumaha mole e pili ana i 86000. ʻO kēia huahana he mea semi-synthetic, he hapa ia o ka methyl a me ka hapa o ka polyhydroxypropyl ether o cellulose. Hiki ke hana ʻia ma nā ʻano ʻelua: ʻo ka hoʻokahi ʻo ka mālama ʻia ʻana o ka māka kūpono o ka methyl cellulose me NaOH, a laila hoʻopili ʻia me ka propylene oxide ma lalo o ke kiʻekiʻe o ka wela a me ke kaomi. Hoʻopili ʻia ke ʻano i ke apo anhydroglucose o cellulose, a hiki ke hiki i ka pae kūpono; ʻO ka mea ʻē aʻe e mālama i ka pulupulu linter a i ʻole ka pulupulu lāʻau pulupulu me ka soda caustic, a e hana me ka methyl chloride a me ka propylene oxide i mea e loaʻa ai, a laila e hoʻomaʻemaʻe hou aʻe, e ʻoki ʻia e hana i ka pauka a i ʻole granules. He ʻano like ʻole o ka cellulose mea kanu maoli ʻo HPMC, a he mea hoʻohana maikaʻi loa ia no ka lāʻau lapaʻau, a he nui nā kumu. I kēia manawa, hoʻohana nui ʻia ia ma ka home a ma waho, a ʻo ia kekahi o nā mea hoʻohana lāʻau lapaʻau me ka helu kiʻekiʻe o ka hoʻohana ʻana i nā lāʻau lapaʻau waha.
He keʻokeʻo kēia huahana a hiki i ka waiu keʻokeʻo i ka waihoʻoluʻu, ʻaʻohe mea ʻawaʻawa a ʻono ʻole, a aia ma ke ʻano o ka pauda granular a i ʻole fibrous e kahe maʻalahi. Ua kūpaʻa ʻo ia ma lalo o ka ʻike māmā a me ka haʻahaʻa. Huhū ia i loko o ka wai anuanu e hana i ka waiu keʻokeʻo colloidal solution, nona kahi degere o ka viscosity, a hiki ke ʻano o ka sol-gel interconversion ma muli o ka hoʻololi ʻana o ka mahana o kekahi ʻano o ka hopena. Hiki ke hoʻoheheʻe ʻia i loko o 70% waiʻona a i ʻole dimethyl ketone, ʻaʻole e hoʻoheheʻe ʻia i loko o ka waiʻona piha, chloroform a ethoxyethane paha.
Aia ka pH o hypromellose ma waena o 4.0 a me 8.0, he kūpaʻa maikaʻi kona, a hiki ke noho paʻa ke noho ka pH ma waena o 3.0 a me 11.0. Ke 20 ° C ka mahana a ʻo ka haʻahaʻa haʻahaʻa he 80%, mālama ʻia no 10 mau lā. He 6.2% ka nui o ka hoʻoheheʻe ʻana o ka wai o HPMC.
Ma muli o ka ʻokoʻa o ka methoxy a me ka hydroxypropyl i ke ʻano o ka hypromellose, ua ʻike ʻia nā ʻano huahana like ʻole. I nā kikoʻī kikoʻī, loaʻa nā ʻano huahana like ʻole i ka viscosity kikoʻī a me nā mahana gelation Thermal, no laila, loaʻa nā waiwai like ʻole a hiki ke hoʻohana ʻia no nā kumu like ʻole. ʻO nā pharmacopoeias o nā ʻāina like ʻole he ʻokoʻa nā lula a me nā hiʻohiʻona o nā hiʻohiʻona: ʻo ka European Pharmacopoeia, e like me nā māka like ʻole o nā viscosities like ʻole a me nā degere o ka hoʻololi ʻana i nā huahana i kūʻai ʻia ma ka mākeke, ua hōʻike ʻia e nā māka me nā helu, a ʻo ka mPa ·s; i ka United States Pharmacopoeia, ka inoa maʻamau E hoʻohui i nā huahelu 4 ma ka hope e hōʻike i ka ʻike a me ke ʻano o kēlā me kēia mea pani o hypromellose, e like me hypromellose 2208, ʻo nā huahelu mua ʻelua e hōʻike ana i ka pākēneka kokoke o ka methoxy, a ʻo nā huahelu ʻelua hope e hōʻike ana i ka hydroxypropyl. Pākēneka pili.
2. Ke ano o ka hoopau ana i ka HPMC i ka wai
2.1 ʻano wai wela
ʻAʻole hoʻoheheʻe ʻia ka hypromellose i ka wai wela, hiki ke hoʻopuehu like ʻia i ka wai wela i ka hoʻomaka ʻana, a laila hoʻomaha. ʻElua mau ʻano maʻamau i wehewehe ʻia penei:
(1) E hoʻokomo i ka nui o ka wai wela i loko o ka pahu, a wela iā ia ma kahi o 70 ° C, e hoʻohui mālie i kēia huahana ma lalo o ka hoʻoulu lohi, i ka hoʻomaka ʻana, lana kēia huahana ma ka ʻili o ka wai, a laila hana mālie slurry, stirring E hooluolu i ka slurry ilalo.
(2) E hoʻohui i 1/3 a i ʻole 2/3 o ka nui o ka wai i makemake ʻia i loko o ka pahu a hoʻomehana iā 70 ° C e hoʻopuehu i ka huahana e hoʻomākaukau i kahi slurry wai wela, a laila e hoʻohui i ke koena o ka wai anuanu a i ʻole ka wai hau a hiki i ka wai wela I loko o kahi slurry, hoʻoluʻu ka hui ʻana ma hope o ka hoʻoulu ʻana.
2.2 ʻano hui ʻana o ka pauda
Hoʻopuehu piha ʻia nā ʻāpana pauda e ka hui ʻana me ka nui like a ʻoi aku paha o nā mea pauda, a laila hoʻoheheʻe ʻia i ka wai. I kēia manawa, hiki ke hoʻoheheʻe ʻia ka hypromellose me ka ʻole o ka agglomeration.
3. Pono o HPMC
3.1 Hiki i ka wai anuanu
Hiki ke hoʻoheheʻe ʻia i loko o ka wai anuanu ma lalo o 40°C a i ʻole 70% ethanol, ʻaʻole hiki ke hoʻoheheʻe ʻia i ka wai wela ma luna o 60°C, akā hiki ke hoʻoheheʻe ʻia.
3.2 Kemika inertness
ʻO Hypromellose (HPMC) kahi ʻano o ka cellulose ether non-ionic. ʻAʻohe o ka hoʻonā ionic charge a ʻaʻole pili pū me nā paʻakai metala a i ʻole nā pūhui organik ionic. No laila, ʻaʻole i pane aku nā mea ʻē aʻe me ia i ka wā o ka hoʻomākaukau ʻana.
3.3 Paʻa
He paʻa paʻa ia i ka waikawa a me ka alkali, a hiki ke mālama ʻia no ka manawa lōʻihi ma waena o ka pH 3 a me 1l me ka ʻole o ka loli ʻana o ka viscosity. ʻO ka hopena wai o hypromellose (HPMC) he hopena anti-mildew a hiki ke mālama i ka paʻa viscosity maikaʻi i ka wā mālama lōʻihi. ʻO nā lāʻau lapaʻau e hoʻohana ana i ka HPMC ma ke ʻano he mea hoʻopōmaikaʻi ʻoi aku ka maikaʻi o ka paʻa ma mua o ka poʻe e hoʻohana ana i nā excipients kuʻuna (e like me dextrin, starch, etc.).
3.4 Hiki ke hoʻololi i ka viscosity
Hiki ke hui pū ʻia nā derivatives viscosity like ʻole o HPMC e like me nā lakio like ʻole, a hiki ke hoʻololi i kona viscosity e like me kekahi mau lula, a he pilina laina maikaʻi, no laila hiki ke koho ʻia ka lākiō e like me nā koi.
3.5 Metabolic inertia
ʻAʻole hoʻokomo ʻia ʻo HPMC a i ʻole metabolized i loko o ke kino, ʻaʻole hāʻawi i ka wela, no laila he mea hoʻomākaukau lāʻau palekana palekana.
3.6 Palekana
Manaʻo nui ʻia ʻo HPMC he mea ʻawaʻawa ʻole a hoʻonāukiuki ʻole. He 5g/kg ka nui o ka make make no ka iole, a he 5.2g/kg ka nui o ka make make no ka iole. ʻAʻole pōʻino i nā kānaka ka nui o kēlā me kēia lā.
4. Hoʻohana ʻana i ka HPMC i ka hoʻomākaukau ʻana
4.1 Ma ke ʻano he mea uhi kiʻiʻoniʻoni a me nā mea hana kiʻiʻoniʻoni
ʻO ka hoʻohana ʻana i ka hypromellose (HPMC) ma ke ʻano he papa kiʻiʻoniʻoni i hoʻopaʻa ʻia, i hoʻohālikelike ʻia me nā papa kuʻuna i uhi ʻia e like me nā papa i uhi ʻia i ke kō, ʻaʻohe pono o nā papa i uhi ʻia i ka uhi ʻana i ka ʻono o ka lāʻau lapaʻau a me ke ʻano, akā ʻo ko lākou paʻakikī a me ka friability, ka hoʻoheheʻe ʻana i ka wai, ʻoi aku ka maikaʻi o ka wehe ʻana, ka uhi ʻana i ke kaumaha a me nā hōʻailona maikaʻi ʻē aʻe. Hoʻohana ʻia ka haʻahaʻa haʻahaʻa haʻahaʻa o kēia huahana ma ke ʻano he mea hoʻoheheʻe kiʻiʻoniʻoni wai no nā papa a me nā pila, a hoʻohana ʻia ka pae kiʻekiʻe-viscosity ma ke ʻano he kiʻi ʻoniʻoni no nā ʻōnaehana solvent organik. ʻO ka maʻamau ka 2.0% a 20%.
4.2 E like me ka mea hoʻopaʻa a me ka hoʻokaʻawale
Hiki ke hoʻohana ʻia ka papa haʻahaʻa haʻahaʻa o kēia huahana ma ke ʻano he mea hoʻopaʻa a me ka disintegrant no nā papa, nā pila, a me nā granules, a hiki ke hoʻohana wale ʻia ke kiʻekiʻe-viscosity ma ke ʻano he mea hoʻopili. ʻOkoʻa ka dosage me nā ʻano like ʻole a me nā koi. ʻO ka maʻamau, ʻo ke ʻano o ka binder no nā papa granulation maloʻo he 5%, a ʻo ke ʻano o ka binder no nā papa granulation maloʻo he 2%.
4.3 Ma ke ʻano he luna hoʻomaha
ʻO ka mea hoʻopaneʻe he mea gel viscous me ka hydrophilicity, hiki ke hoʻolohi i ka wikiwiki o ka sedimentation o nā ʻāpana i ka wā e hoʻohana ʻia ai i ka mea hoʻokuʻu, a hiki ke hoʻopili ʻia i ka ʻili o nā ʻāpana e pale ai i nā ʻāpana mai ka hōʻuluʻulu ʻana a me ka emi ʻana i loko o kahi pōpō. . He kuleana koʻikoʻi nā mea hoʻokuʻu i ka hana ʻana i nā hoʻokuʻu. He ʻano maikaʻi loa ʻo HPMC o nā mea hoʻopaneʻe, a hiki i kāna solution colloidal hoʻoheheʻe ke hoʻemi i ka ʻāʻī o ka wai-paʻa paʻa a me ka ikehu manuahi ma nā ʻāpana paʻa liʻiliʻi, a laila e hoʻonui ai i ke kūpaʻa o ka ʻōnaehana heterogeneous dispersion. Hoʻohana ʻia ka pae kiʻekiʻe-viscosity o kēia huahana ma ke ʻano he hoʻomākaukau wai wai hoʻomaha i hoʻomākaukau ʻia ma ke ʻano he mea hoʻomaha. Loaʻa iā ia kahi hopena hoʻomaha maikaʻi, maʻalahi e hoʻopuʻi hou, ʻaʻole pili i ka paia, a loaʻa nā ʻāpana flocculated maikaʻi. ʻO ka dosage maʻamau he 0.5% a 1.5%.
4.4 Ma ke ʻano he blocker, hoʻokuʻu hoʻomau a me ka mea hoʻoheheʻe pore
Hoʻohana ʻia ka papa kiʻekiʻe-viscosity o kēia huahana no ka hoʻomākaukau ʻana i ka hydrophilic gel matrix sustained-release papa, blockers a me nā mea hoʻokuʻu hoʻokuʻu ʻia no nā papa hoʻokuʻu ʻia matrix matrix, a loaʻa iā ia ka hopena o ka hoʻopaneʻe ʻana i ka lāʻau lapaʻau. ʻO 10% ~ 80% (W / W) kona hoʻohana ʻana. Hoʻohana ʻia nā māka haʻahaʻa haʻahaʻa ma ke ʻano he pore-forming agents no ka hoʻomau hoʻokuʻu ʻana a i ʻole hoʻomākaukau hoʻokuʻu ʻia. Hiki ke hoʻokō koke ʻia ka hopena mua i koi ʻia no ka hopena therapeutic o kēia ʻano papa, a laila e hoʻokau i kahi hopena hoʻokuʻu a hoʻokuʻu ʻia paha, a mālama ʻia ke ʻano o ka lāʻau lapaʻau kūpono i ke kino. Ke hui ka hypromellose i ka wai, hoʻomaʻemaʻe ia e hana i kahi papa gel. ʻO ke ʻano o ka hoʻokuʻu ʻana i ka lāʻau mai ka papa matrix ka mea nui i ka diffusion o ka papa gel a me ka erosion o ka papa gel.
4.5 Ke kāpili pale e like me ka mānoanoa a me ka colloid
Ke hoʻohana ʻia kēia huahana e like me ka mānoanoa, ʻo ka hoʻohana maʻamau ʻo 0.45% ~ 1.0%. Hiki i kēia huahana ke hoʻonui i ka paʻa o ka hydrophobic glue, hana i kahi colloid pale, pale i nā ʻāpana mai ka agglomerating a me ka agglomerating, no laila ke kāohi nei i ka hoʻokumu ʻana o ka sediment, a ʻo kona ʻano maʻamau he 0.5% ~ 1.5%.
4.6 Mea hoʻopaʻa no nā capsules
ʻO ka mea maʻamau, hoʻokumu ʻia ka mea capsule shell capsule ma ka gelatin. He maʻalahi ke kaʻina hana o ka gelatin capsule shell, akā aia kekahi mau pilikia a me nā hanana e like me ka pale maikaʻi ʻole i ka wai a me nā lāʻau lapaʻau oxygen, haʻahaʻa haʻahaʻa lāʻau dissolution, a lohi i ka wehe ʻana o ka pūpū capsule i ka wā mālama. No laila, hoʻohana ʻia ka hypromellose, ma ke ʻano he pani no nā capsules gelatin, i ka hoʻomākaukau ʻana i nā capsules, kahi e hoʻomaikaʻi ai i ka formability a me ka hoʻohana ʻana i ka hopena o nā capsules, a ua hoʻolaha nui ʻia ma ka home a ma waho.
4.7 e like me ka bioadhesive
ʻO ka ʻenehana Bioadhesion, ka hoʻohana ʻana i nā excipients me nā polymers bioadhesive, ma o ka hoʻopili ʻana i ka mucosa biological, hoʻonui i ka hoʻomau a me ka paʻa o ka pilina ma waena o ka hoʻomākaukau ʻana a me ka mucosa, i hoʻokuʻu mālie ʻia ka lāʻau lapaʻau e ka mucosa e hoʻokō i nā kumu therapeutic. Hoʻohana nui ʻia i kēia manawa Hoʻohana ʻia e mālama i nā maʻi o ka nasal cavity, waha mucosa a me nā ʻāpana ʻē aʻe. ʻO ka ʻenehana bioadhesion gastrointestinal kahi ʻōnaehana lawe lāʻau hou i kūkulu ʻia i nā makahiki i hala. ʻAʻole ia e hoʻolōʻihi i ka manawa noho o ka hoʻomākaukau lāʻau lapaʻau ma ka ʻōpū o ka ʻōpū, akā hoʻomaikaʻi pū i ka hana pili ma waena o ka lāʻau lapaʻau a me ka membrane cell ma ka wahi absorption, hoʻololi i ka wai o ka membrane cell, Hoʻonui i ke komo ʻana o ka lāʻau i ka ʻōpū. nā pūnaewele epithelial, e hoʻomaikaʻi ai i ka bioavailability o ka lāʻau.
4.8 E like me ka gel topical
Ma ke ʻano he hoʻomākaukau paʻa no ka ʻili, loaʻa i ka gel kahi ʻano o nā pono e like me ka palekana, ka nani, ka hoʻomaʻemaʻe maʻalahi, ke kumu kūʻai haʻahaʻa, ke kaʻina hana hoʻomākaukau maʻalahi, a me ka launa maikaʻi me nā lāʻau lapaʻau. kuhikuhi.
Ka manawa hoʻouna: Dec-15-2022