ʻO nā mea hoʻohui maʻamau o nā ʻano hoʻopaʻa paʻa waha

ʻO ka hoʻomākaukau paʻa i kēia manawa ka mea i hoʻolaha nui ʻia a hoʻohana nui ʻia i ka mākeke, a ʻelua mau mea nui a me nā excipients. ʻO nā excipients, ʻike ʻia hoʻi he excipients, e pili ana i ka huaʻōlelo maʻamau no nā mea hou aʻe i loko o ka hoʻomākaukau paʻa koe wale nō ka lāʻau lapaʻau nui. Wahi a nā ʻano like ʻole a me nā hana o nā excipients, ua hoʻokaʻawale pinepine ʻia nā excipients o ka hoʻomākaukau paʻa i: fillers, binders, disintegrants, lubricants, release regulators, a i kekahi manawa hiki ke hoʻohui ʻia nā mea pena a me nā mea ʻono e like me nā koi o ka hoʻomākaukau. e hoʻomaikaʻi A i ʻole e hoʻoponopono i ke ʻano a me ka ʻono o ka hoʻokumu ʻana.
Pono nā mea kōkua o ka hoʻomākaukau paʻa e hoʻokō i nā koi no ka hoʻohana ʻana i ka lāʻau lapaʻau, a loaʻa iā ia nā ʻano penei: ①Pono ke kūpaʻa kemika kiʻekiʻe a ʻaʻohe hopena kino a me ka lāʻau nui; ②ʻAʻole pono e hoʻopili i ka hopena therapeutic a me ka hoʻoholo ʻana i ka ʻike o ka lāʻau nui; ③ʻAʻohe pōʻino i ke kino o ke kanaka He ʻino, ʻelima mau mea make, ʻaʻohe hopena ʻino.
1. Hoʻopiha (mea lahilahi)
Ma muli o ka haʻahaʻa haʻahaʻa o ka lāʻau lapaʻau nui, ʻo ka nui o kekahi mau lāʻau i kekahi manawa he mau milligrams a i ʻole ka liʻiliʻi, ʻaʻole kūpono i ka hoʻokumu ʻana i ka papa a i ʻole ka hoʻokele lāʻau lapaʻau. No laila, inā emi ka nui o ka lāʻau lapaʻau ma mua o 50mg, pono e hoʻohui ʻia kahi ʻano o ka hoʻopihapiha, i ʻike ʻia ʻo diluent.
Pono ka mea hoʻopihapiha kūpono i ka physiologically a me ka chemically inert a ʻaʻole pili i ka bioavailability o ka mea hana o ka lāʻau lapaʻau. ʻO nā mea hoʻopiha maʻamau e hoʻohana nui ʻia: ① Starch, me ka starch palaoa, ka starch kulina, a me ka starch uala, a ma waena o ia mea ʻo ka starch ka mea maʻamau i hoʻohana ʻia; paʻa i ke ʻano, haʻahaʻa i ka hygroscopicity, akā ʻilihune i ka compressibility; ② Lactose, maikaʻi i loko o nā waiwai a me ka compressible, maikaʻi fluidity; ③ sucrose, he hygroscopicity ikaika; ④ pregelatinized starch, i ʻike ʻia ʻo ka starch compressible, loaʻa ka compressibility maikaʻi, ka wai a me ka lubricity ponoʻī; ⑤ microcrystalline cellulose, i kapa ʻia ʻo MCC, he ikaika hoʻopaʻa paʻa a me ka compressibility maikaʻi; ʻike ʻia ʻo "dry binder"; ⑥Mannitol, i hoʻohālikelike ʻia me nā mea hoʻopihapiha ma luna, ua ʻoi aku ke kumu kūʻai, a hoʻohana pinepine ʻia i nā papa chewable, a he ʻono ʻono hoʻi; ⑦ ʻO nā paʻakai anorganic, ka mea nui me ka calcium sulfate, ka calcium phosphate, ka calcium carbonate, a me nā mea ʻē aʻe, me nā waiwai kino a me nā kemika.
2. Mea hoʻomaloʻo a hoʻopili
ʻO nā mea hoʻomaʻemaʻe a me nā mea hoʻopaʻa i hoʻohui ʻia i ka wā o ka granulation. ʻO ka mea hoʻomaʻemaʻe pono'īʻaʻole ia he viscous, akā, he wai e hoʻoulu ai i ka viscosity o ka mea ma ka puluʻana i ka mea. ʻO ka wai hoʻomaʻemaʻe a me ka ethanol ka mea maʻamau i hoʻohana ʻia, ʻo ia ka wai hoʻomaʻemaʻe ke koho mua.
ʻO nā mea hoʻopili e pili ana i nā mea kōkua e hilinaʻi nei i ko lākou viscosity ponoʻī e hāʻawi i nā mea viscous ʻole a lawa ʻole paha me ka viscosity kūpono. ʻO nā mea hoʻopili maʻamau i hoʻohana nui ʻia: ① Starch slurry, ʻo ia kekahi o nā mea hoʻopili maʻamau i hoʻohana ʻia, he cheap, a he hana maikaʻi, a ʻo ka hoʻohana maʻamau ʻo 8% -15%; ②Methylcellulose, i kapa ʻia ʻo MC, maikaʻi ka hoʻoheheʻe wai; ③Hydroxypropylcellulose, i kapa ʻia ʻo HPC, hiki ke hoʻohana ʻia ma ke ʻano he pauka paʻa papa kuhikuhi; ④Hydroxypropylmethylcellulose, i kapa ʻia ʻo HPMC, hiki ke hoʻoheheʻe ʻia ka mea i ka wai anuanu; ⑤Carboxymethylcellulose sodium, i kapa ʻia ʻo CMC-Na, kūpono i nā lāʻau lapaʻau me ka maikaʻi ʻole o ka compressibility; ⑥Ethylcellulose, i kapa ʻia ʻo EC, ʻaʻole hiki ke hoʻoheheʻe ʻia ka mea i ka wai, akā hiki ke hoʻoheheʻe ʻia i ka ethanol; ⑦Povidone, i kapa ʻia ʻo PVP, he hygroscopic loa ka mea, hiki ke hoʻoheheʻe ʻia i ka wai a me ka ethanol; ⑧ Eia kekahi, aia nā polyethylene glycol (i kapa ʻia ʻo PEG), nā mea e like me ka gelatin.
3. Disintegrant
Hōʻike nā disintegrants i nā mea kōkua e hāpai i ka wāwahi wikiwiki ʻana o nā papa i loko o nā ʻāpana maikaʻi i loko o nā wai o ka ʻōpū. Koe wale no nā papa waha me nā koi kūikawā e like me nā papa hoʻokuʻu hoʻomau, nā papa hoʻokuʻu hoʻokuʻu ʻia, a me nā papa chewable, pono e hoʻohui ʻia nā disintegrants. ʻO nā mea hoʻoheheʻe maʻamau: ① maloʻo maloʻo, kūpono i nā lāʻau hiki ʻole ke hoʻoheheʻe ʻia; ② carboxymethyl starch sodium, i kapa ʻia ʻo CMS-Na, ʻo kēia mea he disintegrant kiʻekiʻe; ③ hydroxypropyl cellulose haʻahaʻa i hoʻololi ʻia, i kapa ʻia ʻo L -HPC, hiki ke pehu wikiwiki ma hope o ka lawe ʻana i ka wai; ④Cross-linked methyl cellulose sodium, i kapa ʻia ʻo CCMC-Na; pehu mua ka mea i loko o ka wai a laila hoʻoheheʻe ʻia, a ʻaʻole hiki ke hoʻoheheʻe ʻia i ka ethanol; ʻO ka hemahema ʻo ia ka hygroscopicity ikaika a hoʻohana maʻamau ʻia i ka granulation o nā papa effervescent a i ʻole nā ​​​​papa chewable; ⑥Hoʻokomo nui ʻia nā disintegrants effervescent i ka hui ʻana o ka sodium bicarbonate a me ka waikawa citric, a me ka waikawa citric, ka waikawa fumaric, a me ka sodium carbonate hiki ke hoʻohana ʻia, Potassium Carbonate a me Potassium Bicarbonate etc.
4. Lubricant
Hiki ke hoʻokaʻawale nui ʻia nā Lubricants i ʻekolu mau ʻāpana, me nā glidants, anti-sticking agents, a me nā lubricants ma kahi ʻano haiki. ① Glidant: ʻo kāna hana nui e hōʻemi i ka hakakā ma waena o nā ʻāpana, hoʻomaikaʻi i ka wai o ka pauka, a kōkua i ka hōʻemi ʻana i ka ʻokoʻa o ka paona papa; ② anti-sticking agent: ʻo kāna hana nui ka pale ʻana i ka hoʻopili ʻana i ka wā o ka hoʻopaʻa ʻana i ka papa, I mea e hōʻoia ai i ka hana maʻemaʻe o ka hoʻopili ʻana i ka papa, hiki iā ia ke hoʻomaikaʻi i ke ʻano o nā papa; ③ chivalrous lubricant: e hoʻemi i ka friction ma waena o ka mea a me ka pā mold, i mea e hōʻoia ai i ka hana maʻemaʻe o ka paʻi papa a me ka paʻi ʻana. ʻO nā lubricants maʻamau (ma ke ʻano ākea) ka pauka talc, magnesium stearate (MS), micronized silica gel, polyethylene glycols, sodium lauryl sulfate, hydrogenated vegetable oil, etc.
5. Hoʻokuʻu modulator
ʻO nā regulators hoʻokuʻu i loko o nā papa waha he kūpono ia no ka mālama ʻana i ka wikiwiki a me ke kiʻekiʻe o ka hoʻokuʻu ʻana i ka lāʻau lapaʻau i nā hoʻomākaukau hoʻokuʻu ʻana i ka waha, i mea e hōʻoia ai i ka hāʻawi ʻia ʻana o ka lāʻau lapaʻau i ka wahi maʻi i kekahi wikiwiki a mālama i kekahi ʻano i loko o nā ʻiʻo a i ʻole nā ​​wai kino. , ma laila e loaʻa ai ka hopena therapeutic i manaʻo ʻia a hōʻemi i nā hopena ʻona a me nā hopena ʻaoʻao. Hoʻokaʻawale ʻia nā mea hoʻoponopono hoʻokuʻu maʻamau i ke ʻano matrix, polymer hoʻokuʻu lohi i uhi ʻia i ke kiʻiʻoniʻoni a me ka mānoanoa.
(1) Mea hoʻokuʻu ʻano matrix
①Hydrophilic gel skeleton material: pehu ia i ka wā e ʻike ʻia ai i ka wai e hana i kahi pale gel e kāohi ai i ka hoʻokuʻu ʻana i ka lāʻau, hoʻohana maʻamau ʻo methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, povidone, carbomer, alginic acid Salt, chitosan, etc.
② Mea iwi iwi ʻaʻole hiki ke hoʻoheheʻe ʻia: ʻO nā mea iwi iwi hiki ʻole ke hoʻoheheʻe ʻia e pili ana i ka polymer molecular kiʻekiʻe ʻaʻole hiki ke hoʻoheheʻe ʻia i ka wai a i ʻole ka liʻiliʻi o ka wai. Hoʻohana maʻamau ka ethyl cellulose, polyethylene, five-toxic polyethylene, polymethacrylic acid, ethylene-vinyl acetate copolymer, silicone rubber, etc.
③ Bioerodible framework material: ʻO nā mea hoʻohana maʻamau bioerodible framework ka nui o ka momona holoholona, ​​​​ka hinu ʻaila hydrogenated, beeswax, stearyl alcohol, carnauba wax, glyceryl monostearate, a pēlā aku.
(2) Hoʻololi hoʻokuʻu i uhi ʻia
① Nā mea polymer hiki ʻole ke hoʻoheheʻe ʻia: nā mea iwi iwi hiki ʻole ke hoʻoheheʻe ʻia e like me EC.
②Enteric polymer material: ʻO nā mea polymer enteric maʻamau ka nui o ka resin acrylic, L-type a me S-type, hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate phthalate (CAP), hydroxypropylmethylcellulose phthalate (HPMCP), a me nā mea ʻē aʻe. ma luna o nā mea i loko o ka wai ʻōpū, a hoʻoheheʻe i nā ʻāpana kikoʻī e pāʻani i kahi kuleana.
6. Nā mea hana ʻē aʻe
Ma waho aʻe o nā mea hoʻohana maʻamau i hoʻohana ʻia ma luna, ua hoʻohui ʻia nā mea ʻē aʻe i mea e hoʻokō pono ai i nā pono o ka hoʻokele lāʻau, hoʻomaikaʻi i ka ʻike lāʻau a hoʻomaikaʻi i ka hoʻokō. No ka laʻana, kala, ʻono a me nā mea ʻono.
① ʻAi kala: ʻO ke kumu nui o ka hoʻohui ʻana i kēia mea ʻo ia ka hoʻomaikaʻi ʻana i ke ʻano o ka papa a e maʻalahi ka ʻike a me ka ʻike. Pono nā puaʻa i hoʻohana maʻamau i nā kikoʻī lāʻau lapaʻau, a ʻo ka nui i hoʻohui ʻia ʻaʻole pono ma mua o 0.05%.
②Aromatics a me nā mea ʻono: ʻO ke kumu nui o nā mea ʻala a me nā mea ʻono ka hoʻomaikaʻi ʻana i ka ʻono o nā lāʻau lapaʻau, e like me nā papa chewable a me nā papa hoʻoheheʻe waha. ʻO nā mea ʻala maʻamau i hoʻohana nui ʻia i nā essences, nā ʻaila ʻala like ʻole, etc.; ʻO nā mea ʻono i hoʻohana pinepine ʻia me ka sucrose, aspartame, etc.