A comparison of the effect of temperature and moisture on the solid dispersions: Aging and crystallization

Tian, Bin; Zhang, Ling; Pan, Zhendong; Gou, Jingxin; Tang, Xing

doi:10.1016/j.ijpharm.2014.09.010

Cited by 37 publications

(19 citation statements)

References 29 publications

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“…28 Unfortunately, the poor physical stability and low drug loading (,20%) of SD have severely limited the widespread application of this technology. 29 Combinations of NCs and SD technology may be a very interesting strategy for solidification of NC suspensions. In this work, to enhance drug loading and redispersibility of NCs, an NC-based SD (NC-SD) was developed by dispersing NCs into special matrix formers, which was expected to have dual advantages of NCs and SD.…”

Section: Introductionmentioning

confidence: 99%

Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide

Ma¹,

Yang²,

Xie³

et al. 2018

IJN

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ObjectiveThe current study sought to design a quickly dissolving, high drug loading nanocrystal-based solid dispersion (NC-SD) in order to improve the dissolution of poorly soluble drugs.MethodsThe NC-SD was prepared by means of combination of homogenization and spray-drying. Polymer hydroxypropylmethylcellulose (HPMC) was used as baseline dispersant for NC-SD of the model drug – andrographolide (AG). Three superdisintegrants cohomogenized with HPMC were used as codispersant for AG-NC-SD and compared to common water-soluble dispersants – mannitol and lactose. The dissolution characterization and oral bioavailability of AG-NC-SD were evaluated.ResultsThe AG-NC-SD with the higher concentration of HPMC exhibited fast dissolution due to the enhanced wettability of HPMC. The water-soluble codispersants (mannitol and lactose) did not completely prevent AG-NC from aggregation during spray-drying. To achieve much faster AG release, cohomogenized superdisintegrants at a level of 20% must be used along with 25% HPMC. Compared with water-soluble dispersants like mannitol and lactose, superdisintegrants with high swelling capacity were much more effective dispersants for enhancing fast redispersion/dissolution of AG-NC-SD via a swelling-triggered erosion/disintegration mechanism. Surfactant-free AG-NC-SD with 15% cohomogenized sodium carboxymethyl starch combined with 15% HPMC and 10% lactose enhanced the dissolution further, without comprising drug loading, exhibited a barely compromised dissolution rate compared to precursor NC suspensions (f2>50), and possessed drug loading up to 67.83%±1.26%. The pharmacokinetics results also demonstrated that the AG-NC-SD significantly improved the bioavailability in vivo of AG (P<0.05), compared with to the coarse AG.ConclusionThis study illustrates that a quickly dissolving, high drug load, surfactant-free NC-SD can be prepared by using a superdisintegrant as codispersant, and provides a feasible strategy to improve the oral bioavailability of poorly soluble drugs.

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Section: Introductionmentioning

confidence: 99%

Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide

Ma¹,

Yang²,

Xie³

et al. 2018

IJN

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“…Interestingly the results showed rapid release rates for all CRC/SOL formulations with 56 -96% release within 1hr. SOL was used a drug carrier due to its amphiphilic nature and proven capacity to increase the solubility and bioavailability of water insoluble drugs by acting as solubilizer (Maniruzzaman et al, 2013;Tian et al, 2014). In our case SOL demonstrated increased solubilisation capacity especially for the CRC/SOL (1:2) ratio where 96% of the drug is release after 1hr.…”

Section: Resultsmentioning

confidence: 68%

Inkjet printing of transdermal microneedles for the delivery of anticancer agents

Uddin

Scoutaris

Klepetsanis

et al. 2015

International Journal of Pharmaceutics

152

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A novel inkjet printing technology is introduced as a process to coat metal microneedle arrays with three anticancer agents 5-fluororacil, curcumin and cisplatin for transdermal delivery. The hydrophilic graft copolymer Soluplus® was used as a drug carrier and the coating formulations consisted of drug -polymer solutions at various ratios. A piezoelectric dispenser jetted microdroplets on the microneedle surface to develop uniform, accurate and reproducible coating layers without any material losses. Inkjet printing was found to depend on the nozzle size, the applied voltage (mV) and the duration of the pulse (s). The drug release rates were determined in vitro using Franz type diffusion cells with dermatomed porcine skin. The drug release rates depended on the drug-polymer ratio, the drug lipophilicity and the skin thickness. All drugs presented increased release profiles (750 m skin thickness), which were retarded for 900 m skin thickness. Soluplus assisted the drug release especially for the water insoluble curcumin and cisplatin due to its solubilizing capacity. Inkjet printing was proved an effective technology for coating of metal microneedles which can then be used for further transdermal drug delivery applications.

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“…Pada proses penuaan fisik, terjadi penurunan energi bebas permukaan partikel obat yang dapat memberikan efek yaitu penurunan disolusi dari dispersi padat meskipun kristalinitas obatnya tidak berubah. Hal ini disebabkan karena tingginya energi bebas permukaan pada dispersi padat menyebabkan stabilitasnya menjadi rendah dan cenderung mengalami aglomerasi untuk menurunkan energi bebas permukaan dengan mengurangi luas permukaannya 29,30 . Meningkatnya ukuran molekul obat akibat aglomerasi dapat menjadi salah satu penyebab turunnya laju disolusi.…”

Section: Diskusiunclassified

Formulasi dan Evaluasi Sistem Dispersi Padat Ibuprofen dengan Polimer Dekstrosa dalam Sediaan Suppositoria

permatsari

2017

PJI

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Kata kunci : dekstrosa, dispersi padat, efisiensi disolusi, ibuprofen, supositoria A B S T R A K Berdasarkan klasifikasi BCS, ibuprofen tergolong ke dalam BCS kelas II yang memiliki kelarutan rendah dalam air. Metode dispersi padat telah banyak digunakan untuk meningkatkan laju disolusi obat dengan kelarutan rendah. Tujuan dari penelitian ini adalah untuk meningkatkan kelarutan ibuprofen menggunakan metode dispersi padat dengan polimer dekstrosa pada sediaan supositoria berbasis lemak cokelat. Penelitian dilakukan dengan membuat supositoria yang mengandung ibuprofen murni, dispersi padat ibuprofen: dekstrosa 1:1 dan 1:2. Pembuatan dispersi padat dilakukan menggunakan metode pelelehan. Karakterisasi yang dilakukan meliputi uji disolusi, XRD, waktu leleh dan keseragaman bobot supositoria. Hasil uji difraksi sinar X menunjukkan bahwa terjadi penurunan intensitas pola difraksi ibuprofen pada dispersi padat dibandingkan dengan ibuprofen murni yang menunjukkan terjadinya penurunan derajat kristalinitas. Pengujian disolusi menunjukkan bahwa jumlah ibuprofen yang terdisolusi selama 120 menit dan efisiensi disolusi pada menit ke-120 meningkat pada supositoria dengan sistem dispersi padat. Analisis statistik dengan Oneway Anova menunjukkan bahwa terdapat peningkatan persen terdisolusi dan efisiensi disolusi yang signifikan dari supositoria yang mengandung dispersi padat dibandingkan dengan ibuprofen murni. Dari hasil penelitian dapat disimpulkan bahwa penggunaan dekstrosa sebagai polimer hidrofilik dalam dispersi padat dapat meningkatkan profil disolusi pada sediaan supositoria berbasis lemak cokelat. Formula dispersi padat yang optimum dalam meningkatkan profil disolusi adalah pada perbandingan ibuprofen dan dekstrosa sebesar 1:2. Formulation and Evaluation of Ibuprofen Solid Dispersion using Dextrose as a Carrier in SuppositoriesKeywords: dextrose, dissolution efficiency, ibuprofen, solid dispersion, suppositories A B S T R A C T Based on Biopharmaceutical Classification System (BCS), ibuprofen belongs to class II which has a poor water solubility. Solid dispersion technique is widely used to improve dissolution rate of drugs with poor solubility. The aim of this study was to increase the solubility of ibuprofen by solid dispersion method in suppositories. Suppositories were prepared containing pure ibuprofen, solid dispersion of ibuprofen: dextrose in the ratio of 1:1 and 1:2. Solid dispersions were prepared by melting method. Suppositories were characterized by dissolution testing, X-ray diffraction, melting time and weight uniformity. The Xray diffraction test results showed that there is a decrease in intensity of peak diffraction of solid dispersion compared to pure ibuprofen which indicated a decrease of degree of crystallinity. The dissolution test results showed that the amount of the ibuprofen dissolved during 120 minutes and dissolution efficiency in 120 minutes from suppositories were improved using solid dispersion technique. Statistical analysis by Oneway Anova showed a significant increase in percentage of...

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A comparison of the effect of temperature and moisture on the solid dispersions: Aging and crystallization

Cited by 37 publications

References 29 publications

Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide

Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of andrographolide

Inkjet printing of transdermal microneedles for the delivery of anticancer agents

Formulasi dan Evaluasi Sistem Dispersi Padat Ibuprofen dengan Polimer Dekstrosa dalam Sediaan Suppositoria

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