Displaying publications 1 - 20 of 30 in total

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  1. KIANG AK, DOUGLAS B, MORSINGH F
    J Pharm Pharmacol, 1961 Feb;13:98-104.
    PMID: 13755798
  2. Yap SP, Yuen KH, Wong JW
    J Pharm Pharmacol, 2001 Jan;53(1):67-71.
    PMID: 11206194
    We have investigated the pharmacokinetics and bioavailability of alpha-, gamma- and delta-tocotrienols under fed and fasted conditions in eight healthy volunteers. The volunteers were administered a single oral dose of mixed tocotrienols (300 mg) under fed or fasted conditions. The bioavailability of tocotrienols under the two conditions was compared using the parameters peak plasma concentration (Cmax), time to reach peak plasma concentration (Tmax) and total area under the plasma concentration-time curve (AUC(o-infinity)). A statistically significant difference was observed between the fed and fasted logarithmic transformed values of Cmax (P < 0.01) and AUC(0-infinity) (P < 0.01) for all three tocotrienols. In addition, the 90% confidence intervals for the ratio of the logarithmic transformed AUC(0-infinity) values of alpha-, gamma- and delta-tocotrienols under the fed state over those of the fasted state were found to lie between 2.24-3.40, 2.05-4.09 and 1.59-3.81, respectively, while those of the Cmax were between 2.28-4.39, 2.31-5.87 and 1.52-4.05, respectively. However, no statistically significant difference was observed between the fed and fasted Tmax values of the three homologues. The mean apparent elimination half-life (t(1/2)) of alpha-, gamma- and delta-tocotrienols was estimated to be 4.4, 4.3 and 2.3 h, respectively, being between 4.5- to 8.7-fold shorter than that reported for alpha-tocopherol. No statistically significant difference was observed between the fed and fasted t(1/2) values. The mean apparent volume of distribution (Vd/f) values under the fed state were significantly smaller than those of the fasted state, which could be attributed to increased absorption of the tocotrienols in the fed state.
  3. Yap SP, Yuen KH, Lim AB
    J Pharm Pharmacol, 2003 Jan;55(1):53-8.
    PMID: 12625867
    A study was conducted to evaluate the bioavailability of alpha-, gamma- and delta-tocotrienols administered via oral, intravenous, intramuscular and intraperitoneal routes in rats. Three separate experiments, each conducted according to a two-way crossover design, were carried out to compare intravenous and oral, intramuscular and oral, and intraperitoneal and oral administration. Oral absorption of all three tocotrienols was found to be incomplete. Of the three tocotrienols, alpha-tocotrienol had the highest oral bioavailability, at about 27.7+/-9.2%, compared with gamma- and delta-tocotrienols, which had values of 9.1+/-2.4% and 8.5+/-3.5%, respectively. Such biodiscrimination was also observed in their total clearance rates (estimated from the intravenous data). alpha-Tocotrienol showed the lowest clearance rate at about 0.16 L kg(-1) h(-1), whereas that of delta- and gamma-tocotrienols was quite similar, with values of 0.24 and 0.23 L kg(-1) h(-1), respectively. Interestingly, all three tocotrienols were found to be negligibly absorbed when administered intraperitoneally and intramuscularly. Thus, these two routes of administration should be avoided when evaluating the biological activities of the tocotrienols in whole animal experiments.
  4. Wong JW, Yuen KH, Nagappan S, Shahul WS, Ho SS, Gan EK, et al.
    J Pharm Pharmacol, 2003 Feb;55(2):193-8.
    PMID: 12631411
    We have evaluated the therapeutic equivalence of a beta-cyclodextrin-artemisinin complex at an artemisinin dose of 150 mg, with a commercial reference preparation, Artemisinin 250 at a recommended dose of 250 mg. One hundred uncomplicated falciparum malarial patients were randomly assigned to orally receive either beta-cyclodextrin-artemisinin complex (containing 150 mg artemisinin) twice daily for five days or the active comparator (containing 250 mg artemisinin) twice daily for five days. The patients were hospitalized for seven days and were required to attend follow up assessments on days 14, 21, 28 and 35. All patients in both treatment groups were cured of the infection and achieved therapeutic success. At day seven of treatment, all patient blood was clear of the parasites and the sublingual temperature of all patients was less than 37.5 degrees C. Moreover, the parasite clearance time in both treatment groups was similar, being approximately three days after initiation of treatment. Comparable plasma artemisinin concentrations were observed between patients in both treatment groups at 1.5 and 3.0 h, although slightly higher levels were obtained with patients in the beta-cyclodextrin-artemisinin complex-treated group. The beta-cyclodextrin-artemisinin complex at a dose of 150 mg artemisinin was therapeutically equivalent to 250 mg Artemisinin 250. Additionally, patients receiving beta-cyclodextrin-artemisinin complex showed less variability in their plasma artemisinin concentrations at 1.5 h post-dosing, which suggested a more consistent rate of drug absorption.
  5. Bagalkotkar G, Sagineedu SR, Saad MS, Stanslas J
    J Pharm Pharmacol, 2006 Dec;58(12):1559-70.
    PMID: 17331318
    This review discusses the medicinal plant Phyllanthus niruri Linn. (Euphorbiaceae), its wide variety of phytochemicals and their pharmacological properties. The active phytochemicals, flavonoids, alkaloids, terpenoids, lignans, polyphenols, tannins, coumarins and saponins, have been identified from various parts of P. niruri. Extracts of this herb have been proven to have therapeutic effects in many clinical studies. Some of the most intriguing therapeutic properties include anti-hepatotoxic, anti-lithic, anti-hypertensive, anti-HIV and anti-hepatitis B. Therefore, studies relating to chemical characteristics and structural properties of the bioactive phytochemicals found in P. niruri are very useful for further research on this plant as many of the phytochemicals have shown preclinical therapeutic efficacies for a wide range of human diseases, including HIV/AIDS and hepatitis B.
  6. Manikam SD, Manikam ST, Stanslas J
    J Pharm Pharmacol, 2009 Jan;61(1):69-78.
    PMID: 19126299 DOI: 10.1211/jpp/61.01.0010
    The growth inhibiting potential of andrographolide was evaluated in three acute promyelocytic leukaemia cell line models (HL-60, NB4 and all-trans retinoic acid (ATRA)-resistant NB4-R2).
  7. Ling SS, Yuen KH, Magosso E, Barker SA
    J Pharm Pharmacol, 2009 Apr;61(4):445-9.
    PMID: 19298690 DOI: 10.1211/jpp/61.04.0005
    A liposome preparation that is amenable to receptor-mediated endocytosis has been developed to enhance the oral bioavailability of poorly absorbable peptidomimetic drugs by use of folic acid as the mediator of liposomal uptake.
  8. Tan SY, Kan E, Lim WY, Chay G, Law JH, Soo GW, et al.
    J Pharm Pharmacol, 2011 Jul;63(7):918-25.
    PMID: 21635257 DOI: 10.1111/j.2042-7158.2011.01296.x
    The pharmacokinetic interaction between metronidazole, an antibiotic-antiparasitic drug used to treat anaerobic bacterial and protozoal infections, and imatinib, a CYP3A4, P-glycoprotein substrate kinase inhibitor anticancer drug, was evaluated.
  9. Wong TW
    J Pharm Pharmacol, 2011 Dec;63(12):1497-512.
    PMID: 22060280 DOI: 10.1111/j.2042-7158.2011.01347.x
    Use of alginate graft copolymers in oral drug delivery reduces dosage form manufacture complexity with reference to mixing or coating processes. It is deemed to give constant or approximately steady weight ratio of alginate to covalently attached co-excipient in copolymers, thereby leading to controllable matrix processing and drug release. This review describes various grafting approaches and their outcome on oral drug release behaviour of alginate graft copolymeric matrices. It examines drug release modulation mechanism of alginate graft copolymers against that of co-excipients in non-grafted formulations.
  10. Jantan I, Bukhari SN, Lajis NH, Abas F, Wai LK, Jasamai M
    J Pharm Pharmacol, 2012 Mar;64(3):404-12.
    PMID: 22309272 DOI: 10.1111/j.2042-7158.2011.01423.x
    A series of 43 curcumin diarylpentanoid analogues were synthesized and evaluated for their inhibitory effects on the chemiluminescence and chemotactic activity of phagocytes in vitro.
  11. Muthiah YD, Ong CE, Sulaiman SA, Tan SC, Ismail R
    J Pharm Pharmacol, 2012 Dec;64(12):1761-9.
    PMID: 23146039 DOI: 10.1111/j.2042-7158.2012.01551.x
    To investigate the effect of Tualang honey on cytochrome P450 2C8 (CYP2C8) activity in vitro using an amodiaquine N-desethylase assay.
  12. Kirby BP, Pabari R, Chen CN, Al Baharna M, Walsh J, Ramtoola Z
    J Pharm Pharmacol, 2013 Oct;65(10):1473-81.
    PMID: 24028614 DOI: 10.1111/jphp.12125
    In this study, we examined the relative cellular uptake of nanoparticles (NPs) formulated using poly(lactic-co-glycolic acid) (PLGA) polymers with increasing degree of pegylation (PLGA-PEG) and their potential to deliver loperamide to the brain of a mouse.
  13. Wong TW, Sumiran N
    J Pharm Pharmacol, 2014 May;66(5):646-57.
    PMID: 24329400 DOI: 10.1111/jphp.12192
    Objective: Examine the formation of pectin-insulin nanoparticles and their blood glucose lowering properties.

    Methods: The calcium pectinate nanoparticles were prepared by ionotropic gelation method, with alginate, sodium chloride or Tween 80 as additive. Their in vitro physicochemical, drug release and in vivo blood glucose lowering characteristics were evaluated.

    Key findings: Spherical calcium pectinate-insulin nanoparticles were characterized by size, zeta potential, insulin content and insulin association efficiency of 348.4 ± 12.9 nm, -17.9 ± 0.8 mV, 8.4 ± 1.0% and 63.8 ± 7.4%, respectively. They released less than 25% insulin following 24 h in simulated intestinal medium and exhibited delayed blood glucose lowering effect in rats. Incorporation of solubilizer sodium chloride or Tween 80 into nanoparticles did not enhance blood glucose lowering capacity owing to sodium chloride reduced matrix insulin content and Tween 80 interacted with water and had its blood glucose dilution effect negated. Combination of nanoparticles with alginate gel to allow prolonged intestinal residence and more insulin release did not enhance their blood glucose lowering capacity because of calcium alginate-cross-linked gel formation that could retard insulin release and migration into systemic circulation.

    Conclusion: Physicochemical responses of additives in vivo affected blood glucose regulation property of pectin-insulin nanoparticles.

    Keywords: Tween 80; alginate; insulin; nanoparticle; pectin.
  14. Abeer MM, Mohd Amin MC, Martin C
    J Pharm Pharmacol, 2014 Aug;66(8):1047-61.
    PMID: 24628270 DOI: 10.1111/jphp.12234
    The field of pharmaceutical technology is expanding rapidly because of the increasing number of drug delivery options. Successful drug delivery is influenced by multiple factors, one of which is the appropriate identification of materials for research and engineering of new drug delivery systems. Bacterial cellulose (BC) is one such biopolymer that fulfils the criteria for consideration as a drug delivery material.
  15. Jafari SF, Khadeer Ahamed MB, Iqbal MA, Al Suede FS, Khalid SH, Haque RA, et al.
    J Pharm Pharmacol, 2014 Oct;66(10):1394-409.
    PMID: 25039905 DOI: 10.1111/jphp.12272
    Recently, we have isolated koetjapic acid (KA) from Sandoricum koetjape and identified its selective anticancer potentiality against colorectal carcinoma. KA is quite likely to be useful as a systemic anticancer agent against colorectal malignancy. However, with extremely low solubility, KA has to be converted into a biocompatible solubilized form without compromising the bioefficacy. Objective of this study is to enhance solubility of KA and to evaluate anticancer efficacy of potassium koetjapate in human colorectal cancer cells.
  16. Lim AW, Löbmann K, Grohganz H, Rades T, Chieng N
    J Pharm Pharmacol, 2016 Jan;68(1):36-45.
    PMID: 26663364 DOI: 10.1111/jphp.12494
    The objective was to characterize the structural behaviour of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems (1 : 1 molar ratio) prepared by quench cooling, co-evaporation and ball milling.
  17. Fung WY, Liong MT, Yuen KH
    J Pharm Pharmacol, 2016 Feb;68(2):159-69.
    PMID: 26730452 DOI: 10.1111/jphp.12502
    OBJECTIVES: This study aimed to prepare Coenzyme Q10 (CoQ10) microparticles using electrospraying technology, and evaluate the in-vitro properties and in-vivo oral bioavailability.
    KEY FINDINGS: Electrospraying was successfully used to prepare CoQ10 to enhance its solubility and dissolution properties. In-vitro evaluation of the electrosprayed microparticles showed bioavailability-enhancing properties such as reduced crystallinity and particle size. The formulation was evaluated using dissolution study and in-vivo oral bioavailability using rat model. The dissolution study revealed enhanced dissolution properties of electrosprayed microparticles compared with physical mixture and raw material. The absorption profiles showed increasing mean plasma levels CoQ10 in the following order: raw material < physical mixture < electrosprayed microparticles.
    CONCLUSION: Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.
  18. Abubakar IB, Loh HS
    J Pharm Pharmacol, 2016 Apr;68(4):423-32.
    PMID: 26887962 DOI: 10.1111/jphp.12523
    OBJECTIVES: Tabernaemontana is a genus from the plant family, Apocynaceae with vast medicinal application and widespread distribution in the tropics and subtropics of Africa, Americas and Asia. The objective of this study is to critically evaluate the ethnobotany, medicinal uses, pharmacology and phytochemistry of the species, Tabernaemontana corymbosa (Roxb. ex Wall.) and provide information on the potential future application of alkaloids isolated from different parts of the plant.

    KEY FINDINGS: T. corymbosa (Roxb. ex Wall.) parts are used as poultice, boiled juice, decoctions and infusions for treatment against ulceration, fracture, post-natal recovery, syphilis, fever, tumours and orchitis in Malaysia, China, Thailand and Bangladesh. Studies recorded alkaloids as the predominant phytochemicals in addition to phenols, saponins and sterols with vast bioactivities such as antimicrobial, analgesic, anthelmintic, vasorelaxation, antiviral and cytotoxicity.

    SUMMARY: An evaluation of scientific data and traditional medicine revealed the medicinal uses of different parts of T. corymbosa (Roxb. ex Wall.) across Asia. Future studies exploring the structure-bioactivity relationship of alkaloids such as jerantinine and vincamajicine among others could potentially improve the future application towards reversing anticancer drug resistance.

  19. Lee NY, Khoo WK, Adnan MA, Mahalingam TP, Fernandez AR, Jeevaratnam K
    J Pharm Pharmacol, 2016 Jun 10.
    PMID: 27283048 DOI: 10.1111/jphp.12565
    Phyllanthus niruri is a traditional shrub of the genus Phyllanthaceae with long-standing Ayurvedic, Chinese and Malay ethnomedical records. Preliminary studies from cell and animal model have provided valuable scientific evidence for its use.
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